META SUBSTITUTED PHENYLPYRAZOLO- AND PHENYLPYRROLO- PYRIDAZINE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN

Abstract

The present invention relates to meta substituted phenylpyrazolo- and phenylpyrrolo-pyridazine derivatives having dual pharmacological activity towards both the 2 subunit, in particular the 2-1 subunit, of the voltage-gated calcium channel and the NET receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

Claims

1-14. (canceled)

15. A compound of general formula (I): ##STR00212## wherein m is 0, 1, 2, 3 or 4; n is 0, 1, 2, 3 or 4; p is 0, 1, 2, 3 or 4; W is nitrogen or C(R.sub.4); X is selected from the group consisting of a bond, substituted or unsubstituted aryl or C(R.sub.xR.sub.x); R.sub.x is selected from the group consisting of substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; R.sub.x is selected from the group consisting of hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl; R.sub.1 is selected from the group consisting of NR.sub.6R.sub.6 and substituted or unsubstituted N-containing-heterocyclyl; wherein R.sub.6 and R.sub.6 are independently selected from the group consisting of hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; R.sub.2 is selected from the group consisting of hydrogen, NR.sub.7R.sub.7, CN, CHR.sub.7R.sub.7 and substituted or unsubstituted heterocyclyl; wherein R.sub.7 and R.sub.7 are independently selected from the group consisting of hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; R.sub.3 is selected from the group consisting of hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl; R.sub.4 is selected from the group consisting of hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl; R.sub.4 is selected from the group consisting of hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl; R.sub.5 and R.sub.5 are independently selected from the group consisting of hydrogen, halogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkyheterocyclyl, OR.sub.8, NO.sub.2, NR.sub.8R.sub.8, NR.sub.8C(O)R.sub.8, NR.sub.8S(O).sub.2R.sub.8, S(O).sub.2NR.sub.8R.sub.8, NR.sub.8C(O)NR.sub.8R.sub.8, SR.sub.8, S(O)R.sub.8, S(O).sub.2R.sub.8, CN, haloalkyl, haloalkoxy, C(O)OR.sub.8, C(O)NR.sub.8R.sub.8, OCH.sub.2CH.sub.2OR.sub.8, NR.sub.8S(O).sub.2NR.sub.8R.sub.8 and C(CH.sub.3).sub.2OR.sub.8; wherein R.sub.8, R.sub.8 and R.sub.8 are independently selected from the group consisting of hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl; R.sub.c and R.sub.c are independently selected from the group consisting of hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl; alternatively, R.sub.c and R.sub.c, together with the carbon atom to which they are attached, form a substituted or unsubstituted cycloalkyl; optionally as a stereoisomer, including enantiomers and diastereomers, a racemate or as a mixture of at least two stereoisomers, including enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

16. The compound according to claim 15, wherein the compound of Formula (I) is a compound of Formula (I) ##STR00213##

17. The compound according to claim 15, wherein the compound of Formula (I) is a compound of Formula (I.sup.2): ##STR00214##

18. The compound according claim 15, wherein R.sub.1 is selected from the group consisting of NR.sub.6R.sub.6 and substituted or unsubstituted N-containing-heterocyclyl, wherein R.sub.6 and R.sub.6R.sub.6 and R.sub.6 are independently selected from the group consisting of hydrogen, substituted or unsubstituted C.sub.1-6 alkyl and substituted or unsubstituted alkylaryl.

19. The compound according to claim 18, wherein R.sub.1 is: NR.sub.6R.sub.6, wherein R.sub.6 and R.sub.6 are independently selected from the group consisting of hydrogen, substituted or unsubstituted C.sub.1-6 alkyl and substituted or unsubstituted alkylaryl, or an N-containing-heterocyclyl selected from the group consisting of: ##STR00215## wherein R.sub.6a is substituted or unsubstituted alkylaryl.

20. The compound according to claim 15, wherein R.sub.2 is selected from the group consisting of NR.sub.7R.sub.7, and substituted or unsubstituted heterocyclyl; wherein R.sub.7 and R.sub.7 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl.

21. The compound according to claim 20, wherein R.sub.7 and R.sub.7 are independently selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl.

22. The compound according to claim 15, wherein X is selected from the group consisting of a bond, substituted or unsubstituted aryl and C(R.sub.xR.sub.x), wherein R.sub.x is selected from the group consisting of substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl and substituted or unsubstituted heterocyclyl; and R.sub.x is hydrogen.

23. The compound according to claim 22, wherein X is a bond or C(R.sub.xR.sub.x), wherein R.sub.x is hydrogen, and R.sub.X is a group selected from the group consisting of: ##STR00216## wherein R.sub.xa is independently selected from the group consisting of hydrogen, halogen, OR.sub.10, CN, haloalkoxy and C(O)NR.sub.10R.sub.10, wherein R.sub.10 and R.sub.10 independently represent hydrogen or substituted or unsubstituted C.sub.1-6 alkyl.

24. The compound according to claim 15, which is selected from the group consisting of: N,N,3,4-Tetramethyl-2-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(3-(dimethylamino)-1-phenylpropoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(3-(ethylamino)-1-phenylpropoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(3-amino-1-phenylpropoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(1-(3-fluorophenyl)-3-(methylamino)propoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, N,N,3,4-tetramethyl-2-(3-(4-(methylamino)-1-phenylbutoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, 4-(1-(3-(7-(dimethylamino)-3,4-dimethyl-2H-pyrazolo[3,4-d]pyridazin-2-yl)phenoxy)-3-(methylamino)propyl)benzonitrile, 2-(3-(1-(4-fluorophenyl)-3-(methylamino)propoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, N,N,3,4-tetramethyl-2-(3-(3-(methylamino)-1-(pyridin-2-yl)propoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, N,N,3,4-tetramethyl-2-(3-(3-(methylamino)-1-(pyridin-4-yl)propoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, 3-(1-(3-(7-(dimethylamino)-3,4-dimethyl-2H-pyrazolo[3,4-d]pyridazin-2-yl)phenoxy)-3-(methylamino)propyl)benzonitrile, N,N,3,4-tetramethyl-2-(3-((R)-((S)-morpholin-2-yl)(phenyl)methoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, N,N,3,4-tetramethyl-2-(3-((S)-((S)-morpholin-2-yl)(phenyl)methoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(3-amino-3-phenylpropoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, N,N,3,4-tetramethyl-2-(3-(2-(methylamino)-2-phenylethoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, N,N,3,4-tetramethyl-2-(3-((1,2,3,4-tetrahydroisoquinolin-4-yl)oxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(3-(ethylamino)-1-(3-fluorophenyl)propoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(1-(3,5-difluorophenyl)-3-(methylamino)propoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(3-amino-1-(2-fluorophenyl)propoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(3-amino-1-(4-fluorophenyl)propoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(3-amino-1-(3-fluorophenyl)propoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(1-(2-fluorophenyl)-3-(methylamino)propoxy)phenyl)-N,3,4-trimethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(3-amino-1-(2-fluorophenyl)propoxy)phenyl)-N,3,4-trimethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(3-amino-1-phenylpropoxy)phenyl)-N,3,4-trimethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, N,3,4-trimethyl-2-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(1-(2-fluorophenyl)-3-(methylamino)propoxy)phenyl)-3,4-dimethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, 3,4-dimethyl-2-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(3-amino-1-(2-fluorophenyl)propoxy)phenyl)-3,4-dimethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, N,N,3,4-tetramethyl-2-(3-(piperidin-4-ylmethoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(1-(2-Fluorophenyl)-3-(methylamino)propoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-((2-(3-(1-(2-fluorophenyl)-3-(methylamino)propoxy)phenyl)-3,4-dimethyl-2H-pyrazolo[3,4-d]pyridazin-7-yl)(methyl)amino)ethanol, 3-((2-(3-(1-(2-fluorophenyl)-3-(methylamino)propoxy)phenyl)-3,4-dimethyl-2H-pyrazolo[3,4-d]pyridazin-7-yl)(methyl)amino)propan-1-ol, 3-(2-fluorophenyl)-3-(3-(7-(3-methoxyazetidin-1-yl)-3,4-dimethyl-2H-pyrazolo[3,4-d]pyridazin-2-yl)phenoxy)-N-methylpropan-1-amine, N,N,3,4-Tetramethyl-2-(3-(3-(methylamino)-1-(thiazol-2-yl)propoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, N,N,3,4-tetramethyl-2-(3-(2-(methylamino)-1-phenylethoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(1-(2-methoxyphenyl)-3-(methylamino)propoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine (*), 2-(3-(2-(dimethylamino)-1-phenylethoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, N,N,3,4-tetramethyl-2-(3-((4-(methylamino)-1-phenylbutan-2-yl)oxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(1-(3-methoxyphenyl)-3-(methylamino)propoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine (*), N,N,3,4-tetramethyl-2-(3-(2-(methylamino)-1-(thiophen-2-yl)ethoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine (*), 2-(3-(1-(2-fluorophenyl)-2-(methylamino)ethoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, N,N,3,4-tetramethyl-2-(3-(3-(methylamino)-1-(pyridin-3-yl)propoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(1-(3-fluorophenyl)-2-(methylamino)ethoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-((1-(benzyl(methyl)amino)-3-phenylpropan-2-yl)oxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, N,N,3,4-tetramethyl-2-(3-(2-(methylamino)-1-(pyridin-3-yl)ethoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, N,N,3,4-tetramethyl-2-(3-(3-(methylamino)-1-(4-(trifluoromethoxy)phenyl)propoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, N,N,3,4-tetramethyl-2-(3-(2-(methylamino)-3-phenylpropoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, N,N,3,4-tetramethyl-2-(3-(3-(methylamino)-1-(thiazol-5-yl)propoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, N,N,3,4-tetramethyl-2-(3-(2-(1-(methylamino)cyclopropyl)-1-phenylethoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(3-amino-1-(pyridin-3-yl)propoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, N,N,3,4-Tetramethyl-2-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(2-(Dimethylamino)-1-(pyridin-3-yl)ethoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, N,N,3,4-Tetramethyl-2-(3-((1-phenethylpiperidin-4-yl)methoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(3-((2-fluoroethyl)amino)-1-phenylpropoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, 2-(3-(3-((2,2-difluoroethyl)amino)-1-phenylpropoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, 3-(1-(3-(7-(Dimethylamino)-3,4-dimethyl-2H-pyrazolo[3,4-d]pyridazin-2-yl)phenoxy)-3-(methylamino)propyl)benzamide, 4-(1-(3-(7-(dimethylamino)-3,4-dimethyl-2H-pyrazolo[3,4-d]pyridazin-2-yl)phenoxy)-3-(methylamino)propyl)benzamide, (S)-N,N,3,4-Tetramethyl-2-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, (R)-N,N,3,4-tetramethyl-2-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, (R)-N,N,3,4-Tetramethyl-2-(3-(2-(methylamino)-1-phenylethoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, (S)-N,N,3,4-tetramethyl-2-(3-(2-(methylamino)-1-phenylethoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, (R)-2-(3-(1-(2-Fluorophenyl)-3-(methylamino)propoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, (S)-2-(3-(1-(2-fluorophenyl)-3-(methylamino)propoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine, (S)-N,N,3,4-tetramethyl-2-(3-(3-(methylamino)-1-(pyridin-3-yl)propoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, (R)-N,N,3,4-tetramethyl-2-(3-(3-(methylamino)-1-(pyridin-3-yl)propoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine, 3-(2-fluorophenyl)-N-methyl-3-(3-(1,4,5,7-tetramethyl-6H-pyrrolo[3,4-d]pyridazin-6-yl)phenoxy)propan-1-amine, 3-(3-fluorophenyl)-N-methyl-3-(3-(1,4,5,7-tetramethyl-6H-pyrrolo[3,4-d]pyridazin-6-yl)phenoxy)propan-1-amine, (S)-3-(3-Fluorophenyl)-N-methyl-3-(3-(1,4,5,7-tetramethyl-6H-pyrrolo[3,4-d]pyridazin-6-yl)phenoxy)propan-1-amine and (R)-3-(3-fluorophenyl)-N-methyl-3-(3-(1,4,5,7-tetramethyl-6H-pyrrolo[3,4-d]pyridazin-6-yl)phenoxy)propan-1-amine.

25. A process for the preparation of the compound of formula (I) according to claim 15, wherein when the group [CH.sub.2].sub.pR.sub.2 is attached to the core structure through a carbon atom, said process comprises treating a compound of formula III ##STR00217## wherein Z represents a halogen, including chloro, or triflate with a suitable organometallic reagent of formula IVa, ##STR00218## wherein V represents a suitable organometallic reagent, including a boron or zinc reagent, or when the group [CH.sub.2].sub.pR.sub.2 is NR.sub.7R.sub.7, said process comprises treating a compound of formula III ##STR00219## wherein Z represents a halogen, including chloro, or triflate with an amine of formula IVb
HNR.sub.7R.sub.7IVb, or said process comprises treating a compound of formula VH ##STR00220## with a compound of formula VI ##STR00221## wherein Y represents a leaving group, including halogen, mesylate, tosylate, nosylate or triflate, or OH.

26. A process for the preparation of the compound according of formula (I) according to claim 15, employing a compound of Formula II, IIP, III, IIIP, IIIH, IVa, IVb, VP, VH, VI, VII, VIIP, VIII, IX, IXP, X, XI, XIP, IIa, IIaP, XII, XIII, XIVa, XIVb, XV, XVP, Ib, VbP or VbH ##STR00222## ##STR00223## ##STR00224## ##STR00225## ##STR00226## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.4, R.sub.5, R.sub.5, R.sub.c, R.sub.c, X, W, m, n and p are as defined in claim 15; Z represents a halogen, including chloro, or triflate; Y represents a leaving group, including halogen, mesylate, tosylate, nosylate or triflate, or OH; V represents an organometallic reagent, including a boron or zinc reagent; L and L represent halogen, including fluorine, chlorine, bromine or iodine; P represents a suitable protecting group, including alkyl, including methyl, or benzyl; and Q represents an alkyl group, including methyl or ethyl.

27. A pharmaceutical composition which comprises the compound according to claim 15, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.

28. A method of treating pain in a subject in need thereof, comprising administration of an effective amount of the compound according to claim 15.

29. The method according to claim 28, wherein the pain is selected from the group consisting of medium to severe pain, visceral pain, chronic pain, cancer pain, migraine, inflammatory pain, acute pain or neuropathic pain, allodynia and hyperalgesia.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0036] The invention is directed to a family of structurally distinct meta substituted phenylpyrazolo- and phenylpyrrolo-pyridazine derivatives which have a dual pharmacological activity towards both the .sub.2 subunit, in particular the .sub.2-1 subunit, of the voltage-gated calcium channel and the NET receptor.

[0037] The invention is directed to compounds having a dual activity binding to the .sub.2 subunit, in particular the .sub.2-1 subunit, of the voltage-gated calcium channel and the NET receptor for use in the treatment of pain.

[0038] As this invention is aimed at providing a compound or a chemically related series of compounds which act as dual ligands of the .sub.2 subunit, in particular the .sub.2-1 subunit, of the voltage-gated calcium channel and the NET receptor it is a preferred embodiment if the compound has a binding expressed as K.sub.i responding to the following scales:

K.sub.i(NET) is preferably <1000 nM, more preferably <500 nM, even more preferably <100 nM.
K.sub.i(.sub.2-1) is preferably <10000 nM, more preferably <5000 nM, even more preferably <500 nM or even more preferably <100 nM.

[0039] In its broader aspect, the present invention is directed to compounds of general Formula (I):

##STR00002##

wherein
m is 0, 1, 2, 3 or 4;
n is 0, 1, 2, 3 or 4;
p is 0, 1, 2, 3 or 4;
W is nitrogen or C(R.sub.4);
X is selected from a bond, substituted or unsubstituted aryl or C(R.sub.xR.sub.x); [0040] R.sub.x is selected from substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; [0041] R.sub.x, is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
R.sub.1 is selected from NR.sub.6R.sub.6 and substituted or unsubstituted N-containing-heterocyclyl; [0042] wherein R.sub.6 and R.sub.6 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl;
R.sub.2 is selected from hydrogen, NR.sub.7R.sub.7, CN, CHR.sub.7R.sub.7 and substituted or unsubstituted heterocyclyl; [0043] wherein R.sub.7 and R.sub.7 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl;
R.sub.3 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
R.sub.4 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
R.sub.4 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
R.sub.5 and R.sub.5, are independently selected from hydrogen, halogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkyheterocyclyl, OR.sub.8, NO.sub.2, NR.sub.8R.sub.8, NR.sub.8C(O)R.sub.8, NR.sub.8S(O).sub.2R.sub.8, S(O).sub.2NR.sub.8R.sub.8, NR.sub.8C(O)NR.sub.8R.sub.8, SR.sub.8, S(O)R.sub.8, S(O).sub.2R.sub.8, CN, haloalkyl, haloalkoxy, C(O)OR.sub.8, C(O)NR.sub.8R.sub.8, OCH.sub.2CH.sub.2OR.sub.8, NR.sub.8S(O).sub.2NR.sub.8R.sub.8, and C(CH.sub.3).sub.2OR.sub.8; [0044] wherein R.sub.8, R.sub.8, and R.sub.8 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl;
R.sub.c and R.sub.c are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
alternatively, R.sub.c and R.sub.c may form with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;

[0045] These compounds according to the invention are optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0046] In another embodiment, these compounds according to the invention are optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof.

[0047] In a particular embodiment the following proviso applies:

[CH.sub.2].sub.mX[C(R.sub.cR.sub.c)].sub.nR.sub.1 is attached to the oxygen atom through a carbon atom.

[0048] In a further embodiment the compound according to the invention of general Formula (I) is a compound of general Formula (I)

##STR00003## [0049] wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.5, R.sub.c, R.sub.c, X, m, n and p are as defined below in the detailed description,
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0050] In a further embodiment the compound according to the invention of general Formula (I) is a compound of general Formula (I)

##STR00004##

wherein
m is 0, 1, 2, 3 or 4;
n is 0, 1, 2, 3 or 4;
p is 0, 1, 2, 3 or 4;
X is selected from a bond, substituted or unsubstituted aryl or C(R.sub.xR.sub.x); [0051] R.sub.x is selected from substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; [0052] R.sub.x is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
R.sub.1 is selected from NR.sub.6R.sub.6, and substituted or unsubstituted N-containing-heterocyclyl; [0053] wherein R.sub.6 and R.sub.6, are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl;
R.sub.2 is selected from hydrogen, NR.sub.7R.sub.7, CN, CHR.sub.7R.sub.7 and substituted or unsubstituted heterocyclyl; [0054] wherein R.sub.7 and R.sub.7 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl;
R.sub.3 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
R.sub.4 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
R.sub.4, is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
R.sub.5 and R.sub.5 are independently selected from hydrogen, halogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkyheterocyclyl, OR.sub.8, NO.sub.2, NR.sub.8R.sub.8, NR.sub.8C(O)R.sub.8, NR.sub.8S(O).sub.2R.sub.8, S(O).sub.2NR.sub.8R.sub.8, NR.sub.8C(O)NR.sub.8R.sub.8, SR.sub.8, S(O)R.sub.8, S(O).sub.2R.sub.8, CN, haloalkyl, haloalkoxy, C(O)OR.sub.8, C(O)NR.sub.8R.sub.8, OCH.sub.2CH.sub.2OR.sub.8, NR.sub.8S(O).sub.2NR.sub.8R.sub.8, and C(CH.sub.3).sub.2OR.sub.8; [0055] wherein R.sub.8, R.sub.8 and R.sub.8 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl;
R.sub.c and R.sub.c are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
alternatively, R.sub.c and R.sub.c40 may form with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0056] In a further embodiment the compound according to the invention of general Formula (I) is a compound of general Formula (I.sup.2)

##STR00005## [0057] wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.5, R.sub.c, R.sub.c, X, m, n and p are as defined below in the detailed description,
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0058] In a further embodiment the compound according to the invention of general Formula (I) is a compound of general Formula (I.sup.2)

##STR00006##

wherein
m is 0, 1, 2, 3 or 4;
n is 0, 1, 2, 3 or 4;
p is 0, 1, 2, 3 or 4;
X is selected from a bond, substituted or unsubstituted aryl or C(R.sub.xR.sub.x); [0059] R.sub.x is selected from substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; [0060] R.sub.x is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
R.sub.1 is selected from NR.sub.6R.sub.6 and substituted or unsubstituted N-containing-heterocyclyl; [0061] wherein R.sub.6 and R.sub.6 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl;
R.sub.2 is selected from hydrogen, NR.sub.7R.sub.7, CN, CHR.sub.7R.sub.7 and substituted or unsubstituted heterocyclyl; [0062] wherein R.sub.7 and R.sub.7 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl;
R.sub.3 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
R.sub.4 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
R.sub.4 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
R.sub.5 and R.sub.5 are independently selected from hydrogen, halogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkyheterocyclyl, OR.sub.8, NO.sub.2, NR.sub.8R.sub.8, NR.sub.8C(O)R.sub.8, NR.sub.8S(O).sub.2R.sub.8, S(O).sub.2NR.sub.8R.sub.8, NR.sub.8C(O)NR.sub.8R.sub.8, SR.sub.8, S(O)R.sub.8, S(O).sub.2R.sub.8, CN, haloalkyl, haloalkoxy, C(O)OR.sub.8, C(O)NR.sub.8R.sub.8, OCH.sub.2CH.sub.2OR.sub.8, NR.sub.8S(O).sub.2NR.sub.8R.sub.8, and C(CH.sub.3).sub.2OR.sub.8; [0063] wherein R.sub.8, R.sub.8 and R.sub.8 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl;
R.sub.c and R.sub.c are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
alternatively, R.sub.c and R.sub.c may form with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0064] For clarity purposes, all groups and definitions described in the present description and referring to compounds of general Formula (I), also apply to compounds of general Formulae (I) and (I.sup.2), (where applicable), and to all intermediate of synthesis, when those groups are present in the mentioned general Markush formulae, since compounds of general Formulae (I) and (I.sup.2) are included within the scope of the larger definition of general Formula (I).

[0065] For clarity purposes, the general Markush Formula (I)

##STR00007##

is equivalent to

##STR00008##

wherein only C(R.sub.CR.sub.C) and CH.sub.2 are included into the brackets, and n, m and p mean the number of times that C(R.sub.CR.sub.C) and CH.sub.2 are repeated, respectively. The same would apply, when applicable, to general Markush Formulae (I) and (I.sup.2), and to all intermediates of synthesis.

[0066] In addition, and for clarity purposes, it should further be understood that naturally if m is 0, the oxygen and/or X are still present in general Markush Formulae (I), (I) and (I.sup.2). In the same way when n is 0, R.sub.1 and/or X are still present, when applicable, in general Markush Formulae (I), (I) and (I.sup.2) and to all intermediates of synthesis. In the same way when p is 0, R.sub.2 is still present, when applicable, in general Markush Formulae (I), (I) and (I.sup.2), and to all intermediates of synthesis.

[0067] For clarity purposes, the expression the cycloalkyl in R.sub.c and R.sub.c means the cycloalkyl resulting when R.sub.c and R.sub.c form, together with the carbon to which they are attached, a cycloalkyl. This cycloalkyl can then be substituted or not.

[0068] For clarity purposes, reference is also made to the following statements below in the definitions of substitutions on alkyl etc. or aryl etc. that wherein when different radicals R.sub.1 to R.sub.14, are present simultaneously in Formula (I) they may be identical or different. This statement is reflected in the below general Formula (I.sup.3) being derived from and falling into general Formula (I),

##STR00009##

wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.5, R.sub.c, R.sub.c, X, W, m, n and p are as defined in the description. In addition, R.sub.c and R.sub.c are added. As said above, this statement is thus reflected in that R.sub.c, and R.sub.c are or could be different from R.sub.c and R.sub.c or not.

[0069] The same would be applicable mutatis mutandis for general Formulas like general Formula (I) as well as the other general Formulas (I.sup.1) to (I.sup.2) above and to all intermediates of synthesis.

[0070] In the context of this invention, alkyl is understood as meaning saturated, linear or branched hydrocarbons, which may be unsubstituted or substituted once or several times. It encompasses e.g. CH.sub.3 and CH.sub.2CH.sub.3. In these radicals, C.sub.1-2-alkyl represents C1- or C2-alkyl, C.sub.1-3-alkyl represents C1-, C2- or C3-alkyl, C.sub.1-4-alkyl represents C1-, C2-, C3- or C4-alkyl, C.sub.1-5-alkyl represents C1-, C2-, C3-, C4-, or C5-alkyl, C.sub.1-6-alkyl represents C1-, C2-, C3-, C4-, C5- or C6-alkyl, C.sub.1-7-alkyl represents C1-, C2-, C3-, C4-, C5-, C6- or C7-alkyl, C.sub.1-8-alkyl represents C1-, C2-, C3-, C4-, C5-, C6-, C7- or C8-alkyl, C.sub.1-10-alkyl represents C1-, C2-, C3-, C4-, C5-, C6-, C7-, C8-, C9- or C10-alkyl and C.sub.1-18-alkyl represents C1-, C2-, C3-, C4-, C5-, C6-, C7-, C8-, C9-, C10-, C11-, C12-, C13-, C14-, C15-, C16-, C17- or C18-alkyl. The alkyl radicals are preferably methyl, ethyl, propyl, methylethyl, butyl, 1-methylpropyl, 2-methylpropyl, 1,1-dimethylethyl, pentyl, 1,1-dimethylpropyl, 1,2-dimethylpropyl, 2,2-dimethylpropyl, hexyl, 1-methylpentyl, if substituted also CHF.sub.2, CF.sub.3 or CH.sub.2OH etc. Preferably alkyl is understood in the context of this invention as C.sub.1-8alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl, or octyl; preferably is C.sub.1-6alkyl like methyl, ethyl, propyl, butyl, pentyl, or hexyl; more preferably is C.sub.1-4alkyl like methyl, ethyl, propyl or butyl.

[0071] Alkenyl is understood as meaning unsaturated, linear or branched hydrocarbons, which may be unsubstituted or substituted once or several times. It encompasses groups like e.g. CHCHCH.sub.3. The alkenyl radicals are preferably vinyl (ethenyl), allyl (2-propenyl). Preferably in the context of this invention alkenyl is C.sub.2-10-alkenyl or C.sub.2-8-alkenyl like ethylene, propylene, butylene, pentylene, hexylene, heptylene or octylene; or is C.sub.2-6-alkenyl like ethylene, propylene, butylene, pentylene, or hexylene; or is C.sub.2-4-alkenyl, like ethylene, propylene, or butylenes.

[0072] Alkynyl is understood as meaning unsaturated, linear or branched hydrocarbons, which may be unsubstituted or substituted once or several times. It encompasses groups like e.g. CCCH.sub.3 (1-propinyl). Preferably alkynyl in the context of this invention is C.sub.2-10-alkynyl or C.sub.2-8-alkynyl like ethyne, propyne, butyene, pentyne, hexyne, heptyne, or octyne; or is C.sub.2-6-alkynyl like ethyne, propyne, butyene, pentyne, or hexyne; or is C.sub.2-4-alkynyl like ethyne, propyne, butyene, pentyne, or hexyne.

