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NOVEL 1,4-THIAZINE DERIVATIVE, PRODUCTION THEREOF AND ANTIENDOTOXIN SHOCK AGENT

申请公布号:JPS63301876(A)

申请号:JP19870136870

申请日期:1987.05.30

申请公布日期:1988.12.08

申请人:
ZENYAKU KOGYO KK

发明人:TAKASE MUNEAKI;SAITO HIROHISA;HARADA HIDENORI

分类号:C07D279/12;A61K31/54;A61P9/00;A61P37/00;A61P37/04;C07D417/04

主分类号:C07D279/12

摘要:NEW MATERIAL:A 1,4-thiazine derivative expressed by formula I (R1 is nitrogen- containing hetero ring residue, hydroxyl group, lower alkoxy, amino, lower alkylamino, arylamino, cycloalkylamino, heteroamino, hetero lower alkylamino, mercapto, lower alkylthio, arylthio, cycloalkylthio or heterothio; R2 is H or lower alkyl) and acid addition salt thereof. EXAMPLE:3-(1-Imidazoly)-5-methyl-2-oxo-1,4-thiazine. USE:The aimed compound has antiendotoxin shock action and is used in prevention and remedy for e.g. lowering of blood pressure and heart function, formation of hepatitis and thrombus or diffuse vascular solidification. The compound exhibit low toxicity. PREPARATION:A compound expressed by formula II (R' is lower alkyl) is hydrolyzed with an acid and chlorinated and the resultant product is reacted with a nucleophilic agent expressed by formula III to provide the compound expressed by formula I.

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