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 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|