Benzimidazoles having antithrombotic activity

US6248770A · kind A · utility

Assignee

• BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG · DE

Inventors

• Uwe Ries · Biberach an der Riß, DE
• Iris Kauffmann · Biberach, DE
• Norbert Hauel · Schemmerhofen, DE
• Henning Priepke · Warthausen, DE
• Herbert Nar · Ochsenhausen, DE
• Jean-Marie Stassen · Bad Buchau, DE
• Wolfgang Wienen · Äpfingen, DE

Key dates

• Filing date: Jun 24, 1999
• Grant date: Jun 19, 2001
• Expiry date: Jun 24, 2019

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D403/08
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present invention relates to new benzimidazoles of general formula ##STR1## wherein PA1 R.sub.a to R.sub.c, A, Ar and B are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof the prodrugs, the derivatives thereof which contain a group which is negatively charged under physiological conditions, instead of a carboxy group, and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties. The compounds of the above general formula I wherein R.sub.c denotes a cyano group are valuable intermediates for preparing the other compounds of general formula I, and the compounds of the above general formula I wherein R.sub.c denotes one of the amidino groups mentioned in claim 1 which have valuable pharmacological properties, particularly an antithrombotic activity.