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.
本发明涉及具有一般式(I)的22R-羟基胆甾-8,14-二烯衍
生物,其中R1为OR、OS03H或═NOR;其中R为H、(C1-6)烷基或(C1-6)酰基;R2和R3各自独立地为氢或(C1-6)烷基;R4为氢、(C1-6)烷基或(C1-6)酰基;R5为氢;或R5与R6一起表示在R5和R6所处的碳原子之间的额外键;R6为氢、羟基或卤素;或R6与R5一起表示在R6和R5所处的碳原子之间的额外键;R7和R8各自独立地为氢或(C1-4)烷基,可选地被OH、(C1-4)烷氧基或卤素取代;或其药学上可接受的盐。本发明中的化合物具有减数分裂抑制活性,可用于控制生育率。