发明名称 26,27-homologated-20-epi-2-alkyl-19-nor-vitamin D compounds
摘要 This invention provides a novel class of vitamin D related compounds, namely, the 2-alkyl-19-nor-vitamin D derivatives, as well as a general method for their chemical synthesis. The compounds have the formula: where Y1 and Y2, which may be the same or different, are each selected from the group consisting of hydrogen and a hydroxy-protecting group, R6 is selected from the group consisting of alkyl, hydroxyalkyl and fluoroalkyl, and where the group R represents any of the typical side chains known for vitamin D type compounds. These 2-substituted compounds, especially the 2alpha-methyl and the 2alpha-methyl-20S derivatives, are characterized by relatively high intestinal calcium transport activity and relatively high bone calcium mobilization activity resulting in novel therapeutic agents for the treatment of diseases where bone formation is desired, particularly low bone turnover osteoporosis. These compounds also exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as anti-cancer agents and for the treatment of diseases such as psoriasis.
申请公布号 US2002123638(A1) 申请公布日期 2002.09.05
申请号 US20010999299 申请日期 2001.10.31
申请人 WISCONSIN ALUMNI RESEARCH FOUNDATION 发明人 DELUCA HECTOR F.;SICINSKI RAFAL R.
分类号 A61K31/593;A61P17/06;A61P19/08;A61P19/10;A61P35/00;A61P35/02;C07C401/00;(IPC1-7):C07C401/00 主分类号 A61K31/593
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