24,24-difluorinated analogs of 1-alpha,25-dihydroxy vitamin d3

Details 24,24-difluorinated analogs of 1-alpha,25-dihydroxy vitamin d3 24,24-difluorinated analogs of 1-alpha,25-dihydroxy vitamin d3

C - Chemistry, Metallurgy

07

C

C07C 401/00 (2006.01)

Patent

CA 2334347

Fluorinated analogs of 1.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 (see formul below)

Analogues fluorés de 1 alpha ,25-dihydroxyvitamine D3. Ces analogues sont synthétisés de façon convergente par réunion de fragments de noyau A et de noyau C,D. Chaque analogue hybride, étant donné qu'il possède un groupe 1-hydroxyméthyle abaissant la calcémie et un noyau C,D 16-ène-24, 24-difluoré, ainsi qu'une chaîne latérale, potentialisants est conçu pour être lipophile et inerte envers le catabolisme de l'enzyme 24-hydroxylase. Chaque analogue hybride possédant une stéréochimie de 1 beta ,3 alpha -substituant s'avère présenter une combinaison avantageuse sur le plan pharmacologique d'activités puissantes d'antiprolifération et de transcription in vitro et également une activité calcémique limitée in vivo.

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