发明名称 22-thio vitamin D derivatives
摘要 PCT No. PCT/DK93/00425 Sec. 371 Date Apr. 11, 1995 Sec. 102(e) Date Apr. 11, 1995 PCT Filed Dec. 17, 1993 PCT Pub. No. WO94/14766 PCT Pub. Date Jul. 7, 1994The present invention relates to compounds of the following formula <IMAGE> in which Y is sulfur, S(O), or S(O)2; R stands for C1-C3 alkyl, or can form a C3-C8 carbocyclic ring. Q is a C1-C8 hydrocarbylene diradical; and derivatives thereof. The compounds can be made by reacting a 20(S)-formyl vitamin D derivative with tert-butyl hypochlorite to form the corresponding acid chloride which is then reacted with potassium O-ethyl dithiocarbonate followed by photochemical reaction and decarbonylation, treatment with aminoethanol, and conversion to the 22-thiol. The 22-thiol is then alkylated to form the desired sidechain. The compounds show antiinflammatory and immunomodulating effects. They also exhibit strong activity in inducing differentiation and inhibiting undesirable proliferation of certain cells.
申请公布号 US5554599(A) 申请公布日期 1996.09.10
申请号 US19950411634 申请日期 1995.04.11
申请人 LEO PHARMACEUTICAL PRODUCTS LTD. 发明人 GRUE-S+526 RENSEN, GUNNAR;UTTOSEN, ERIK R.
分类号 A61K31/59;A61P3/02;A61P3/08;A61P9/12;A61P17/00;A61P35/00;A61P37/00;A61P43/00;C07C401/00;(IPC1-7):A61K31/59 主分类号 A61K31/59
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