发明名称 Vitamin D analogues having a halogen-or azido- substituted side chain
摘要 PCT No. PCT/DK95/00305 Sec. 371 Date Jan. 3, 1995 Sec. 102(e) Date Jan. 3, 1995 PCT Filed Sep. 23, 1993 PCT Pub. No. WO94/07851 PCT Pub. Date Apr. 14, 1994A compound of formula I <IMAGE> I wherein R stands for a straight or branched, saturated or unsaturated alkyl group containing from 4 to 12 carbon atoms optionally substituted with a hydroxy group, and possibly containing a ring structure, and in which at least one of the carbon atoms not bearing hydroxyl group is substituted with one or more halogen atoms or an azido group; and prodrugs of I in which one or more of the hydroxy groups are masked as groups which can be reconverted to hydroxy groups in vivo, in pure form or in mixtures. 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 oxidizing 1(S),3(R)-bis-(tert-butyldimethylsilyloxy)-20(S)formyl-9,10-seco-pregna-5(E),7(E),10(19)-triene, reducing the resulting product; alkylating the reduction product and then subjecting the alkylated product to triplet-sensitized photoisomerization.
申请公布号 US5612325(A) 申请公布日期 1997.03.18
申请号 US19950367206 申请日期 1995.01.03
申请人 LEO PHARMACEUTICAL PRODUCTS LTD. A/S (L+526 VENS KEMISKE FABRIK PRODUKTIONSAKTIESELSKAB) 发明人 HANSEN, KAI;PEDERSEN, HENRIK
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;(IPC1-7):A61K31/59 主分类号 A61K31/59
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