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    • 1. 发明授权
    • 22R-hydroxycholesta-8, 14-diene derivatives for the inhibition of meiosis
    • 22R-羟胆甾-8 -14-二烯衍生物用于抑制减数分裂
    • US06518262B1
    • 2003-02-11
    • US09914061
    • 2001-08-22
    • D. LeysenJ. van der LouwR. G. J. M. HanssenAnja Wiersma
    • D. LeysenJ. van der LouwR. G. J. M. HanssenAnja Wiersma
    • A61K3156
    • C07J9/00C07J31/006C07J41/0094
    • The invention relates to 22R-hydroxycholesta-8,14-diene derivatives having general formula (I) wherein R1 is OR, OS03H 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 of 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 inhibiting activity and can be used for the control of fertility.
    • 本发明涉及通式(I)的22R-羟基胆甾-8,14-二烯衍生物,其中R 1为OR,OSO 3 H或= NOR; 其中R为H,(C 1-6)烷基或(C 1-6)酰基; R 2和R 3各自独立地为氢或(C 1-6)烷基; R4是氢,(C1-6)烷基或(C1-6)酰基; R5是氢; 或R 5与R 6一起在R5和R6所在的碳原子之间加上另外的键; R6是氢,羟基或卤素; 或R 6与R 5一起表示R6和R5所在的碳原子之间的附加键; R 7和R 8各自独立地为氢或任选被OH,(C 1-4)烷氧基或卤素取代的(C 1-4)烷基; 或其药学上可接受的盐。 本发明的化合物具有减数分裂抑制活性,可用于控制生育力。