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 US2014256948(A1) 申请公布日期 2014.09.11
申请号 US201414285760 申请日期 2014.05.23
申请人 Janssen Pharmaceutica NV 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 C07D215/54 主分类号 C07D215/54
代理机构 代理人
主权项
地址 Beerse BE