2-ARYLQUINOLINE DERIVATIVES, PREPARATION AND THERA

专利名称：2-ARYLQUINOLINE DERIVATIVES,

PREPARATION AND THERAPEUTIC USETHEREOF

发明人：BOVY, PHILIPPE, R.,BRAUN, ALAIN,PHILIPPO,

CHRISTOPHE

申请号：EP00988858.7申请日：20001121公开号：EP1240146A1公开日：20020918

摘要：2-Aryl quinoline derivatives (I), their enantiomers and diastereoisomers, theirsalts are new. 2-Aryl quinoline derivatives (I), their enantiomers and diastereoisomers,their salts are new. A = H, 1-3C alkoxy, 1-6C hydroxy alkyl, 1-3C alkoxy 1-3C alkyl, thiol, 1-6C alkane sulfonyl, or halogen; B' and D = H, 1-6C alkyl or fluoroalkyl, 1 or 2C

perfluoroalkyl, or together they form oxo; R1 = phenyl, naphthyl, or heteroaryl having 4or 5 C atoms and O, N, or S as heteroatom, the phenyl and naphthyl being optionallysubstituted by 1-3 substituents selected from halogen, OH, NO2, amino, azido, 1-6C alkyl,hydroxy alkyl, alkyl carbonyl, fluoro alkyl or alkylamino, di(1-6C alkyl) amino, 1 or 2 Cperfluoroalkyl, 1-6C alkoxy, phenyl, benzyl, or benzyloxy; R2, R3 = H, halogen, or 1-6Calkyl; R4 = H, OH, or halogen; and R5, R6 = H, 1-6C alkyl or fluoroalkyl, 2-6C alkenyl, 3-6Ccycloalkyl or cycloalkenyl, 1 or 2C perfluoroalkyl; or R5+R6 together = a 2-6C alkylenechain or a 3-6C alkenylene chain to form a heterocycle which may be substituted by a 1-4C alkyl group. Independent claims are also included for (1) intermediates of formula(III); and (2) pharmaceutical compositions containing (I) together with one or more

excipients.

申请人：SANOFI-SYNTHELABO

地址：174, Avenue de France 75013 Paris FR

国籍：FR

代理机构：Thouret-Lemaitre, Elisabeth

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