COMPOUND ACTING ON CIRCULATORY SYSTEM

PROBLEM TO BE SOLVED: To provide the subject new compound acting on the vascular system of mammals and useful for the improvement of cerebral circulation and the prevention and treatment of stenocardia, hypertension, thrombosis, etc., by the relaxation of vascular muscle or the suppression of platel...

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Hauptverfasser: INABA TAKAYUKI, INOUE TSUTOMU, KIDOKORO SHINPEI, MORITA TADASHI, ISHIKAWA TOMOHIKO, NAITO KENJI, SAKUMA OSAMU, HIDAKA HIROYOSHI, YUASA MASAYUKI
Format: Patent
Sprache:eng
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Zusammenfassung:PROBLEM TO BE SOLVED: To provide the subject new compound acting on the vascular system of mammals and useful for the improvement of cerebral circulation and the prevention and treatment of stenocardia, hypertension, thrombosis, etc., by the relaxation of vascular muscle or the suppression of platelet aggregation. SOLUTION: The objective compound is expressed by the formula I (R1 and R6 are each H, hydroxymethyl, etc.; R7 is H or together with R1 or R6 forms carbonyl, etc.; R8 is methyl, carboxyl, etc.; Ar is benzene ring, etc.; Z is methyl, benzyl, etc.), e.g. 3-amino-5-anilino-4-(2-pyridyl)-2-thiophenecarboxylic acid ethyl ester. The compound of the formula I can be produced by reacting a compound of the formula II (R1 and R2 are each H, methoxy, etc.; R3 is H, etc.) with a halide of the formula X-R4 (X is a halogen; R4 is a substituted lower alkyl) in the presence of a base and optionally subjecting the obtained compound of the formula III (R5 is methyl, etc.), to dealkylation, transesterification, amination, deprotection, esterification, reduction, etc.