Selective thrombin inhibitors

Details Selective thrombin inhibitors Selective thrombin inhibitors

C - Chemistry, Metallurgy

07

C

C07C 311/18 (2006.01) A61K 31/16 (2006.01) A61K 31/195 (2006.01) A61K 31/215 (2006.01) A61K 31/445 (2006.01) A61K 31/495 (2006.01) C07C 257/22 (2006.01) C07C 311/19 (2006.01) C07C 311/29 (2006.01) C07C 311/41 (2006.01) C07C 311/42 (2006.01) C07D 211/60 (2006.01) C07D 241/04 (2006.01) C07D 295/16 (2006.01) C07D 295/185 (2006.01) C07D 295/205 (2006.01) C07D 295/26 (2006.01)

Patent

CA 2188690

The present invention relates to a novel selective thrombin inhibitor having the following formula (I), which is also effec- tive by oral administration: Image in which R1 represents acetyl substituted with aryl or aryloxy, or represents sulfonyl substituted with substituted or unsub- stituted aryl or N-containing heterocyclic group, X represents a group of formula Image R2 and R3 independently of one another represent hydrogen; cy- cloalkyl substituted or unsubstituted with carboxyl or alkoxycarbonyl; arylalkyloxy; hydroxy; or lower alkyl substi tuted or unsubstituted with carboxyl, alkoxycarbonyl or hydroxy, or R2 and R3 together with nitrogen atom to which they are attached can form a piperidine group substituted with carboxyl or alkoxycarbonyl, R4 represents hydrogen, lower alkyl or lower alkoxy, R5 represents alkanesulfonyl; alkoxycarbonyl; alkylcarbonyl; formyl; lower alkyl; aryl substituted or unsubstituted with alkoxy or haloalkyl; or hydroxy-substituted lower alkyl, and R6 and R7 independently of one another represent hydrogen, lower alkyl or amino, and to a process four preparation thereof and a pharmaceutical composition for thrombin inhibition which comprises the compound of formula (I) as an active ingredient.

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