发明授权
US4950659A 16,17-acetalsubstituted androstane-17.beta.-carboxylic acid esters
prossessing high binding affinity to the glucocorticosteroid receptor
失效
16,17-乙缩醛取代的雄甾烷-17β-羧酸酯,其对糖皮质激素受体具有高结合亲和力
- 专利标题: 16,17-acetalsubstituted androstane-17.beta.-carboxylic acid esters prossessing high binding affinity to the glucocorticosteroid receptor
- 专利标题(中): 16,17-乙缩醛取代的雄甾烷-17β-羧酸酯,其对糖皮质激素受体具有高结合亲和力
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申请号: US843771申请日: 1986-03-25
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公开(公告)号: US4950659A公开(公告)日: 1990-08-21
- 发明人: Paul H. Andersson , Per T. Andersson , Bengt I. Axelsson , Bror A. Thalen , Jan W. Trofast
- 申请人: Paul H. Andersson , Per T. Andersson , Bengt I. Axelsson , Bror A. Thalen , Jan W. Trofast
- 申请人地址: SEX Lund
- 专利权人: Aktiebolaget Draco
- 当前专利权人: Aktiebolaget Draco
- 当前专利权人地址: SEX Lund
- 优先权: SEX8501693 19850404
- 主分类号: A61K31/58
- IPC分类号: A61K31/58 ; A61P5/38 ; A61P29/00 ; C07F3/00 ; C07J1/00 ; C07J5/00 ; C07J71/00
摘要:
The invention refers to compounds having anti-inflamatory activity characterized by the formula ##STR1## or a stereoisomeric component thereof, in which formula the 1,2-position is saturated or is a double bondX.sub.1 is selected from hydrogen, fluorine, chlorine and bromineX.sub.2 is selected from hydrogen, fluorine, chlorine and bromineR.sub.1 is selected from hydrogen or a straight or branched hydrocarbon chain having 1-4 carbon atomsR.sub.2 is selected from hydrogen or straight and branched hydrocarbon chains having 1-10 carbon atoms andR.sub.3 is selected from ##STR2## is O or S R.sub.4 is selected from hydrogen, straight or branched hydrocarbon chains having 1-10 carbon atoms or from phenylR.sub.5 is selected from hydrogen or methyl andR.sub.6 is selected from hydrogen, straight or branched, saturated or unsaturated hydrocarbon chains having 1-10 carbon atoms, an alkyl group substituted by at least one halogen atom, a heterocyclic ring system containing 3-10 atoms in the ring system, ##STR3## (m=0,1,2; n=2,3,4,5,6), phenyl or benzyl groups which are unsubstituted or substituted by one or more alkyl, nitro, carboxy, alkoxy, halogen, cyano, carbalkoxy or trifluoromethyl group(s),provided that when R.sub.2 is hydrogen R.sub.1 is methyl.The invention also refers to a process and intermediates for the prearation of these compunds, a pharmaceutical preparation containing one of the compunds and a method for the treatment of inflammatory conditions.
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