发明授权
- 专利标题: Novel 10.beta.-alkynyl-steroids
- 专利标题(中): 新型10个β-炔基 - 类固醇
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申请号: US18199申请日: 1987-02-24
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公开(公告)号: US4987128A公开(公告)日: 1991-01-22
- 发明人: Lucien Nedelec , Francois Nique , Anne-Marie Moura
- 申请人: Lucien Nedelec , Francois Nique , Anne-Marie Moura
- 申请人地址: FRX Paris
- 专利权人: Roussel Uclaf
- 当前专利权人: Roussel Uclaf
- 当前专利权人地址: FRX Paris
- 优先权: FRX8602510 19860224
- 主分类号: A61K31/585
- IPC分类号: A61K31/585 ; A61P9/00 ; C07J1/00 ; C07J21/00 ; C07J31/00 ; C07J33/00 ; C07J43/00 ; C07J53/00
摘要:
Novel 10.beta.-alkynyl-steroids of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, optionally substituted alkyl and alkoxy of 1 to 8 carbon atoms, optionally substituted alkenyl and alkynyl of 2 to 8 carbon atoms, optionally substituted aryl and aralkyl, optionally esterified carboxy, dialkylamino with alkyl of 1 to 6 carbon atoms, halogen and trialkylsilyl of 1 to 7 alkyl carbon atoms, R.sub.6 and R.sub.7 taken together with the carbon atoms to which they are attached form cyclopropyl or R.sub.6 is hydrogen and R.sub.7 is R.sub.1, R.sub.1 is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms, optionally substituted alkenyl and alkynyl of 2 to 6 carbon atoms and acetylthio, R.sub.2 is methyl or ethyl, X and Y taken together form a member selected from the group consisting of ##STR2## Alk is alkyl of 1 to 8 carbon atoms or X is hydroxy and Y is ##STR3## or X is optionally acylated or etherified hydroxy and Y is selected from the group consisting of --CH.sub.2 --CH.sub.2 --CH.sub.2 --OH, hydrogen, R.sub.4, and --CH.sub.2 --CH.sub.2 --COOM, M is selected from the group consisting of hydrogen, --NH.sub.4 and alkali metal and R.sub.4 is selected from the group consisting of alkyl of 1 to 6 carbon atoms and alkenyl and alkynyl of 2 to 6 carbon atoms, the dotted lines indicate the optional presence of a second carbon-carbon bond when R.sub.6 and R.sub.7 and the carbon to which they are attached do not form cyclopropyl and the wavy lines indicate that R.sub.6 and R.sub.7 may be in the .alpha. or .beta. position with the proviso that R is not hydrogen when R.sub.6 and R.sub.7 are hydrogen, R.sub.2 is methyl, X is optionally acylated or etherified hydroxy, Y is hydrogen or R.sub.4 and the dotted lines are not a second carbon-carbon bond having aldosterone antagonistic activity and increased hydrosodic diuresis with organic potassium conservation with little secondary hormone effects.
公开/授权文献
- US5333778A Packaging with integrated partitioning 公开/授权日:1994-08-02
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