BICYCLIC AROMATIC AMIDINE DERIVATIVE

PROBLEM TO BE SOLVED: To obtain the subject new compound shown by a specific formula, having blood coagulation factor Xa inhibitory activity, thus useful as a preventive/therapeutic agent for diseases due to thrombus, embolism, etc. SOLUTION: This new compound is shown by formula I (Ar is benzene ri...

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Hauptverfasser: KAWAMOTO HIROSHI, NOMOTO TAKASHI, HAYASHI KYOKO, MIYAJI MITSURU, SATO YOSHIYUKI, TAKAENOKI YOUKO
Format: Patent
Sprache:eng
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Zusammenfassung:PROBLEM TO BE SOLVED: To obtain the subject new compound shown by a specific formula, having blood coagulation factor Xa inhibitory activity, thus useful as a preventive/therapeutic agent for diseases due to thrombus, embolism, etc. SOLUTION: This new compound is shown by formula I (Ar is benzene ring or a heteroaromatic ring bearing 1 to 3 heteroatom(s); Q is a 3-7C alkylene, alkenylene or alkynylene; Y is a 5- to 10-membered monocyclic or bicyclic heterocyclic group bearing at least one N (atom), e.g. (E)-2-(7-amidino-2- naphthyl)-5-(isoindolin-5-yl)-4-pentenonic ethyl ester dihydrochloride. This compound of formula I is obtained, pref., for example, by reaction of a compound of formula II with hydrogen chloride directly in an alcohol solvent. The compound of formula II is prepared, pref. by uncleophilic substitution reaction between a compound of formula III and a compound of formula IV.