[0073] In connection with alkyl (also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl), alkenyl, alkynyl and O-alkylunless defined otherwisethe term substituted in the context of this invention is understood as meaning replacement of at least one hydrogen radical on a carbon atom by halogen (F, Cl, Br, I), NR.sub.kR.sub.k, SR.sub.k, S(O)R.sub.k, S(O).sub.2R.sub.k, OR.sub.k, C(O)R.sub.k, C(O)OR.sub.k, CN, C(O)NR.sub.kR.sub.k, haloalkyl, haloalkoxy, being R.sub.k represented by R.sub.9, R.sub.11, R.sub.12, or R.sub.13, (being R.sub.k represented by R.sub.9, R.sub.11, R.sub.12, or R.sub.13; being R.sub.k represented by R.sub.9, R.sub.11, R.sub.12, or R.sub.13; wherein R.sub.1 to R.sub.14, and R.sub.x and R.sub.x, and R.sub.c and R.sub.c are as defined in the description, and wherein when different radicals R.sub.1 to R.sub.14, and R.sub.x and R.sub.x and R.sub.c and R.sub.c are present simultaneously in Formula I they may be identical or different.

[0074] Most preferably in connection with alkyl (also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl), alkenyl, alkynyl or O-alkyl, substituted is understood in the context of this invention that any alkyl (also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl), alkenyl, alkynyl or O-alkyl which is substituted with one or more of halogen (F, Cl, Br, I), NR.sub.kR.sub.k, OR.sub.k, CN, SR.sub.k, haloalkyl, haloalkoxy, being R.sub.k represented by R.sub.9, R.sub.11, R.sub.12, or R.sub.13, (being R.sub.k represented by R.sub.9, R.sub.11, R.sub.12, or R.sub.13; being R.sub.k represented by R.sub.9, R.sub.11, R.sub.12, or R.sub.13; wherein R.sub.1 to R.sub.14, and R.sub.x and R.sub.x and R.sub.c and R.sub.c are as defined in the description, and wherein when different radicals R.sub.1 to R.sub.14 and R.sub.x and R.sub.x and R.sub.c and R.sub.c are present simultaneously in Formula I they may be identical or different.

[0075] More than one replacement on the same molecule and also on the same carbon atom is possible with the same or different substituents. This includes for example 3 hydrogens being replaced on the same C atom, as in the case of CF.sub.3, or at different places of the same molecule, as in the case of e.g. CH(OH)CHCHCHCl.sub.2.

[0076] In the context of this invention haloalkyl is understood as meaning an alkyl being substituted once or several times by a halogen (selected from F, Cl, Br, I). It encompasses e.g. CH.sub.2Cl, CH.sub.2F, CHCl.sub.2, CHF.sub.2, CCl.sub.3, CF.sub.3 and CH.sub.2CHCl.sub.2. Preferably haloalkyl is understood in the context of this invention as halogen-substituted C.sub.1-4-alkyl representing halogen substituted C1-, C2-, C3- or C4-alkyl. The halogen-substituted alkyl radicals are thus preferably methyl, ethyl, propyl, and butyl. Preferred examples include CH.sub.2Cl, CH.sub.2F, CHCl.sub.2, CHF.sub.2, and CF.sub.3.

[0077] In the context of this invention haloalkoxy is understood as meaning an O-alkyl being substituted once or several times by a halogen (selected from F, Cl, Br, I). It encompasses e.g. OCH.sub.2Cl, OCH.sub.2F, OCHCl.sub.2, OCHF.sub.2, OCCl.sub.3, OCF.sub.3 and OCH.sub.2CHCl.sub.2. Preferably haloalkyl is understood in the context of this invention as halogen-substituted OC.sub.1-4-alkyl representing halogen substituted C1-, C2-, C3- or C4-alkoxy. The halogen-substituted alkyl radicals are thus preferably O-methyl, O-ethyl, O-propyl, and O-butyl. Preferred examples include OCH.sub.2Cl, OCH.sub.2F, OCHCl.sub.2, OCHF.sub.2, and OCF.sub.3.

[0078] In the context of this invention cycloalkyl is understood as meaning saturated and unsaturated (but not aromatic) cyclic hydrocarbons (without a heteroatom in the ring), which can be unsubstituted or once or several times substituted. Furthermore, C.sub.3-4-cycloalkyl represents C3- or C4-cycloalkyl, C.sub.3-5-cycloalkyl represents C3-, C4- or C5-cycloalkyl, C.sub.3-6-cycloalkyl represents C3-, C4-, C5- or C6-cycloalkyl, C.sub.3-7-cycloalkyl represents C3-, C4-, C5-, C6- or C7-cycloalkyl, C.sub.3-8-cycloalkyl represents C3-, C4-, C5-, C6-, C7- or C8-cycloalkyl, C.sub.4-5-cycloalkyl represents C4- or C5-cycloalkyl, C.sub.4-6-cycloalkyl represents C4-, C5- or C6-cycloalkyl, C.sub.4-7-cycloalkyl represents C4-, C5-, C6- or C7-cycloalkyl, C.sub.5-6-cycloalkyl represents C5- or C6-cycloalkyl and C.sub.5-7-cycloalkyl represents C5-, C6- or C7-cycloalkyl. Examples are cyclopropyl, 2-methylcyclopropyl, cyclopropylmethyl, cyclobutyl, cyclopentyl, cyclopentylmethyl, cyclohexyl, cycloheptyl, cyclooctyl, and also adamantyl. Preferably in the context of this invention cycloalkyl is C.sub.3-8cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; or is C.sub.3-7cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; or is C.sub.3-6cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl, especially cyclopentyl or cyclohexyl.

[0079] Aryl is understood as meaning 5 to 18 membered mono or polycyclic ring systems with at least one aromatic ring but without heteroatoms even in only one of the rings. Examples are phenyl, naphthyl, fluoranthenyl, fluorenyl, tetralinyl or indanyl, 9H-fluorenyl or anthracenyl radicals, which can be unsubstituted or once or several times substituted. Most preferably aryl is understood in the context of this invention as phenyl, naphthyl or anthracenyl, preferably is phenyl.

[0080] A heterocyclyl radical or group (also called heterocyclyl hereinafter) is understood as meaning 5 to 18 membered mono or polycyclic heterocyclic ring systems, with at least one saturated or unsaturated ring which contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring. A heterocyclic group can also be substituted once or several times.

[0081] Examples include non-aromatic heterocyclyls such as tetrahydropyrane, oxazepane, morpholine, piperidine, pyrrolidine as well as heteroaryls such as furan, benzofuran, thiophene, benzothiophene, pyrrole, pyridine, pyrimidine, pyrazine, quinoline, isoquinoline, phthalazine, thiazole, benzothiazole, indole, benzotriazole, carbazole and quinazoline.

[0082] Subgroups inside the heterocyclyls as understood herein include heteroaryls and non-aromatic heterocyclyls. [0083] the heteroaryl (being equivalent to heteroaromatic radicals or aromatic heterocyclyls) is an aromatic 5 to 18 membered mono or polycyclic heterocyclic ring system of one or more rings of which at least one aromatic ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a 5 to 18 membered mono or polycyclic aromatic heterocyclic ring system of one or two rings of which at least one aromatic ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from furan, benzofuran, thiophene, benzothiophene, pyrrole, pyridine, pyrimidine, pyrazine, quinoline, isoquinoline, phthalazine, benzothiazole, indole, benzotriazole, carbazole, quinazoline, thiazole, imidazole, pyrazole, oxazole, thiophene and benzimidazole; [0084] the non-aromatic heterocyclyl is a 5 to 18 membered mono or polycyclic heterocyclic ring system of one or more rings of which at least one ringwith this (or these) ring(s) then not being aromaticcontains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a 5 to 18 membered mono or polycyclic heterocyclic ring system of one or two rings of which one or both ringswith this one or two rings then not being aromaticcontain/s one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepam, pyrrolidine, piperidine, piperazine, tetrahydropyran, morpholine, indoline, oxopyrrolidine, benzodioxane, especially is benzodioxane, morpholine, tetrahydropyran, piperidine, oxopyrrolidine and pyrrolidine.

[0085] Preferably in the context of this invention heterocyclyl is defined as a 5 to 18 membered mono or polycyclic heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring. Preferably it is a 5 to 18 membered mono or polycyclic heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring.

[0086] Preferred examples of heterocyclyls include oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, tetrahydroisoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline, especially is pyridine, pyrazine, indazole, benzodioxane, thiazole, benzothiazole, morpholine, tetrahydropyrane, pyrazole, imidazole, piperidine, thiophene, indole, benzimidazole, pyrrolo[2,3b]pyridine, benzoxazole, oxopyrrolidine, pyrimidine, oxazepane and pyrrolidine.

[0087] In the context of this invention oxopyrrolidine is understood as meaning pyrrolidin-2-one.

[0088] In connection with aromatic heterocyclyls (heteroaryls), non-aromatic heterocyclyls, aryls and cycloalkyls, when a ring system falls within two or more of the above cycle definitions simultaneously, then the ring system is defined first as an aromatic heterocyclyl (heteroaryl) if at least one aromatic ring contains a heteroatom. If no aromatic ring contains a heteroatom, then the ring system is defined as a non-aromatic heterocyclyl if at least one non-aromatic ring contains a heteroatom. If no non-aromatic ring contains a heteroatom, then the ring system is defined as an aryl if it contains at least one aryl cycle. If no aryl is present, then the ring system is defined as a cycloalkyl if at least one non-aromatic cyclic hydrocarbon is present.

[0089] In the context of this invention alkylaryl is understood as meaning an aryl group (see above) being connected to another atom through a C.sub.1-6-alkyl (see above) which may be branched or linear and is unsubstituted or substituted once or several times. Preferably alkylaryl is understood as meaning an aryl group (see above) being connected to another atom through 1 to 4 (CH.sub.2) groups. Most preferably alkylaryl is benzyl (i.e. CH.sub.2-phenyl).

[0090] In the context of this invention alkylheterocyclyl is understood as meaning an heterocyclyl group being connected to another atom through a C.sub.1-6-alkyl (see above) which may be branched or linear and is unsubstituted or substituted once or several times. Preferably alkylheterocyclyl is understood as meaning an heterocyclyl group (see above) being connected to another atom through 1 to 4 (CH.sub.2) groups. Most preferably alkylheterocyclyl is CH.sub.2-pyridine.

[0091] In the context of this invention alkylcycloalkyl is understood as meaning an cycloalkyl group being connected to another atom through a C.sub.1-6-alkyl (see above) which may be branched or linear and is unsubstituted or substituted once or several times. Preferably alkylcycloalkyl is understood as meaning an cycloalkyl group (see above) being connected to another atom through 1 to 4 (CH.sub.2) groups. Most preferably alkylcycloalkyl is CH.sub.2-cyclopropyl.

[0092] Preferably, the aryl is a monocyclic aryl. More preferably the aryl is a 5, 6 or 7 membered monocyclic aryl. Even more preferably the aryl is a 5 or 6 membered monocyclic aryl.

[0093] Preferably, the heteroaryl is a monocyclic heteroaryl. More preferably the heteroaryl is a 5, 6 or 7 membered monocyclic heteroaryl. Even more preferably the heteroaryl is a 5 or 6 membered monocyclic heteroaryl.

[0094] Preferably, the non-aromatic heterocyclyl is a monocyclic non-aromatic heterocyclyl. More preferably the non-aromatic heterocyclyl is a 4, 5, 6 or 7 membered monocyclic non-aromatic heterocyclyl. Even more preferably the non-aromatic heterocyclyl is a 5 or 6 membered monocyclic non-aromatic heterocyclyl.

[0095] Preferably, the cycloalkyl is a monocyclic cycloalkyl. More preferably the cycloalkyl is a 3, 4, 5, 6, 7 or 8 membered monocyclic cycloalkyl. Even more preferably the cycloalkyl is a 3, 4, 5 or 6 membered monocyclic cycloalkyl.

[0096] In connection with aryl (including alkyl-aryl), cycloalkyl (including alkyl-cycloalkyl), or heterocyclyl (including alkyl-heterocyclyl), substituted is understoodunless defined otherwiseas meaning substitution of the ring-system of the aryl or alkyl-aryl, cycloalkyl or alkyl-cycloalkyl; heterocyclyl or alkyl-heterocyclyl with one or more of halogen (F, Cl, Br, I), R.sub.k, OR.sub.k, CN, NO.sub.2, NR.sub.kR.sub.k, C(O)OR.sub.k, NR.sub.kC(O)R.sub.k, C(O)NR.sub.kR.sub.k, NR.sub.kS(O).sub.2R.sub.k, O, OCH.sub.2CH.sub.2OH, NR.sub.kC(O)NR.sub.kR.sub.k, S(O).sub.2NR.sub.kR.sub.k, NR.sub.kS(O).sub.2NR.sub.kR.sub.k, haloalkyl, haloalkoxy, SR.sub.k, S(O)R.sub.k, S(O).sub.2R.sub.k or C(CH.sub.3)OR.sub.k, or substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl, substituted or unsubstituted alkylheterocyclyl, with R.sub.k, R.sub.k and R.sub.k independently being either H or a saturated or unsaturated, linear or branched, substituted or unsubstituted C.sub.1-6-alkyl; a saturated or unsaturated, linear or branched, substituted or unsubstituted C.sub.1-6-alkyl; a saturated or unsaturated, linear or branched, substituted or unsubstituted OC.sub.1-6-alkyl (alkoxy); a saturated or unsaturated, linear or branched, substituted or unsubstituted SC.sub.1-6-alkyl; a saturated or unsaturated, linear or branched, substituted or unsubstituted C(O)C.sub.1-6-alkyl-group; a saturated or unsaturated, linear or branched, substituted or unsubstituted C(O)OC.sub.1-6-alkyl-group; a substituted or unsubstituted aryl or alkyl-aryl; a substituted or unsubstituted cycloalkyl or alkyl-cycloalkyl; a substituted or unsubstituted heterocyclyl or alkyl-heterocyclyl, being R.sub.k one of R.sub.10, R.sub.11, R.sub.12 or R.sub.14, (being R.sub.k one of R.sub.10, R.sub.11, R.sub.12 or R.sub.14, being R.sub.k one of R.sub.10, R.sub.11, R.sub.12, or R.sub.14; wherein R.sub.1 to R.sub.14 and R.sub.x and R.sub.x and R.sub.c and R.sub.c are as defined in the description, and wherein when different radicals R.sub.1 to R.sub.14 and R.sub.x and R.sub.x and R.sub.c and R.sub.c are present simultaneously in Formula I they may be identical or different.

[0097] Most preferably in connection with aryl (including alkyl-aryl), cycloalkyl (including alkyl-cycloalkyl), or heterocyclyl (including alkyl-heterocyclyl), substituted is understood in the context of this invention that any aryl, cycloalkyl and heterocyclyl which is substituted is substituted (also in an alyklaryl, alkylcycloalkyl or alkylheterocyclyl) with one or more of halogen (F, Cl, Br, I), R.sub.k, OR.sub.k, CN, NO.sub.2, NR.sub.kR.sub.k, NR.sub.kC(O)R.sub.k, NR.sub.kS(O).sub.2R.sub.k, S(O).sub.2NR.sub.kR.sub.k, NR.sub.kC(O)NR.sub.kR.sub.k, haloalkyl, haloalkoxy, SR.sub.k, S(O)R.sub.k or S(O).sub.2R.sub.k, or substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl, substituted or unsubstituted alkylheterocyclyl, being R.sub.k one of R.sub.10, R.sub.11, R.sub.12 or R.sub.14, (being R.sub.k one of R.sub.10, R.sub.11, R.sub.12 or R.sub.14; being R.sub.k one of R.sub.10, R.sub.11, R.sub.12, or R.sub.14; wherein R.sub.1 to R.sub.14, and R.sub.x and R.sub.x, and R.sub.c and R.sub.c are as defined in the description, and wherein when different radicals R.sub.1 to R.sub.14, and R.sub.x and R.sub.x and R.sub.c and R.sub.c are present simultaneously in Formula I they may be identical or different.

[0098] In connection with cycloalkyl (including alkyl-cycloalkyl), or heterocyclyl (including alkylheterocyclyl) namely non-aromatic heterocyclyl (including non-aromatic alkyl-heterocyclyl), substituted is also understoodunless defined otherwiseas meaning substitution of the ring-system of the cycloalkyl or alkyl-cycloalkyl; non-aromatic heterocyclyl or non aromatic alkyl-heterocyclyl with

##STR00010##

(leading to a spiro structure) or with O.

[0099] A ring system is a system consisting of at least one ring of connected atoms but including also systems in which two or more rings of connected atoms are joined with joined meaning that the respective rings are sharing one (like a spiro structure), two or more atoms being a member or members of both joined rings.

[0100] The term leaving group means a molecular fragment that departs with a pair of electrons in heterolytic bond cleavage. Leaving groups can be anions or neutral molecules. Common anionic leaving groups are halides such as Cl, Br, and I, and sulfonate esters, such as tosylate (TsO) or mesylate.

[0101] The term salt is to be understood as meaning any form of the active compound used according to the invention in which it assumes an ionic form or is charged and is coupled with a counter-ion (a cation or anion) or is in solution. By this are also to be understood complexes of the active compound with other molecules and ions, in particular complexes via ionic interactions.

[0102] The term physiologically acceptable salt means in the context of this invention any salt that is physiologically tolerated (most of the time meaning not being toxic-especially not caused by the counter-ion) if used appropriately for a treatment especially if used on or applied to humans and/or mammals.

[0103] These physiologically acceptable salts can be formed with cations or bases and in the context of this invention is understood as meaning salts of at least one of the compounds used according to the inventionusually a (deprotonated) acidas an anion with at least one, preferably inorganic, cation which is physiologically toleratedespecially if used on humans and/or mammals. The salts of the alkali metals and alkaline earth metals are particularly preferred, and also those with NH.sub.4, but in particular (mono)- or (di)sodium, (mono)- or (di)potassium, magnesium or calcium salts.

[0104] Physiologically acceptable salts can also be formed with anions or acids and in the context of this invention is understood as meaning salts of at least one of the compounds used according to the invention as the cation with at least one anion which are physiologically toleratedespecially if used on humans and/or mammals. By this is understood in particular, in the context of this invention, the salt formed with a physiologically tolerated acid, that is to say salts of the particular active compound with inorganic or organic acids which are physiologically toleratedespecially if used on humans and/or mammals. Examples of physiologically tolerated salts of particular acids are salts of: hydrochloric acid, hydrobromic acid, sulfuric acid, methanesulfonic acid, formic acid, acetic acid, oxalic acid, succinic acid, malic acid, tartaric acid, mandelic acid, fumaric acid, lactic acid or citric acid.

[0105] The compounds of the invention may be present in crystalline form or in the form of free compounds like a free base or acid.

[0106] Any compound that is a solvate of a compound according to the invention like a compound according to general formula I defined above is understood to be also covered by the scope of the invention. Methods of solvation are generally known within the art. Suitable solvates are pharmaceutically acceptable solvates. The term solvate according to this invention is to be understood as meaning any form of the active compound according to the invention in which this compound has attached to it via non-covalent binding another molecule (most likely a polar solvent). Especially preferred examples include hydrates and alcoholates, like methanolates or ethanolates.

[0107] Any compound that is a prodrug of a compound according to the invention like a compound according to general formula I defined above is understood to be also covered by the scope of the invention. The term prodrug is used in its broadest sense and encompasses those derivatives that are converted in vivo to the compounds of the invention. Such derivatives would readily occur to those skilled in the art, and include, depending on the functional groups present in the molecule and without limitation, the following derivatives of the present compounds: esters, amino acid esters, phosphate esters, metal salts sulfonate esters, carbamates, and amides. Examples of well known methods of producing a prodrug of a given acting compound are known to those skilled in the art and can be found e.g. in Krogsgaard-Larsen et al. Textbook of Drug design and Discovery Taylor & Francis (April 2002).

[0108] Any compound that is a N-oxide of a compound according to the invention like a compound according to general formula I defined above is understood to be also covered by the scope of the invention.

[0109] Unless otherwise stated, the compounds of the invention are also meant to include compounds which differ only in the presence of one or more isotopically enriched atoms. For example, compounds having the present structures except for the replacement of a hydrogen by a deuterium or tritium, or the replacement of a carbon by .sup.13C- or .sup.14C-enriched carbon or of a nitrogen by .sup.15N-enriched nitrogen are within the scope of this invention. This would especially also apply to the provisos described above so that any mentioning of hydrogen or any H in a formula would also cover deuterium or tritium.

[0110] The compounds of formula (I) as well as their salts or solvates of the compounds are preferably in pharmaceutically acceptable or substantially pure form. By pharmaceutically acceptable form is meant, inter alia, having a pharmaceutically acceptable level of purity excluding normal pharmaceutical additives such as diluents and carriers, and including no material considered toxic at normal dosage levels. Purity levels for the drug substance are preferably above 50%, more preferably above 70%, most preferably above 90%. In a preferred embodiment it is above 95% of the compound of formula (I), or of its salts. This applies also to its solvates or prodrugs.

[0111] In a further embodiment the compound according to the invention of general Formula (I)

##STR00011##

wherein
m is 0, 1, 2, 3 or 4;
n is 0, 1, 2, 3 or 4;
p is 0, 1, 2, 3 or 4;
W is nitrogen or C(R.sub.4);
X is selected from a bond, substituted or unsubstituted aryl or C(R.sub.xR.sub.x); [0112] R.sub.x is selected from substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; [0113] R.sub.x, is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
the alkyl, alkenyl or alkynyl in R.sub.x or R.sub.x, if substituted, is substituted with one or more substituent/s selected from OR.sub.9, halogen, CN, haloalkyl, haloalkoxy, and NR.sub.9R.sub.9; [0114] wherein R.sub.9 and R.sub.9, are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl;
the aryl, heterocyclyl or cycloalkyl, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, in R.sub.x, if substituted, is substituted with one or more substituent/s selected from halogen, R.sub.10, OR.sub.10, NO.sub.2, NR.sub.10R.sub.10, NR.sub.10C(O)R.sub.10, NR.sub.10S(O).sub.2R.sub.10, S(O).sub.2NR.sub.10R.sub.10, NR.sub.10C(O)NR.sub.10R.sub.10, SR.sub.10, S(O)R.sub.10, S(O).sub.2R.sub.10, CN, haloalkyl, haloalkoxy, C(O)OR.sub.10, C(O)NR.sub.10R.sub.10, OCH.sub.2CH.sub.2OR.sub.10, NR.sub.10S(O).sub.2NR.sub.10R.sub.10, and C(CH.sub.3).sub.2OR.sub.10; [0115] wherein R.sub.10, R.sub.10 and R.sub.10 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, unsubstituted C.sub.2-6 alkynyl, unsubstituted aryl, unsubstituted alkylaryl, unsubstituted cycloalkyl and unsubstituted alkylcycloalkyl, unsubstituted heterocyclyl and unsubstituted alkyheterocyclyl;
R.sub.1 is selected from NR.sub.6R.sub.6, and substituted or unsubstituted N-containing-heterocyclyl; [0116] wherein R.sub.6 and R.sub.6, are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; [0117] wherein said cycloalkyl, aryl or heterocyclyl in R.sub.1 or R.sub.6, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, if substituted, is substituted with one or more substituent/s selected from halogen, R.sub.11, OR.sub.11, NO.sub.2, NR.sub.11R.sub.11, NR.sub.11C(O)R.sub.11, NR.sub.11S(O).sub.2R.sub.11, S(O).sub.2NR.sub.11R.sub.11, NR.sub.11C(O)NR.sub.11R.sub.11, SR.sub.11, S(O)R.sub.11, S(O).sub.2R.sub.11, CN, haloalkyl, haloalkoxy, C(O)OR.sub.11, C(O)NR.sub.11R.sub.11, OCH.sub.2CH.sub.2OH, NR.sub.11S(O).sub.2NR.sub.11R.sub.11, C(CH.sub.3).sub.2OR.sub.11, substituted or unsubstituted alkylaryl, substituted or unsubstituted alkylcycloalkyl and substituted or unsubstituted alkyheterocyclyl; [0118] wherein the alkyl, alkenyl or alkynyl in R.sub.6 or R.sub.6, if substituted, is substituted with one or more substituent/s selected from OR.sub.11, halogen, CN, haloalkyl, haloalkoxy and NR.sub.11R.sub.11; [0119] wherein R.sub.11, R.sub.11 and R.sub.11, are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl and unsubstituted C.sub.2-6 alkynyl;
R.sub.2 is selected from hydrogen, NR.sub.7R.sub.7, CN, CHR.sub.7R.sub.7 and substituted or unsubstituted heterocyclyl; [0120] wherein R.sub.7 and R.sub.7 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; [0121] wherein said cycloalkyl, aryl or heterocyclyl in R.sub.2, R.sub.7 or R.sub.7, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, if substituted, is substituted with one or more substituent/s selected from halogen, R.sub.12, OR.sub.12, NO.sub.2, NR.sub.12R.sub.12, NR.sub.12C(O)R.sub.12, NR.sub.12S(O).sub.2R.sub.12, S(O).sub.2NR.sub.12R.sub.12, NR.sub.12C(O)NR.sub.12R.sub.12, SR.sub.12, S(O)R.sub.12, S(O).sub.2R.sub.12, CN, haloalkyl, haloalkoxy, C(O)OR.sub.12, C(O)NR.sub.12R.sub.12, OCH.sub.2CH.sub.2OR.sub.12, NR.sub.12S(O).sub.2NR.sub.12R.sub.12 and C(CH.sub.3).sub.2OR.sub.12; [0122] wherein the alkyl, alkenyl or alkynyl in R.sub.7 or R.sub.7, if substituted, is substituted with one or more substituent/s selected from OR.sub.12, halogen, CN, haloalkyl, haloalkoxy and NR.sub.12R.sub.12; [0123] wherein R.sub.12, R.sub.12 and R.sub.12 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, and unsubstituted C.sub.2-6 alkenyl and unsubstituted C.sub.2-6 alkynyl;
R.sub.3 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
R.sub.4 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
R.sub.4 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
R.sub.5 and R.sub.5 are independently selected from hydrogen, halogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkyheterocyclyl, OR.sub.8, NO.sub.2, NR.sub.8R.sub.8, NR.sub.8C(O)R.sub.8, NR.sub.8S(O).sub.2R.sub.8, S(O).sub.2NR.sub.8R.sub.8, NR.sub.8C(O)NR.sub.8R.sub.8, SR.sub.8, S(O)R.sub.8, S(O).sub.2R.sub.8, CN, haloalkyl, haloalkoxy, C(O)OR.sub.8, C(O)NR.sub.8R.sub.8, OCH.sub.2CH.sub.2OR.sub.8, NR.sub.8S(O).sub.2NR.sub.8R.sub.8, and C(CH.sub.3).sub.2OR.sub.8; [0124] wherein R.sub.8, R.sub.8 and R.sub.8 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl;
R.sub.c and R.sub.c are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
alternatively, R.sub.c and R.sub.c may form with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;
the alkyl, alkenyl or alkynyl, other than those defined in R.sub.x, R.sub.x, R.sub.6, R.sub.6, R.sub.7 or R.sub.7, if substituted, is substituted with one or more substituent/s selected from OR.sub.13, halogen, CN, haloalkyl, haloalkoxy and NR.sub.13R.sub.13; [0125] wherein R.sub.13 and R.sub.13 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl;
the aryl, heterocyclyl or cycloalkyl, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, other than those defined in R.sub.x, R.sub.x, R.sub.1, R.sub.2, R.sub.6, R.sub.6, R.sub.7 or R.sub.7, if substituted, is substituted with one or more substituent/s selected from halogen, R.sub.14, OR.sub.14, NO.sub.2, NR.sub.14R.sub.14, NR.sub.14C(O)R.sub.14, NR.sub.14S(O).sub.2R.sub.14, S(O).sub.2NR.sub.14R.sub.14, NR.sub.14C(O)NR.sub.14R.sub.14, SR.sub.14, S(O)R.sub.14, S(O).sub.2R.sub.14, CN, haloalkyl, haloalkoxy, C(O)OR.sub.14, C(O)NR.sub.14R.sub.14, OCH.sub.2CH.sub.2OR.sub.14, NR.sub.14S(O).sub.2NR.sub.14R.sub.14 and C(CH.sub.3).sub.2OR.sub.14; [0126] wherein R.sub.14, R.sub.14 and R.sub.14 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, unsubstituted C.sub.2-6 alkynyl, unsubstituted aryl, unsubstituted alkylaryl, unsubstituted cycloalkyl and unsubstituted alkylcycloalkyl, unsubstituted heterocyclyl and unsubstituted alkyheterocyclyl;

