Patent ID: 7312211
Filing Date: 2007-12-25
Classification: A61P,C07D

Abstract:
1. A compound of formula (Ia) or (Ib): wherein for the formulas Ib or Ib: Y is: wherein Y is optionally substituted by one or more R 5 ; R 1 is heterocyclyl selected from morpholinyl, thiomorpholinyl, piperazinyl, oxazolyl, isoxazolyl, thiazolyl, imidazolyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrazolyl, benzimidazolyl, benzthiazolyl, benzoxazolyl, benzisoxazolyl, quinazolinyl, tetrahydroquinazolinyl and quinoxalinyl, heterocyclyloxy wherein the heterocyclyl moiety is selected from those herein described in this paragraph; wherein R 1 is optionally substituted by one or more R a ; R or R or R or aryl, or R R 2 is hydrogen or C1-3 alkyl; R 3 is a bond, hydrogen, alkyl wherein one or more carbon atoms are optionally replaced by O, S or N wherein it shall be understood if N is not substituted by R c then it is NH, or R 3 is C2-10alkylene, heterocyclyl C1-5 alkyl wherein the heterocyclic moiety is selected from pyrrolidinyl, piperidinyl, morpholinyl, thiomorpholinyl, 8-aza-bicyclo[3.2.1]octane, silinane, piperazinyl, indolinyl, furanyl, tetrahydrofuranyl, pyranyl, tetrahydropyranyl, tetrahydrothiopyranyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, indolyl, dihydrobenzofuranyl, octohydrobenzofuranyl, benzofuranyl, benzothienyl, benzimidazolyl, benzthiazolyl, tetrahydroquinolinyl, quinolinyl, tetrahydroisoquinolinyl, isoquinolinyl, quinazolinyl and quinoxalinyl, C3-8 cycloalkyl, arylC1-5alkyl or aryl wherein R 3 is optionally substituted by one or more R c ; R or R or R R 2 and R 3 together with the carbon they are attached optionally form a nonaromatic 5-7 membered cycloalkyl or heterocyclic ring; each R 4 is independently hydrogen, hydroxy or C1-3 alkyl; R 5 is alkyl or acyl each optionally substituted by alkoxy, aryloxy, benzyloxy, hydroxy, carboxy, aryl, benzyl, heterocyclyl chosen from pyrrolidinyl, piperidinyl, morpholinyl, thiomorpholinyl and piperazinyl or amino wherein the N atom is optionally mono- or di-substituted by alkyl, aryl or benzyl, or R 5 is carboxy; R 6 is hydrogen, hydroxy, nitrile or a C1-6 saturated or unsaturated branched or unbranched alkyl optionally partially or fully halogenated wherein one or more C atoms are optionally replaced by O, NH, S(O), S(O) 2 or S and wherein said chain is optionally independently substituted with 1-2 oxo groups, —NH 2 , one or more C1-4 alkyl or C3-7 cycloalkyl; wherein R 1 and R 6 in the formulas (Ia) or (Ib) optionally form a 4 to 8 membered mono—or 7-14 membered polycyclo heteroring system containing 2 heteroatoms, each aromatic or nonaromatic, wherein each ring is optionally substituted by one or more R 7 ; each R 7 and R 8 are independently: hydrogen, C1-5 alkyl chain optionally interrupted by one or two N, O or S(O) m and optionally substituted by 1-2 oxo, amino, hydroxy, halogen, C1-4alkyl, aryl, aryloxy, aroyl, C1-5 alkanoyl, C1-5 alkoxycarbonyl, aryloxycarbonyl, benzyloxycarbonyl, C1-5 alkanoylamino, aroylamino, C1-5 alkylthio, arylthio C1-5 alkylsulfonylamino, arylsulfonylamino, C1-5 alkylaminosulfonyl, arylaminosulfonyl, C3-6 cycloalkyl or benzyloxy each of the aforementioned are optionally halogenated, halogen, hydroxy, oxo, carboxy, nitrile, nitro or NH 2 C(O)—; m is 0, 1 or 2; and X is ═O, ═S or ═N—R 6 wherein R 6 is as defined above, or the pharmaceutically acceptable salts, esters, isomers or tautomers thereof.