JP2844329B

• Main Authors: FUAN SUNRYURU, I GU, O YONSU, FUAN SANYORU, JON INA, PPON SONUON, KIMU SANSU, I YONHI, SHIN YUSUN, YUN MIKYON
• Format: Patent
• Language: English
• Published: 06.01.1999
• Edition: 6
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

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