Patent ID: 6720321
Filing Date: 2004-04-13
Classification: A61P,C07D

Abstract:
A compound of the formula (I): wherein:n is 1, 2, 3, 4 or 5 such that the cycloalkyl group is chosen from cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl, each optionally independently substituted by one to two R1 or R2; X is O; p is 0; z is 0; m is 0, 1 or 2; ring A is: fused saturated or unsaturated ring containing 3-5 carbon atoms wherein ring A or the phenyl ring to which it is fused is optionally substituted by one or more C1-6 branched or unbranched alkyl optionally partially or fully halogenated, acetyl, aroyl, C1-6 branched or unbranched alkoxy optionally partially or fully halogenated, halogen, methoxycarbonyl, phenylsulfonyl, hydroxy, amino, mono- or di-(C1-4 alkyl)amino, mono- or di-(C1-4 alkyl)amino-S(O)2, cyano, nitro or H2NSO2; L is: (i) an acyclic group chosen from â€”Oâ€”; â€”NHâ€”; >C(O); >C(S); C1-10 saturated or unsaturated branched or unbranched carbon chain; wherein one or more carbon atoms are optionally independently replaced by heteroatoms chosen from O, N and S(O)m; and wherein said acyclic group is optionally substituted with 0-2 oxo groups, one or more C1-4 branched or unbranched alkyl optionally substituted by one or more halogen atoms, hydroxy, amino or imino; Q is pyrimidinyl optionally substituted with one to three oxo, C1-6 alkyl, phenyl, C1-6 alkoxy or hydroxyl; R1 is phenyl, benzyl, naphthyl, pyrrolyl, pyrrolidinyl, imidazolyl, pyrazolyl, thiazolyl, oxazoyl, [1,3,4]oxadiazol, triazolyl, tetrazolyl, thienyl, furanyl, tetrahydrofuranyl, tetrahydropyranyl, isoxazolyl, isothiazolyl, benzimidazolyl, benzofuranyl, benzoxazolyl, benzisoxazolyl, benzpyrazolyl, benzothiofuranyl, each of the aforementioned is optionally substituted with one to three phenyl, naphthyl, heterocycle or heteroaryl as hereinabove described in this paragraph, C1-6 branched or unbranched alkyl which is optionally partially or fully halogenated, C3-7 cycloalkylC0-2 alkyl, bicyclopentanyl, bicyclohexanyl, bicycloheptanyl, phenyl C1-5 alkyl, naphthyl C1-5 alkyl, halogen, hydroxy, oxo, nitrile, C1-3 alkoxy optionally partially or fully halogenated, phenyloxy, naphthyloxy, heteroaryloxy or heterocyclicoxy wherein the heterocyclic or heteroaryl moiety is as hereinabove described in this paragraph, nitro, amino, mono- or di-(C1-3alky)lamino, phenylamino, naphthylamino, heteroaryl or heterocyclic amino wherein the heteroaryl heterocyclic moiety is as hereinabove described in this paragraph, NH2C(O), a mono- or di-(C1-3alkyl) aminocarbonyl, C1-5 alkyl-C(O)â€”C1-4 alkyl, amino-C1-5 alkyl, mono- or di-(C1-5alkyl)amino, mono- or di -(C1-3alkyl)amino-C1-5 alkyl, C1-5 alkyl-S(O)m, amino-S(O)m, di-(C1-3alkyl)amino-S(O)m, R3â€”C1-5 alkyl, R3â€”C1-5 alkoxy, R3â€”C(O)â€”C1-5 alkyl, R3â€”C1-5 alkyl(R4)N, C1-6 acyl, C1-6 alkoxyCl-3 acyl, carboxy-mono- or di-(C1-5alkyl)-amino; C3-7 cycloalkylC0-5 alkyl, bicyclopentanyl, bicyclohexanyl or bicycloheptanyl, each being optionally be partially or fully halogenated and optionally substituted with one to three C1-3 alkyl groups; cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclohexadienyl, cycloheptadienyl, bicyclohexenyl or bicycloheptenyl, each optionally substituted with one to three C1-3 alkyl groups; C1-4 alkyl-phenyl-C(O)â€”C1-4 alkyl-, C1-4 alkyl-C(O)â€”C1-4 alkyl- or C1-4 alkyl-phenyl-S(O)mâ€”C1-4 alkyl-; C1-6 alkyl or C1-6 alkoxy each of which is branched or unbranched and optionally partially or fully halogenated or optionally substituted with R3; R2, is a C1-6 branched or unbranched alkyl optionally partially or fully halogenated, C1-6acyl, aroyl, C1-4 branched or unbranched alkoxy, each being optionally partially or fully halogenated, carboxy, nitrile, nitro, halogen, C1-6 alkoxycarbonyl, C1-6 alkyl-S(O)m optionally partially or fully halogenated, phenyl-S(O)m, amino or aminocarbonyl wherein the N atom is optionally mono-or-disubstituted by C1-6 branched or unbranched alkyl, C1-6acyl, phenyl or benzyl; each R3 is independently: nitrile, C3-7 cycloalkyl, phenyl or NR5R6; each R4 is independently: hydrogen or C1-4 alkyl optionally partially or fully halogenated; Y, is covalently attached to Q, and is C1-5 alkyl branched or unbranched, optionally substituted by one to three hydroxy, oxo, C1-4 alkyl, C1-3 alkoxy, C1-4 acyl, C1-5 alkoxycarbonyl, NR5R6 or NR5R6â€”C(O)â€”; wherein Y is further covalently attached to morpholinyl optionally substituted by one to three hydroxy, oxo, C1-3 alkyl, C1-3 alkoxy, C1-5 alkoxycarbonyl, NR5R6 or NR5R6â€”C(O)â€”; each R5 and R6 are independently hydrogen, C3-7 cycloalkylC0-4 alkyl, arylC0-3 alkyl optionally subtituted by halogen, C1-3 alkyl or diC1-5 alkyl amino, or R5 and R6 are C1-3 acyl, aroyl or C1-6 branched or unbranched alkyl optionally substituted by C1-5 alkoxy, hydroxy, mono- or di-C1-3alkylaminocarbonyl or mono or diC1-3 alkyl amino wherein said C1-6 alkyl optionally partially or fully halogenated; and the pharmaceutically acceptable salts, tautomers or stereoisomers thereof.