发明名称 |
24,24-DIFLUORINATED ANALOGS OF 1-ALPHA,25-DIHYDROXY VITAMIN D3 |
摘要 |
Fluorinated analogs of l.alpha.,25-dihydroxy vitamin D3. These analogs are synthesized in a convergent manner by joining A-ring and C,D-ring fragments. Each hybrid analog, having a calcemia-lowering 1-hydroxymethyl group and a potentiating 16-ene-24,24-difluorinated C,D-ring and side chain, is designed to be lipophilic and inert toward 24-hydroxylase enzyme catabolism. Each hybrid analog with 1.beta.,3.alpha.-substituent stereochemistry shows a pharmacologically desirable combination of high antiproliferative and high transcriptional activities in vitro and also low calcemic activity in vivo.< /SDOAB>
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申请公布号 |
CA2334347(A1) |
申请公布日期 |
1999.12.09 |
申请号 |
CA19992334347 |
申请日期 |
1999.06.02 |
申请人 |
JOHNS HOPKINS UNIVERSITY |
发明人 |
LEE, JAE KYOO;WANG, QIANG;POSNER, GARY H. |
分类号 |
A61K31/59;(IPC1-7):C07C401/00 |
主分类号 |
A61K31/59 |
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