发明授权
- 专利标题: Renin inhibiting polyhydroxy-monoamides
- 专利标题(中): 肾素抑制多羟基 - 单酰胺
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申请号: US990779申请日: 1992-12-10
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公开(公告)号: US5354767A公开(公告)日: 1994-10-11
- 发明人: Paul C. Anderson , Gary W. Bantle , Grace L. Jung , Pierre Lavallee , Bruno Simoneau
- 申请人: Paul C. Anderson , Gary W. Bantle , Grace L. Jung , Pierre Lavallee , Bruno Simoneau
- 申请人地址: CAX Laval
- 专利权人: Bio-Mega, Inc.
- 当前专利权人: Bio-Mega, Inc.
- 当前专利权人地址: CAX Laval
- 优先权: CAX2058603 19911230
- 主分类号: C07C235/08
- IPC分类号: C07C235/08 ; C07C235/26 ; C07C235/34 ; C07D233/54 ; C07D233/88 ; C07D277/36 ; C07D307/58 ; A61K31/16
摘要:
Disclosed herein are compounds of the formula:R.sup.1 CH.sub.2 CH(X)CH(Y)CH(Z)CHR.sup.2 C(O)NHCHR.sup.3 CH(OH)CH(OH)R.sup.4wherein R.sup.1 is a terminal unit, for example lower cycloalkyl or phenyl; R.sup.2 is, for example, an optionally substituted alkyl, cycloalkylmethyl, benzyl, 4-imidazolylmethyl, 2-thienylmethyl or 4-thiazolylmethyl; R.sup.3 is alkyl, cycloalkylmethyl or an optionally substituted benzyl; R.sup.4 is alkyl or cycloalkyl; and X and Y each is hydroxy and Z is hydrogen, or X and Z each is hydroxy and Y is hydrogen; with the provisos that (a) the carbon atom bearing R.sup.2 has the "R" configuration except when R.sup.2 is 2-thienylmethyl or 2-thiazolylmethyl, X and Y each is hydroxy and Z is hydrogen, then the carbon atom bearing R.sup.2 has the "S" configuration; (b) the carbon atoms bearing R.sup.3 and R.sup.4 each has the "S" configuration; and (c) the carbon atom located between the last-said two carbon atoms has the "R" configuration. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure.
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