[0127] These preferred compounds according to the invention are optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0128] In a further embodiment the compound according to the invention of general Formula (I)

##STR00012##

wherein
m is 0, 1, 2, 3 or 4;
n is 0, 1, 2, 3 or 4;
p is 0, 1, 2, 3 or 4;
X is selected from a bond, substituted or unsubstituted aryl or C(R.sub.xR.sub.x); [0129] R.sub.x is selected from substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; [0130] R.sub.x, is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
the alkyl, alkenyl or alkynyl in R.sub.x or R.sub.x, if substituted, is substituted with one or more substituent/s selected from OR.sub.9, halogen, CN, haloalkyl, haloalkoxy, and NR.sub.9R.sub.9; [0131] wherein R.sub.9 and R.sub.9 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl;
the aryl, heterocyclyl or cycloalkyl, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, in R.sub.x, if substituted, is substituted with one or more substituent/s selected from halogen, R.sub.10, OR.sub.10, NO.sub.2, NR.sub.10R.sub.10, NR.sub.10C(O)R.sub.10, NR.sub.10S(O).sub.2R.sub.10, S(O).sub.2NR.sub.10R.sub.10, NR.sub.10C(O)NR.sub.10R.sub.10, SR.sub.10, S(O)R.sub.10, S(O).sub.2R.sub.10, CN, haloalkyl, haloalkoxy, C(O)OR.sub.10, C(O)NR.sub.10R.sub.10, OCH.sub.2CH.sub.2OR.sub.10, NR.sub.10S(O).sub.2NR.sub.10R.sub.10 and C(CH.sub.3).sub.2OR.sub.10; [0132] wherein R.sub.10, R.sub.10 and R.sub.10 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, unsubstituted C.sub.2-6 alkynyl, unsubstituted aryl, unsubstituted alkylaryl, unsubstituted cycloalkyl and unsubstituted alkylcycloalkyl, unsubstituted heterocyclyl and unsubstituted alkyheterocyclyl;
R.sub.1 is selected from NR.sub.6R.sub.6, and substituted or unsubstituted N-containing-heterocyclyl; [0133] wherein R.sub.6 and R.sub.6, are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; [0134] wherein said cycloalkyl, aryl or heterocyclyl in R.sub.1 or R.sub.6, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, if substituted, is substituted with one or more substituent/s selected from halogen, R.sub.11, OR.sub.11, NO.sub.2, NR.sub.11R.sub.11, NR.sub.11C(O)R.sub.11, NR.sub.11S(O).sub.2R.sub.11, S(O).sub.2NR.sub.11R.sub.11, NR.sub.11C(O)NR.sub.11R.sub.11, SR.sub.11, S(O)R.sub.11, S(O).sub.2R.sub.11, CN, haloalkyl, haloalkoxy, C(O)OR.sub.11, C(O)NR.sub.11R.sub.11, OCH.sub.2CH.sub.2OH, NR.sub.11S(O).sub.2NR.sub.11R.sub.11, C(CH.sub.3).sub.2OR.sub.11, substituted or unsubstituted alkylaryl, substituted or unsubstituted alkylcycloalkyl and substituted or unsubstituted alkyheterocyclyl; [0135] wherein the alkyl, alkenyl or alkynyl in R.sub.6 or R.sub.6, if substituted, is substituted with one or more substituent/s selected from OR.sub.11, halogen, CN, haloalkyl, haloalkoxy and NR.sub.11R.sub.11; [0136] wherein R.sub.11, R.sub.11 and R.sub.11 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl and unsubstituted C.sub.2-6 alkynyl;
R.sub.2 is selected from hydrogen, NR.sub.7R.sub.7, CN, CHR.sub.7R.sub.7 and substituted or unsubstituted heterocyclyl; [0137] wherein R.sub.7 and R.sub.7 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; [0138] wherein said cycloalkyl, aryl or heterocyclyl in R.sub.2, R.sub.7 or R.sub.7, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, if substituted, is substituted with one or more substituent/s selected from halogen, R.sub.12, OR.sub.12, NO.sub.2, NR.sub.12R.sub.12, NR.sub.12C(O)R.sub.12, NR.sub.12S(O).sub.2R.sub.12, S(O).sub.2NR.sub.12R.sub.12, NR.sub.12C(O)NR.sub.12R.sub.12, SR.sub.12, S(O)R.sub.12, S(O).sub.2R.sub.12, CN, haloalkyl, haloalkoxy, C(O)OR.sub.12, C(O)NR.sub.12R.sub.12, OCH.sub.2CH.sub.2OR.sub.12, NR.sub.12S(O).sub.2NR.sub.12R.sub.12 and C(CH.sub.3).sub.2OR.sub.12; [0139] wherein the alkyl, alkenyl or alkynyl in R.sub.7 or R.sub.7, if substituted, is substituted with one or more substituent/s selected from OR.sub.12, halogen, CN, haloalkyl, haloalkoxy and NR.sub.12R.sub.12; [0140] wherein R.sub.12, R.sub.12 and R.sub.12 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, and unsubstituted C.sub.2-6 alkenyl and unsubstituted C.sub.2-6 alkynyl;
R.sub.3 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
R.sub.4 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
R.sub.4 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
R.sub.5 and R.sub.5 are independently selected from hydrogen, halogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkyheterocyclyl, OR.sub.8, NO.sub.2, NR.sub.8R.sub.8, NR.sub.8C(O)R.sub.8, NR.sub.8S(O).sub.2R.sub.8, S(O).sub.2NR.sub.8R.sub.8, NR.sub.8C(O)NR.sub.8R.sub.8, SR.sub.8, S(O)R.sub.8, S(O).sub.2R.sub.8, CN, haloalkyl, haloalkoxy, C(O)OR.sub.8, C(O)NR.sub.8R.sub.8, OCH.sub.2CH.sub.2OR.sub.8, NR.sub.8S(O).sub.2NR.sub.8R.sub.8, and C(CH.sub.3).sub.2OR.sub.8; [0141] wherein R.sub.8, R.sub.8, and R.sub.8 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl;
R.sub.c and R.sub.c are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
alternatively, R.sub.c and R.sub.c may form with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;
the alkyl, alkenyl or alkynyl, other than those defined in R.sub.x, R.sub.x, R.sub.6, R.sub.6, R.sub.7 or R.sub.7, if substituted, is substituted with one or more substituent/s selected from OR.sub.13, halogen, CN, haloalkyl, haloalkoxy and NR.sub.13R.sub.13; [0142] wherein R.sub.13 and R.sub.13 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl;
the aryl, heterocyclyl or cycloalkyl, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, other than those defined in R.sub.x, R.sub.x, R.sub.1, R.sub.2, R.sub.6, R.sub.6, R.sub.7 or R.sub.7, if substituted, is substituted with one or more substituent/s selected from halogen, R.sub.14, OR.sub.14, NO.sub.2, NR.sub.14R.sub.14, NR.sub.14C(O)R.sub.14, NR.sub.14S(O).sub.2R.sub.14, S(O).sub.2NR.sub.14R.sub.14, NR.sub.14C(O)NR.sub.14R.sub.14, SR.sub.14, S(O)R.sub.14, S(O).sub.2R.sub.14, CN, haloalkyl, haloalkoxy, C(O)OR.sub.14, C(O)NR.sub.14R.sub.14, OCH.sub.2CH.sub.2OR.sub.14, NR.sub.14S(O).sub.2NR.sub.14R.sub.14 and C(CH.sub.3).sub.2OR.sub.14; [0143] wherein R.sub.14, R.sub.14 and R.sub.14 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, unsubstituted C.sub.2-6 alkynyl, unsubstituted aryl, unsubstituted alkylaryl, unsubstituted cycloalkyl and unsubstituted alkylcycloalkyl, unsubstituted heterocyclyl and unsubstituted alkyheterocyclyl;

[0144] These preferred compounds according to the invention are optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0145] In a further embodiment the compound according to the invention of general Formula (I.sup.2)

##STR00013##

wherein
m is 0, 1, 2, 3 or 4;
n is 0, 1, 2, 3 or 4;
p is 0, 1, 2, 3 or 4;
X is selected from a bond, substituted or unsubstituted aryl or C(R.sub.xR.sub.x); [0146] R.sub.x is selected from substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; [0147] R.sub.x is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
the alkyl, alkenyl or alkynyl in R.sub.x or R.sub.x, if substituted, is substituted with one or more substituent/s selected from OR.sub.9, halogen, CN, haloalkyl, haloalkoxy, and NR.sub.9R.sub.9; [0148] wherein R.sub.9 and R.sub.9 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl;
the aryl, heterocyclyl or cycloalkyl, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, in R.sub.x, if substituted, is substituted with one or more substituent/s selected from halogen, R.sub.10, OR.sub.10, NO.sub.2, NR.sub.10R.sub.10, NR.sub.10C(O)R.sub.10, NR.sub.10S(O).sub.2R.sub.10, S(O).sub.2NR.sub.10R.sub.10, NR.sub.10C(O)NR.sub.10R.sub.10, SR.sub.10, S(O)R.sub.10, S(O).sub.2R.sub.10, CN, haloalkyl, haloalkoxy, C(O)OR.sub.10, C(O)NR.sub.10R.sub.10, OCH.sub.2CH.sub.2OR.sub.10, NR.sub.10S(O).sub.2NR.sub.10R.sub.10 and C(CH.sub.3).sub.2OR.sub.10; [0149] wherein R.sub.10, R.sub.10 and R.sub.10 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, unsubstituted C.sub.2-6 alkynyl, unsubstituted aryl, unsubstituted alkylaryl, unsubstituted cycloalkyl and unsubstituted alkylcycloalkyl, unsubstituted heterocyclyl and unsubstituted alkyheterocyclyl;
R.sub.1 is selected from NR.sub.6R.sub.6, and substituted or unsubstituted N-containing-heterocyclyl; [0150] wherein R.sub.6 and R.sub.6, are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; [0151] wherein said cycloalkyl, aryl or heterocyclyl in R.sub.1 or R.sub.6, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, if substituted, is substituted with one or more substituent/s selected from halogen, R.sub.11, OR.sub.11, NO.sub.2, NR.sub.11R.sub.11, NR.sub.11C(O)R.sub.11, NR.sub.11S(O).sub.2R.sub.11, S(O).sub.2NR.sub.11R.sub.11, NR.sub.11C(O)NR.sub.11R.sub.11, SR.sub.11, S(O)R.sub.11, S(O).sub.2R.sub.11, CN, haloalkyl, haloalkoxy, C(O)OR.sub.11, C(O)NR.sub.11R.sub.11, OCH.sub.2CH.sub.2OH, NR.sub.11S(O).sub.2NR.sub.11R.sub.11, C(CH.sub.3).sub.2OR.sub.11, substituted or unsubstituted alkylaryl, substituted or unsubstituted alkylcycloalkyl and substituted or unsubstituted alkyheterocyclyl; [0152] wherein the alkyl, alkenyl or alkynyl in R.sub.6 or R.sub.6, if substituted, is substituted with one or more substituent/s selected from OR.sub.11, halogen, CN, haloalkyl, haloalkoxy and NR.sub.11R.sub.11; [0153] wherein R.sub.11, R.sub.11 and R.sub.11 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl and unsubstituted C.sub.2-6 alkynyl;
R.sub.2 is selected from hydrogen, NR.sub.7R.sub.7, CN, CHR.sub.7R.sub.7 and substituted or unsubstituted heterocyclyl; [0154] wherein R.sub.7 and R.sub.7 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; [0155] wherein said cycloalkyl, aryl or heterocyclyl in R.sub.2, R.sub.7 or R.sub.7, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, if substituted, is substituted with one or more substituent/s selected from halogen, R.sub.12, OR.sub.12, NO.sub.2, NR.sub.12R.sub.12, NR.sub.12C(O)R.sub.12, NR.sub.12S(O).sub.2R.sub.12, S(O).sub.2NR.sub.12R.sub.12, NR.sub.12C(O)NR.sub.12R.sub.12, SR.sub.12, S(O)R.sub.12, S(O).sub.2R.sub.12, CN, haloalkyl, haloalkoxy, C(O)OR.sub.12, C(O)NR.sub.12R.sub.12, OCH.sub.2CH.sub.2OR.sub.12, NR.sub.12S(O).sub.2NR.sub.12R.sub.12 and C(CH.sub.3).sub.2OR.sub.12; [0156] wherein the alkyl, alkenyl or alkynyl in R.sub.7 or R.sub.7, if substituted, is substituted with one or more substituent/s selected from OR.sub.12, halogen, CN, haloalkyl, haloalkoxy and NR.sub.12R.sub.12; [0157] wherein R.sub.12, R.sub.12 and R.sub.12 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, and unsubstituted C.sub.2-6 alkenyl and unsubstituted C.sub.2-6 alkynyl;
R.sub.3 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
R.sub.4 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
R.sub.4 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
R.sub.5 and R.sub.5 are independently selected from hydrogen, halogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkyheterocyclyl, OR.sub.8, NO.sub.2, NR.sub.8R.sub.8, NR.sub.8C(O)R.sub.8, NR.sub.8S(O).sub.2R.sub.8, S(O).sub.2NR.sub.8R.sub.8, NR.sub.8C(O)NR.sub.8R.sub.8, SR.sub.8, S(O)R.sub.8, S(O).sub.2R.sub.8, CN, haloalkyl, haloalkoxy, C(O)OR.sub.8, C(O)NR.sub.8R.sub.8, OCH.sub.2CH.sub.2OR.sub.8, NR.sub.8S(O).sub.2NR.sub.8R.sub.8 and C(CH.sub.3).sub.2OR.sub.8; [0158] wherein R.sub.8, R.sub.8, and R.sub.8 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl;
R.sub.c and R.sub.c are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
alternatively, R.sub.c and R.sub.c may form with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;
the alkyl, alkenyl or alkynyl, other than those defined in R.sub.x, R.sub.x, R.sub.6, R.sub.6, R.sub.7 or R.sub.7, if substituted, is substituted with one or more substituent/s selected from OR.sub.13, halogen, CN, haloalkyl, haloalkoxy and NR.sub.13R.sub.13; [0159] wherein R.sub.13 and R.sub.13 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl;
the aryl, heterocyclyl or cycloalkyl, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, other than those defined in R.sub.x, R.sub.x, R.sub.1, R.sub.2, R.sub.6, R.sub.6, R.sub.7 or R.sub.7, if substituted, is substituted with one or more substituent/s selected from halogen, R.sub.14, OR.sub.14, NO.sub.2, NR.sub.14R.sub.14, NR.sub.14C(O)R.sub.14, NR.sub.14S(O).sub.2R.sub.14, S(O).sub.2NR.sub.14R.sub.14, NR.sub.14C(O)NR.sub.14R.sub.14, SR.sub.14, S(O)R.sub.14, S(O).sub.2R.sub.14, CN, haloalkyl, haloalkoxy, C(O)OR.sub.14, C(O)NR.sub.14R.sub.14, OCH.sub.2CH.sub.2OR.sub.14, NR.sub.14S(O).sub.2NR.sub.14R.sub.14 and C(CH.sub.3).sub.2OR.sub.14; [0160] wherein R.sub.14, R.sub.14 and R.sub.14 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, unsubstituted C.sub.2-6 alkynyl, unsubstituted aryl, unsubstituted alkylaryl, unsubstituted cycloalkyl and unsubstituted alkylcycloalkyl, unsubstituted heterocyclyl and unsubstituted alkyheterocyclyl;

[0161] These preferred compounds according to the invention are optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0162] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

m is 0, 1, 2, 3 or 4;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0163] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

m is 0, 1 or 2;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0164] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

n is 0, 1, 2, 3 or 4;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0165] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

n is 0, 1, 2 or 3;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0166] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

p is 0, 1, 2, 3 or 4;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0167] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

p is 0;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0168] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

W is nitrogen or C(R.sub.4);
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0169] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

W is nitrogen;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0170] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

X is selected from a bond, substituted or unsubstituted aryl or C(R.sub.xR.sub.x);
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0171] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

X is a bond;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0172] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

X is C(R.sub.xR.sub.x);
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0173] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein [0174] R.sub.x is selected from substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0175] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein [0176] R.sub.x is selected from substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0177] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein [0178] R.sub.x is selected from substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl and substituted or unsubstituted heterocyclyl
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0179] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein [0180] R.sub.x is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0181] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein [0182] R.sub.x is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0183] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

R.sub.xa is independently selected from hydrogen, halogen, OR.sub.10, CN, haloalkoxy, and C(O)NR.sub.10R.sub.10;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0184] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

R.sub.1 is selected from NR.sub.6R.sub.6 and substituted or unsubstituted N-containing-heterocyclyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0185] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

R.sub.2 is selected from hydrogen, NR.sub.7R.sub.7, CN, CHR.sub.7R.sub.7 and substituted or unsubstituted heterocyclyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0186] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

R.sub.2 is selected from NR.sub.7R.sub.7 and substituted or unsubstituted heterocyclyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0187] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

R.sub.3 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0188] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

R.sub.3 is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0189] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

R.sub.3 is substituted or unsubstituted C.sub.1-6 alkyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0190] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

R.sub.4 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0191] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

R.sub.4 is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0192] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

R.sub.4 is substituted or unsubstituted C.sub.1-6 alkyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0193] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

R.sub.4 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0194] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

R.sub.4 is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0195] In a further embodiment the compound according to the invention of general Formula (I) is a compound wherein

R.sub.5 and R.sub.5 are independently selected from hydrogen, halogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkyheterocyclyl, OR.sub.8, NO.sub.2, NR.sub.8R.sub.8, NR.sub.8C(O)R.sub.8, NR.sub.8S(O).sub.2R.sub.8, S(O).sub.2NR.sub.8R.sub.8, NR.sub.8C(O)NR.sub.8R.sub.8, SR.sub.8, S(O)R.sub.8, S(O).sub.2R.sub.8, CN, haloalkyl, haloalkoxy, C(O)OR.sub.8, C(O)NR.sub.8R.sub.8, OCH.sub.2CH.sub.2OR.sub.8, NR.sub.8S(O).sub.2NR.sub.8R.sub.8, and C(CH.sub.3).sub.2OR.sub.8;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0196] In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein

R.sub.5 and R.sub.5 are independently selected from hydrogen, halogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkyheterocyclyl, OR.sub.8, NO.sub.2, NR.sub.8R.sub.8, NR.sub.8C(O)R.sub.8, NR.sub.8S(O).sub.2R.sub.8, S(O).sub.2NR.sub.8R.sub.8, NR.sub.8C(O)NR.sub.8R.sub.8, SR.sub.8, S(O)R.sub.8, S(O).sub.2R.sub.8, CN, haloalkyl, haloalkoxy, C(O)OR.sub.8, C(O)NR.sub.8R.sub.8, OCH.sub.2CH.sub.2OR.sub.8, NR.sub.8S(O).sub.2NR.sub.8R.sub.8, and C(CH.sub.3).sub.2OR.sub.8;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0197] In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein

R.sub.c and R.sub.c are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0198] In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein

R.sub.c and R.sub.c are independently selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0199] In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein

R.sub.c and R.sub.c may form with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0200] In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein

R.sub.6 and R.sub.6 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0201] In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein

R.sub.6 and R.sub.6 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0202] In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein

R.sub.6 and R.sub.6 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl and substituted or unsubstituted alkylaryl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0203] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

R.sub.6a is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl and substituted or unsubstituted alkylaryl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0204] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

R.sub.6a is substituted or unsubstituted alkylaryl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0205] In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein

R.sub.7 and R.sub.7 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0206] In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein

R.sub.7 and R.sub.7 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0207] In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein

R.sub.7 and R.sub.7 are independently selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0208] In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein

R.sub.8, R.sub.8 and R.sub.8 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0209] In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein

R.sub.8, R.sub.8 and R.sub.8 are independently selected from hydrogen and unsubstituted C.sub.1-6 alkyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0210] In another preferred embodiment of the compound according to the invention of general Formula (I) is a compound wherein

R.sub.9 and R.sub.9 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0211] In another preferred embodiment of the compound according to the invention of general Formula (I) is a compound wherein

R.sub.9 and R.sub.9 are independently selected from hydrogen and unsubstituted C.sub.1-6 alkyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0212] In another preferred embodiment of the compound according to the invention of general Formula (I) is a compound wherein

R.sub.10, R.sub.10 and R.sub.10 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, unsubstituted C.sub.2-6 alkynyl, unsubstituted aryl, unsubstituted alkylaryl, unsubstituted cycloalkyl and unsubstituted alkylcycloalkyl, unsubstituted heterocyclyl and unsubstituted alkyheterocyclyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0213] In another preferred embodiment of the compound according to the invention of general Formula (I) is a compound wherein

R.sub.10, R.sub.10 and R.sub.10 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted aryl, unsubstituted alkylaryl, unsubstituted cycloalkyl and unsubstituted alkylcycloalkyl, unsubstituted heterocyclyl and unsubstituted alkyheterocyclyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0214] In another preferred embodiment of the compound according to the invention of general Formula (I) is a compound wherein

R.sub.10, R.sub.10 and R.sub.10 are independently selected from hydrogen and unsubstituted C.sub.1-6 alkyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0215] In another preferred embodiment of the compound according to the invention of general Formula (I) is a compound wherein

R.sub.11, R.sub.11 and R.sub.11 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl and unsubstituted C.sub.2-6 alkynyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0216] In another preferred embodiment of the compound according to the invention of general Formula (I) is a compound wherein

R.sub.11, R.sub.11 and R.sub.11 are independently selected from hydrogen and unsubstituted C.sub.1-6 alkyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0217] In another preferred embodiment of the compound according to the invention of general Formula (I) is a compound wherein

R.sub.12, R.sub.12 and R.sub.12 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, and unsubstituted C.sub.2-6 alkenyl and unsubstituted C.sub.2-6 alkynyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0218] In another preferred embodiment of the compound according to the invention of general Formula (I) is a compound wherein

R.sub.12, R.sub.12 and R.sub.12 are independently selected from hydrogen and unsubstituted C.sub.1-6 alkyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0219] In another preferred embodiment of the compound according to the invention of general Formula (I) is a compound wherein

R.sub.13 and R.sub.13 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0220] In another preferred embodiment of the compound according to the invention of general Formula (I) is a compound wherein

R.sub.13 and R.sub.13 are independently selected from hydrogen and unsubstituted C.sub.1-6 alkyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0221] In another preferred embodiment of the compound according to the invention of general Formula (I) is a compound wherein

R.sub.14, R.sub.14 and R.sub.14 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, unsubstituted C.sub.2-6 alkynyl, unsubstituted aryl, unsubstituted alkylaryl, unsubstituted cycloalkyl and unsubstituted alkylcycloalkyl, unsubstituted heterocyclyl and unsubstituted alkyheterocyclyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0222] In another preferred embodiment of the compound according to the invention of general Formula (I) is a compound wherein

R.sub.14, R.sub.14 and R.sub.14 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted aryl, unsubstituted alkylaryl, unsubstituted cycloalkyl and unsubstituted alkylcycloalkyl, unsubstituted heterocyclyl and unsubstituted alkyheterocyclyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0223] In another preferred embodiment of the compound according to the according to the invention of general Formula (I) is a compound wherein

