20-aralkyl-5.alpha.-pregnane derivatives

Details 20-aralkyl-5.alpha.-pregnane derivatives 20-aralkyl-5.alpha.-pregnane derivatives

C - Chemistry, Metallurgy

07

J

C07J 9/00 (2006.01) A61K 31/575 (2006.01) C07J 31/00 (2006.01) C07J 41/00 (2006.01) C07J 51/00 (2006.01)

Patent

CA 2289675

The invention relates to 20-aralkyl-5.alpha.-pregnane derivative having general formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 is (H,OR), (H,OSO3H) or NOR; R is H, (C1-6)alkyl or (C1-6)acyl; each of R2 and R3 is independently hydrogen or (C1-6)alkyl; X is a straight chain divalent C1- 8 hydrocarbon radical, optionally comprising a double or a triple bond; or X is -(CH2)m-CR7R8-; m = 0-4; at least one of R7 and R8 is (C1-4)alkyl, hydroxy, (C1-4)alkoxy or halogen; the other, if present, being hydrogen; or R7 and R8 together represent O or NOR'; R' is H, (C1-6)alkyl or (C1-6)acyl; each of R4, R5 and R6 is independently hydrogen, hydroxy, (C1-4)alkoxy, halogen, NR9, R10 or (C1-4)alkyl, optionally substituted by hydroxy, alkoxy, halogen or oxo; each of R9 and R10 is independently hydrogen or (C1-4)alkyl; and the dotted lines indicate a .DELTA.7 or a .DELTA.8 double bond, or a pair of conjugated double bonds selected from .DELTA.7,14, .DELTA.8,14 and .DELTA.6,8(14). The compounds of the invention have meiosis activating activity and can be used for the control of fertility.

La présente invention concerne un dérivé de 20-aralkyl-5.alpha.-pregnane présentant la formule générale (I) ou un sel pharmaceutiquement acceptable de ce dernier. Dans la formule, R¿1? est (H,OR), (HOSO¿3?H) ou NOR; R est H, alkyle (C¿1-6?) ou acyle (C¿1-6?). Chaque élément parmi R¿2? et R¿3? est indépendamment hydrogène ou alkyle (C¿1-6?); X est radical d'hydrocarbure C¿1-8? divalent à chaîne droite, comprenant éventuellement une double ou triple liaison; ou X est -(CH¿2?)¿m?-CR¿7?R¿8?-; m = 0-4; au moins un élément parmi R¿7? et R¿8? est alkyle (C¿1-4?), hydroxy, alcoxy (C¿1-4?) ou halogène. L'autre élément, lorsqu'il est présent est de l'hydrogène; ou R¿7? et R¿8? ensemble représentent O ou NOR'. R' est H, alkyle (C¿1-6?) ou acyle (C¿1-6?). Chaque élément parmi R¿4?, R¿5? et R¿6? est indépendamment de l'hydrogène, hydroxy, alcoxy (C¿1-4?), halogène, NR¿9?, R¿10? ou alkyle (C¿1-4?), éventuellement substitué par hydroxy, alcoxy, halogène ou oxo. Chaque élément parmi R¿9? et R¿10? est indépendamment de l'hydrogène ou alkyle (C¿1-4?); et les lignes pointillés indiquent une double liaison .DELTA.?7¿, ou .DELTA.?8¿, ou une paire de doubles liaisons conjuguées sélectionnées parmi .DELTA.?7,14¿, .DELTA.?8,14¿ et .DELTA.?6,8(14)¿. Les composés selon l'invention assure une activation de la méiose et permettent de contrôler la fertilité.

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