The invention relates to 3-((hetero-)aryl)-8-amino-2-oxo-1,3 -diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.

The invention relates to 3-((hetero-)aryl)-8-amino-2-oxo-1,3 -diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.

Provided herein are Aminopurine compounds of Formula I: ##STR00001## or pharmaceutically acceptable salts, tautomers, isotopologues, or stereoisomers thereof, wherein R.sup.1, R.sup.2, and R.sup.3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing animal and human protozoal infections.

Provided herein are Aminopurine compounds of Formula I: ##STR00001## or pharmaceutically acceptable salts, tautomers, isotopologues, or stereoisomers thereof, wherein R.sup.1, R.sup.2, and R.sup.3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing animal and human protozoal infections.

This invention concerns HIV replication inhibitors of formula ##STR00001##
the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a.sup.1=a.sup.2-a.sup.3=a.sup.4- and -b.sup.1=b.sup.2-b.sup.3=b.sup.4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R.sup.1 is hydrogen; aryl; formyl; C.sub.1-6alkylcarbonyl; C.sub.1-6alkyl; C.sub.1-6alkyloxycarbonyl; substituted C.sub.1-6alkyl, C.sub.1-6alkylcarbonyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkylcarbonyloxy; substituted C.sub.1-6alkyloxyC.sub.1-6alkylcarbonyl; R.sup.2 is hydroxy, halo, optionally substituted C.sub.1-6alkyl, C.sub.3-7cycloalkyl, optionally substituted C.sub.2-6alkenyl, optionally substituted C.sub.2-6alkynyl, C.sub.1-6alkyloxy, C.sub.1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C.sub.1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, S(?O).sub.pR.sup.6, NHS(?O).sub.pR.sup.6, C(?O)R.sup.6, NHC(?O)H, C(?O)NHNH.sub.2, NHC(?O)R.sup.6, C(?NH)R.sup.6 or a 5-membered heterocycle; X.sub.1 is NR.sup.5, NHNH, N?N, O, C(?O), C.sub.1-4alkanediyl, CHOH, S, S(?O).sub.p, X.sub.2C.sub.1-4alkanediyl- or C.sub.1-4alkanediyl-X.sub.2; R.sup.3 is NHR.sup.13; NR.sup.13R.sup.14; C(?O)NHR.sup.13; C(?O)NR.sup.13R.sup.14; C(?O)R.sup.15; CH?NNHC(?O)R.sup.16; substituted C.sub.1-6alkyl; optionally substituted C.sub.1-6alkyloxyC.sub.1-6alkyl; substituted C.sub.2-6alkenyl; substituted C.sub.2-6alkynyl; C.sub.1-6alkyl substituted with hydroxy and a second substituent; C(?NOR.sup.8)C.sub.1-4alkyl; R.sup.7; or X.sub.3R.sup.7; R.sup.4 is halo, hydroxy, C.sub.1-6alkyl, C.sub.3-7cycloalkyl, C.sub.1-6alkyloxy, cyano, nitro, polyhaloC.sub.1-6alkyl, polyhaloC.sub.1-6alkyloxy, aminocarbonyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkylcarbonyl, formyl, amino, mono- or di(C.sub.1-4alkyl)amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

A series of 3-hydroxy-5-(isoxazol-5-yl) pyridine formylglycine compounds, a preparation method, a pharmaceutical composition, and the use. A structure of the compounds is shown as formula (I), and the compound derivatives comprise pharmaceutically acceptable salt thereof. The compounds and the pharmaceutical composition thereof have a high inhibition effect on HIF inhibition factors, and the activity can optimally reach the nano-molar concentration level, so that the compounds can be used for preparing a drug for treating fat metabolic diseases.

##STR00001##

Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.

Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile compounds (referred to herein as TFM compounds) which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or a thymidylate synthase (TS) inhibitor; (d) a microtubule targeted agent; (e) ionising radiation; (f) an inhibitor of a mitosis regulator or a mitotic checkpoint regulator; (g) an inhibitor of a DNA damage signal transducer; or (h) an inhibitor of a DNA damage repair enzyme.

##STR00001##

Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.