发明名称 3-CYANO-QUINOLINE DERIVATIVES WITH ANTIPROLIFERATIVE ACTIVITY
摘要 The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH; Y represents -C3-9alkyl-, -C1-5alkyl-NR12-C1-5alkyl-, -C1-6alkyl-NH-CO- or -CO-NH-C1-6alkyl-; X1 represents -O-; X2 represents a direct bond, -NR11-C1-2alkyl-, -NR11-CH2-, -C1-2alkyl-, -O-C1-2alkyl, -O- or -O-CH2-; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen, hydroxy, C1-4alkyloxy-, Ar4-C1-4alkyloxy or R3 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R10 represents hydrogen; R11 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R12 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferably methyl; Het14 represents morpholinyl; Het16 represents a heterocycle selected from morpholinyl or pyrrolidinyl; Ar4 represents phenyl; Ar5 represents phenyl optionally substituted with cyano.
申请公布号 US2013197022(A1) 申请公布日期 2013.08.01
申请号 US201313796377 申请日期 2013.03.12
申请人 JANSSEN PHARMACEUTICA N.V.;JANSSEN PHARMACEUTICA N.V. 发明人 FREYNE EDDY JEAN EDGARD;BUIJNSTERS PETER JACOBUS JOHANNES;VAN EMELEN KRISTOF;EMBRECHTS WERNER CONSTANT JOHAN;PERERA TIMOTHY PIETRO SUREN
分类号 A61K31/4748;C07D215/54;C07D498/08 主分类号 A61K31/4748
代理机构 代理人
主权项
地址