The present invention relates to oxa-azaspiro compounds having pharmacological activity towards the sigma () 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.

The present invention relates to spiro-cyclic amine derivatives of the formula (I) ##STR00001## wherein R1 is selected from cyano, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkyl each optionally substituted with CN or one or more fluoro atoms, (3-6C)cycloalkyl, (4-6C)cycloalkenyl or a (8-10C)bicyclic group, each optionally substituted with halogen or (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, cyano, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-6C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino and (3-6C)cycloalkyl optionally substituted with phenyl which may be substituted with (1-4C)alkyl or halogen, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl optionally substituted with one or more fluoro atoms, monocyclic heterocycle optionally independently substituted with halogen, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (3-6C)cycloalkyl, or phenyl optionally substituted with (1-4C)alkyl or halogen, and bicyclic heterocycle optionally substituted with halogen or (1-4C)alkyl optionally substituted with one or more fluoro atoms; Y(C.sub.n-alkylene)-X is a linking group wherein Y is attached to R1 and selected from a bond, O, CO, S, SO, SO.sub.2, NH, CHCH, C(CF.sub.3)CH, CC, CH.sub.2O, OCO, COO, CONH, NHCO, and trans-cyclopropylene; n is an integer from 0 to 10; and X is attached to the phenylene/pyridyl moiety and selected from a bond, O, S, SO, SO.sub.2, NH, CO, CHCH, and trans-cyclopropylene; R2 is H or independently selected from one or more substituents selected from halogen, (1-4C)alkoxy and (1-4C)alkyl optionally substituted with one or more fluor atoms; and R3 is (1-4C)alkylene-R4 wherein the alkylene group may be substituted with one or more halogen atoms or with (CH.sub.2).sub.2 to form a cyclopropyl moiety, or R3 is (3-6C)cycloalkylene-R4, CH.sub.2-(3-6C)cycloalkylene-R4, (3-6C)cycloalkylene-CH.sub.2R4 or COCH.sub.2R4, wherein R4 is OH, PO.sub.3H.sub.2, OPO.sub.3H.sub.2, COOH, COO(1-4C)alkyl or tetrazol-5-yl; Q is a bond or O; W-T- is selected from CHCH, CH.sub.2CH.sub.2, CH.sub.2O, OCH.sub.2, OCH.sub.2CH.sub.2, and COO; R5 is H or independently selected from one or more halogens; Z is CH, CR2 or N; and A represents a morpholine ring structure or a 5-, 6- or 7-membered cyclic amine; or a pharmaceutically acceptable salt, a solvate or hydrate thereof or one or more N-oxides thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation o

The present invention relates to spiro-cyclic amine derivatives of the formula (I) ##STR00001## wherein R1 is selected from cyano, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkyl each optionally substituted with CN or one or more fluoro atoms, (3-6C)cycloalkyl, (4-6C)cycloalkenyl or a (8-10C)bicyclic group, each optionally substituted with halogen or (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, cyano, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-6C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino and (3-6C)cycloalkyl optionally substituted with phenyl which may be substituted with (1-4C)alkyl or halogen, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl optionally substituted with one or more fluoro atoms, monocyclic heterocycle optionally independently substituted with halogen, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (3-6C)cycloalkyl, or phenyl optionally substituted with (1-4C)alkyl or halogen, and bicyclic heterocycle optionally substituted with halogen or (1-4C)alkyl optionally substituted with one or more fluoro atoms; Y(C.sub.n-alkylene)-X is a linking group wherein Y is attached to R1 and selected from a bond, O, CO, S, SO, SO.sub.2, NH, CHCH, C(CF.sub.3)CH, CC, CH.sub.2O, OCO, COO, CONH, NHCO, and trans-cyclopropylene; n is an integer from 0 to 10; and X is attached to the phenylene/pyridyl moiety and selected from a bond, O, S, SO, SO.sub.2, NH, CO, CHCH, and trans-cyclopropylene; R2 is H or independently selected from one or more substituents selected from halogen, (1-4C)alkoxy and (1-4C)alkyl optionally substituted with one or more fluor atoms; and R3 is (1-4C)alkylene-R4 wherein the alkylene group may be substituted with one or more halogen atoms or with (CH.sub.2).sub.2 to form a cyclopropyl moiety, or R3 is (3-6C)cycloalkylene-R4, CH.sub.2-(3-6C)cycloalkylene-R4, (3-6C)cycloalkylene-CH.sub.2R4 or COCH.sub.2R4, wherein R4 is OH, PO.sub.3H.sub.2, OPO.sub.3H.sub.2, COOH, COO(1-4C)alkyl or tetrazol-5-yl; Q is a bond or O; W-T- is selected from CHCH, CH.sub.2CH.sub.2, CH.sub.2O, OCH.sub.2, OCH.sub.2CH.sub.2, and COO; R5 is H or independently selected from one or more halogens; Z is CH, CR2 or N; and A represents a morpholine ring structure or a 5-, 6- or 7-membered cyclic amine; or a pharmaceutically acceptable salt, a solvate or hydrate thereof or one or more N-oxides thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation o

The present invention provides a novel compound having an antiviral activity, in particular, an HIV replication inhibiting activity, as well as a pharmaceutical composition, in particular, an anti-HIV agent.

##STR00001##

wherein ring A is substituted or unsubstituted carbocycle or substituted or unsubstituted heterocycle; R.sup.1 is substituted or unsubstituted alkyl etc.; R.sup.2 is substituted or unsubstituted alkyloxy etc.; n is 1 or 2; R.sup.3 is substituted or unsubstituted carbocyclyl or substituted or unsubstituted heterocyclyl; R.sup.4 is a hydrogen atom etc.; R.sup.6 is substituted or unsubstituted alkyl etc.

The present invention provides a novel compound having an antiviral activity, in particular, an HIV replication inhibiting activity, as well as a pharmaceutical composition, in particular, an anti-HIV agent.

##STR00001##

wherein ring A is substituted or unsubstituted carbocycle or substituted or unsubstituted heterocycle; R.sup.1 is substituted or unsubstituted alkyl etc.; R.sup.2 is substituted or unsubstituted alkyloxy etc.; n is 1 or 2; R.sup.3 is substituted or unsubstituted carbocyclyl or substituted or unsubstituted heterocyclyl; R.sup.4 is a hydrogen atom etc.; R.sup.6 is substituted or unsubstituted alkyl etc.

The present invention is directed to compounds of Formula I:

##STR00001## and pharmaceutically acceptable salts, prodrugs, solvates, hydrates, tautomers, or isomers or thereof, wherein R.sub.1, R.sub.2, R.sub.2, L, X, W, Y.sup.1, Y.sup.2, Y.sup.3, and Y.sup.4 are described herein.

The present invention is directed to compounds of Formula I:

##STR00001## and pharmaceutically acceptable salts, prodrugs, solvates, hydrates, tautomers, or isomers or thereof, wherein R.sub.1, R.sub.2, R.sub.2, L, X, W, Y.sup.1, Y.sup.2, Y.sup.3, and Y.sup.4 are described herein.

The present invention relates to oxa-azaspiro compounds having pharmacological activity towards the sigma () 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.

The present invention relates to oxa-azaspiro compounds having pharmacological activity towards the sigma () 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.

The present invention relates to the compounds of the formulae (1) and (2) and to organic electroluminescent devices, in particular blue-emitting devices, in which these compounds are used as host material or dopant in the emitting layer and/or as hole-transport material and/or as electron-transport material.

##STR00001##