发明授权
US4307086A Branched chain and cycloaliphatic esters of the androstane and destrane series and pharmaceutical compositions containing same 失效
雄甾烷和脱水系列的支链和脂环族酯以及含有它们的药物组合物

  • 专利标题: Branched chain and cycloaliphatic esters of the androstane and destrane series and pharmaceutical compositions containing same
  • 专利标题(中): 雄甾烷和脱水系列的支链和脂环族酯以及含有它们的药物组合物
  • 申请号: US120607
    申请日: 1980-02-12
  • 公开(公告)号: US4307086A
    公开(公告)日: 1981-12-22
  • 发明人: Lambert J. W. M. Tax
  • 申请人: Lambert J. W. M. Tax
  • 申请人地址: NC Asheville
  • 专利权人: Akzona Incorporated
  • 当前专利权人: Akzona Incorporated
  • 当前专利权人地址: NC Asheville
  • 优先权: NLX763248 19761126
  • 主分类号: A61K31/565
  • IPC分类号: A61K31/565 C07J1/00 A01N45/00
Branched chain and cycloaliphatic esters of the androstane and destrane
series and pharmaceutical compositions containing same
摘要:
There are disclosed branched chain and cycloaliphatic esters of steroids having the formula: ##STR1## where R is H or CH.sub.3 ;R.sub.1 is H or CH.sub.3 ;R.sub.2 is H or CH.sub.3 ;R.sub.3 is H, OH, CH.sub.3 or Cl;R.sub.4 is H or C.sub.1 to C.sub.4 alkyl;R.sub.5 is H, C.sub.1 to C.sub.4 alkyl or CF.sub.3 ;R.sub.6 is H, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy, halogen or .beta.-OH providing that when R.sub.6 is .beta.-OH, the steroid also contains 9.alpha.-F and further providing that R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 represent at least 4 and at most 5 hydrogen atoms, except in the case of a .DELTA..sup.1,4 -steroid, in which case R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are all hydrogen;R.sub.7 is H or CH.sub.3 ;R.sub.8 is ##STR2## providing the R.sub.8 is --OH or ##STR3## when the steroid has an aromatic ring A and the 3-position is substituted by ##STR4## R.sub.9 is ##STR5## where n is 0, 1 or 2;R.sub.10 is C.sub.1 to C.sub.10 alkyl;R.sub.11 is H or C.sub.1 to C.sub.10 alkyl;R.sub.12 is an aliphatic group with 1 to 18 carbon atoms, or R.sub.10 and R.sub.12 taken together with the carbon atom to which they are attached form a C.sub.7 to C.sub.12 cycloaliphatic group providing the total carbon atom content in the carboxylic acid residue is 8 to 20;ring A is either saturated or has one of the following types of unsaturation: .DELTA..sup.1 ; .DELTA..sup.4 ; .DELTA..sup.1,4 ; .DELTA..sup.5(10) ; .DELTA..sup.1,3,5(10), andX is .dbd.O, --OH or ##STR6## providing that X is OH or ##STR7## when the steroid has an aromatic ring A, The steroid esters have androgenic, anabolic, oestrogenic or anti-oestrogenic properties depending upon the ring configurations and the substituent(s). Pharmaceutical compositions containing the steroid esters are also disclosed.
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