发明名称 Substituted piperidines as Par-1 antagonists
摘要 The invention relates to novel substituted piperidines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of cardiovascular disorders and tumor disorders.
申请公布号 US8987248(B2) 申请公布日期 2015.03.24
申请号 US201013202707 申请日期 2010.03.12
申请人 Bayer Intellectual Property GmbH 发明人 Jeske Mario;Heimbach Dirk;Röhrig Susanne;Cancho Grande Yolanda;Schneider Dirk;Rester Ulrich;Bender Eckhard;Meininghaus Mark;Zimmermann Katja;Zubov Dmitry;Buchmüller Anja;Von Degenfeld Georges;Gerdes Christoph;Gerisch Michael;Gnoth Mark Jean;Gericke Kersten Matthias
分类号 A61K31/5377;C07D413/06;C07D211/60;C07D211/42;C07D211/56;C07D211/62;C07D401/06;C07D405/06;C07D405/12;C07D409/12;C07D413/12;C07D417/06 主分类号 A61K31/5377
代理机构 代理人 King Karen B.
主权项 1. A compound of formula (I) in which A represents a group of the formula where# is the point of attachment to the piperidine ring,* is the point of attachment to R2,R4 represents hydrogen or C1-C3-alkyl,andR5 represents hydrogen or C1-C3-alkyl, R1 represents phenyl, where phenyl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of monofluoromethyl, difluoromethyl, trifluoromethyl, monofluoromethoxy, difluoromethoxy, trifluoromethoxy, monofluoromethylsulphanyl, difluoromethylsulphanyl, trifluoromethylsulphanyl, methylsulphonyl, C1-C4-alkyl, C1-C4-alkoxy and C1-C4-alkoxycarbonyl, R2 represents phenyl where phenyl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of halogen, cyano, hydroxyl, amino, monofluoromethyl, difluoromethyl, trifluoromethyl, monofluoromethoxy, difluoromethoxy, trifluoromethoxy, monofluoromethylsulphanyl, difluoromethylsulphanyl, trifluoromethylsulphanyl, C1-C4-alkyl, C1-C4-alkoxy, C1-C6-alkylamino and phenyl, where phenyl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of halogen and trifluoromethyl, R3 represents 4- to 7-membered heterocyclyl, where heterocyclyl, may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of halogen, cyano, oxo, hydroxyl, amino, monofluoromethyl, difluoromethyl, trifluoromethyl, monofluoromethoxy, difluoromethoxy, trifluoromethoxy, monofluoromethylsulphanyl, difluoromethylsulphanyl, trifluoromethylsulphanyl, hydroxycarbonyl, aminocarbonyl, C1-C4-alkyl, C1-C4-alkoxy, C1-C6-alkylamino, C1-C4-alkoxycarbonyl, C1-C4-alkylaminocarbonyl and cyclopropyl, where alkyl may be substituted by a hydroxyl substituent, or a salt thereof.
地址 Monheim DE