发明授权
US5589471A Vitamin D analogues containing a hydroxy or alkylated hydroxy group in
the 20-position
失效
在20位含有羟基或烷基化羟基的维生素D类似物
- 专利标题: Vitamin D analogues containing a hydroxy or alkylated hydroxy group in the 20-position
- 专利标题(中): 在20位含有羟基或烷基化羟基的维生素D类似物
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申请号: US362550申请日: 1995-01-03
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公开(公告)号: US5589471A公开(公告)日: 1996-12-31
- 发明人: Kai Hansen , Claus Aage S. Bretting
- 申请人: Kai Hansen , Claus Aage S. Bretting
- 申请人地址: DKX Ballerup
- 专利权人: Fabrik Produktionsaktieselskab Leo Pharmaceutical Products Ltd.
- 当前专利权人: Fabrik Produktionsaktieselskab Leo Pharmaceutical Products Ltd.
- 当前专利权人地址: DKX Ballerup
- 优先权: GBX9220439 19920928
- 主分类号: A61K31/59
- IPC分类号: A61K31/59 ; A61K31/593 ; A61P3/08 ; A61P9/12 ; A61P11/00 ; A61P17/00 ; A61P29/00 ; A61P35/00 ; A61P37/00 ; A61P43/00 ; C07C401/00
摘要:
Compounds of formula ##STR1## wherein Q is a --CH.sub.2 --, --CH.dbd.CH-- or --C.dbd.C--; U is a C.sub.1 -C.sub.6 alkylene; R.sup.1 is hydrogen, a C.sub.1 -C.sub.4 alkyl or YR' in which Y stands for the radicals --SO-- or --SO.sub.2 -- and R' stands for a C.sub.1 -C.sub.4 alkyl; R.sup.2 and R.sup.3 are independently hydrogen or C.sub.1 -C.sub.4 alkyl, and additionally R.sup.2 and R.sup.3, when taken together with the starred carbon atom, may form a C.sub.3 -C.sub.6 carbocyclic ring; Z is hydrogen or hydroxy; and derivatives thereof. The compounds show antiinflammatory and immunomodulating effects as well as strong activity in inducing differentiation and inhibiting undesirable proliferation of certain cells. The compounds are prepared by adding an anion R.sup.- to 1(S),1(R)-bis-(tert-butyldimethylsilyl-oxy)-9,10-secopregna-5(E),7(E),10(19)-triene-20-one and the resulting compound is alkylated or acylated with R.sup.1 X.sup.1 where X.sup.1 is a leaving group followed by triplet-sensitized photoisomerization and deprotection to give the compound of formula I.
公开/授权文献
- US06091095A Semiconductor storage 公开/授权日:2000-07-18
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