X is selected from a bond, substituted or unsubstituted aryl or C(R.sub.xR.sub.x); [0224] R.sub.x is selected from substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; [0225] R.sub.x is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0226] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

m is 0, 1, 2, 3 or 4; preferably m is 0, 1 or 2;
and/or
n is 0, 1, 2, 3 or 4; preferably n is 0, 1, 2 or 3;
and/or
p is 0, 1, 2, 3 or 4; preferably p is 0;
and/or
W is nitrogen or C(R.sub.4); preferably W is nitrogen;
and/or
X is selected from a bond, substituted or unsubstituted aryl or C(R.sub.xR.sub.x); preferably X is selected from a bond, CH(phenyl)-, CH(benzyl)-, CH(pyridine)-, CH(thiophen)- and CH(thiazole)-;
and/or
R.sub.x is selected from substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; preferably R.sub.x is selected from substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl and substituted or unsubstituted heterocyclyl; more preferably R.sub.x is selected from substituted or unsubstituted phenyl, substituted or unsubstituted benzyl, substituted or unsubstituted pyridine, substituted or unsubstituted thiophen and substituted or unsubstituted thiazole;
and/or [0227] R.sub.x is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl; preferably R.sub.x is hydrogen;
and/or
R.sub.xa is independently selected from hydrogen, halogen, OR.sub.10, CN, haloalkoxy, and C(O)NR.sub.10R.sub.10, preferably R.sub.xa is independently selected from hydrogen, fluorine, O methyl, OCF.sub.3, C(O)NH.sub.2 and CN;
and/or
R.sub.1 is selected from NR.sub.6R.sub.6 and substituted or unsubstituted N-containing-heterocyclyl; preferably R.sub.1 is selected from substituted or unsubstituted piperidin, substituted or unsubstituted tetrahydroisoquinoline, substituted or unsubstituted morpholine, NH-methyl, N(methyl).sub.2, NH-ethyl, NH.sub.2, N(methyl)(benzyl)-, NHCH.sub.2CH.sub.2F and NHCH.sub.2CHF.sub.2;
and/or
R.sub.2 is selected from hydrogen, NR.sub.7R.sub.7, CN, CHR.sub.7R.sub.7 and substituted or unsubstituted heterocyclyl; preferably R.sub.2 is selected from NH.sub.2, substituted or unsubstituted NH-methyl, substituted or unsubstituted N(methyl).sub.2, substituted or unsubstituted N(ethyl)(methyl), substituted or unsubstituted N(methyl)(propyl), substituted or unsubstituted azetidine; more preferably R.sub.2 is selected from NH methyl, N(methyl).sub.2, N(methyl)(CH.sub.2CH.sub.2OH), N(methyl)(CH.sub.2CH.sub.2CH.sub.2OH) and substituted or unsubstituted azetidine;
and/or
R.sub.3 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl; preferably R.sub.3 is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; more preferably R.sub.3 is substituted or unsubstituted methyl;
and/or
R.sub.4 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl; preferably R.sub.4 is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; more preferably R.sub.4 is substituted or unsubstituted methyl;
and/or
R.sub.4 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
and/or
R.sub.5 and R.sub.5 are independently selected from hydrogen, halogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkyheterocyclyl, OR.sub.8, NO.sub.2, NR.sub.8R.sub.8, NR.sub.8C(O)R.sub.8, NR.sub.8S(O).sub.2R.sub.8, S(O).sub.2NR.sub.8R.sub.8, NR.sub.8C(O)NR.sub.8R.sub.8, SR.sub.8, S(O)R.sub.8, S(O).sub.2R.sub.8, CN, haloalkyl, haloalkoxy, C(O)OR.sub.8, C(O)NR.sub.8R.sub.8, OCH.sub.2CH.sub.2OR.sub.8, NR.sub.8S(O).sub.2NR.sub.8R.sub.8 and C(CH.sub.3).sub.2OR.sub.8; preferably R.sub.5 and R.sub.5 are both hydrogen;
and/or
R.sub.6 and R.sub.6 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; preferably R.sub.6 and R.sub.6 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl and substituted or unsubstituted alkylaryl; more preferably R.sub.6 and R.sub.6 are independently selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl and substituted or unsubstituted benzyl; even more preferably R.sub.6 and R.sub.6 are independently selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl, CH.sub.2CH.sub.2F, CH.sub.2CHF.sub.2 and substituted or unsubstituted benzyl
and/or
R.sub.6a is selected from substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkyheterocyclyl substituted or unsubstituted alkylaryl; preferably R.sub.6a is substituted or unsubstituted phenethyl;
and/or
R.sub.7 and R.sub.7 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; preferably R.sub.7 and R.sub.7 are independently selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; more preferably R.sub.7 and R.sub.7 are independently selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl, substituted or unsubstituted propyl; even more preferably R.sub.7 and R.sub.7 are independently selected from hydrogen, substituted or unsubstituted methyl, CH.sub.2CH.sub.2OH and CH.sub.2CH.sub.2CH.sub.2OH;
and/or
R.sub.8, R.sub.8 and R.sub.8 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl;
and/or
R.sub.c and R.sub.c are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl; preferably, R.sub.c and R.sub.c are both hydrogen;
and/or
R.sub.c and R.sub.c may form with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; preferably, R.sub.c and R.sub.c form a cyclopropyl;
and/or
R.sub.9 and R.sub.9 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl; preferably R.sub.9 and R.sub.9 are independently selected from hydrogen and unsubstituted C.sub.1-6 alkyl;
and/or
R.sub.10, R.sub.10 and R.sub.10 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, unsubstituted C.sub.2-6 alkynyl, unsubstituted aryl, unsubstituted alkylaryl, unsubstituted cycloalkyl and unsubstituted alkylcycloalkyl, unsubstituted heterocyclyl and unsubstituted alkyheterocyclyl; preferably R.sub.10, R.sub.10 and R.sub.10 are independently selected from hydrogen and unsubstituted C.sub.1-6 alkyl; more preferably R.sub.10 and R.sub.10 are independently selected from hydrogen and unsubstituted methyl;
and/or
R.sub.11, R.sub.11 and R.sub.11 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl and unsubstituted C.sub.2-6 alkynyl; preferably R.sub.11, R.sub.11 and R.sub.11 are independently selected from hydrogen and unsubstituted C.sub.1-6 alkyl;
and/or
R.sub.12, R.sub.12, and R.sub.12 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, and unsubstituted C.sub.2-6 alkenyl and unsubstituted C.sub.2-6 alkynyl; preferably R.sub.12, R.sub.12 and R.sub.12, are independently selected from hydrogen and unsubstituted methyl;
and/or
R.sub.13 and R.sub.13 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl;
and/or
R.sub.14, R.sub.14 and R.sub.14 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, unsubstituted C.sub.2-6 alkynyl, unsubstituted aryl, unsubstituted alkylaryl, unsubstituted cycloalkyl and unsubstituted alkylcycloalkyl, unsubstituted heterocyclyl and unsubstituted alkyheterocyclyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0228] In another preferred embodiment of the compound according to the invention of general Formula (I) is a compound wherein

m is 0, 1, 2, 3 or 4;
and/or
n is 0, 1, 2, 3 or 4;
and/or
p is 0, 1, 2, 3 or 4;
and/or
W is nitrogen or C(R.sub.4);
and/or
X is selected from a bond, substituted or unsubstituted aryl or C(R.sub.xR.sub.x);
wherein [0229] the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl;
and/or
R.sub.x is selected from substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl
wherein [0230] the alkyl is C.sub.1-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; more preferably the alkyl is methyl; [0231] and/or [0232] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0233] and/or [0234] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0235] and/or [0236] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; [0237] and/or [0238] the cycloalkyl is C.sub.3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C.sub.3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C.sub.3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; [0239] and/or [0240] the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; preferably the aryl is phenyl; [0241] and/or [0242] the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline; preferably the heterocyclyl is pyridine, thiophen or thiazole;
and/or
R.sub.x is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
wherein [0243] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl, [0244] and/or [0245] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0246] and/or [0247] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
and/or
R.sub.1 is selected from NR.sub.6R.sub.6 and substituted or unsubstituted N-containing-heterocyclyl;
wherein [0248] the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline; even more preferably the heterocyclyl is piperidin, tetrahydroisoquinoline or morpholine; [0249] and/or
R.sub.2 is selected from hydrogen, NR.sub.7R.sub.7, CN, CHR.sub.7R.sub.7 and substituted or unsubstituted heterocyclyl; [0250] wherein [0251] the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline; even more preferably the heterocyclyl is azetidine; [0252] and/or
R.sub.3 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl
wherein [0253] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl, more preferably the C.sub.1-6 alkyl is methyl; [0254] and/or [0255] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0256] and/or [0257] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; [0258] and/or
R.sub.4 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
wherein [0259] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl, more preferably the C.sub.1-6 alkyl is methyl; [0260] and/or [0261] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0262] and/or [0263] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; [0264] and/or
R.sub.4 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
wherein [0265] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably methyl; [0266] and/or [0267] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0268] and/or [0269] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; [0270] and/or
R.sub.5 and R.sub.5 are independently selected from hydrogen, halogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkyheterocyclyl, OR.sub.8, NO.sub.2, NR.sub.8R.sub.8, NR.sub.8C(O)R.sub.8, NR.sub.8S(O).sub.2R.sub.8, S(O).sub.2NR.sub.8R.sub.8, NR.sub.8C(O)NR.sub.8R.sub.8, SR.sub.8, S(O)R.sub.8, S(O).sub.2R.sub.8, CN, haloalkyl, haloalkoxy, C(O)OR.sub.8, C(O)NR.sub.8R.sub.8, OCH.sub.2CH.sub.2OR.sub.8, NR.sub.8S(O).sub.2NR.sub.8R.sub.8 and C(CH.sub.3).sub.2OR.sub.8;
wherein [0271] the alkyl is C.sub.1-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0272] and/or [0273] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0274] and/or [0275] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0276] and/or [0277] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; [0278] and/or [0279] the cycloalkyl is C.sub.3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C.sub.3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C.sub.3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; [0280] and/or [0281] the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; [0282] and/or [0283] the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole, oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline; [0284] and/or
R.sub.c and R.sub.c are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
wherein [0285] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0286] and/or [0287] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0288] and/or [0289] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; [0290] and/or
R.sub.c and R.sub.c may form with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;
wherein [0291] the cycloalkyl is C.sub.3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C.sub.3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C.sub.3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; preferably the cycloalkyl is cyclopropyl; [0292] and/or
R.sub.6 and R.sub.6 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl;
wherein [0293] the alkyl is C.sub.1-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the alkyl is methyl; [0294] and/or [0295] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl, more preferably the C.sub.1-6 alkyl is methyl or ethyl; [0296] and/or [0297] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0298] and/or [0299] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; [0300] and/or [0301] the cycloalkyl is C.sub.3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C.sub.3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C.sub.3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; [0302] and/or [0303] the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; more preferably the aryl is phenyl; [0304] and/or [0305] the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole, oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline; [0306] and/or
R.sub.6a is selected from substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkyheterocyclyl substituted or unsubstituted alkylaryl;
wherein [0307] the alkyl is C.sub.1-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the alkyl is ethyl; [0308] and/or [0309] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the C.sub.1-6 alkyl is methyl [0310] and/or [0311] the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; preferably the aryl is phenyl; [0312] and/or
R.sub.7 and R.sub.7 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl;
wherein [0313] the alkyl is C.sub.1-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0314] and/or [0315] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl, more preferably the C.sub.1-6 alkyl is methyl, ethyl or propyl; [0316] and/or [0317] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0318] and/or [0319] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; [0320] and/or [0321] the cycloalkyl is C.sub.3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C.sub.3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C.sub.3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; [0322] and/or [0323] the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; [0324] and/or [0325] the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole, oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline; [0326] and/or
R.sub.8, R.sub.8 and R.sub.8 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl and unsubstituted C.sub.2-6 alkynyl;
wherein [0327] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0328] and/or [0329] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0330] and/or [0331] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; [0332] and/or
R.sub.9 and R.sub.9 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl;
wherein [0333] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0334] and/or [0335] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0336] and/or [0337] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
and/or
R.sub.10, R.sub.10 and R.sub.10 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, unsubstituted C.sub.2-6 alkynyl, unsubstituted aryl, unsubstituted alkylaryl, unsubstituted cycloalkyl and unsubstituted alkylcycloalkyl, unsubstituted heterocyclyl and unsubstituted alkyheterocyclyl;
wherein [0338] the alkyl is C.sub.1-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0339] and/or [0340] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl, more preferably the C.sub.1-6 alkyl is methyl; and/or [0341] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0342] and/or [0343] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; [0344] and/or [0345] the cycloalkyl is C.sub.3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C.sub.3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C.sub.3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; [0346] and/or [0347] the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; [0348] and/or [0349] the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole, oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline; [0350] and/or
R.sub.11, R.sub.11 and R.sub.11 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl and unsubstituted C.sub.2-6 alkynyl;
wherein [0351] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0352] and/or [0353] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0354] and/or [0355] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; [0356] and/or
R.sub.12, R.sub.12 and R.sub.12 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, and unsubstituted C.sub.2-6 alkenyl and unsubstituted C.sub.2-6 alkynyl;
wherein [0357] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl, more preferably the C.sub.1-6 alkyl is methyl; [0358] and/or [0359] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0360] and/or [0361] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; [0362] and/or
R.sub.13 and R.sub.13 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl; [0363] wherein [0364] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0365] and/or [0366] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0367] and/or [0368] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; [0369] and/or
R.sub.14, R.sub.14 and R.sub.14 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, unsubstituted C.sub.2-6 alkynyl, unsubstituted aryl, unsubstituted alkylaryl, unsubstituted cycloalkyl and unsubstituted alkylcycloalkyl, unsubstituted heterocyclyl and unsubstituted alkyheterocyclyl;
wherein [0370] the alkyl is C.sub.1-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0371] and/or [0372] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0373] and/or [0374] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0375] and/or [0376] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; [0377] and/or [0378] the cycloalkyl is C.sub.3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C.sub.3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C.sub.3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; [0379] and/or [0380] the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; [0381] and/or [0382] the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole, oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0383] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R.sub.x as defined in any of the embodiments of the present invention, [0384] the alkyl is C.sub.1-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; more preferably the alkyl is methyl; [0385] and/or [0386] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0387] and/or [0388] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0389] and/or [0390] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; [0391] and/or [0392] the cycloalkyl is C.sub.3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C.sub.3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C.sub.3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; [0393] and/or [0394] the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; preferably the aryl is phenyl; [0395] and/or [0396] the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline; preferably the heterocyclyl is pyridine, thiophen or thiazole;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0397] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R.sub.x, as defined in any of the embodiments of the present invention, [0398] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl, [0399] and/or [0400] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0401] and/or [0402] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0403] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R.sub.1 as defined in any of the embodiments of the present invention, [0404] the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline; even more preferably the heterocyclyl is piperidin, tetrahydroisoquinoline or morpholine;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0405] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R.sub.2 as defined in any of the embodiments of the present invention, [0406] the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline; even more preferably the heterocyclyl is azetidine;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0407] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R.sub.3 as defined in any of the embodiments of the present invention, [0408] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl, more preferably the C.sub.1-6 alkyl is methyl; [0409] and/or [0410] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0411] and/or [0412] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0413] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R.sub.4 as defined in any of the embodiments of the present invention, [0414] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl, more preferably the C.sub.1-6 alkyl is methyl; [0415] and/or [0416] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0417] and/or [0418] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0419] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R.sub.4 as defined in any of the embodiments of the present invention, [0420] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably methyl; [0421] and/or [0422] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0423] and/or [0424] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0425] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R.sub.5 and R.sub.5 as defined in any of the embodiments of the present invention, [0426] the alkyl is C.sub.1-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0427] and/or [0428] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0429] and/or [0430] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0431] and/or [0432] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; [0433] and/or [0434] the cycloalkyl is C.sub.3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C.sub.3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C.sub.3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; [0435] and/or [0436] the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; [0437] and/or [0438] the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole, oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0439] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R.sub.c and R.sub.c as defined in any of the embodiments of the present invention, [0440] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0441] and/or [0442] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0443] and/or [0444] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0445] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R.sub.c and R.sub.c as defined in any of the embodiments of the present invention, [0446] the cycloalkyl is C.sub.3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C.sub.3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C.sub.3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; preferably the cycloalkyl is cyclopropyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0447] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R.sub.6 and R.sub.6 as defined in any of the embodiments of the present invention, [0448] the alkyl is C.sub.1-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the alkyl is methyl; [0449] and/or [0450] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl, more preferably the C.sub.1-6 alkyl is methyl or ethyl; [0451] and/or [0452] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0453] and/or [0454] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; [0455] and/or [0456] the cycloalkyl is C.sub.3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C.sub.3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C.sub.3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; [0457] and/or [0458] the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; more preferably the aryl is phenyl; [0459] and/or [0460] the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole, oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0461] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R.sub.6a as defined in any of the embodiments of the present invention, [0462] the alkyl is C.sub.1-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the alkyl is ethyl; [0463] and/or [0464] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the C.sub.1-6 alkyl is methyl [0465] and/or [0466] the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; preferably the aryl is phenyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0467] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R.sub.7 and R.sub.7 as defined in any of the embodiments of the present invention, [0468] the alkyl is C.sub.1-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0469] and/or [0470] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl, more preferably the C.sub.1-6 alkyl is methyl, ethyl or propyl; [0471] and/or [0472] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0473] and/or [0474] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; [0475] and/or [0476] the cycloalkyl is C.sub.3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C.sub.3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C.sub.3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; [0477] and/or [0478] the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; [0479] and/or [0480] the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole, oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0481] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R.sub.8, R.sub.8 and R.sub.8 as defined in any of the embodiments of the present invention, [0482] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0483] and/or [0484] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0485] and/or [0486] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0487] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R.sub.9 and R.sub.9as defined in any of the embodiments of the present invention, [0488] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0489] and/or [0490] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0491] and/or [0492] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0493] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R.sub.10, R.sub.10 and R.sub.10 as defined in any of the embodiments of the present invention, [0494] the alkyl is C.sub.1-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0495] and/or [0496] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl, more preferably the C.sub.1-6 alkyl is methyl; [0497] and/or [0498] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0499] and/or [0500] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; [0501] and/or [0502] the cycloalkyl is C.sub.3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C.sub.3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C.sub.3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; [0503] and/or [0504] the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; [0505] and/or [0506] the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole, oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0507] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R.sub.11, R.sub.11 and R.sub.11 as defined in any of the embodiments of the present invention, [0508] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0509] and/or [0510] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0511] and/or [0512] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0513] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R.sub.12, R.sub.12 and R.sub.12 as defined in any of the embodiments of the present invention, [0514] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl, more preferably the C.sub.1-6 alkyl is methyl; [0515] and/or [0516] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0517] and/or [0518] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0519] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R.sub.13 and R.sub.13 as defined in any of the embodiments of the present invention, [0520] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0521] and/or [0522] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0523] and/or [0524] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0525] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein in R.sub.14, R.sub.14 and R.sub.14 as defined in any of the embodiments of the present invention, [0526] the alkyl is C.sub.1-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0527] and/or [0528] the C.sub.1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; [0529] and/or [0530] the C.sub.2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; [0531] and/or [0532] the C.sub.2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; [0533] and/or [0534] the cycloalkyl is C.sub.3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C.sub.3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C.sub.3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; [0535] and/or [0536] the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; [0537] and/or [0538] the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole, oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0539] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

m is 0, 1, 2, 3 or 4; preferably m is 0, 1 or 2;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0540] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

n is 0, 1, 2, 3 or 4; preferably n is 0, 1, 2 or 3;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0541] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

p is 0, 1, 2, 3 or 4; preferably p is 0;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0542] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

W is nitrogen or C(R.sub.4); preferably W is nitrogen;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0543] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

X is selected from a bond, substituted or unsubstituted aryl or C(R.sub.xR.sub.x); preferably X is selected from a bond, CH(phenyl)-, CH(benzyl)-, CH(pyridine)-, CH(thiophen)- and CH(thiazole)-;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0544] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein [0545] R.sub.x is selected from substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; preferably R.sub.x is selected from substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl and substituted or unsubstituted heterocyclyl; more preferably R.sub.x is selected from substituted or unsubstituted phenyl, substituted or unsubstituted benzyl, substituted or unsubstituted pyridine, substituted or unsubstituted thiophen and substituted or unsubstituted thiazole;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0546] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein [0547] R.sub.x is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl; preferably R.sub.x is hydrogen;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0548] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

R.sub.xa is independently selected from hydrogen, halogen, OR.sub.10, CN, haloalkoxy, and C(O)NR.sub.10R.sub.10, preferably R.sub.xa is independently selected from hydrogen, fluorine, O methyl, OCF.sub.3, C(O)NH.sub.2 and CN;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0549] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

R.sub.1 is selected from NR.sub.6R.sub.6 and substituted or unsubstituted N-containing-heterocyclyl; preferably R.sub.1 is selected from substituted or unsubstituted piperidin, substituted or unsubstituted tetrahydroisoquinoline, substituted or unsubstituted morpholine, NH-methyl, N(methyl).sub.2, NH-ethyl, NH.sub.2, N(methyl)(benzyl)-, NHCH.sub.2CH.sub.2F and NHCH.sub.2CHF.sub.2;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0550] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

R.sub.2 is selected from hydrogen, NR.sub.7R.sub.7, CN, CHR.sub.7R.sub.7 and substituted or unsubstituted heterocyclyl; preferably R.sub.2 is selected from NH.sub.2, substituted or unsubstituted NH-methyl, substituted or unsubstituted N(methyl).sub.2, substituted or unsubstituted N(ethyl)(methyl), substituted or unsubstituted N(methyl)(propyl), substituted or unsubstituted azetidine; more preferably R.sub.2 is selected from NH.sub.2, NH-methyl, N(methyl).sub.2, N(methyl)(CH.sub.2CH.sub.2OH), N(methyl)(CH.sub.2CH.sub.2CH.sub.2OH) and substituted or unsubstituted azetidine;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0551] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

R.sub.3 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl; preferably R.sub.3 is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; more preferably R.sub.3 is substituted or unsubstituted methyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0552] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

R.sub.4 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl; preferably R.sub.4 is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; more preferably R.sub.4 is substituted or unsubstituted methyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0553] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

R.sub.4 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl; preferably selected from hydrogen and substituted or unsubstituted methyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0554] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

R.sub.5 and R.sub.5 are independently selected from hydrogen, halogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkyheterocyclyl, OR.sub.8, NO.sub.2, NR.sub.8R.sub.8, NR.sub.8C(O)R.sub.8, NR.sub.8S(O).sub.2R.sub.8, S(O).sub.2NR.sub.8R.sub.8, NR.sub.8C(O)NR.sub.8R.sub.8, SR.sub.8, S(O)R.sub.8, S(O).sub.2R.sub.8, CN, haloalkyl, haloalkoxy, C(O)OR.sub.8, C(O)NR.sub.8R.sub.8, OCH.sub.2CH.sub.2OR.sub.8, NR.sub.8S(O).sub.2NR.sub.8R.sub.8, and C(CH.sub.3).sub.2OR.sub.8; preferably R.sub.5 and R.sub.5 are both hydrogen;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0555] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

R.sub.6 and R.sub.6 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; preferably R.sub.6 and R.sub.6 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl and substituted or unsubstituted alkylaryl; more preferably R.sub.6 and R.sub.6 are independently selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl and substituted or unsubstituted benzyl; even more preferably R.sub.6 and R.sub.6 are independently selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl, CH.sub.2CH.sub.2F, CH.sub.2CHF.sub.2 and substituted or unsubstituted benzyl
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0556] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

R.sub.6a is selected from substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkyheterocyclyl substituted or unsubstituted alkylaryl; preferably R.sub.6a is substituted or unsubstituted phenethyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0557] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

R.sub.7 and R.sub.7 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; preferably R.sub.7 and R.sub.7 are independently selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; more preferably R.sub.7 and R.sub.7 are independently selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl, substituted or unsubstituted propyl; even more preferably R.sub.7 and R.sub.7 are independently selected from hydrogen, substituted or unsubstituted methyl, CH.sub.2CH.sub.2OH and CH.sub.2CH.sub.2CH.sub.2OH;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0558] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

R.sub.8, R.sub.8 and R.sub.8 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0559] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

R.sub.c and R.sub.c are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl; preferably, R.sub.c and R.sub.c are both hydrogen;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0560] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

R.sub.c and R.sub.c may form with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; preferably, R.sub.c and R.sub.c form a cyclopropyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0561] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

R.sub.9 and R.sub.9 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl; preferably R.sub.9 and R.sub.9 are independently selected from hydrogen and unsubstituted C.sub.1-6 alkyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0562] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

R.sub.10, R.sub.10 and R.sub.10 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, unsubstituted C.sub.2-6 alkynyl, unsubstituted aryl, unsubstituted alkylaryl, unsubstituted cycloalkyl and unsubstituted alkylcycloalkyl, unsubstituted heterocyclyl and unsubstituted alkyheterocyclyl; preferably R.sub.10, R.sub.10 and R.sub.10 are independently selected from hydrogen and unsubstituted C.sub.1-6 alkyl; more preferably R.sub.10 and R.sub.10 are independently selected from hydrogen and unsubstituted methyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0563] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

R.sub.11, R.sub.11 and R.sub.11 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl and unsubstituted C.sub.2-6 alkynyl; preferably R.sub.11, R.sub.11 and R.sub.11 are independently selected from hydrogen and unsubstituted C.sub.1-6 alkyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0564] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

R.sub.12, R.sub.12 and R.sub.12 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, and unsubstituted C.sub.2-6 alkenyl and unsubstituted C.sub.2-6 alkynyl; preferably R.sub.12, R.sub.12 and R.sub.12 are independently selected from hydrogen and unsubstituted methyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0565] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

R.sub.13 and R.sub.13 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0566] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

R.sub.14, R.sub.14 and R.sub.14 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, unsubstituted C.sub.2-6 alkynyl, unsubstituted aryl, unsubstituted alkylaryl, unsubstituted cycloalkyl and unsubstituted alkylcycloalkyl, unsubstituted heterocyclyl and unsubstituted alkyheterocyclyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0567] In another preferred embodiment of the invention according to general Formula (I) the compound is a compound, wherein

m is 0, 1 or 2;
and
n is 0, 1, 2 or 3;
and
p is 0;
and
W is nitrogen;
and
X is selected from a bond, CH(phenyl)-, CH(benzyl)-, CH(pyridine)-, CH(thiophen)- and CH(thiazole)-;
and
R.sub.x is selected from substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl and substituted or unsubstituted heterocyclyl; more preferably R.sub.x is selected from substituted or unsubstituted phenyl, substituted or unsubstituted benzyl, substituted or unsubstituted pyridine, substituted or unsubstituted thiophen and substituted or unsubstituted thiazole;
and
R.sub.x is hydrogen;
and
R.sub.xa independently represents hydrogen, fluorine, O-methyl, OCF.sub.3, C(O)NH.sub.2 or CN;
and
R.sub.1 is selected from substituted or unsubstituted piperidin, substituted or unsubstituted tetrahydroisoquinoline, substituted or unsubstituted morpholine, NH-methyl, N(methyl).sub.2, NH-ethyl, NH.sub.2, N(methyl)(benzyl)-, NHCH.sub.2CH.sub.2F and NHCH.sub.2CHF.sub.2;
and
R.sub.2 is selected from NH.sub.2, substituted or unsubstituted NH-methyl, substituted or unsubstituted N(methyl).sub.2, substituted or unsubstituted N(ethyl)(methyl), substituted or unsubstituted N(methyl)(propyl), substituted or unsubstituted azetidine; more preferably R.sub.2 is selected from NH.sub.2, NH-methyl, N(methyl).sub.2, N(methyl)(CH.sub.2CH.sub.2OH), N(methyl)(CH.sub.2CH.sub.2CH.sub.2OH) and substituted or unsubstituted azetidine;
and
R.sub.3 is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; more preferably R.sub.3 is substituted or unsubstituted methyl;
and
R.sub.4 is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; more preferably R.sub.4 is substituted or unsubstituted methyl;
and
R.sub.5 and R.sub.5 are both hydrogen;
and
R.sub.6 and R.sub.6 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl and substituted or unsubstituted alkylaryl; more preferably R.sub.6 and R.sub.6 are independently selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl and substituted or unsubstituted benzyl; even more preferably R.sub.6 and R.sub.6 are independently selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl, CH.sub.2CH.sub.2F, CH.sub.2CHF.sub.2 and substituted or unsubstituted benzyl
and
R.sub.6a is substituted or unsubstituted phenethyl;
and
R.sub.7 and R.sub.7 are independently selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; more preferably R.sub.7 and R.sub.7 are independently selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl, substituted or unsubstituted propyl; even more preferably R.sub.7 and R.sub.7 are independently selected from hydrogen, substituted or unsubstituted methyl, CH.sub.2CH.sub.2OH and CH.sub.2CH.sub.2CH.sub.2OH;
and
R.sub.c and R.sub.c are both hydrogen or R.sub.c and R.sub.c form with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; preferably a cyclopropyl;
and
R.sub.10, R.sub.10 and R.sub.10 are independently selected from hydrogen and unsubstituted C.sub.1-6 alkyl; more preferably R.sub.10 and R.sub.10 are independently selected from hydrogen and unsubstituted methyl;
and
R.sub.12, R.sub.12 and R.sub.12 are independently selected from hydrogen and unsubstituted C.sub.1-6 alkyl; preferably selected from hydrogen and unsubstituted methyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0568] In a preferred embodiment

m is 0, 1 or 2;

[0569] In a preferred embodiment

n is 0, 1, 2 or 3;

[0570] In a preferred embodiment

p is 0 or 1;

[0571] In a preferred embodiment

W is nitrogen or CR4, preferably nitrogen or substituted or unsubstituted methyl, more preferably nitrogen or unsubstituted methyl;

[0572] In a preferred embodiment

X is selected from a bond, CH(phenyl)-, CH(benzyl)-, CH(pyridine)-, CH(thiophen)- and CH(thiazole)-;

[0573] In a preferred embodiment

R.sub.x is selected from substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl and substituted or unsubstituted heterocyclyl; more preferably R.sub.x is selected from substituted or unsubstituted phenyl, substituted or unsubstituted benzyl, substituted or unsubstituted pyridine, substituted or unsubstituted thiophen and substituted or unsubstituted thiazole;

[0574] In a preferred embodiment

R.sub.x is hydrogen;

[0575] In a preferred embodiment

R.sub.x is selected from substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl and substituted or unsubstituted heterocyclyl; more preferably R.sub.x is selected from substituted or unsubstituted phenyl, substituted or unsubstituted benzyl, substituted or unsubstituted pyridine, substituted or unsubstituted thiophen and substituted or unsubstituted thiazole;

[0576] In a preferred embodiment

R.sub.x is a group selected from:

##STR00014##

[0577] In a preferred embodiment

R.sub.x is hydrogen;

[0578] In a preferred embodiment

R.sub.xa is independently selected from hydrogen, halogen, OR.sub.10, CN, haloalkoxy and C(O)NR.sub.10R.sub.10; preferably R.sub.xa is independently selected from hydrogen, fluorine, O methyl, CN, C(O)NH.sub.2 and OCF.sub.3.

