发明授权
US5187271A N-substituted (.alpha.-imidazolyl-toluyl) pyrrole compounds for
treatment of circulatory disorders
失效
N-取代((ALPHA)-IMIDAZOLYL-TOLUYL)用于治疗循环障碍的吡咯化合物
- 专利标题: N-substituted (.alpha.-imidazolyl-toluyl) pyrrole compounds for treatment of circulatory disorders
- 专利标题(中): N-取代((ALPHA)-IMIDAZOLYL-TOLUYL)用于治疗循环障碍的吡咯化合物
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申请号: US662584申请日: 1991-02-28
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公开(公告)号: US5187271A公开(公告)日: 1993-02-16
- 发明人: Philippe R. Bovy , Joe T. Collins , Robert E. Manning
- 申请人: Philippe R. Bovy , Joe T. Collins , Robert E. Manning
- 申请人地址: IL Chicago
- 专利权人: G. D. Searle & Co.
- 当前专利权人: G. D. Searle & Co.
- 当前专利权人地址: IL Chicago
- 主分类号: C07D403/10
- IPC分类号: C07D403/10 ; C07D403/14
摘要:
A class of N-substituted (.alpha.-imidazolyl-toluyl)pyrrole compounds described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein m is one; wherein each of R.sup.0 and R.sup.1 is independently selected from hydrido, alkyl, hydroxyalkyl, formyl, halo, haloalkyl, cycloalkylcarbonyl, alkoxy, aroyl, aryloxy, aralkoxy, alkylcarbonyl, alkoxycarbonyl, cyano, nitro, carboxyl, alkylcarbonyloxy, alkylcarbonyloxyalkyl, alkoxycarbonylalkyl, aralkoxycarbonylalkyl, alkylsulfonyl, aralkylsulfonyl, arylsulfonyl; wherein R.sup.2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, propylthio, butylthio, and hydroxyalkyl; wherein each of R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 is independently selected from hydrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl and methoxycarbonyl; with the proviso that at least one of R.sup.5 and R.sup.8 must be selected from COOH, PO.sub.3 H.sub.2, SO.sub.3 H, CONHNH.sub.2, CONHNHSO.sub.2 CF.sub.3, ##STR2## wherein each of R.sup.42 and R.sup.43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-aceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.
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