Phosphonic acid derivative having inhibitory activity against carboxypeptidase B

• Main Authors: Fushihara, Kenichi, Kikuchi, Chika, Matsushima, Tetsuya, Kanemoto, Kenichi, Satoh, Eriko, Yamamoto, Takehiro, Suzuki, Kokichi
• Format: Patent
• Language: English
• Published: 18.05.2004

The present invention relates to phosphonic acid derivatives having inhibitory activity against carboxypeptidase B, and to pharmaceutical compositions which comprise at least one of said derivative as an active ingredient and are useful for therapeutic and preventive treatment of various thrombosis, diseases caused by a vascular disorder, and organ disorders resulting from reduction of fibrinolysis. A compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof: wherein Rrepresents hydrogen atom, an alkyl group, a substituted alkyl group and the like; Rand Rrepresent hydrogen atom, an alkyl group, a substituted alkyl group, an alkoxyl group and the like; X represents -CH-, -O-, or -NH-; A represents the following group (II): [in which Rand Rrepresent hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group and the like; Rand Rrepresents hydrogen atom, a halogen atom, hydroxyl group, phenyl group, an alkyl group and the like] and the like; and E represents hydrogen atom and the like, which has inhibitory activity against carboxypeptidase B and is useful for therapeutic and/or preventive treatment of a thrombotic disease.