[0579] In a preferred embodiment

R.sub.1 is selected from substituted or unsubstituted piperidin, substituted or unsubstituted tetrahydroisoquinoline, substituted or unsubstituted morpholine, NH-methyl, N(methyl).sub.2, NH-ethyl, NH.sub.2, N(methyl)(benzyl)-, NHCH.sub.2CH.sub.2F and NHCH.sub.2CHF.sub.2;

[0580] In a preferred embodiment

R.sub.1 is selected from NH-methyl, N(methyl).sub.2, NH-ethyl, NH.sub.2, N(methyl)(benzyl)-, NHCH.sub.2CH.sub.2F and NHCH.sub.2CHF.sub.2 or a substituted or unsubstituted group selected from

##STR00015##

more preferably

##STR00016##

[0581] In a preferred embodiment

R.sub.2 is selected from hydrogen, substituted or unsubstituted methyl, NH.sub.2, substituted or unsubstituted NH-methyl, substituted or unsubstituted N(methyl).sub.2, substituted or unsubstituted N(ethyl)(methyl), substituted or unsubstituted N(methyl)(propyl), substituted or unsubstituted azetidine; more preferably R.sub.2 is selected from hydrogen, unsubstituted methyl, NH-methyl, N(methyl).sub.2, N(methyl)(CH.sub.2CH.sub.2OH), N(methyl)(CH.sub.2CH.sub.2CH.sub.2OH) and substituted or unsubstituted azetidine;

[0582] In a preferred embodiment

R.sub.2 is selected from hydrogen, substituted or unsubstituted methyl, NH.sub.2, substituted or unsubstituted NH-methyl, substituted or unsubstituted N(methyl).sub.2, substituted or unsubstituted N(ethyl)(methyl), substituted or unsubstituted N(methyl)(propyl), substituted or unsubstituted azetidine; more preferably R.sub.2 is selected from hydrogen, unsubstituted methyl, NH-methyl, N(methyl).sub.2, N(methyl)(CH.sub.2CH.sub.2OH), N(methyl)(CH.sub.2CH.sub.2CH.sub.2OH) and substituted or unsubstituted azetidine of formula

##STR00017##

preferably

##STR00018##

more preferably

##STR00019##

even more preferably

##STR00020##

In a preferred embodiment
R.sub.3 is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; preferably R.sub.3 is substituted or unsubstituted methyl, more preferably unsubstituted methyl.

[0583] In a preferred embodiment

R.sub.4 is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; preferably R.sub.4 is substituted or unsubstituted methyl, more preferably unsubstituted methyl.

[0584] In a preferred embodiment

R.sub.4 is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; preferably R.sub.4 is substituted or unsubstituted methyl, more preferably unsubstituted methyl.

[0585] In a preferred embodiment

R.sub.4 is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; preferably R.sub.4 is hydrogen or substituted or unsubstituted methyl, more preferably hydrogen or unsubstituted methyl.

[0586] In a preferred embodiment

R.sub.3 is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; preferably R.sub.3 is substituted or unsubstituted methyl, more preferably unsubstituted methyl, while R.sub.4 is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; preferably R.sub.4 is substituted or unsubstituted methyl, more preferably unsubstituted methyl.

[0587] In a preferred embodiment

R.sub.3 and R.sub.4 are both unsubstituted methyl.

[0588] In a preferred embodiment

R.sub.5 and R.sub.5 are both hydrogen;

[0589] In a preferred embodiment

R.sub.6 and R.sub.6 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl and substituted or unsubstituted alkylaryl; more preferably R.sub.6 and R.sub.6 are independently selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl and substituted or unsubstituted benzyl; even more preferably R.sub.6 and R.sub.6 are independently selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl, CH.sub.2CH.sub.2F, CH.sub.2CHF.sub.2 and substituted or unsubstituted benzyl.

[0590] In a preferred embodiment

R.sub.6 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl and substituted or unsubstituted alkylaryl; more preferably R.sub.6 is selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl and substituted or unsubstituted benzyl; even more preferably R.sub.6 is selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl, CH.sub.2CH.sub.2F, CH.sub.2CHF.sub.2 and substituted or unsubstituted benzyl.

[0591] In a preferred embodiment

R.sub.6 is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; more preferably R.sub.6 is selected from hydrogen and substituted or unsubstituted methyl; even more preferably R.sub.6 is selected from hydrogen and unsubstituted methyl.

[0592] In a preferred embodiment

R.sub.6 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl and substituted or unsubstituted alkylaryl; more preferably R.sub.6 is selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl and substituted or unsubstituted benzyl; even more preferably R.sub.6 is selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl, CH.sub.2CH.sub.2F, CH.sub.2CHF.sub.2 and substituted or unsubstituted benzyl, while R.sub.6 is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; more preferably from hydrogen and substituted or unsubstituted methyl; even more preferably from hydrogen and unsubstituted methyl.

[0593] In a preferred embodiment

R.sub.6 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl and substituted or unsubstituted alkylaryl; more preferably R.sub.6 is selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl and substituted or unsubstituted benzyl; even more preferably R.sub.6 is selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl, CH.sub.2CH.sub.2F, CH.sub.2CHF.sub.2 and substituted or unsubstituted benzyl, while R.sub.6 is hydrogen.

[0594] In a preferred embodiment

R.sub.6 is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl and substituted or unsubstituted alkylaryl; more preferably R.sub.6 is selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl and substituted or unsubstituted benzyl; even more preferably R.sub.6 is selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl, CH.sub.2CH.sub.2F, CH.sub.2CHF.sub.2 and substituted or unsubstituted benzyl, while R.sub.6 is substituted or unsubstituted C.sub.1-6 alkyl; more preferably substituted or unsubstituted methyl; even more preferably unsubstituted methyl.

[0595] In a preferred embodiment

R.sub.6 is substituted or unsubstituted C.sub.1-6 alkyl; more preferably substituted or unsubstituted methyl, while R.sub.6 is hydrogen.

[0596] In a preferred embodiment

R.sub.6 and R.sub.6 are both hydrogen.

[0597] In a preferred embodiment

R.sub.6 is a substituted or unsubstituted

##STR00021##

more preferably unsubstituted

##STR00022##

[0598] In a preferred embodiment

R.sub.6a is substituted or unsubstituted alkylaryl; preferably substituted or unsubstituted phenethyl; more preferably unsubstituted phenethyl of formula

##STR00023##

[0599] In a preferred embodiment

R.sub.7 and R.sub.7 are independently selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; more preferably R.sub.7 and R.sub.7 are independently selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl, substituted or unsubstituted propyl; even more preferably R.sub.7 and R.sub.7 are independently selected from hydrogen, substituted or unsubstituted methyl, CH.sub.2CH.sub.2OH and CH.sub.2CH.sub.2CH.sub.2OH;

[0600] In a preferred embodiment

R.sub.7 is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; more preferably R.sub.7 is selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl, substituted or unsubstituted propyl; even more preferably R.sub.7 is selected from hydrogen, substituted or unsubstituted methyl, CH.sub.2CH.sub.2OH and CH.sub.2CH.sub.2CH.sub.2OH;

[0601] In a preferred embodiment

R.sub.7 is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; more preferably R.sub.7 is selected from hydrogen and substituted or unsubstituted methyl; even more preferably R.sub.7 is selected from hydrogen and substituted or unsubstituted methyl;

[0602] In a preferred embodiment

R.sub.7 is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; more preferably R.sub.7 is selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl, substituted or unsubstituted propyl; even more preferably R.sub.7 is selected from hydrogen, substituted or unsubstituted methyl, CH.sub.2CH.sub.2OH and CH.sub.2CH.sub.2CH.sub.2OH, while R.sub.7 is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; more preferably R.sub.7 is selected from hydrogen and substituted or unsubstituted methyl; even more preferably R.sub.7 is selected from hydrogen and substituted or unsubstituted methyl;

[0603] In a preferred embodiment

R.sub.7 is selected from hydrogen and substituted or unsubstituted C.sub.1-6 alkyl; more preferably R.sub.7 is selected from hydrogen, substituted or unsubstituted methyl, substituted or unsubstituted ethyl, substituted or unsubstituted propyl; even more preferably R.sub.7 is selected from hydrogen, substituted or unsubstituted methyl, CH.sub.2CH.sub.2OH and CH.sub.2CH.sub.2CH.sub.2OH, while R.sub.7 is substituted or unsubstituted C.sub.1-6 alkyl; preferably substituted or unsubstituted methyl; even more preferably substituted or unsubstituted methyl;

[0604] In a preferred embodiment

R.sub.7 and R.sub.7 are both substituted or unsubstituted C.sub.1-6 alkyl; preferably substituted or unsubstituted methyl; more preferably unsubstituted methyl;

[0605] In a preferred embodiment

R.sub.c is hydrogen.

[0606] In a preferred embodiment

R.sub.c is hydrogen.

[0607] In a preferred embodiment

R.sub.c and R.sub.c are both hydrogen.

[0608] In a preferred embodiment

R.sub.c and R.sub.c form a cyclopropyl.

[0609] In a preferred embodiment

R.sub.10 is selected from hydrogen and unsubstituted C.sub.1-6 alkyl; preferably selected from hydrogen and unsubstituted methyl.

[0610] In a preferred embodiment

R.sub.10 is hydrogen.

[0611] In a preferred embodiment

R.sub.10 is selected from hydrogen and unsubstituted C.sub.1-6 alkyl; preferably selected from hydrogen and unsubstituted methyl, while R.sub.10 is hydrogen.

[0612] In a preferred embodiment

R.sub.10 and R.sub.10 are both hydrogen.

[0613] In a preferred embodiment

R.sub.12 is selected from hydrogen and unsubstituted methyl;

[0614] In an particular embodiment

the halogen is fluorine, chlorine, iodine or bromine.

[0615] In an particular embodiment

the halogen is fluorine.

[0616] In an particular embodiment

the haloalcoxy is OCF.sub.3.

[0617] In a preferred further embodiment, the compounds of the general Formula (I) are selected from

TABLE-US-00001 EX Structure Chemical name 1 [00024] N,N,3,4-Tetramethyl-2-(3-(3- (methylamino)-1- phenylpropoxy)phenyl)-2H- pyrazolo[3,4-d]pyridazin-7-amine 2 [00025] 2-(3-(3-(dimethylamino)-1- phenylpropoxy)phenyl)-N,N,3,4- tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine 3 [00026] 2-(3-(3-(ethylamino)-1- phenylpropoxy)phenyl)-N,N,3,4- tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine 4 [00027] 2-(3-(3-amino-1- phenylpropoxy)phenyl)-N,N,3,4- tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine 5 [00028] 2-(3-(1-(3-fluorophenyl)-3- (methylamino)propoxy)phenyl)- N,N,3,4-tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine 6 [00029] N,N,3,4-tetramethyl-2-(3-(4- (methylamino)-1-phenylbutoxy)phenyl)- 2H-pyrazolo[3,4-d]pyridazin-7-amine 7 [00030] 4-(1-(3-(7-(dimethylamino)-3,4- dimethyl-2H-pyrazolo[3,4-d]pyridazin- 2-yl)phenoxy)-3- (methylamino)propyl)benzonitrile 8 [00031] 2-(3-(1-(4-fluorophenyl)-3- (methylamino)propoxy)phenyl)- N,N,3,4-tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine 9 [00032] N,N,3,4-tetramethyl-2-(3-(3- (methylamino)-1-(pyridin-2- yl)propoxy)phenyl)-2H-pyrazolo[3,4- d]pyridazin-7-amine 10 [00033] N,N,3,4-tetramethyl-2-(3-(3- (methylamino)-1-(pyridin-4- yl)propoxy)phenyl)-2H-pyrazolo[3,4- d]pyridazin-7-amine 11 [00034] 3-(1-(3-(7-(dimethylamino)-3,4- dimethyl-2H-pyrazolo[3,4-d]pyridazin- 2-yl)phenoxy)-3- (methylamino)propyl)benzonitrile 12 [00035] N,N,3,4-tetramethyl-2-(3-((R)-((S)- morpholin-2- yl)(phenyl)methoxy)phenyl)-2H- pyrazolo[3,4-d]pyridazin-7-amine .sup.(1) 13 [00036] N,N,3,4-tetramethyl-2-(3-((S)-((S)- morpholin-2- yl)(phenyl)methoxy)phenyl)-2H- pyrazolo[3,4-d]pyridazin-7-amine .sup.(2) 14 [00037] 2-(3-(3-amino-3- phenylpropoxy)phenyl)-N,N,3,4- tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine 15 [00038] N,N,3,4-tetramethyl-2-(3-(2- (methylamino)-2-phenylethoxy)phenyl)- 2H-pyrazolo[3,4-d]pyridazin-7-amine 16 [00039] N,N,3,4-tetramethyl-2-(3-((1,2,3,4- tetrahydroisoquinolin-4-yl)oxy)phenyl)- 2H-pyrazolo[3,4-d]pyridazin-7-amine 17 [00040] 2-(3-(3-(ethylamino)-1-(3- fluorophenyl)propoxy)phenyl)-N,N,3,4- tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine 18 [00041] 2-(3-(1-(3,5-difluorophenyl)-3- (methylamino)propoxy)phenyl)- N,N,3,4-tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine 19 [00042] 2-(3-(3-amino-1-(2- fluorophenyl)propoxy)phenyl)-N,N,3,4- tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine 20 [00043] 2-(3-(3-amino-1-(4- fluorophenyl)propoxy)phenyl)-N,N,3,4- tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine 21 [00044] 2-(3-(3-amino-1-(3- fluorophenyl)propoxy)phenyl)-N,N,3,4- tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine 22 [00045] 2-(3-(1-(2-fluorophenyl)-3- (methylamino)propoxy)phenyl)-N,3,4- trimethyl-2H-pyrazolo[3,4-d]pyridazin- 7-amine 23 [00046] 2-(3-(3-amino-1-(2- fluorophenyl)propoxy)phenyl)-N,3,4- trimethyl-2H-pyrazolo[3,4-d]pyridazin- 7-amine 24 [00047] 2-(3-(3-amino-1- phenylpropoxy)phenyl)-N,3,4-trimethyl- 2H-pyrazolo[3,4-d]pyridazin-7-amine 25 [00048] N,3,4-trimethyl-2-(3-(3-(methylamino)- 1-phenylpropoxy)phenyl)-2H- pyrazolo[3,4-d]pyridazin-7-amine 26 [00049] 2-(3-(1-(2-fluorophenyl)-3- (methylamino)propoxy)phenyl)-3,4- dimethyl-2H-pyrazolo[3,4-d]pyridazin- 7-amine 27 [00050] 3,4-dimethyl-2-(3-(3-(methylamino)-1- phenylpropoxy)phenyl)-2H- pyrazolo[3,4-d]pyridazin-7-amine 28 [00051] 2-(3-(3-amino-1-(2- fluorophenyl)propoxy)phenyl)-3,4- dimethyl-2H-pyrazolo[3,4-d]pyridazin- 7-amine 29 [00052] N,N,3,4-tetramethyl-2-(3-(piperidin-4- ylmethoxy)phenyl)-2H-pyrazolo[3,4- d]pyridazin-7-amine 30 [00053] 2-(3-(1-(2-Fluorophenyl)-3- (methylamino)propoxy)phenyl)- N,N,3,4-tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine 31 [00054] 2-((2-(3-(1-(2-fluorophenyl)-3- (methylamino)propoxy)phenyl)-3,4- dimethyl-2H-pyrazolo[3,4-d]pyridazin- 7-yl)(methyl)amino)ethanol 32 [00055] 3-((2-(3-(1-(2-fluorophenyl)-3- (methylamino)propoxy)phenyl)-3,4- dimethyl-2H-pyrazolo[3,4-d]pyridazin- 7-yl)(methyl)amino)propan-1-ol 33 [00056] 3-(2-fluorophenyl)-3-(3-(7-(3- methoxyazetidin-1-yl)-3,4-dimethyl-2H- pyrazolo[3,4-d]pyridazin-2-yl)phenoxy)- N-methylpropan-1-amine 34 [00057] N,N,3,4-Tetramethyl-2-(3-(3- (methylamino)-1-(thiazol-2- yl)propoxy)phenyl)-2H-pyrazolo[3,4- d]pyridazin-7-amine 35 [00058] N,N,3,4-tetramethyl-2-(3-(2- (methylamino)-1-phenylethoxy)phenyl)- 2H-pyrazolo[3,4-d]pyridazin-7-amine 36 [00059] 2-(3-(1-(2-methoxyphenyl)-3- (methylamino)propoxy)phenyl)- N,N,3,4-tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine (*) 37 [00060] 2-(3-(2-(dimethylamino)-1- phenylethoxy)phenyl)-N,N,3,4- tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine 38 [00061] N,N,3,4-tetramethyl-2-(3-((4- (methylamino)-1-phenylbutan-2- yl)oxy)phenyl)-2H-pyrazolo[3,4- d]pyridazin-7-amine 39 [00062] 2-(3-(1-(3-methoxyphenyl)-3- (methylamino)propoxy)phenyl)- N,N,3,4-tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine (*) 40 [00063] N,N,3,4-tetramethyl-2-(3-(2- (methylamino)-1-(thiophen-2- yl)ethoxy)phenyl)-2H-pyrazolo[3,4- d]pyridazin-7-amine (*) 41 [00064] 2-(3-(1-(2-fluorophenyl)-2- (methylamino)ethoxy)phenyl)-N,N,3,4- tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine 42 [00065] N,N,3,4-tetramethyl-2-(3-(3- (methylamino)-1-(pyridin-3- yl)propoxy)phenyl)-2H-pyrazolo[3,4- d]pyridazin-7-amine 43 [00066] 2-(3-(1-(3-fluorophenyl)-2- (methylamino)ethoxy)phenyl)-N,N,3,4- tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine 44 [00067] 2-(3-((1-(benzyl(methyl)amino)-3- phenylpropan-2-yl)oxy)phenyl)- N,N,3,4-tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine 45 [00068] N,N,3,4-tetramethyl-2-(3-(2- (methylamino)-1-(pyridin-3- yl)ethoxy)phenyl)-2H-pyrazolo[3,4- d]pyridazin-7-amine 46 [00069] N,N,3,4-tetramethyl-2-(3-(3- (methylamino)-1-(4- (trifluoromethoxy)phenyl)propoxy) phenyl)-2H-pyrazolo[3,4-d]pyridazin- 7-amine 47 [00070] N,N,3,4-tetramethyl-2-(3-(2- (methylamino)-3- phenylpropoxy)phenyl)-2H- pyrazolo[3,4-d]pyridazin-7-amine 48 [00071] N,N,3,4-tetramethyl-2-(3-(3- (methylamino)-1-(thiazol-5- yl)propoxy)phenyl)-2H-pyrazolo[3,4- d]pyridazin-7-amine 49 [00072] N,N,3,4-tetramethyl-2-(3-(2-(1- (methylamino)cyclopropyl)-1- phenylethoxy)phenyl)-2H-pyrazolo[3,4- d]pyridazin-7-amine 50 [00073] 2-(3-(3-amino-1-(pyridin-3- yl)propoxy)phenyl)-N,N,3,4- tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine 51 [00074] N,N,3,4-Tetramethyl-2-(3-(3- (methylamino)-1-(thiophen-2- yl)propoxy)phenyl)-2H-pyrazolo[3,4- d]pyridazin-7-amine 52 [00075] 2-(3-(2-(Dimethylamino)-1-(pyridin-3- yl)ethoxy)phenyl)-N,N,3,4-tetramethyl- 2H-pyrazolo[3,4-d]pyridazin-7-amine 53 [00076] N,N,3,4-Tetramethyl-2-(3-((1- phenethylpiperidin-4- yl)methoxy)phenyl)-2H-pyrazolo[3,4- d]pyridazin-7-amine 54 [00077] 2-(3-(3-((2-fluoroethyl)amino)-1- phenylpropoxy)phenyl)-N,N,3,4- tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine 55 [00078] 2-(3-(3-((2,2-difluoroethyl)amino)-1- phenylpropoxy)phenyl)-N,N,3,4- tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine 56 [00079] 3-(1-(3-(7-(Dimethylamino)-3,4- dimethyl-2H-pyrazolo[3,4-d]pyridazin- 2-yl)phenoxy)-3- (methylamino)propyl)benzamide 57 [00080] 4-(1-(3-(7-(dimethylamino)-3,4- dimethyl-2H-pyrazolo[3,4-d]pyridazin- 2-yl)phenoxy)-3- (methylamino)propyl)benzamide 58 [00081] (S)-N,N,3,4-Tetramethyl-2-(3-(3- (methylamino)-1- phenylpropoxy)phenyl)-2H- pyrazolo[3,4-d]pyridazin-7-amine 59 [00082] (R)-N,N,3,4-tetramethyl-2-(3-(3- (methylamino)-1- phenylpropoxy)phenyl)-2H- pyrazolo[3,4-d]pyridazin-7-amine 60 [00083] (R)-N,N,3,4-Tetramethyl-2-(3-(2- (methylamino)-1-phenylethoxy)phenyl)- 2H-pyrazolo[3,4-d]pyridazin-7-amine 61 [00084] (S)-N,N,3,4-tetramethyl-2-(3-(2- (methylamino)-1-phenylethoxy)phenyl)- 2H-pyrazolo[3,4-d]pyridazin-7-amine 62 [00085] (R)-2-(3-(1-(2-Fluorophenyl)-3- (methylamino)propoxy)phenyl)- N,N,3,4-tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine 63 [00086] (S)-2-(3-(1-(2-fluorophenyl)-3- (methylamino)propoxy)phenyl)- N,N,3,4-tetramethyl-2H-pyrazolo[3,4- d]pyridazin-7-amine 64 [00087] (S)-N,N,3,4-tetramethyl-2-(3-(3- (methylamino)-1-(pyridin-3- yl)propoxy)phenyl)-2H-pyrazolo[3,4- d]pyridazin-7-amine 65 [00088] (R)-N,N,3,4-tetramethyl-2-(3-(3- (methylamino)-1-(pyridin-3- yl)propoxy)phenyl)-2H-pyrazolo[3,4- d]pyridazin-7-amine
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0618] In a preferred further embodiment, the compounds of the general Formula (I) are selected from

TABLE-US-00002 EX Structure Chemical name 66 [00089] 3-(2-fluorophenyl)-N-methyl-3-(3- (1,4,5,7-tetramethyl-6H-pyrrolo[3,4- d]pyridazin-6-yl)phenoxy)propan-1- amine 67 [00090] 3-(3-fluorophenyl)-N-methyl-3-(3- (1,4,5,7-tetramethyl-6H-pyrrolo[3,4- d]pyridazin-6-yl)phenoxy)propan-1- amine 68 [00091] (S)-3-(3-Fluorophenyl)-N-methyl-3-(3- (1,4,5,7-tetramethyl-6H-pyrrolo[3,4- d]pyridazin-6-yl)phenoxy)propan-1- amine 69 [00092] (R)-3-(3-fluorophenyl)-N-methyl-3-(3- (1,4,5,7-tetramethyl-6H-pyrrolo[3,4- d]pyridazin-6-yl)phenoxy)propan-1- amine
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0619] In a preferred embodiment of the compound according to the invention of general Formula (I), [0620] R.sub.x is selected from substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; [0621] R.sub.x is selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl and substituted or unsubstituted C.sub.2-6 alkynyl;
the alkyl, alkenyl or alkynyl in R.sub.X or R.sub.X, if substituted, is substituted with one or more substituent/s selected from OR.sub.9, halogen, CN, haloalkyl, haloalkoxy, and NR.sub.9R.sub.9; [0622] wherein R.sub.9 and R.sub.9 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl;
the aryl, heterocyclyl or cycloalkyl, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, in R.sub.X, if substituted, is substituted with one or more substituent/s selected from halogen, R.sub.10, OR.sub.10, NO.sub.2, NR.sub.10R.sub.10, NR.sub.10C(O)R.sub.10, NR.sub.10S(O).sub.2R.sub.10, S(O).sub.2NR.sub.10R.sub.10, NR.sub.10C(O)NR.sub.10R.sub.10, SR.sub.10, S(O)R.sub.10, S(O).sub.2R.sub.10, CN, haloalkyl, haloalkoxy, C(O)OR.sub.10, C(O)NR.sub.10R.sub.10, OCH.sub.2CH.sub.2OR.sub.10, NR.sub.10S(O).sub.2NR.sub.10R.sub.10 and C(CH.sub.3).sub.2OR.sub.10; [0623] wherein R.sub.10, R.sub.10 and R.sub.10 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, unsubstituted C.sub.2-6 alkynyl, unsubstituted aryl, unsubstituted alkylaryl, unsubstituted cycloalkyl and unsubstituted alkylcycloalkyl, unsubstituted heterocyclyl and unsubstituted alkyheterocyclyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0624] In a preferred embodiment of the compound according to the invention of general Formula (I),

