New prodrugs of benzimidazole-5-carboxamide derivative thrombin inhibitor, useful for treating or preventing thrombotic diseases, are well tolerated on subcutaneous injection

摘要

1-Methyl-2-(4-amidinophenylaminomethyl)-benzimidazole-5-carboxylic acid N-(2-pyridyl)-N-(2-carboxyethyl)-amide prodrugs (I) are new. 1-Methyl-2-(4-amidinophenylaminomethyl)-benzimidazole-5-carboxylic acid N-(2-pyridyl)-N-(2-carboxyethyl)-amide prodrugs of formula (I) and their tautomers and salts are new. R' = H or 1-6C (preferably 1-3C) alkyl; R = COOMe or OH; and provided that either: (1) R' is H and R is COOMe; or (2) R is OH and R' is H or 1-6C alkyl. An Independent claim is included for the preparation of (I).