Non-calcemic, antiproliferative, transcriptionally active 24-fluorinated hybrid analogs of 1.alpha.,-25-dihydroxy vitamin D.sub.3
US6043386A · kind A · utility
5Cited by
6References
6Claims
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Key dates
| Filing date | Jun 1, 1999 |
| Grant date | Mar 28, 2000 |
| Priority date | — |
| Expiry date | Jun 1, 2019 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K31/59
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Fluorinated analogs of 1.alpha.,25-dihydroxyvitamin D.sub.3. 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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.