R.sub.1 is selected from NR.sub.6R.sub.6 and substituted or unsubstituted N-containing-heterocyclyl; [0625] wherein R.sub.6 and R.sub.6 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; [0626] wherein said cycloalkyl, aryl or heterocyclyl in R.sub.1 or R.sub.6, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, if substituted, is substituted with one or more substituent/s selected from halogen, R.sub.11, OR.sub.11, NO.sub.2, NR.sub.11R.sub.11, NR.sub.11C(O)R.sub.11, NR.sub.11S(O).sub.2R.sub.11, S(O).sub.2NR.sub.11R.sub.11, NR.sub.11C(O)NR.sub.11R.sub.11, SR.sub.11, S(O)R.sub.11, S(O).sub.2R.sub.11, CN, haloalkyl, haloalkoxy, C(O)OR.sub.11, C(O)NR.sub.11R.sub.11, OCH.sub.2CH.sub.2OH, NR.sub.11S(O).sub.2NR.sub.11R.sub.11, C(CH.sub.3).sub.2OR.sub.11, substituted or unsubstituted alkylaryl, substituted or unsubstituted alkylcycloalkyl and substituted or unsubstituted alkyheterocyclyl; [0627] wherein the alkyl, alkenyl or alkynyl in R.sub.6 or R.sub.6, if substituted, is substituted with one or more substituent/s selected from OR.sub.11, halogen, CN, haloalkyl, haloalkoxy and NR.sub.11R.sub.11; [0628] wherein R.sub.11, R.sub.11 and R.sub.11 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl and unsubstituted C.sub.2-6 alkynyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0629] In a preferred embodiment of the compound according to the invention of general Formula (I),

R.sub.2 is selected from hydrogen, NR.sub.7R.sub.7, CN, CHR.sub.7R.sub.7 and substituted or unsubstituted heterocyclyl; [0630] wherein R.sub.7 and R.sub.7 are independently selected from hydrogen, substituted or unsubstituted C.sub.1-6 alkyl, substituted or unsubstituted C.sub.2-6 alkenyl, substituted or unsubstituted C.sub.2-6 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted alkylaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted heterocyclyl and substituted or unsubstituted alkyheterocyclyl; [0631] wherein said cycloalkyl, aryl or heterocyclyl in R.sub.2, R.sub.7 or R.sub.7, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, if substituted, is substituted with one or more substituent/s selected from halogen, R.sub.12, OR.sub.12, NO.sub.2, NR.sub.12R.sub.12, NR.sub.12C(O)R.sub.12, NR.sub.12S(O).sub.2R.sub.12, S(O).sub.2NR.sub.12R.sub.12, NR.sub.12C(O)NR.sub.12R.sub.12, SR.sub.12, S(O)R.sub.12, S(O).sub.2R.sub.12, CN, haloalkyl, haloalkoxy, C(O)OR.sub.12, C(O)NR.sub.12R.sub.12, OCH.sub.2CH.sub.2OR.sub.12, NR.sub.12S(O).sub.2NR.sub.12R.sub.12 and C(CH.sub.3).sub.2OR.sub.12; [0632] wherein the alkyl, alkenyl or alkynyl in R.sub.7 or R.sub.7, if substituted, is substituted with one or more substituent/s selected from OR.sub.12, halogen, CN, haloalkyl, haloalkoxy and NR.sub.12R.sub.12; [0633] wherein R.sub.12, R.sub.12 and R.sub.12 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, and unsubstituted C.sub.2-6 alkenyl and unsubstituted C.sub.2-6 alkynyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0634] In another embodiment of the invention the compound of general Formula (I),

the alkyl, alkenyl or alkynyl, other than those defined in R.sub.x, R.sub.x, R.sub.6, R.sub.6, R.sub.7 or R.sub.7, if substituted, is substituted with one or more substituent/s selected from OR.sub.13, halogen, CN, haloalkyl, haloalkoxy and NR.sub.13R.sub.13; [0635] wherein R.sub.13 and R.sub.13 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, and unsubstituted C.sub.2-6 alkynyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0636] In another embodiment of the invention the compound of general Formula (I),

the aryl, heterocyclyl or cycloalkyl, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, other than those defined in R.sub.x, R.sub.x, R.sub.1, R.sub.2, R.sub.6, R.sub.6, R.sub.7 or R.sub.7, if substituted, is substituted with one or more substituent/s selected from halogen, R.sub.14, OR.sub.14, NO.sub.2, NR.sub.14R.sub.14, NR.sub.14C(O)R.sub.14, NR.sub.14S(O).sub.2R.sub.14, S(O).sub.2NR.sub.14R.sub.14, NR.sub.14C(O)NR.sub.14R.sub.14, SR.sub.14, S(O)R.sub.14, S(O).sub.2R.sub.14, CN, haloalkyl, haloalkoxy, C(O)OR.sub.14, C(O)NR.sub.14R.sub.14, OCH.sub.2CH.sub.2OR.sub.14, NR.sub.14S(O).sub.2NR.sub.14R.sub.14 and C(CH.sub.3).sub.2OR.sub.14; [0637] wherein R.sub.14, R.sub.14 and R.sub.14 are independently selected from hydrogen, unsubstituted C.sub.1-6 alkyl, unsubstituted C.sub.2-6 alkenyl, unsubstituted C.sub.2-6 alkynyl, unsubstituted aryl, unsubstituted alkylaryl, unsubstituted cycloalkyl and unsubstituted alkylcycloalkyl, unsubstituted heterocyclyl and unsubstituted alkyheterocyclyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0638] In a preferred embodiment of the compound according to the invention of general Formula (I),

the alkyl, alkenyl or alkynyl in R.sub.X or R.sub.X, if substituted, is substituted with one or more substituent/s selected from OR.sub.9, halogen, CN, haloalkyl, haloalkoxy, and NR.sub.9R.sub.9;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0639] In a preferred embodiment of the compound according to the invention of general Formula (I),

the aryl, heterocyclyl or cycloalkyl, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, in R.sub.X, if substituted, is substituted with one or more substituent/s selected from halogen, R.sub.10, OR.sub.10, NO.sub.2, NR.sub.10R.sub.10, NR.sub.10C(O)R.sub.10, NR.sub.10S(O).sub.2R.sub.10, S(O).sub.2NR.sub.10R.sub.10, NR.sub.10C(O)NR.sub.10R.sub.10, SR.sub.10, S(O)R.sub.10, S(O).sub.2R.sub.10, CN, haloalkyl, haloalkoxy, C(O)OR.sub.10, C(O)NR.sub.10R.sub.10, OCH.sub.2CH.sub.2OR.sub.10, NR.sub.10S(O).sub.2NR.sub.10R.sub.10 and C(CH.sub.3).sub.2OR.sub.10;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0640] In a preferred embodiment of the compound according to the invention of general Formula (I),

the aryl, heterocyclyl or cycloalkyl, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, in R.sub.X, if substituted, is substituted with one or more substituent/s selected from halogen, OR.sub.10, CN, haloalkoxy and C(O)NR.sub.10R.sub.10;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0641] In a preferred embodiment of the compound according to the invention of general Formula (I),

the aryl, heterocyclyl or cycloalkyl, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, in R.sub.X, if substituted, is substituted with one or more substituent/s selected from halogen, OR.sub.10, CN, haloalkoxy and C(O)NR.sub.10R.sub.10;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0642] In a preferred embodiment of the compound according to the invention of general Formula (I), [0643] the cycloalkyl, aryl or heterocyclyl in R.sub.1 or R.sub.6, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, if substituted, is substituted with one or more substituent/s selected from halogen, R.sub.11, OR.sub.11, NO.sub.2, NR.sub.11R.sub.11, NR.sub.11C(O)R.sub.11, NR.sub.11S(O).sub.2R.sub.11, S(O).sub.2NR.sub.11R.sub.11, NR.sub.11C(O)NR.sub.11R.sub.11, SR.sub.11, S(O)R.sub.11, S(O).sub.2R.sub.11, CN, haloalkyl, haloalkoxy, C(O)OR.sub.11, C(O)NR.sub.11R.sub.11, OCH.sub.2CH.sub.2OH, NR.sub.11S(O).sub.2NR.sub.11R.sub.11, C(CH.sub.3).sub.2OR.sub.11, substituted or unsubstituted alkylaryl, substituted or unsubstituted alkylcycloalkyl and substituted or unsubstituted alkyheterocyclyl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0644] In a preferred embodiment of the compound according to the invention of general Formula (I), [0645] the cycloalkyl, aryl or heterocyclyl in R.sub.1, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, if substituted, is substituted with one or more substituted or unsubstituted alkylaryl;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0646] In a preferred embodiment of the compound according to the invention of general Formula (I),

the alkyl, alkenyl or alkynyl in R.sub.6 or R.sub.6, if substituted, is substituted with one or more substituent/s selected from OR.sub.11, halogen, CN, haloalkyl, haloalkoxy and NR.sub.11R.sub.11;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0647] In a preferred embodiment of the compound according to the invention of general Formula (I),

the cycloalkyl, aryl or heterocyclyl in R.sub.2, R.sub.7 or R.sub.7, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, if substituted, is substituted with one or more substituent/s selected from halogen, R.sub.12, OR.sub.12, NO.sub.2, NR.sub.12R.sub.12, NR.sub.12C(O)R.sub.12, NR.sub.12S(O).sub.2R.sub.12, S(O).sub.2NR.sub.12R.sub.12, NR.sub.12C(O)NR.sub.12R.sub.12, SR.sub.12, S(O)R.sub.12, S(O).sub.2R.sub.12, CN, haloalkyl, haloalkoxy, C(O)OR.sub.12, C(O)NR.sub.12R.sub.12, OCH.sub.2CH.sub.2OR.sub.12, NR.sub.12S(O).sub.2NR.sub.12R.sub.12 and C(CH.sub.3).sub.2OR.sub.12;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0648] In a preferred embodiment of the compound according to the invention of general Formula (I),

the alkyl, alkenyl or alkynyl in R.sub.7 or R.sub.7, if substituted, is substituted with one or more substituent/s selected from OR.sub.12, halogen, CN, haloalkyl, haloalkoxy and NR.sub.12R.sub.12;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0649] In a preferred embodiment of the compound according to the invention of general Formula (I),

the alkyl, alkenyl or alkynyl in R.sub.7 or R.sub.7, if substituted, is substituted with one or more substituent/s selected OR.sub.12;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0650] In a preferred embodiment of the compound according to the invention of general Formula (I),

the alkyl, alkenyl or alkynyl, other than those defined in R.sub.x, R.sub.x, R.sub.6, R.sub.6, R.sub.7 or R.sub.7, if substituted, is substituted with one or more substituent/s selected from OR.sub.13, halogen, CN, haloalkyl, haloalkoxy and NR.sub.13R.sub.13;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0651] In a preferred embodiment of the compound according to the invention of general Formula (I),

the aryl, heterocyclyl or cycloalkyl, also in alkylaryl, alkylcycloalkyl and alkylheterocyclyl, other than those defined in R.sub.x, R.sub.x, R.sub.1, R.sub.2, R.sub.6, R.sub.6, R.sub.7 or R.sub.7, if substituted, is substituted with one or more substituent/s selected from halogen, R.sub.14, OR.sub.14, NO.sub.2, NR.sub.14R.sub.14, NR.sub.14C(O)R.sub.14, NR.sub.14S(O).sub.2R.sub.14, S(O).sub.2NR.sub.14R.sub.14, NR.sub.14C(O)NR.sub.14R.sub.14, SR.sub.14, S(O)R.sub.14, S(O).sub.2R.sub.14, CN, haloalkyl, haloalkoxy, C(O)OR.sub.14, C(O)NR.sub.14R.sub.14, OCH.sub.2CH.sub.2OR.sub.14, NR.sub.14S(O).sub.2NR.sub.14R.sub.14 and C(CH.sub.3).sub.2OR.sub.14;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0652] In an embodiment of the compound according to the invention of general Formula (I),

the halogen is fluorine, chlorine, iodine or bromine;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0653] In a most preferred embodiment of the compound according to the invention of general Formula (I)

the halogen is fluorine;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0654] In an embodiment of the compound according to the invention of general Formula (I),

the haloalkyl is CF3;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0655] In another embodiment of the compound according to the invention of general Formula (I),

the haloalkoxy is OCF3;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[0656] As this invention is aimed at providing a compound or a chemically related series of compounds which act as dual ligands of the 2 subunit, particularly the 2-1 subunit, of the voltage-gated calcium channel and the NET receptor it is a very preferred embodiment in which the compounds are selected which act as dual ligands of the 2 subunit, particularly the 2-1 ubunit, of the voltage-gated calcium channel and the NET receptor and especially compounds which have a binding expressed as K.sub.i responding to the following scales:

K.sub.i(NET) is preferably <1000 nM, more preferably <500 nM, even more preferably <100 nM.
K.sub.i(21) is preferably <10000 nM, more preferably <5000 nM, even more preferably <500 nM.

[0657] In the following the phrase compound of the invention is used. This is to be understood as any compound according to the invention as described above according to general Formula (I), (I), (I.sup.2), (I.sup.3) and (IZ).

[0658] The compounds of the invention represented by the above described Formula (I) may include enantiomers depending on the presence of chiral centres or isomers depending on the presence of multiple bonds (e.g. Z, E). The single isomers, enantiomers or diastereoisomers and mixtures thereof fall within the scope of the present invention.

[0659] For the sake of clarity the expression a compound according to Formula (I), wherein e.g. R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.5, R.sub.c, R.sub.c, X, W, m, n and p are as defined below in the detailed description would (just like the expression a compound of Formula (I) as defined in any one of claims e.g. 1 to 8 found in the claims) refer to a compound according to Formula (I), wherein the definitions of the respective substituents R.sub.1 etc. (also from the cited claims) are applied. In addition, this would also mean, though (especially in regards to the claims) that also one or more disclaimers defined in the description (or used in any of the cited claims like e.g. claim 1) would be applicable to define the respective compound. Thus, a disclaimer found in e.g. claim 1 would be also used to define the compound of Formula (I) as defined in any one of the corresponding related claims e.g. 1 to 8.

[0660] In general the processes are described below in the experimental part. The starting materials are commercially available or can be prepared by conventional methods.

[0661] A preferred aspect of the invention is also a process for the production of a compound according to Formula (I), following scheme 1, scheme 2 or scheme 3.

[0662] A preferred embodiment of the invention is a process for the production of a compound according to Formula (I), wherein, if not defined otherwise, m, n, p, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.4, R.sub.5, R.sub.5, R.sub.c, R.sub.c, W and X have the meanings defined in the description.

[0663] In a particular embodiment there is a process for the production of a compound according to Formula (I),

##STR00093##

wherein when the group [CH.sub.2].sub.pR.sub.2 is attached to the core structure through a carbon atom, said process comprises treating a compound of formula III

##STR00094##

wherein Z represents a halogen, preferably chloro, or triflate with a suitable organometallic reagent of formula IVa,

##STR00095##

wherein V represents a suitable organometallic reagent, preferably a boron or zinc reagent.

[0664] In a particular embodiment there is a process for the production of a compound according to Formula (I),

##STR00096##

wherein when the group [CH.sub.2].sub.pR.sub.2 is NR.sub.7R.sub.7, said process comprises treating a compound of formula III

##STR00097##

wherein Z represents a halogen, preferably chloro, or triflate with an amine of formula IVb

HNR.sub.7R.sub.7IVb.

[0665] In a particular embodiment there is a process for the production of a compound according to Formula (I),

##STR00098##

said process comprises treating a compound of formula VH

##STR00099##

with a compound of formula VI

##STR00100##

wherein Y represents a leaving group, such as halogen, mesylate, tosylate, nosylate or triflate, or OH.

[0666] In a particular embodiment there is a process for the production of a compound according to Formula (III), (IIIP) or (IIIH),

##STR00101##

wherein P represents a suitable protecting group, such as alkyl or benzyl, preferably methyl, Y represents a leaving group, such as halogen, mesylate, tosylate, nosylate or triflate, or OH, and Z represents an halogen, preferably chloro, or triflate, following the method described for scheme 1.

[0667] In a particular embodiment there is a process for the production of a compound according to Formula (I), (VP) or (VH),

##STR00102##

wherein P represents a suitable protecting group, such as alkyl or benzyl, preferably methyl, Y represents a leaving group, such as halogen, mesylate, tosylate, nosylate or triflate, or OH, and Z represents an halogen, preferably chloro, or triflate, following the method described for scheme 1.

[0668] In a particular embodiment there is a process for the production of a compound according to Formula (IX) or (IXP),

##STR00103##

wherein P represents a suitable protecting group, such as alkyl or benzyl, preferably methyl, and L represents halogen, like fluorine, chlorine, bromine or iodine, following the method described for scheme 2.

[0669] In a particular embodiment there is a process for the production of a compound according to Formula (XI) or (XIP),

##STR00104##

wherein P represents a suitable protecting group, such as alkyl or benzyl, preferably methyl, and Q represents an alkyl group, preferably methyl or ethyl, following the method described for scheme 2.

[0670] In a particular embodiment there is a process for the production of a compound according to Formula (IIa) or (IIaP),

##STR00105##

wherein P represents a suitable protecting group, such as alkyl or benzyl, preferably methyl, and Q represents an alkyl group, preferably methyl or ethyl, following the method described for scheme 2.

[0671] In a particular embodiment there is a process for the production of a compound according to Formula (XIII) or (XIIIP),

##STR00106##

wherein P represents a suitable protecting group, such as alkyl or benzyl, preferably methyl, following the method described for scheme 3.

[0672] In a particular embodiment there is a process for the production of a compound according to Formula (XV) or (XVP),

##STR00107##

wherein P represents a suitable protecting group, such as alkyl or benzyl, preferably methyl, and L represents halogen, like fluorine, chlorine, bromine or iodine, following the method described for scheme 3.

[0673] In a particular embodiment there is a process for the production of a compound according to Formula (Ib), (VbP) or (VbH),

##STR00108##

wherein P represents a suitable protecting group, such as alkyl or benzyl, preferably methyl, Y represents a leaving group, such as halogen, mesylate, tosylate, nosylate or triflate, or OH, following the method described for scheme 3.

[0674] In a particular embodiment there is a process for the production of a compound according to Formula (I), by the reduction reaction of a carbonyl derivative with a suitable reductive reagent, preferably sodium borohydride, in an organic solvent, preferably MeOH, to afford a hydroxyl compound.

[0675] In a particular embodiment there is a process for the production of a compound according to Formula (I), by deprotection reaction of a compound of formula I that contains an amine protecting group such as a carbamate, preferably tert-butoxy carbonyl, by any suitable method, such as treatment with an acid, preferably HCl or trifluoroacetic acid in an appropriate solvent such as 1,4-dioxane, DCM, ethyl acetate or a mixture of an organic solvent and water.

[0676] In a particular embodiment there is a process for the production of a compound according to Formula (I), by reductive amination reaction of a compound of formula I that contains an amino group with an aldehyde, preferably carried out with a reductive reagent, preferably sodium triacetoxyborohydride, in an organic solvent, preferably DCE, in the presence of an organic base, preferably DIPEA or TEA. Alternatively, the reaction can be carried out in the presence of an acid, preferably acetic acid.

[0677] In a particular embodiment there is a process for the production of a compound according to Formula (I), by reaction of a compound of formula I that contains an amino group with an alkylating reagent, in the presence of a base, preferably DIPEA or K.sub.2CO.sub.3, in an organic solvent, preferably acetonitrile, at suitable temperature, such as in the range of 0-120 C.

[0678] In a particular embodiment there is a process for the production of a compound according to Formula (I), by reaction of a compound of formula I that contains an amino group with a vinyl derivative, in an organic solvent, preferably 2-methoxyethanol, at suitable temperature, such as in the range of 20-140 C.

[0679] In a particular embodiment a compound of Formula (II),

##STR00109##

is used for the preparation of compounds of Formula (I).

[0680] In a particular embodiment a compound of Formula (IIIP),

##STR00110##

wherein P is a suitable protecting group, such as alkyl or benzyl, preferably methyl, is used for the preparation of compounds of Formula (I).

[0681] In a particular embodiment a compound of Formula (III),

##STR00111##

is used for the preparation of compounds of Formula (I).

[0682] In a particular embodiment a compound of Formula (IIIP),

##STR00112##

wherein P is a suitable protecting group, such as alkyl or benzyl, preferably methyl, and Z represents an halogen, preferably chloro, or triflate, is used for the preparation of compounds of Formula (I).

[0683] In a particular embodiment a compound of Formula (IIIH),

##STR00113##

wherein Z represents an halogen, preferably chloro, or triflate, is used for the preparation of compounds of Formula (I).

[0684] In a particular embodiment a compound of Formula (IVa),

##STR00114##

wherein V represents a suitable organometallic reagent, preferably a boron or zinc reagent, is used for the preparation of compounds of Formula (I).

[0685] In a particular embodiment a compound of Formula (IVb),

HNR.sub.7R.sub.7IVb

is used for the preparation of compounds of Formula (I).

[0686] In a particular embodiment a compound of Formula (VP),

##STR00115##

wherein P is a suitable protecting group, such as alkyl or benzyl, preferably methyl, is used for the preparation of compounds of Formula (I).

[0687] In a particular embodiment a compound of Formula (VH),

##STR00116##

is used for the preparation of compounds of Formula (I).

[0688] In a particular embodiment a compound of Formula (VI),

##STR00117##

wherein Y is a leaving group, such as halogen, mesylate, tosylate, nosylate or triflate, or OH, is used for the preparation of compounds of Formula (I).

[0689] In a particular embodiment a compound of Formula (VII),

##STR00118##

is used for the preparation of compounds of Formula (I).

[0690] In a particular embodiment a compound of Formula (VIIP),

##STR00119##

wherein P is a suitable protecting group, such as alkyl or benzyl, preferably methyl, is used for the preparation of compounds of Formula (I).

[0691] In a particular embodiment a compound of Formula (VIII),

##STR00120##

wherein Q is an alkyl group, preferably methyl or ethyl, is used for the preparation of compounds of Formula (I).

[0692] In a particular embodiment a compound of Formula (IX),

##STR00121##

wherein L represents halogen, like fluorine, bromine, iodine or chlorine, is used for the preparation of compounds of Formula (I).

[0693] In a particular embodiment a compound of Formula (IXP),

##STR00122##

wherein P is a suitable protecting group, such as alkyl or benzyl, preferably methyl, Q is an alkyl group, preferably methyl or ethyl and L represents halogen, like fluorine, bromine, iodine or chlorine, is used for the preparation of compounds of Formula (I).

[0694] In a particular embodiment a compound of Formula (X),

##STR00123##

is used for the preparation of compounds of Formula (I).

[0695] In a particular embodiment a compound of Formula (XI),

##STR00124##

wherein Q is an alkyl group, preferably methyl or ethyl, is used for the preparation of compounds of Formula (I).

[0696] In a particular embodiment a compound of Formula (XIP),

##STR00125##

wherein P is a suitable protecting group, such as alkyl or benzyl, preferably methyl and Q is an alkyl group, preferably methyl or ethyl, is used for the preparation of compounds of Formula (I).

[0697] In a particular embodiment a compound of Formula (IIa),

##STR00126##

is used for the preparation of compounds of Formula (I).

[0698] In a particular embodiment a compound of Formula (IIaP),

##STR00127##

wherein P is a suitable protecting group, such as alkyl or benzyl, preferably methyl, is used for the preparation of compounds of Formula (I).

[0699] In a particular embodiment a compound of Formula (XII),

##STR00128##

is used for the preparation of compounds of Formula (I).

[0700] In a particular embodiment a compound of Formula (XIII),

##STR00129##

is used for the preparation of compounds of Formula (I).

[0701] In a particular embodiment a compound of Formula (XIIIP),

##STR00130##

wherein P is a suitable protecting group, such as alkyl or benzyl, preferably methyl, is used for the preparation of compounds of Formula (I).

[0702] In a particular embodiment a compound of Formula (XIVa),

##STR00131##

wherein L represents halogen, like fluorine, bromine, iodine or chlorine, is used for the preparation of compounds of Formula (I).

[0703] In a particular embodiment a compound of Formula (XIVb),

##STR00132##

is used for the preparation of compounds of Formula (I).

[0704] In a particular embodiment a compound of Formula (XV),

##STR00133##

is used for the preparation of compounds of Formula (I).

[0705] In a particular embodiment a compound of Formula (XVP),

##STR00134##

wherein P is a suitable protecting group, such as alkyl or benzyl, preferably methyl, is used for the preparation of compounds of Formula (I).

[0706] In a particular embodiment a compound of Formula (Ib),

##STR00135##

is used for the preparation of compounds of Formula (I).

[0707] In a particular embodiment a compound of Formula (VbP),

##STR00136##

wherein P is a suitable protecting group, such as alkyl or benzyl, preferably methyl, is used for the preparation of compounds of Formula (I).

[0708] In a particular embodiment a compound of Formula (VbH),

##STR00137##

is used for the preparation of compounds of Formula (I).

[0709] The obtained reaction products may, if desired, be purified by conventional methods, such as crystallisation and chromatography. Where the above described processes for the preparation of compounds of the invention give rise to mixtures of stereoisomers, these isomers may be separated by conventional techniques such as preparative chromatography. If there are chiral centers the compounds may be prepared in racemic form, or individual enantiomers may be prepared either by enantiospecific synthesis or by resolution.

[0710] One preferred pharmaceutically acceptable form of a compound of the invention is the crystalline form, including such form in pharmaceutical composition. In the case of salts and also solvates of the compounds of the invention the additional ionic and solvent moieties must also be non-toxic. The compounds of the invention may present different polymorphic forms, it is intended that the invention encompasses all such forms.

[0711] Another aspect of the invention refers to a pharmaceutical composition which comprises a compound according to the invention as described above according to general formula I or a pharmaceutically acceptable salt or stereoisomer thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle. The present invention thus provides pharmaceutical compositions comprising a compound of this invention, or a pharmaceutically acceptable salt or stereoisomers thereof together with a pharmaceutically acceptable carrier, adjuvant, or vehicle, for administration to a patient.

[0712] Examples of pharmaceutical compositions include any solid (tablets, pills, capsules, granules etc.) or liquid (solutions, suspensions or emulsions) composition for oral, topical or parenteral administration.

[0713] In a preferred embodiment the pharmaceutical compositions are in oral form, either solid or liquid. Suitable dose forms for oral administration may be tablets, capsules, syrops or solutions and may contain conventional excipients known in the art such as binding agents, for example syrup, acacia, gelatin, sorbitol, tragacanth, or polyvinylpyrrolidone; fillers, for example lactose, sugar, maize starch, calcium phosphate, sorbitol or glycine; tabletting lubricants, for example magnesium stearate; disintegrants, for example starch, polyvinylpyrrolidone, sodium starch glycollate or microcrystalline cellulose; or pharmaceutically acceptable wetting agents such as sodium lauryl sulfate.

[0714] The solid oral compositions may be prepared by conventional methods of blending, filling or tabletting. Repeated blending operations may be used to distribute the active agent throughout those compositions employing large quantities of fillers. Such operations are conventional in the art. The tablets may for example be prepared by wet or dry granulation and optionally coated according to methods well known in normal pharmaceutical practice, in particular with an enteric coating.

[0715] The pharmaceutical compositions may also be adapted for parenteral administration, such as sterile solutions, suspensions or lyophilized products in the appropriate unit dosage form. Adequate excipients can be used, such as bulking agents, buffering agents or surfactants.

