发明名称 2,3-DISUBSTITUTED 1 -ACYL-4-AMINO-1,2,3,4-TETRAHYDROQUINOLINE DERIVATIVES AND THEIR USE AS BROMODOMAIN INHIBITORS
摘要 The present invention relates to novel compounds of formula (I), wherein R1 is C1-4alkyl; R2 is C1-4alkyl, C3-7cycloalkyl, -CH2CF3, -CH2OCH3 or heterocyclyl; R3 is C1-4alkyl, -CH2F, -CH2OH or -CH2O(O)CH3; R4 when present is as defined in claim 1; R5 when present is H, halo, hydroxy or C1-6alkoxy; A is -NH-, -O-, -S-, -SO-, -SO2-, -N(C1-4alkyl)- or -NC(O)(CH3)-; V is phenyl, heteroaromatic or pyridone any of which may be optionally substituted by 1, 2 or 3 substituents; W is CH or N; X is C or N; Y is C or N; and Z is CH or N; subject to the proviso that no more than 2 of W, X, Y and Z are N, pharmaceutical compositions containing such compounds and to their use as bromodomain inhibitors.
申请公布号 WO2014140076(A1) 申请公布日期 2014.09.18
申请号 WO2014EP54795 申请日期 2014.03.12
申请人 GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED 发明人 AMANS, DOMINIQUE;ATKINSON, STEPHEN JOHN;HARRISON, LEE ANDREW;HIRST, DAVID JONATHAN;LAW, ROBERT PETER;LINDON, MATTHEW;PRESTON, ALEXANDER;SEAL, JONATHAN THOMAS;WELLAWAY, CHRISTOPHER ROLAND
分类号 C07D215/227;A61K31/4375;A61K31/4706;A61K31/4709;C07D215/44;C07D215/46;C07D215/48;C07D401/04;C07D401/12;C07D401/14;C07D405/04;C07D405/14;C07D409/12;C07D409/14;C07D413/04 主分类号 C07D215/227
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