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1. 发明授权

US06518262B1 22R-hydroxycholesta-8, 14-diene derivatives for the inhibition of meiosis 失效
标题翻译： 22R-羟胆甾-8 -14-二烯衍生物用于抑制减数分裂
公开(公告)号：US06518262B1
公开(公告)日：2003-02-11
申请号：US09914061
申请日：2001-08-22
申请人： D. Leysen , J. van der Louw , R. G. J. M. Hanssen , Anja Wiersma
发明人： D. Leysen , J. van der Louw , R. G. J. M. Hanssen , Anja Wiersma
IPC分类号： A61K3156
CPC分类号： C07J9/00 , C07J31/006 , C07J41/0094
摘要： 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.
摘要翻译：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。

2. 发明授权

US06528501B1 22s-hydroxycholesta-8, 14-diene derivatives with meiosis regulating activity 失效
标题翻译：具有减数分裂调节活性的22s-羟胆甾-8 -14-二烯衍生物
公开(公告)号：US06528501B1
公开(公告)日：2003-03-04
申请号：US09857731
申请日：2001-07-16
申请人： Dirk D. Leysen , Jaap J. van der Louw , Robert Gerard Jules Marie Hanssen , A. Anja Wiersma
发明人： Dirk D. Leysen , Jaap J. van der Louw , Robert Gerard Jules Marie Hanssen , A. Anja Wiersma
IPC分类号： C07J900
CPC分类号： C07J9/00
摘要： 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.

3. 发明授权

US06552011B1 (Androst-5-en-17beta -yl)alkyl sulfoxides and sulfones and their use for control of fertility 失效
标题翻译：（雄甾-5-en-17β-基）烷基亚砜和砜及其用于控制生育力的用途
公开(公告)号：US06552011B1
公开(公告)日：2003-04-22
申请号：US09913932
申请日：2001-08-20
申请人： Dirk Leysen , Jaap van der Louw , Anja Wiersma
发明人： Dirk Leysen , Jaap van der Louw , Anja Wiersma
IPC分类号： A61K3156
CPC分类号： A61K31/573 , Y10S514/841 , Y10S514/843
摘要： The invention relates to (androst-5-en-17beta-yl)alkylsulfoxides and sulfones having general formula (I), wherein R1, R2, R3, X and Y are defined in the specification. The compounds of the invention have meiosis inhibiting activity and can be used for the control of fertility.
摘要翻译：本发明涉及具有通式（I）的（雄甾-5-烯-17β-基）烷基亚砜和砜，其中R1，R2，R3，X和Y在本说明书中定义。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。

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