[0716] The mentioned formulations will be prepared using standard methods such as those described or referred to in the Spanish and US Pharmacopoeias and similar reference texts.

[0717] Administration of the compounds or compositions of the present invention may be by any suitable method, such as intravenous infusion, oral preparations, and intraperitoneal and intravenous administration. Oral administration is preferred because of the convenience for the patient and the chronic character of the diseases to be treated.

[0718] Generally an effective administered amount of a compound of the invention will depend on the relative efficacy of the compound chosen, the severity of the disorder being treated and the weight of the sufferer. However, active compounds will typically be administered once or more times a day for example 1, 2, 3 or 4 times daily, with typical total daily doses in the range of from 0.1 to 1000 mg/kg/day.

[0719] The compounds and compositions of this invention may be used with other drugs to provide a combination therapy. The other drugs may form part of the same composition, or be provided as a separate composition for administration at the same time or at different time.

[0720] Another aspect of the invention refers to the use of a compound of the invention or a pharmaceutically acceptable salt or isomer thereof in the manufacture of a medicament.

[0721] Another aspect of the invention refers to a compound of the invention according as described above according to general formula I, or a pharmaceutically acceptable salt or isomer thereof, for use as a medicament for the treatment of pain. Preferably the pain is medium to severe pain, visceral pain, chronic pain, cancer pain, migraine, inflammatory pain, acute pain or neuropathic pain, allodynia or hyperalgesia. This may include mechanical allodynia or thermal hyperalgesia.

[0722] Another aspect of the invention refers to the use of a compound of the invention in the manufacture of a medicament for the treatment or prophylaxis of pain.

[0723] In a preferred embodiment the pain is selected from medium to severe pain, visceral pain, chronic pain, cancer pain, migraine, inflammatory pain, acute pain or neuropathic pain, allodynia or hyperalgesia, also preferably including mechanical allodynia or thermal hyperalgesia.

[0724] Another aspect of this invention relates to a method of treating or preventing pain which method comprises administering to a patient in need of such a treatment a therapeutically effective amount of a compound as above defined or a pharmaceutical composition thereof. Among the pain syndromes that can be treated are medium to severe pain, visceral pain, chronic pain, cancer pain, migraine, inflammatory pain, acute pain or neuropathic pain, allodynia or hyperalgesia, whereas this could also include mechanical allodynia or thermal hyperalgesia.

[0725] The present invention is illustrated below with the aid of examples. These illustrations are given solely by way of example and do not limit the general spirit of the present invention.

General Experimental Part (Methods and Equipment of the Synthesis and Analysis

Synthesis Description

[0726] A two-step process is described for the preparation of compounds of general formula (I) starting from a compound of formula II, as shown in Scheme 1.

##STR00138##

wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.5, R.sub.7, R.sub.7, R.sub.c, R.sub.c, W, X, m, n and p have the meanings as defined above for a compound of formula (I), Y represents a leaving group (such as halogen, mesylate, tosylate, nosylate or triflate) or OH, Z represents an halogen (preferably chloro) or triflate, V represents a suitable organometallic reagent (preferably a boron or zinc reagent) and P represents a suitable protecting group (such as alkyl or benzyl, preferably methyl).

[0727] The two-step process can be carried out as described below:

Step 1: A compound of formula III, where Z represents chloro, can be prepared by treating a compound of formula II with a suitable chlorinating reagent such as phosphorus oxychloride, optionally in the presence of a suitable solvent, preferably heating. When Z represents a triflate group, the reaction can be performed by treating a compound of formula II with trifluoromethane sulphonic anhydride in the presence of pyridine.
Step 2: A compound of formula I can be prepared by reacting a compound of formula III with suitable compounds and reaction conditions depending on the meaning of the group [CH.sub.2].sub.pR.sub.2: [0728] a) When the group [CH.sub.2].sub.pR.sub.2 is attached through a carbon atom, the reaction can be performed by treating a compound of formula III with a suitable organometallic reagent of formula IVa, preferably a boron or zinc reagent. The coupling reaction may be carried out using a suitable catalyst (preferably a Pd catalyst) and a suitable ligand (preferably a phosphine ligand), in the presence of a base, such as K.sub.2CO.sub.3 or Cs.sub.2CO.sub.3, in a suitable polar solvent, such as dioxane. [0729] b) When the group [CH.sub.2].sub.pR.sub.2 is attached through a nitrogen atom, as is the case when p is 0 and R.sub.2 is NR.sub.7R.sub.7, the reaction may be performed by treating a compound of formula III with an amine of formula IVb in a suitable solvent, such as isopropanol, ethanol or acetonitrile; optionally in the presence of an organic base such as triethylamine or diisopropylethylamine or an inorganic base such as K.sub.2CO.sub.3 or Cs.sub.2CO.sub.3; at a suitable temperature comprised between room temperature and the reflux temperature, preferably heating, or alternatively, it can be carried out in a microwave reactor. Alternatively, the amine of formula IVb can be introduced, using a Pd catalysed procedure in the presence of a suitable catalyst, a suitable ligand (preferably a phosphine ligand) a suitable base and a suitable solvent, such as dioxane.

[0730] The group [CH.sub.2].sub.mX[C(R.sub.cR.sub.c)].sub.nR.sub.1 can be present from the beginning of the synthesis or alternatively it can be incorporated later on, by reaction of a compound of formula IIIH or VH with a compound of formula VI to render a compound of formula III or I, respectively. A compound of formula IIIH or VH is obtained, in turn, by deprotection of a compound of formula IIIP or VP, wherein P represents a suitable protecting group, such as alkyl or benzyl. When the protecting group P represents alkyl (preferably methyl), the deprotection is carried out by treating a compound of formula IIIP or VP with boron tribromide or boron trichloride, in a suitable solvent such as dichloromethane, at a suitable temperature, preferably cooling below 0 C. When the protecting group P represents benzyl, the deprotection reaction is preferably carried out by hydrogenation under hydrogen atmosphere and metal catalysis, preferably by the use of palladium over charcoal as catalyst in a suitable solvent such as methanol or ethanol, optionally in the presence of an acid such as acetic or hydrochloric acid.

[0731] The reaction of a phenol of formula IIIH or VH with a compound of formula VI to render a compound of formula III or I, respectively, can be carried out under different reaction conditions depending on the meaning of Y: [0732] a) When Y represents a leaving group such as halogen, mesylate, tosylate, nosylate or triflate, the reaction is carried out in a suitable polar solvent, such as dimethylformamide; in the presence of a base such as K.sub.2CO.sub.3, Cs.sub.2CO.sub.3, sodium hydride or potassium tert-butoxide; at a suitable temperature comprised between room temperature and the reflux temperature, preferably heating, or alternatively, the reaction can be carried out in a microwave reactor. Additionally, an activating agent such as sodium iodide can be used. [0733] b) When Y represents OH, the reaction can be carried out by treating a phenol of formula IIIH or VH with an alcohol of formula VI in the presence of an azo compound such as 1,1-(azodicarbonyl)dipiperidine (ADDP), diisopropylazodicarboxylate (DIAD) or diethyl azodicarboxylate (DEAD) and a phosphine such as tributylphosphine or triphenylphoshine. The reaction is carried out in a suitable solvent, such as toluene or tetrahydrofuran; at a suitable temperature comprised between room temperature and the reflux temperature, preferably heating, or alternatively, the reactions can be carried out in a microwave reactor.

[0734] Alternatively, a compound of formula VH can be synthesized from a compound of formula IIIH by reaction with a compound of formula IVa or IVb, following the conditions described for the preparation of a compound of formula I from a compound of formula III.

[0735] The compounds of formula IIIP and VP can be obtained following the two-step process described in Scheme 1, starting from a protected compound of formula IIP.

[0736] The compounds of formula II and IIP can be synthesized following procedures described in the literature. As a way of example, the preparation of compounds of general formula II or IIP, wherein W represents nitrogen (compounds of formula IIa or IIaP), is described in Scheme 2:

##STR00139##

wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.5, R.sub.c, R.sub.c, X, m, n and p have the meanings as defined above for a compound of formula (I), L represents halogen, Q represents an alkyl group (preferably methyl or ethyl) and P represents a suitable protecting group (such as alkyl or benzyl, preferably methyl).

[0737] The reaction of an aniline compound of formula VII with a compound of formula VIII under suitable reaction conditions renders a compound of formula IX. As a way of example, when L represents Cl, a compound of formula IX can be prepared by treating a compound of formula VII with sodium nitrite in a mixture of hydrochloric acid and ethanol at 0 C., followed by reaction with a compound of formula VIII in a mixture of ethanol and water at room temperature.

[0738] A compound of formula IX is then reacted with a di-keto compound of formula X to give a pyrazole of formula XI. The reaction is carried out in the presence of a strong base such as sodium ethoxide and in a suitable solvent such as ethanol.

[0739] Finally, treatment of a compound of formula XI with hydrazine, in a suitable solvent such as ethanol or acetic acid, at a suitable temperature, preferably heating, yields a compound of formula IIa.

[0740] Following the same sequence described in Scheme 2 starting from a conveniently protected aniline of formula VIIP, the corresponding protected compound of formula IIaP can be obtained.

[0741] The preparation of compounds of general formula I wherein W represents CR.sub.4 and wherein the group [CH.sub.2].sub.pR.sub.2 is the same as R.sub.3 (compounds of formula Ib) may be carried out as described in Scheme 3

##STR00140##

wherein R.sub.1, R.sub.3, R.sub.4, R.sub.4, R.sub.5, R.sub.5, R.sub.c, R.sub.c, X, m and n have the meanings as defined above for a compound of formula (I), L represents halogen, Y represents a leaving group (such as halogen, mesylate, tosylate, nosylate or triflate) or OH and P represents a suitable protecting group (such as alkyl or benzyl, preferably methyl).

[0742] The reaction of an aniline compound of formula VII with a di-keto compound of formula XII, in a suitable solvent such as toluene and optionally in the presence of an acid such as acetic acid, renders a pyrrole compound of formula XIII.

[0743] A compound of formula XIII is then treated with an acylating agent of formula XIVa or XIVb to give an acylpyrrole of formula XV. The reaction is carried out using a Lewis acid such as tin(IV) chloride or aluminum chloride, in a suitable solvent such as dichloromethane, dichloroethane or toluene, or mixtures thereof.

[0744] Finally, treatment of a compound of formula XV with hydrazine, in a suitable solvent such as ethanol or acetic acid or mixtures thereof, at a suitable temperature comprised between room temperature and the reflux temperature, preferably at room temperature, yields a compound of formula Ib.

[0745] Following the same sequence described in Scheme 3 starting from a conveniently protected aniline of formula VIIP, the corresponding precursor compound of formula VbP can be obtained.

[0746] The compounds of general formula IVa, IVb, VI, VII, VIIP, VIII, X, XII, XIVa and XIVb wherein R.sub.1, R.sub.2, R.sub.7, R.sub.7, R.sub.c, R.sub.c, R.sub.6, R.sub.6, L, P, Q, V, Y, X, m, n and p have the meanings as defined above, are commercially available or can be prepared by conventional methods described in the bibliography.

[0747] Moreover, certain compounds of the present invention can also be obtained starting from other compounds of formula (I) by appropriate conversion reactions of functional groups, in one or several steps, using well-known reactions in organic chemistry under standard experimental conditions. As a way of example, some of these conversions include the reductive amination of an amino group with an aldehyde or ketone to prepare a further substituted amino group; or the hydrolysis of a cyano group to yield the corresponding carboxamido group.

[0748] In some of the processes described above it may be necessary to protect the reactive or labile groups present with suitable protecting groups, such as for example Boc (tert-butoxycarbonyl) for the protection of amino groups. The procedures for the introduction and removal of these protecting groups are well known in the art and can be found thoroughly described in the literature.

[0749] In addition, a compound of formula I that shows chirality can also be obtained by resolution of a racemic compound of formula I either by chiral preparative HPLC or by crystallization of a diastereomeric salt or co-crystal. Alternatively, the resolution step can be carried out at a previous stage, using any suitable intermediate.

EXAMPLES

[0750] The following abbreviations are used in the examples:

ACN: acetonitrile
AcOH: acetic acid
Anh: anhydrous
ADDP: 1,1-(azodicarbonyl)dipiperidine
Boc: tert-butoxycarbonyl
Conc: concentrated
DCM: dichloromethane
DEA: diethylamine
DMF: dimethylformamide
Eq: equivalent/s
EtOAc; ethyl acetate
EtOH: ethanol
EX: example
h: hour/s
HPLC: high performance liquid chromatography
INT: intermediate

IPA: Isopropanol

[0751] MeOH: methanol
MS: mass spectrometry
Min.: minutes
Quant: quantitative
Ret.: retention
r.t.: room temperature
Sat: saturated
s.m.: starting material
TEA: triethylamine
TFA: trifluoroacetic acid
THF: tetrahydrofuran
Wt: weight

[0752] The following methods were used to determine the HPLC-MS spectra:

Method A

Column: Gemini-NX 304.6 mm, 3 um

Temperature: 40 C.

[0753] Flow: 2.0 mL/min
Gradient: NH.sub.4HCO.sub.3 pH 8: ACN (95:5) - - - 0.5 min - - - (95:5) - - - 6.5 min - - - (0:100) - - - 1 min - - - (0:100)
Sample dissolved approx. 1 mg/mL in NH.sub.4HCO.sub.3 pH 8/ACN

Method B

Column: Kinetex EVO 504.6 mm, 2.6 um

Temperature: 40 C.

[0754] Flow: 2.0 mL/min
Gradient: NH.sub.4HCO.sub.3 pH 8: ACN (95:5) - - - 0.5 min - - - (95:5) - - - 6.5 min - - - (0:100) - - - 1 min - - - (0:100)
Sample dissolved approx. 1 mg/mL in NH.sub.4HCO.sub.3 pH 8/ACN

Method C

Column: Kinetex EVO 504.6 mm, 2.6 um

Temperature: 40 C.

[0755] Flow: 1.5 mL/min
Gradient: NH.sub.4HCO.sub.3 pH 8: ACN (95:5) - - - 0.5 min - - - (95:5) - - - 6.5 min - - - (0:100) - - - 2 min - - - (0:100)
Sample dissolved approx. 1 mg/mL in NH.sub.4HCO.sub.3 pH 8/ACN

Synthesis of Intermediates

Intermediate 1: 7-Chloro-2-(3-methoxyphenyl)-3,4-dimethyl-2H-pyrazolo[3,4-d]pyridazine

[0756] ##STR00141##

[0757] Step 1. (Z)-Ethyl 2-chloro-2-(2-(3-methoxyphenyl)hydrazono)acetate: To a cooled solution of 3-methoxyaniline (20 g, 162 mmol) in a mixture of conc. HCl (32 mL) and EtOH (32 mL), a solution of sodium nitrite (11.2 g, 162 mmol) in water (20 mL) was added dropwise. After stirring for 20 min at 0 C., ethyl 2-chloro-3-oxobutanoate (22.5 mL, 162 mmol) was added. The mixture was diluted with EtOH/water 9:1 v/v (360 mL). Finally, sodium acetate (13.3 g, 162 mmol) was added and it was stirred at room temperature for 2 h. Water (800 mL) was then added, the resulting suspension was filtered and the collected solids were dried under vacuum to afford the title compound (33.7 g, 81% yield).

[0758] Step 2. Ethyl 4-acetyl-1-(3-methoxyphenyl)-5-methyl-1H-pyrazole-3-carboxylate: Acetylacetone (12 mL, 117 mmol) was added to sodium ethoxide (21 wt % in ethanol, 43.6 mL, 117 mmol) and the mixture was stirred at r.t. overnight. Then, the product obtained in step 1 (30 g, 117 mmol) was added. The mixture was stirred at r.t. for 4 h and then it was left standing for 18 h without stirring. Water (420 mL) was added, the suspension was filtered and the solids were dried under vacuum to afford the title compound (28.5 g, 81% yield).

[0759] Step 3. 2-(3-Methoxyphenyl)-3,4-dimethyl-2H-pyrazolo[3,4-d]pyridazin-7(6H)-one: To a solution of the product obtained in step 2 (28.5 g, 94.3 mmol) in EtOH (200 mL), hydrazine (50-60% in water, 27 mL, 282 mmol) was added and the mixture was heated to reflux for 5 h. The suspension was cooled to room temperature and the solids were filtered, washed with cold EtOH and dried under vacuum to obtain afford the title compound (22.4 g, 88% yield).

[0760] Step 4. Title compound: A mixture of the product obtained in step 3 (22.4 g, 82.9 mmol) and POCl.sub.3 (112 mL) was heated at 100 C. for 3 h. POCl.sub.3 was then distilled off. The residue was cooled to 0 C. and it was basified to pH 8 by careful addition (exothermic reaction) of ice and 24% NaOH (approx. 110 mL). The precipitated solids were stirred for 1-2 h at r.t. in order to obtain a filterable suspension and then they were collected by filtration, washed with water and dried under vacuum to yield the title compound (23.0 g, 96% yield).

Intermediate 2: 3-(7-Chloro-3,4-dimethyl-2H-pyrazolo[3,4-d]pyridazin-2-yl)phenol

[0761] ##STR00142##

[0762] To a solution of intermediate 1 (23 g, 80 mmol) in DCM (345 mL), cooled at 78 C., BBr.sub.3 (1M solution in DCM, 278 mL, 80 mmol) was added dropwise. The reaction was slowly warmed to 50 C. during 2 h. Then 1M NaOH was added to adjust pH to 8-9. DCM was distilled off and the resultant suspension was filtered. The solids were filtered, washed with water and dried under vacuum to obtain the title compound (30.3 g, overweight, quantitative yield assumed) as a crude product that was used as such without further purification.

Intermediate 3: 3-(7-(Dimethylamino)-3,4-dimethyl-2H-pyrazolo[3,4-d]pyridazin-2-yl)phenol

[0763] ##STR00143##

[0764] In a round-bottom pressure flask, a mixture of intermediate 2 (63 wt %, 31 g, 72.7 mmol), TEA (20.2 mL, 145 mmol) and dimethylamine (33% in EtOH, 32.7 mL, 182 mmol) in IPA (320 mL) was heated at 120 C. overnight. Then, it was concentrated to dryness. The residue was slurried in water, filtered, washed with water and dried under vacuum to render the title compound (17 g, 82% yield).

[0765] Intermediate 3 has been alternatively prepared following the procedure described for the preparation of intermediate 2, using intermediate 4 as starting material.

[0766] This method was used for the preparation of Intermediates 4-6 using suitable starting materials:

TABLE-US-00003 INT Structure Chemical name s.m. 4 [00144] 2-(3-methoxyphenyl)- N,N,3,4-tetramethyl-2H- pyrazolo[3,4-d] pyridazin-7-amine Interm. 1 5 [00145] 3-(3,4-dimethyl-7- (methylamino)-2H- pyrazolo[3,4-d] pyridazin-2- Interm. 2 6 [00146] 3-(7-amino-3,4- dimethyl-2H- pyrazolo[3,4-d] pyridazin-2- Interm. 2

Intermediate 7: 3-(1,4,5,7-Tetramethyl-6H-pyrrolo[3,4-d]pyridazin-6-yl)phenol

[0767] ##STR00147##

[0768] Step 1. 1-(3-Methoxyphenyl)-2,5-dimethyl-1H-pyrrole: A mixture of 3-methoxyaniline (10.79 g, 88 mmol), hexane-2,5-dione (10.3 mL, 88 mmol) and AcOH (0.9 mL) in toluene (640 mL) was heated to reflux for 3 days. The solvent was evaporated to dryness and the residue was dried under vacuum to afford the title compound as a crude product (19.6 g, overweight, 17.63 g theoretical weight, quant yield assumed).

[0769] Step 2. 1,1-(1-(3-Methoxyphenyl)-2,5-dimethyl-1H-pyrrole-3,4-diyl)diethanone: To a solution of the product obtained in Step 1 (19.6 g, 17.63 g theoretical weight, 88 mmol) in toluene (265 mL), cooled to 0-5 C., SnCl.sub.4 solution (1 M in DCM, 88 mL, 88 mmol) was added dropwise followed by acetyl chloride (12.5 mL, 175 mmol). The reaction mixture was heated at 50 C. overnight. 6 N NaOH was added and it was extracted with EtOAc. The combined organic phases were washed with brine, dried over Na.sub.2SO.sub.4 and concentrated to dryness to afford the title compound (27.1 g, overweight, 24.9 g theoretical weight, quant yield assumed).

[0770] Step 3. 6-(3-Methoxyphenyl)-1,4,5,7-tetramethyl-6H-pyrrolo[3,4-d]pyridazine: To a solution of the product obtained in Step 2 (27.1 g, 24.9 g theoretical weight, 88 mmol) in EtOH (500 mL), hydrazine mono-hydrate (12 mL, 123 mmol) and a few drops of acetic acid were added and the mixture was stirred at r.t. overnight. Then, it was poured onto crushed ice, EtOH was distilled off and the aqueous phase was extracted several times with DCM. The combined organic phases were washed with brine, dried over Na.sub.2SO.sub.4 and concentrated to dryness. The crude product was purified by flash chromatography, silica gel, gradient DCM to MeOH:DCM (1:4) to give the title compound (15.0 g, 61% yield).

[0771] Step 4. 3-(1,4,5,7-Tetramethyl-6H-pyrrolo[3,4-d]pyridazin-6-yl)phenol: BBr.sub.3 (1 M solution in DCM, 35.5 mL, 35.5 mmol) was added dropwise to a solution of the product obtained in Step 3 (2.0 g, 7.11 mmol) in DCM (15 mL), cooled at 78 C., and the mixture was stirred at 30 C. for 3 h. Ice was added to quench the reaction and then DCM was distilled off. 1 N NaOH was added to adjust the pH to 9 and the resulting suspension was stirred at r.t. overnight. The solids were then filtered, washed with water and dried under vacuum to obtain the title compound (2.88 g, overweight, 1.9 g theoretical weight, quant yield assumed) as a crude product that was used as such without further purification.

Synthesis of Examples

Example 1: N,N,3,4-Tetramethyl-2-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine

[0772] ##STR00148##

[0773] Step 1. tert-Butyl (3-chloro-3-phenylpropyl)(methyl)carbamate: To a cooled solution of 3-(methylamino)-1-phenylpropan-1-ol (10 g, 60.5 mmol) in DCM (40 mL), a solution of SOCl.sub.2 (5.3 mL, 72.6 mmol) in DCM (20 mL) was added dropwise. The mixture was stirred at r.t. for 2 h and then the solvent was concentrated to dryness. The crude product thus obtained was dissolved in tert-butanol (52 mL). 1.8 M NaOH solution (70 mL, 127 mmol) and di-tert-butyl dicarbonate (14.5 g, 66.6 mmol) were added and the reaction mixture was stirred for 15 min. Brine and DCM were added, the phases were separated and the aqueous layer was extracted with DCM. The combined organic phases were washed with brine, dried with Na.sub.2SO.sub.4 and concentrated to dryness to obtain the title compound as a crude product (16.3 g, 95% yield), that was used without further purification.

[0774] Step 2. tert-Butyl (3-(3-(7-(dimethylamino)-3,4-dimethyl-2H-pyrazolo[3,4-d]pyridazin-2-yl)phenoxy)-3-phenylpropyl)(methyl)carbamate. A suspension of intermediate 3 (0.6 g, 1.88 mmol), K.sub.2CO.sub.3 (0.78 g, 5.6 mmol) and the crude product obtained in step 1 (0.64 g, 2.25 mmol) in DMF (12 mL) was heated in a sealed tube at 80 C. overnight. Water and EtOAc were added to the cooled reaction mixture and the phases were separated. The aqueous phase was extracted twice with EtOAc. The combined organic phases were washed with brine, dried with Na.sub.2SO.sub.4 and concentrated to dryness. The residue was purified by flash chromatography, silica gel, gradient DCM to MeOH:DCM (1:4) to give the title compound (658 mg, 66% yield).

[0775] Step 3. Title compound: To a solution of the product obtained in step 2 (658 mg, 1.24 mmol) in DCM (16 mL), TFA (1 mL, 12.4 mmol) was added and the reaction mixture was stirred at r.t. until full conversion. It was concentrated to dryness and the residue was re-dissolved in DCM and washed with 1M NaOH. The organic phase was dried with Na.sub.2SO.sub.4 and concentrated. The crude product was purified by flash chromatography, silica gel, gradient DCM to MeOH:DCM (1:4) to give the title compound (305 mg, 57% yield).

[0776] HPLC retention time (method A): 3.26 min; MS: 431.2 (M+H).

