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1. 发明授权

US4739050A 2-phenyl-1,4-benzothiazin-3-one derivatives 失效
公开(公告)号：US4739050A
公开(公告)日：1988-04-19
申请号：US928277
申请日：1986-11-04
申请人： Iwao Jun-ichi , Iso Tadashi , Oya Masayuki
发明人： Iwao Jun-ichi , Iso Tadashi , Oya Masayuki
IPC分类号： A61K31/54 , A61K31/5415 , A61P3/00 , A61P3/14 , A61P7/02 , A61P9/08 , A61P9/10 , A61P9/12 , C07D279/16 , C07D317/00 , C07D417/06 , C07D417/12 , C07D279/10 , A61K31/38
CPC分类号： C07D417/06 , C07D279/16 , C07D417/12
摘要： This invention relates to 2-arylbenzothiazine derivatives of the formula[I] and salts thereof, process of preparation and therapeutic drug comprising them for circulatory diseases, ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are hydrogen, lower alkyl, hydroxy, lower alkoxy, acyloxy, tetrahydropyranyloxy, halogen, nitro, amino, lower alkylamino or ##STR2## and the lower alkoxy group may be substituted by halogen, formyl, lower alkoxy or epoxy;R.sup.3 is hydrogen or lower alkyl;R.sup.4 is hydrogen, lower alkyl, cycloalkyl, hydroxy, lower alkoxy, mercapto, lower alkylthio, arylthio, halogen, cyano, formyl-lower alkyl, lower alkoxy-lower alkyl or ##STR3## R.sup.5,R.sup.6,R.sup.7 and R.sup.8 are the same or different and are hydrogen, lower alkyl, cycloalkyl, acyl, phenyl, pyridyl or substituted lower alkyl, and the phenyl or pyridyl group may be substituted by lower alkyl, hydroxy, lower alkoxy, lower alkylenedioxy, halogen, nitro, cyano, lower alkanoyloxy or halogeno-lower alkyl, and the substituent(s) of the substituted lower alkyl is(are) hydroxy, phenyl, phenyloxy, phenylcarbonyl or pyridyl, and such phenyl ring of the phenyl, phenyloxy or phenylcarbonyl group and the pyridyl group may further be resubstituted by lower alkyl, hydroxy, lower alkoxy, lower alkylenedioxy, halogen, nitro, cyano, lower alkanoyloxy or halogeno lower alkyl;R.sup.5 and R.sup.6, and R.sup.7 and R.sup.8 may join to form piperidine, piperazine or morpholine ring, and the piperidine or piperazine ring may be substituted by lower alkyl, phenyl, hydroxy-lower alkyl, phenyl-lower alkyl, phenylcarbonyl, phenylcarbonyl-lower alkyl, spheny-(hydroxy) lower alkyl, phenyl-lower alkenylcarbonyl or naphthoxy-(hydroxy)lower alkyl, and such phenyl ring of the phenyl, phenyl-lower alkyl, phenylcarbonyl, phenylcarbonyl-lower alkyl, phenyl-(hydroxy)lower alkyl or phenyl-lower alkenylcarbonyl group may further be resubstituted by lower alkyl, lower alkoxy, alkylenedioxy or halogen;Z is hydrogen, lower alkyl, lower alkoxy, hydroxy, halogen, cyano, nitro, halogeno-lower alkyl or lower alkanoyloxy;A is straight or branched lower alkylene;B is straight or branched lower alkylene which may be substituted by hydroxy; andn is 0 or 1, and when n is 0, both R.sup.4 and Z are not represent hydrogen atom at the same time.

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