24-homo vitamin d derivatives, process for their production...

Details 24-homo vitamin d derivatives, process for their production... 24-homo vitamin d derivatives, process for their production...

C - Chemistry, Metallurgy

07

C

167/248, 167/283

C07C 401/00 (2006.01) A61K 31/59 (2006.01)

Patent

CA 2026671

New 24-homo vitamin D derivatives of formula I Image are described, in which R1 means a hydrogen atom, a hydroxy, an alkanoyloxy group with 1 to 8 carbon atoms or an aralkanoyloxy group with up to 8 carbon atoms, R2 and R3, independently of one another, mean a linear or branched alkyl group with 1 to 4 carbon atoms, a trifluoromethyl group or together mean a saturated carbocyclic ring with 3 to 9 carbon atoms formed with carbon atom 25, R4 and R5, independently of one another, mean a hydrogen atom, an alkanoyl group with 1 to 8 carbon atoms, or an aralkanoyl group with up to 8 carbon atoms, and A and B each mean a hydrogen or together a second bond, and n stands for 1, 2, 3, 4 or 5. A process for production, or these derivatives and pharmaceutical preparations which contain them are also provided. These 24-homo vitamin D derivatives have proliferation-inhibiting and cell-differentiating action.

Divulgation de nouveaux dérivés d'homovitamine D substituée en position 24, de formule I Image , dans laquelle R1 représente un atome d'hydrogène, un hydroxyle, un groupement alcanoyloxy comportant de 1 à 8 atomes de carbone ou un groupement aralcanoyloxy comportant de 1 à 8 atomes de carbone, R2 et R3 représentent de manière indépendante un goupement alkyle linéaire ou ramifié comportant de 1 à 4 atomes de carbone, un groupement trifluorométhyle ou représentent ensemble un noyau carbocyclique saturé comportant de 3 à 9 atomes de carbone, formé à l'aide de l'atome de carbone 25, R4 et R5 représentent de manière indépendante un atome d'hydrogène, un groupement alcanoyle comportant de 1 à 8 atomes de carbone ou un groupement aralcanoyle comportant jusqu'à 8 atomes de carbone, A et B représentent un atome d'hydrogène ou ensemble une double liaison, et n est égal à 1, 2, 3, 4 ou 5. Un procédé de production de ces dérivés et de préparations pharmaceutiques les contenant est également dévoilé. Ces dérivés d'homovitamine D substituée en position 24 empêchent la prolifération des cellules et induisent leur différentiation.

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