[0777] This method was used for the preparation of Examples 2-29 using suitable starting materials:

TABLE-US-00004 Ret time MS HPLC EX Structure Chemical name (min) (M + H) Method 2 [00149] 2-(3-(3- (dimethylamino)-1- phenylpropoxy)phenyl- N,N,3,4-tetramethyl- 2H-pyrazolo[3,4-d] pyridazin-7-amine 4.00 445.2 A 3 [00150] 2-(3-(3-(ethylamino)-1- phenylpropoxy)phenyl)- N,N,3,4-tetramethyl- 2H-pyrazolo[3,4-d] pyridazin-7-amine 3.66 445.2 A 4 [00151] 2-(3-(3-amino-1- phenylpropoxy)phenyl- N,N,3,4-tetramethyl- 2H-pyrazolo[3,4-d] pyridazin-7-amine 3.37 417.2 A 5 [00152] 2-(3-(1-(3- fluorophenyl)-3- (methylamino)propoxy) phenyl)-N,N,3,4- tetramethyl-2H- pyrazolo[3,4-d] pyridazin-7-amine 3.79 449.1 A 6 [00153] N,N,3,4-tetramethyl-2- (3-(4-(methylamino)-1- phenylbutoxy)phenyl)- 2H-pyrazolo[3,4-d] pyridazin-7-amine 3.71 445.2 A 7 [00154] 4-(1-(3-(7- (dimethylamino)-3,4- dimethyl-2H- pyrazolo[3,4-d] pyridazin-2- yl)phenoxy)-3- (methylamino)propyl) benzonitrile 3.84 456.2 A 8 [00155] 2-(3-(1-(4- fluorophenyl)-3- (methylamino)propoxy) phenyl)-N,N,3,4- tetramethyl-2H- pyrazolo[3,4-d] pyridazin-7-amine 3.97 449.2 A 9 [00156] N,N,3,4-tetramethyl-2- (3-(3-(methylamino)-1- (pyridin-2- yl)propoxy)phenyl)-2H- pyrazolo[3,4-d] pyridazin-7-amine 3.38 432.1 A 10 [00157] N,N,3,4-tetramethyl-2- (3-(3-(methylamino)-1- (pyridin-4- yl)propoxy)phenyl)-2H- pyrazolo[3,4-d] pyridazin-7-amine 3.38 432.1 A 11 [00158] 3-(1-(3-(7- (dimethylamino)-3,4- dimethyl-2H- pyrazolo[3,4-d] pyridazin-2- yl)phenoxy)-3- (methylamino)propyl) bezonitrile 3.96 456.1 A 12 [00159] N,N,3,4-tetramethyl-2- (3-((R)-((S)-morpholin- 2-yl)(phenyl) methoxy) phenyl)-2H-pyrazolo [3,4-d] pyridazin-7-amine .sup.(1) 3.69 459.1 A 13 [00160] N,N,3,4-tetramethyl-2- (3-((S)-((S)-morpholin- 2-yl)(phenyl)methoxy) phenyl)-2H-pyrazolo [3,4-d] pyridazin-7-amine .sup.(2) 3.53 459.2 A 14 [00161] 2-(3-(3-amino-3- phenylpropoxy)phenyl)- N,N,3,4-tetramethyl- 2H-pyrazolo[3,4-d] pyridazin-7-amine 3.76 417.2 A 15 [00162] N,N,3,4-tetramethyl-2- (3-(2-(methylamino)-2- phenylethoxy)phenyl)- 2H-pyrazolo[3,4-d] pyridazin-7-amine 3.99 417.2 A 16 [00163] N,N,3,4-tetramethyl-2- (3-((1,2,3,4- tetrahydroisoquinolin-4- yl)oxy)phenyl)-2H- pyrazolo[3,4-d] pyridazin-7-amine 3.67 415.2 A 17 [00164] 2-(3-(3-(ethylamino)-1- (3-fluorophenyl) propoxy) phenyl)-N,N,3,4- tetramethyl-2H- pyrazolo[3,4-d] pyridazin-7-amine 3.75 463.3 B 18 [00165] 2-(3-(1-(3,5- difluorophenyl)-3- (methylamino)propoxy) phenyl)-N,N,3,4- tetramethyl-2H- pyrazolo[3,4-d] pyridazin-7-amine 3.74 467.2 B 19 [00166] 2-(3-(3-amino-1-(2- fluorophenyl)propoxy) phenyl)-N,N,3,4- tetramethyl-2H- pyrazolo[3,4-d] pyridazin-7-amine 3.4 435.2 B 20 [00167] 2-(3-(3-amino-1-(4- fluorophenyl)propoxy) phenyl)-N,N,3,4- tetramethyl-2H- pyrazolo[3,4-d] pyridazin-7-amine 3.49 435.2 B 21 [00168] 2-(3-(3-amino-1-(3- fluorophenyl)propoxy) phenyl)-N,N,3,4- tetramethyl-2H- pyrazolo[3,4-d] pyridazin-7-amine 3.48 435.2 B 22 [00169] 2-(3-(1-(2- fluorophenyl)-3- (methylamino)propoxy) phenyl)-N,3,4-trimethyl- 2H-pyrazolo[3,4-d] pyridazin-7-amine 3.17 435.2 C 23 [00170] 2-(3-(3-amino-1-(2- fluorophenyl)propoxy) phenyl)-N,3,4-trimethyl- 2H-pyrazolo[3,4-d] pyridazin-7-amine 3.44 421.0 C 24 [00171] 2-(3-(3-amino-1- phenylpropoxy)phenyl)- N,3,4-trimethyl-2H- pyrazolo[3,4-d] pyridazin-7-amine 3.42 403.1 C 25 [00172] N,3,4-trimethyl-2-(3-(3- (methylamino)-1- phenylpropoxy)phenyl)- 2H-pyrazolo[3,4-d] pyridazin-7-amine 3.46 417.1 C 26 [00173] 2-(3-(1-(2- fluorophenyl)-3- (methylamino)propoxy) phenyl)-3,4-dimethyl- 2H-pyrazolo[3,4-d] pyridazin-7-amine 3.41 421.0 C 27 [00174] 3,4-dimethyl-2-(3-(3- (methylamino)-1- phenylpropoxy)phenyl)- 2H-pyrazolo[3,4-d] pyridazin-7-amine 3.40 403.1 C 28 [00175] 2-(3-(3-amino-1-(2- fluorophenyl)propoxy) phenyl)-3,4-dimethyl-2H- pyrazolo[3,4-d] pyridazin-7-amine 3.34 407.0 C 29 [00176] N,N,3,4-tetramethyl-2- (3-(piperidin-4- ylmethoxy)phenyl)-2H- pyrazolo[3,4-d] pyridazin-7-amine 2.86 381.2 A (1) Product was obtained as a pure diastereomer in racemic form (mixture with N,N,3,4-tetramethyl-2-(3-((S)-((R)-morpholin-2-yl)(phenyl)methoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine) (2) Product was obtained as a pure diastereomer in racemic form (mixture with N,N,3,4-tetramethyl-2-(3-((R)-((R)-morpholin-2-yl)(phenyl)methoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine

Example 30: 2-(3-(1-(2-Fluorophenyl)-3-(methylamino)propoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine

[0778] ##STR00177##

[0779] Step 1. tert-Butyl (3-(3-(7-chloro-3,4-dimethyl-2H-pyrazolo[3,4-d]pyridazin-2-yl)phenoxy)-3-(2-fluorophenyl)propyl)(methyl)carbamate: A suspension of intermediate 2 (0.57 g, 2.07 mmol), K.sub.2CO.sub.3 (0.86 g, 6.2 mmol) and tert-butyl (3-chloro-3-(2-fluorophenyl)propyl)(methyl)carbamate (prepared following the procedure described in Example 1 Step 1, starting from 1-(2-fluorophenyl)-3-(methylamino)propan-1-ol, 0.81 g, 2.7 mmol) in DMF (5.7 mL) was heated in a sealed tube at 100 C. overnight. Water and EtOAc were added to the cooled reaction mixture and the phases were separated. The aqueous phase was extracted twice with EtOAc. The combined organic phases were washed with brine, dried over Na.sub.2SO.sub.4 and concentrated to dryness to afford the title compound (1.2 g, quant yield), which was used without further purification.

[0780] Step 2. tert-Butyl (3-(3-(7-(dimethylamino)-3,4-dimethyl-2H-pyrazolo[3,4-d]pyridazin-2-yl)phenoxy)-3-(2-fluorophenyl)propyl)(methyl)carbamate: A mixture of the product obtained in step 1 (198 mg, 0.36 mmol), TEA (0.1 mL, 0.73 mmol) and dimethylamine (33% in EtOH, 0.07 mL, 0.36 mmol) in IPA (2 mL) was heated in a sealed tube at 80 C. overnight. It was concentrated to dryness and the residue was purified by flash chromatography, silica gel, gradient DCM to MeOH:DCM (1:4) to give the title compound (133 mg, 66% yield).

[0781] Step 3. Title compound: Following a similar procedure to the preparation of Example 1 Step 3, and starting from the compound obtained in Step 2, the title compound was obtained (84 mg, 77% yield).

[0782] HPLC retention time (method A): 3.88 min; MS: 449.2 (M+H).

[0783] This method was used for the preparation of Examples 31-33 using suitable starting materials:

TABLE-US-00005 Ret time MS HPLC EX Structure Chemical name (min) (M + H) Method 31 [00178] 2-((2-(3-(1-(2- fluorophenyl)-3- (methylamino)propoxy) phenyl)-3,4-dimethyl- 2H-pyrazolo[3,4-d] pyridazin-7-yl) (methyl)amino)ethanol 3.43 479.2 A 32 [00179] 3-((2-(3-(1-(2- fluorophenyl)-3- (methylamino)propoxy) phenyl)-3,4-dimethyl- 2H-pyrazolo[3,4-d] pyridazin-7-yl)(methyl)amino) propan-1-ol 3.52 493.2 A 33 [00180] 3-(2-fluorophenyl)-3-(3- (7-(3-methoxyazetidin- 1-yl)-3,4-dimethyl-2H- pyrazolo[3,4-d] pyridazin-2-yl) phenoxy)-N- methylpropan-1-amine 3.42 491.3 B

Example 34: N,N,3,4-Tetramethyl-2-(3-(3-(methylamino)-1-(thiazol-2-yl)propoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine

[0784] ##STR00181##

[0785] Step 1. tert-Butyl (3-(3-(7-(dimethylamino)-3,4-dimethyl-2H-pyrazolo[3,4-d]pyridazin-2-yl)phenoxy)-3-(thiazol-2-yl)propyl)(methyl)carbamate: In a sealed tube, intermediate 3 (118 mg, 0.41 mmol), tert-butyl (3-hydroxy-3-(thiazol-2-yl)propyl)(methyl)carbamate (prepared following the Boc-protection procedure described in Example 1 Step 1, starting from 3-(methylamino)-1-(thiazol-2-yl)propan-1-ol, 113 mg, 0.41 mmol) and tributylphosphine (0.125 mL, 0.5 mmol) were dissolved in toluene (3.3 mL). Then, ADDP (126 mg, 0.5 mmol) was added and the reaction mixture was heated at 100 C. overnight. After cooling, the mixture was filtered over a pad of celite and the cake was washed with toluene. The filtrate was concentrated to dryness and the residue was purified by flash chromatography, silica gel, gradient DCM to MeOH:DCM (1:4) to give the title compound (129 mg, 57% yield).

[0786] Step 2. Title compound: Following a similar procedure to the preparation of Example 1 Step 3, and starting from the compound obtained in Step 1, the title compound was obtained (36 mg, 34% yield).

[0787] HPLC retention time (method A): 3.27 min; MS: 438.1 (M+H).

[0788] This method was used for the preparation of Examples 35-50 using suitable starting materials:

TABLE-US-00006 Ret time MS HPLC EX Structure Chemical name (min) (M + H) Method 35 [00182] N,N,3,4-tetramethyl-2- (3-(2-(methylamino)-1- phenylethoxy)phenyl)- 2H-pyrazolo[3,4-d] pyridazin-7-amine 3.78 417.2 A 36 [00183] 2-(3-(1-(2- methoxyphenyl)-3- (methylamino)propoxy) phenyl)-N,N,3,4- tetramethyl-2H- pyrazolo[3,4-d] pyridazin-7-amine (*) 3.74 461.2 A 37 [00184] 2-(3-(2-(dimethylamino)-1- phenylethoxy)phenyl)- N,N,3,4-tetramethyl- 2H-pyrazolo[3,4-d] pyridazin-7-amine 4.06 431.2 A 38 [00185] N,N,3,4-tetramethyl-2- (3-((4-(methylamino)-1- phenylbutan-2- yl)oxy)phenyl)-2H- pyrazolo[3,4-d] pyridazin-7-amine 4.33 445.2 A 39 [00186] 2-(3-(1-(3- methoxyphenyl)-3- (methylamino)propoxy) phenyl)-N,N,3,4- tetramethyl-2H- pyrazolo[3,4-d] pyridazin-7-amine (*) 4.07 461.2 A 40 [00187] N,N,3,4-tetramethyl-2- (3-(2-(methylamino)-1- (thiophen-2- yl)ethoxy)phenyl)-2H- pyrazolo[3,4-d] pyridazin-7-amine (*) 3.72 423.2 A 41 [00188] 2-(3-(1-(2- fluorophenyl)-2- (methylamino)ethoxy) phenyl)-N,N,3,4- tetramethyl-2H- pyrazolo[3,4-d] pyridazin-7-amine 3.88 435.2 A 42 [00189] N,N,3,4-tetramethyl-2- (3-(3-(methylamino)-1- (pyridin-3- yl)propoxy)phenyl)-2H- pyrazolo[3,4-d] pyridazin-7-amine 3.33 432.2 A 43 [00190] 2-(3-(1-(3- fluorophenyl)-2- (methylamino)ethoxy) phenyl)-N,N,3,4- tetramethyl-2H- pyrazolo[3,4-d] pyridazin-7-amine 3.91 435.2 A 44 [00191] 2-(3-((1- (benzyl(methyl)amino)- 3-phenylpropan-2- yl)oxy)phenyl)-N,N,3,4- tetramethyl-2H- pyrazolo[3,4-d] pyridazin-7-amine 5.55 521.3 A 45 [00192] N,N,3,4-tetramethyl-2- (3-(2-(methylamino)-1- (pyridin-3- yl)ethoxy)phenyl)-2H- pyrazolo[3,4-d] pyridazin-7-amine 3.31 418.1 A 46 [00193] N,N,3,4-tetramethyl-2- (3-(3-(methylamino)-1- (4-(trifluoromethoxy) phenyl)propoxy) phenyl)-2H- pyrazolo[3,4-d] pyridazin-7-amine 4.73 515.2 A 47 [00194] N,N,3,4-tetramethyl-2- (3-(2-(methylamino)-3- phenylpropoxy)phenyl)- 2H-pyrazolo[3,4-d] pyridazin-7-amine 4.1 431.2 A 48 [00195] N,N,3,4-tetramethyl-2- (3-(3-(methylamino)-1- (thiazol-5- yl)propoxy)phenyl)-2H- pyrazolo[3,4-d] pyridazin-7-amine 3.71 438.3 A 49 [00196] N,N,3,4-tetramethyl-2- (3-(2-(1- (methylamino) cyclopropyl)-1- phenylethoxy)phenyl)- 2H-pyrazolo[3,4-d] pyridazin-7-amine 4.48 457.2 B 50 [00197] 2-(3-(3-amino-1- (pyridin-3- yl)propoxy)phenyl)- N,N,3,4-tetramethyl- 2H-pyrazolo[3,4-d] pyridazin-7-amine 2.93 418.2 B (*) Alternatively, deprotection was carried out by treating a solution of the Boc-protected compound in ACN with 2 eq of iodotrimethylsilane at RT.

Example 51: N,N,3,4-Tetramethyl-2-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine

[0789] ##STR00198##

[0790] Step 1. 2-(1,3-Dichloropropyl)thiophene. TEA (1.43 mL, 10.3 mmol) and methanesulfonyl chloride (0.62 mL, 8.0 mmol) were slowly added to a solution of 3-chloro-1-(thiophen-2-yl)propan-1-ol (1.01 g, 5.72 mmol) in DCM (34 mL), previously cooled at 0-5 C. and the mixture was stirred at this temperature overnight. Sat. NaHCO.sub.3 was added and the phases were separated. The aqueous phase was back extracted twice with DCM. The combined organic phases were washed with brine, dried over MgSO.sub.4 and concentrated to dryness to afford the title compound (1.16 g, quant yield) as a crude product that was used without further purification.

[0791] Step 2. 2-(3-(3-Chloro-1-(thiophen-2-yl)propoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine. The product was prepared following the alkylation procedure described in Step 1 of Example 1, starting from Intermediate 3 (0.6 g, 1.87 mmol) and the product obtained in step 1 (0.43 g, 2.25 mmol). After purification by flash chromatography (silica gel, gradient DCM to MeOH:DCM (1:4)), the title compound was obtained (100 mgs, 12% yield).

[0792] Step 3. Title compound: In a sealed tube, a mixture of the product obtained in Step 1 (100 mg, 0.226 mmol) and methylamine (33 wt % in EtOH, 5 mL) were heated at 50 C. overnight. The solvent was concentrated, the residue was dissolved in DCM and the organic phase was washed with 1 M NaOH solution. The organic phase was dried over sodium sulfate and concentrated under vacuum. The crude product was purified by flash chromatography, silica gel, gradient DCM to MeOH:DCM (1:4) to give the title compound (3 mg, 3% yield).

[0793] HPLC retention time (method A): 3.68 min; MS: 437.2 (M+H).

Example 52: 2-(3-(2-(Dimethylamino)-1-(pyridin-3-yl)ethoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine

[0794] ##STR00199##

[0795] To a solution of Example 45 (32 mg, 0.076 mmol) in DCM (2 mL), formaldehyde (37 wt % in water, 27 L, 0.38 mmol) was added. The mixture was stirred at r.t. for 45 min, then sodium tris(acetoxy)borohydride (22 mg, 0.107 mmol) was added and the reaction mixture was stirred at r.t. overnight. It was then diluted with DCM that was washed with a saturated solution of NaHCO.sub.3 and then brine. The organic phase was dried over sodium sulfate and concentrated to dryness. The residue was purified by flash chromatography, silica gel, gradient DCM to MeOH:DCM (1:4) to give the title compound (16 mg, 50% yield).

[0796] HPLC retention time (method A): 3.44 min; MS: 432.2 (M+H).

Example 53. N,N,3,4-Tetramethyl-2-(3-((1-phenethylpiperidin-4-yl)methoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine

[0797] ##STR00200##

[0798] To a solution of Example 29 (70 mg, 0.184 mmol) in THF (2 mL), 2-phenylacetaldehyde (28 L, 0.24 mmol) was added. The mixture was stirred for 15 min at r.t. and then sodium tris(acetoxy)borohydride (120 mg, 0.55 mmol) and AcOH (11 L, 0.184 mmol) were added. The reaction mixture was stirred at r.t. overnight. Then, 1 M NaOH solution was added and it was extracted with EtOAc. The combined organic phases were washed with brine, dried over sodium sulfate and concentrated to dryness. The residue was purified by flash chromatography, silica gel, gradient DCM to MeOH:DCM (1:4) to give the title compound (24 mg, 27% yield).

[0799] HPLC retention time (method A): 4.1 min; MS: 485.3 (M+H).

[0800] This method was used for the preparation of Examples 54-55 using suitable starting materials:

TABLE-US-00007 Ret time MS HPLC EX Structure Chemical name (min) (M + H) Method 54 [00201] 2-(3-(3-((2- fluoroethyl)amino)-1- phenylpropoxy)phenyl)- N,N,3,4-tetramethyl- 2H-pyrazolo[3,4-d] pyridazin-7-amine 4.16 463.2 B 55 [00202] 2-(3-(3-((2,2- difluoroethyl)amino)-1- phenylpropoxy)phenyl)- N,N,3,4-tetramethyl- 2H-pyrazolo[3,4-d] pyridazin-7-amine 4.51 481.2 B

Example 56. 3-(1-(3-(7-(Dimethylamino)-3,4-dimethyl-2H-pyrazolo[3,4-d]pyridazin-2-yl)phenoxy)-3-(methylamino)propyl)benzamide

[0801] ##STR00203##

[0802] To a solution of Example 11 (123 mg, 0.27 mmol) in tert-butanol (1 mL), KOH (151 mg, 2.7 mmol) was added and the mixture was heated at 80 C. overnight. Then, it was concentrated to dryness and the residue was purified by flash chromatography, silica gel, gradient DCM to MeOH:DCM:conc ammonia (1:4:0.15) to give the title compound (109 mg, 85% yield).

[0803] HPLC retention time (method A): 3.28 min; MS: 474.2 (M+H).

[0804] This method was used for the preparation of Example 57 starting from Example 7:

TABLE-US-00008 Ret time MS HPLC EX Structure Chemical name (min) (M + H) Method 57 [00204] 4-(1-(3-(7- (dimethylamino)-3,4- dimethyl-2H- pyrazolo[3,4-d] pyridazin-2- yl)phenoxy)-3- (methylamino)propyl) benzamide 3.22 474.1 A

Examples 58 and 59: (S)-N,N,3,4-Tetramethyl-2-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine and (R)-N,N,3,4-tetramethyl-2-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine

[0805] ##STR00205##

[0806] Starting from Example 1, a chiral preparative HPLC separation (column: Chiralpak ASH; temperature: ambient; flow: 10 mL/min; eluent: n-Heptane/IPA 80/20 v/v+0.2% DEA) was carried out to give the title compounds.

Examples 60 and 61: (R)-N,N,3,4-Tetramethyl-2-(3-(2-(methylamino)-1-phenylethoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine and (S)-N,N,3,4-tetramethyl-2-(3-(2-(methylamino)-1-phenylethoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine

[0807] ##STR00206##

[0808] Starting from Example 35, a chiral preparative HPLC separation (column: Chiralpak IA; temperature: ambient; flow: 20 mL/min; eluent: (IPA+0.2% DEA)/EtOH 60/40 v/v) was carried out to give the title compounds.

Examples 62 and 63: (R)-2-(3-(1-(2-Fluorophenyl)-3-(methylamino)propoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine and (S)-2-(3-(1-(2-fluorophenyl)-3-(methylamino)propoxy)phenyl)-N,N,3,4-tetramethyl-2H-pyrazolo[3,4-d]pyridazin-7-amine

[0809] ##STR00207##

[0810] Starting from Example 30, a chiral preparative HPLC separation (column: Chiralpak IA; temperature: ambient; flow: 5 mL/min; eluent: IPA/(EtOH+0.2% DEA) 50/50 v/v) was carried out to give the title compounds.

Examples 64 and 65: (S)-N,N,3,4-tetramethyl-2-(3-(3-(methylamino)-1-(pyridin-3-yl)propoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine and (R)-N,N,3,4-tetramethyl-2-(3-(3-(methylamino)-1-(pyridin-3-yl)propoxy)phenyl)-2H-pyrazolo[3,4-d]pyridazin-7-amine

[0811] ##STR00208##

[0812] Starting from Example 42, a chiral preparative HPLC separation (column: Chiralpak IA; temperature: ambient; flow: 5 mL/min; eluent: MeOH+0.2% DEA) was carried out to give the title compounds.

[0813] Following the method described for the preparation of Example 1 but starting from Intermediate 7 and suitable starting materials, Examples 66 and 67 were obtained:

TABLE-US-00009 Ret time MS HPLC EX Structure Chemical name (min) (M + H) Method 66 [00209] 3-(2-fluorophenyl)-N- methyl-3-(3-(1,4,5,7- tetramethyl-6H- pyrrolo[3,4-d]pyridazin- 6-yl)phenoxy)propan-1- amine 4.02 433.2 C 67 [00210] 3-(3-fluorophenyl)-N- methyl-3-(3-(1,4,5,7- tetramethyl-6H- pyrrolo[3,4-d]pyridazin- 6-yl)phenoxy)propan-1- amine 4.09 433.2 C

Examples 68 and 69: (S)-3-(3-Fluorophenyl)-N-methyl-3-(3-(1,4,5,7-tetramethyl-6H-pyrrolo[3,4-d]pyridazin-6-yl)phenoxy)propan-1-amine and (R)-3-(3-fluorophenyl)-N-methyl-3-(3-(1,4,5,7-tetramethyl-6H-pyrrolo[3,4-d]pyridazin-6-yl)phenoxy)propan-1-amine

[0814] ##STR00211##

[0815] Starting from Example 67, a chiral preparative SFC separation (column: Chiralpak IG; temperature: 40 C.; flow: 50 mL/min; BPR: 100 BarG; eluent: EtOH:CO.sub.2 35:65 (0.2% v/v DEA)) was carried out to give the title compounds.

Table of Examples with binding to the NET Receptor and the .sub.2-1 Subunit of the voltage-gated calcium channel:

Biological Activity

Pharmacological Study

[0816] Human .sub.2-1 Subunit of Ca.sub.v2.2 Calcium Channel Assay

[0817] Human .sub.2-1 enriched membranes (2.5 g) were incubated with 15 nM of radiolabeled [3H]-Gabapentin in assay buffer containing Hepes-KOH 10 mM, pH 7.4. NSB (non specific binding) was measured by adding 10 M pregabalin. The binding of the test compound was measured at five different concentrations. After 60 min incubation at 27 C., binding reaction was terminated by filtering through Multiscreen GF/C (Millipore) presoaked in 0.5% polyethyleneimine in Vacuum Manifold Station, followed by 3 washes with ice-cold filtration buffer containing 50 mM Tris-HCl, pH 7.4. Filter plates were dried at 60 C. for 1 hour and 30 l of scintillation cocktail were added to each well before radioactivity reading. Readings were performed in a Trilux 1450 Microbeta radioactive counter (Perkin Elmer).

Binding Assay to Human Norepinephrine Transporter (NET).

[0818] Human norepinephrine transporter (NET) enriched membranes (5 g) were incubated with 5 nM of radiolabeled [3H]-Nisoxetin in assay buffer containing 50 mM Tris-HCl, 120 mM NaCl, 5 mM KCl, pH 7.4. NSB (non specific binding) was measured by adding 10 M of desipramine. The binding of the test compound was measured at five different concentrations. After 60 min incubation at 4 C., binding reaction was terminated by filtering through Multiscreen GF/C (Millipore) presoaked in 0.5% polyethyleneimine in Vacuum Manifold Station, followed by 3 washes with ice-cold filtration buffer containing 50 mM Tris-HCl, 0.9% NaCl, pH 7.4. Filter plates were dried at 60 C. for 1 hour and 30 l of scintillation cocktail were added to each well before radioactivity reading. Readings were performed in a Trilux 1450 Microbeta radioactive counter (Perkin Elmer).

Results:

[0819] As this invention is aimed at providing a compound or a chemically related series of compounds which act as dual ligands of the .sub.2 subunit of voltage-gated calcium channels and the NET receptor it is a very preferred embodiment in which the compounds are selected which act as dual ligands of the .sub.2 subunit of voltage-gated calcium channels and the NET receptor and especially compounds which have a binding expressed as K.sub.i responding to the following scales:

K.sub.i(NET) is preferably <1000 nM, more preferably <500 nM, even more preferably <100 nM.
K.sub.i(.sub.2-1) is preferably <10000 nM, more preferably <5000 nM, or even more preferably <500 nM.

[0820] The following scale has been adopted for representing the binding to the NET receptor expressed as K.sub.i: [0821] +Ki-NET>=1000 nM [0822] ++500 nM<Ki-NET<1000 nM [0823] +++100 nM<Ki-NET<500 nM [0824] ++++Ki-NET<100 nM

[0825] The following scale has been adopted for representing the binding to the .sub.2-1 subunit of voltage-gated calcium channels expressed as K.sub.i: [0826] +K.sub.i(.sub.2-1)>=5000 nM [0827] ++500 nM<=K.sub.i(.sub.2-1)<5000 nM [0828] +++K.sub.i(.sub.2-1)<500 nM

[0829] All compounds prepared in the present application exhibit binding to the .sub.2-1 subunit of voltage-gated calcium channels and the NET receptor, in particular the following binding results are shown:

TABLE-US-00010 Binding Binding Example NET 2-1 1 ++++ ++ 2 +++ ++ 3 +++ ++ 4 +++ ++ 5 ++++ ++ 6 +++ ++ 7 +++ ++ 8 ++++ ++ 9 +++ ++ 10 ++++ ++ 11 ++++ ++ 12 +++ ++ 13 ++ ++ 14 +++ ++ 15 ++++ ++ 16 + ++ 17 + ++ 18 +++ ++ 19 +++ ++ 20 +++ ++ 21 +++ ++ 22 ++++ ++ 23 +++ ++ 24 ++ ++ 25 +++ ++ 26 +++ ++ 27 ++++ ++ 28 ++ ++ 29 + + 30 ++++ ++ 31 ++++ ++ 32 ++++ ++ 33 ++ ++ 34 + +++ 35 ++++ ++ 36 +++ ++ 37 +++ ++ 38 +++ ++ 39 ++++ ++ 40 ++ ++ 41 +++ ++ 42 +++ +++ 43 ++++ ++ 44 + + 45 + ++ 46 +++ ++ 47 ++++ +++ 48 ++ +++ 49 ++++ ++ 50 + ++ 51 ++++ ++ 52 + ++ 53 +++ ++ 54 +++ ++ 55 ++ ++ 56 +++ ++ 57 +++ ++ 58 ++++ ++ 59 +++ ++ 60 +++ ++ 61 ++++ ++ 62 ++++ ++ 63 ++++ ++ 64 +++ +++ 65 ++ ++ 66 ++ ++ 67 +++ ++ 68 +++ + 69 +++ +++