2-ALKYLIDENE-19-NOR-VITAMIN D COMPOUNDS,申请号EP19980905102-传众专利搜索

2-ALKYLIDENE-19-NOR-VITAMIN D COMPOUNDS

申请公布号：EP0970047(A1)

申请号：EP19980905102

申请日期：1998.02.11

申请公布日期：2000.01.12

申请人：

WISCONSIN ALUMNI RESEARCH FOUNDATION

发明人：DELUCA, HECTOR, F.;SICINSKI, RAFAL, R.

分类号：A61K31/593;A61P19/08;A61P19/10;C07C35/17;C07C49/743;C07C69/732;C07C69/757;C07C401/00;C07F7/18;C07F9/53;C07F19/00;(IPC1-7):C07C401/00;C07F9/46;A61K31/59

主分类号：A61K31/593

摘要：<p>This invention provides a novel class of vitamin D related compounds, namely, the 2-alkylidene-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 and R8, which may be the same or different, are each selected from hydrogen, alkyl, hydroxyalkyl and fluoroalkyl, or when taken together represent the group -(CH2)x- where x is an integer from 2 to 5, and where the group R represents any of the typical side chains known for vitamin D type compounds. These 2-substituted compounds are characterized by low intestinal calcium transport activity and 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.</p>