公开(公告)号：US07425641B2

公开(公告)日：2008-09-16

申请号：US10938804

申请日：2004-09-10

Applicant: Uwe Ries ,  Henning Priepke ,  Armin Heckel ,  Herbert Nar ,  Wolfgang Wienen ,  Jean Marie Stassen

Inventor： Uwe Ries ,  Henning Priepke ,  Armin Heckel ,  Herbert Nar ,  Wolfgang Wienen ,  Jean Marie Stassen

IPC: C07D272/02 ,  C07D211/06 ,  A61K31/40 ,  A61K31/445

CPC classification number: C07D295/185 ,  C07C257/18 ,  C07C311/21 ,  C07C311/46 ,  C07C2601/08 ,  C07D207/12 ,  C07D211/46 ,  C07D213/68 ,  C07D295/135 ,  C07D295/192

Abstract: The present invention relates to carboxylic acid amides of general formula wherein R1 to R5, Ar, m and n are defined as in claim 1, the tautomers, stereoisomers, mixtures thereof, the prodrugs and the salts thereof which have valuable properties. The compounds of the above general formula I wherein R5 denotes a cyano group are valuable intermediate products for preparing the other compounds of general formula I, and the compounds of the above general formula I wherein R5 denotes one of the amidino groups mentioned in claim 1 have valuable pharmacological properties, particularly an antithrombotic activity and a factor Xa-inhibiting activity.

Abstract translation: 本发明涉及通式其中R 1至R 5，Ar，m和n如权利要求1所定义的羧酸酰胺，互变异构体，立体异构体，混合物 其前体药物及其盐具有有价值的性质。 其中R 5表示氰基的上述通式I的化合物是制备其它通式I化合物的有价值的中间产物，以及上述通式I的化合物，其中R 1， 5 表示权利要求1中提及的脒基之一具有有价值的药理学性质，特别是抗血栓形成活性和因子Xa抑制活性。