发明名称 Dimethylamino (ethylidene) thioamides, their preparation and use thereof in the preparation of angiogenesis inhibitors
摘要 This invention concerns compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; R<1> is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar<1>, Ar<1>NH-, C3-6cycloalkyl, hydroxymethyl or benzyloxymethyl; R<2> is hydrogen, C1-6alkyl, amino, aminocarbonyl, mono- or di(C1-6alkyl)amino, C1-6alkyloxycarbonyl, C1-6alkylcarbonylamino, hydroxy or C1-6alkyloxy; R<3>, R<4> and R<5> are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het<1>; formula (1) is Ar<2>, Ar<2>CH2- or Het<2>; Ar<1> and Ar<2> optionally substituted phenyl; Het<1> and Het<2> are optionally substituted monocyclic heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.
申请公布号 IL149830(A) 申请公布日期 2005.12.18
申请号 IL19980149830 申请日期 1998.06.22
申请人 JANSSEN PHARMACEUTICA N.V. 发明人
分类号 C07D295/14;A61K;A61K31/41;A61K31/433;A61K31/4523;A61K31/495;A61K31/496;A61K31/506;A61P9/00;A61P17/06;A61P19/02;A61P27/02;A61P27/06;A61P29/00;A61P35/00;A61P43/00;C07D;C07D213/83;C07D239/28;C07D241/24;C07D241/26;C07D241/28;C07D285/08;C07D285/12;C07D285/135;C07D295/00;C07D295/155;C07D401/04;C07D403/04;C07D417/04;C07D417/10;C07D417/12;C07D417/14 主分类号 C07D295/14
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