22s-hydroxycholesta-8, 14-diene derivatives with meiosis...

Details 22s-hydroxycholesta-8, 14-diene derivatives with meiosis... 22s-hydroxycholesta-8, 14-diene derivatives with meiosis...

C - Chemistry, Metallurgy

07

J

C07J 9/00 (2006.01) A61K 31/575 (2006.01)

Patent

CA 2352337

The invention relates to 22S-hydroxycholesta-8, 14-diene derivatives having general formula (I) wherein R1 is OR, OSO3H or = NOR; with R being H, (C1-6) alkyl or (C1-6) acyl; each of R2 and R3 is independently hydrogen or (C1-6) alkyl; R4 is hydrogen, (C1-6) alkyl or (C1-6) acyl; R5 is hydrogen; or R5 designates, together with R6, an additional bond between the carbon atoms at which R5 and R6 are placed; R6 is hydrogen, hydroxy or halogen, or R6 designates, together with R5, an additional bond between the carbon atoms at which R6 and R5 are placed; each or R7 and R8 is independently hydrogen or (C1- 4) alkyl, optionally substituted with OH, (C1-4) alkoxy, or halogen; or a pharmaceutically acceptable salt thereof. The compounds of the invention have meiosis activating activity and can be used for the control of fertility.

L'invention concerne des dérivés de 22S-hydroxycholesta-8, 14-diène de formule générale (I) dans laquelle R¿1? désigne OR, OSO¿3?H ou = NOR; R désignant H, (C¿1-6?) alkyle ou (C¿1-6?) acyle; chaque R¿2? et R¿3? désigne indépendamment un hydrogène ou (C¿1-6?) alkyle; R¿4? désigne un hydrogène, (C¿1-6?) alkyle ou (C¿1-6?) acyle; R¿5? désigne un hydrogène; ou R¿5? désigne, avec R¿6?, une liaison supplémentaire entre les atomes de carbone sur laquelle R¿5? et R¿6? sont placés; R¿7? et R¿8? désignent, chacun pris indépendamment, un hydrogène ou (C¿1-4?) alkyle, éventuellement substitué par OH, (C¿1-4?) alcoxy, ou halogène; ou leur sel pharmaceutiquement acceptable. Les composés de cette invention ont une activité stimulant la méiose et peuvent être utilisés pour contrôler la fertilité.

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