发明名称 BICYCLIC HETEROAROMATIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS
摘要 Substituted heteroaromatic compounds of formula wherein X is N or CH; Y is CR1 and V is N; or Y is N and V is CR1; or Y is CR1 and V is CR2; or Y is CR2 and V is CR1; R1 represents a group CH3SO2CH2CH2NHIH2-Ar-, wherein Ar is selected from phenyl, furan, thiophene, pyrrole and thiazole, each of which may optionally be substituted by one or two halo, C1-4alkyl or. C1-4alkoxygroups; R2 is selected from the group comprising hydrogen, halo, hydroxy, C1-4alkyl, C1-4alkoxy, C1-4alkylamino and di[C1-4alkyl]amino; U represents a phenyl, pyridyl, 3H-imidazolyl, indolyl, isoindolyl, indolinyl, isoindolinyl, 1H-indazolyl, 2,3-dihydro-1H-indazolyl, 1H-benzimidazolyl, 2,3-dihydro-1H-benzimidazolyl or 1H-benzotriazolyl group, substituted by an R3 group and optionally substituted by at least one independently selected R4 group; R3 is selected from a group comprising benzyl, halo-, dahlia- and trihalobenzyl, benzoyl, pridylmethyl, pyridylmethoxy, phenoxy, benzyloxy, halo-, dihalo- and trihalobenzyloxy and benzenesulfonyl, or R3 represents trihalomethylbenzyl or trihalomethylbenzyloxy; or R3 represents a group of formula wherein each R5 is independently selected from halogen, C1-4alkyl, C1-4alkoxy, and n is 0 to 3; each R4 is independently hydroxy, halogen, C1-4alkyl, C2-4alkenyl, C2-4 alkynyl, C1-4 alcoxy, amino, C1-4alkylamino, di[C1-4alkyl]amino, C1-4alkylthio, C1-4alylsulphinyl, C1-4alkylsulphonyl, C1-4alkylcarbonyl, carboxy, carbamoyl, C1-4alkoxycarbonyl, C1-4alkanoylamino, N-(C1-4alkyl)carbamoyl, N,N-di(C1-4alkyl)carbamoyl, cyano, nitro and trifluoromethyl; and salts and solvate thereof, are disclosed, as are methods for their preparation, pharmaceutical compositions containing them and their use in medicine. 24 claims
申请公布号 BG104668(A) 申请公布日期 2001.04.30
申请号 BG20000104668D 申请日期 2000.08.07
申请人 GLAXO GROUP LIMITED 发明人 CARTER, MALCOLM C.;COCKERILL, GEORGE S.;GUNTRIP, STEPHEN B.;LACKEY, KAREN E.;SMITH, KATHRYN J.
分类号 A61K31/47;A61K31/4709;A61K31/505;A61K31/517;A61K31/519;A61P9/10;A61P17/06;A61P29/00;A61P35/00;A61P43/00;C07D221/00;C07D239/00;C07D239/94;C07D405/04;C07D405/14;C07D417/04;C07D417/14;C07D471/04 主分类号 A61K31/47
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