公开(公告)号：EP1334088A1

公开(公告)日：2003-08-13

申请号：EP01983584.2

申请日：2001-11-12

申请人： GlaxoSmithKline S.p.A. ,  Laboratoire Glaxosmithkline S.A.S.

发明人： FARINA, Carlo,Nikem Research S.r.l. ,  GIARDINA, Giuseppe,Nikem Research S.r.l. ,  GRUGNI, Mario,Nikem Research S.r.l. ,  NADLER, Guy Margue. Marie Gerard,Glaxosmithkline

IPC分类号： C07D215/52 ,  A61K31/47 ,  A61K31/4709 ,  A61P11/06

CPC分类号： C07D215/52

摘要： Certain compounds of formula (I) below or a pharmaceutically acceptable salt or hydrate thereof: (I) wherein: R1 is H or C1-6 alkyl; R2 is aryl or C3-7 cycloalkyl or heteroaryl; R3 is H or C1-3 alkyl, optionally substituted by one or more fluorines; R4 is R8R9; R8 is a single bond, C1-6 alkyl, or aryl; R9 is H, COO R10, or N R11R12; R10 is H or C1-6 alkyl; R11 and R12 are independently selected from H and C1-6 alkyl; R5 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, aryl, or a single or fused ring aromatic heterocyclic group; R6 represents H or up to three substituents independently selected from the list consisting of: C¿1-6? alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, amino or mono- or di-C1-6 alkylamino; R7 is H or halo; a is 1-6; and any of R2, R5, R8, R10, R11 and R12 may optionally be substituted one or more times by halo, hydroxy, amino, cyano, nitro, carboxy or oxo; a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and composition in medicine.