Novel substituted -amidinobenzene derivative and pharmaceutical compositions thereof

• Main Authors: AKAMATSU, SEIJIRO, ICHIHARA, MASATO, KAWASAKI, TOMIHISA, MATSUMOTO, YUZO, KAKU, SEIJI
• Format: Patent
• Language: English
• Published: 01.09.2000
• Edition: 7
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

A substituted-amidinobenzene derivative of the following general formula (I) or a salt thereof, and a pharmaceutical composition comprising said derivative or a salt thereof and a pharmaceutically acceptable carrier. The symbols in the above formula have the following meanings: R1: a group which can be converted into an amidino group in vivo; R2 and R3: the same or different and each represents a carboxyl group or a group which can be converted into a carboxyl group in vivo; X1 and X2: the same or different and each represents a lower alkylene group; m: 0, 1 or 2; n: 0 or 1, provided that n=1 when m=0. They have GPIIb/IIIa receptor antagonizing activity and are useful as medicines for ameliorating ischemic cardiac disorders, adminicular in cardiosurgery operations or in vascular surgery operations, medicines for ameliorating cerebrovascular disorders, and medicines for ameliorating peripheral artery disorders. In addition, they are useful as a prodrug excellent in peroral absorbability and sustainment of the effect.