13-azathromboxane-mimic compound, its preparation and remedy for disease caused by thromboxane containing said compound as active component

Abstract

Abstract NEW MATERIAL:The compound of formula I [A is group of formula -CH2CH2- (CH2)m- (m is 1-6), etc.; n is 1-6; R<1> is 2-7C acyloxy, OH-substituted 1-6C alkyl, etc.; R<2> is H or CH3; R<3> is H or OH; R<4> is single bond or 1-5C alkylene; R<5> is 1-8C alkyl, etc.], its acid addition salt, and clathrate compound. EXAMPLE:(5Z,15epsilon)-9,11-Methano-10,10-dimethyl-13-aza-15-hydroxy-1 6-phenyl-17,18, 19, 20-tetranor-11a-carbathromb-5-enoic acid pyvaloyl-oxymethyl ester. USE:It has antagonistic activity to thromboxane A2, especially blood platelet coagulation inhibiting activity. It can be prepared to a drug preparation easily because of its high solubility. PREPARATION:The compound of formula I can be prepared by esterifying the carboxylic acid of formula II with preferably a diazo(substituted)alkane compound corresponding to the objective ester in an inert solvent at 0 deg.C.

Inventors

• 👤 Yoshinobu Arai
• 👤 義信 新井
• 👤 Hirohisa Wakatsuka
• 👤 若塚　弘久

Bibliographic Details