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    Compound capable of inhibiting 17-beta hydroxysteriod dehydrogenase
    1.
    发明授权
    Compound capable of inhibiting 17-beta hydroxysteriod dehydrogenase 失效
    化合物能抑制17-β羟基二氢脱氢酶

    公开(公告)号：US08558028B2

    公开(公告)日：2013-10-15

    申请号：US12744044

    申请日：2008-11-19

    申请人： Nigel Vicker ,  Helen Victoria Bailey ,  Wesley Heaton ,  Joanna Mary Day ,  Atul Purohit ,  Barry Victor Lloyd Potter

    发明人： Nigel Vicker ,  Helen Victoria Bailey ,  Wesley Heaton ,  Joanna Mary Day ,  Atul Purohit ,  Barry Victor Lloyd Potter

    IPC分类号： A61K31/125 ,  C07C213/00

    CPC分类号： C07D207/26 ,  C07C217/90 ,  C07C233/43 ,  C07C237/42 ,  C07D211/58 ,  C07D211/62 ,  C07D317/66

    摘要： There is provided a compound having Formula I wherein each of R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently selected from (a) H, (b) R13, —OC(R13)3, —OCH(R13)2, —OCH2R13, C(R13)3, —CH(R13)2, or —CH2R13 wherein R13 is a halogen; (c) —CN; (d) optionally substituted alkyl, (e) optionally substituted heteroalkyl; (f) optionally substituted aryl; (g) optionally substituted heteroaryl; (h) optionally substituted arylalkyl; (i) optionally substituted heteroarylalkyl; (j) hydroxy; (k) alkoxy; (l) aryloxy; (m) —SO2-alkyl; and (n) —N(R14)C(O)R15, wherein R14 and R15 are independently selected from H and hydrocarbyl, wherein the optional substituents of (d) (e) (f) (h) and (i) are selected from the group consisting of: C1-6 alkyl, halo, cyano, nitro, haloalkyl, hydroxy, C1-6 alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl; wherein n and p are independently selected from 0 and 1; X is an optional group selected from O, S, S=0, S(═O)2, C═O, S(═O)2NR16, C═ONR17, NR18, in which R16, R17, and R18 are independently selected from H and hydrocarbyl, R10 is selected from H and hydrocarbyl, R11 is selected from CR19R20 and C═O, in which R19 and R20 are independently selected from H and hydrocarbyl, R12 is selected from a substituted five or six membered carbon rings optionally containing one or more hetero atoms selected from N, S, and O and optionally having fused thereto a further ring, and wherein the one or more substituents are selected from hydrocarbyl groups.

    摘要翻译： 提供具有式I的化合物，其中R1，R2，R3，R4，R5，R6，R7，R8和R9各自独立地选自（a）H，（b）R13，-OC（R13）3， - OCH（R 13）2，-OCH 2 R 13，C（R 13）3，-CH（R 13）2或-CH 2 R 13，其中R 13是卤素; （c）-CN; （d）任选取代的烷基，（e）任选取代的杂烷基; （f）任选取代的芳基; （g）任选取代的杂芳基; （h）任选取代的芳基烷基; （i）任选取代的杂芳基烷基; （j）羟基; （k）烷氧基; （I）芳氧基; （m）-SO 2 - 烷基; 和（n）-N（R 14）C（O）R 15，其中R 14和R 15独立地选自H和烃基，其中选择（d）（e）（f）（h）和（i） 羟基，C 1-6烷氧基，羧基，羧基烷基，羧酰胺，巯基，氨基，烷基氨基，二烷基氨基，磺酰基，亚磺酰氨基，芳基和杂芳基; 其中n和p独立地选自0和1; X是选自O，S，S = 0，S（= O）2，C = O，S（= O）2NR16，C = ONR17，NR18的任选基团，其中R 16，R 17和R 18独立地选自 R 10选自H和烃基，R 11选自CR 19 R 20和C = O，其中R 19和R 20独立地选自H和烃基，R 12选自取代的五或六元碳环，任选含有 一个或多个选自N，S和O的杂原子，并且任选地与另一个环稠合，并且其中一个或多个取代基选自烃基。

    COMPOUND CAPABLE OF INHIBITING 17-BETA HYDROXYSTERIOD DEHYDROGENASE
    3.
    发明申请
    COMPOUND CAPABLE OF INHIBITING 17-BETA HYDROXYSTERIOD DEHYDROGENASE 失效
    抑制17-β羟化酶脱氢酶的化合物

    公开(公告)号：US20100286204A1

    公开(公告)日：2010-11-11

    申请号：US12744044

    申请日：2008-11-19

    申请人： Nigel Vicker ,  Helen Victoria Bailey ,  Wesley Heaton ,  Joanna Mary Day ,  Atul Purohit ,  Barry Victor Lloyd Potter

    发明人： Nigel Vicker ,  Helen Victoria Bailey ,  Wesley Heaton ,  Joanna Mary Day ,  Atul Purohit ,  Barry Victor Lloyd Potter

    IPC分类号： A61K31/4468 ,  C07C233/43 ,  A61K31/167 ,  C07D317/66 ,  A61K31/357 ,  C07D211/58 ,  C07D211/62 ,  A61K31/445 ,  C07C233/81 ,  C07D209/14 ,  A61K31/404 ,  C07D207/27 ,  A61K31/402 ,  A61P35/00

    CPC分类号： C07D207/26 ,  C07C217/90 ,  C07C233/43 ,  C07C237/42 ,  C07D211/58 ,  C07D211/62 ,  C07D317/66

    摘要： There is provided a compound having Formula I wherein each of R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently selected from (a) H, (b) R13, —OC(R13)3, —OCH(R13)2, —OCH2R13, C(R13)3, —CH(R13)2, or —CH2R13 wherein R13 is a halogen; (c) —CN; (d) optionally substituted alkyl, (e) optionally substituted heteroalkyl; (f) optionally substituted aryl; (g) optionally substituted heteroaryl; (h) optionally substituted arylalkyl; (i) optionally substituted heteroarylalkyl; (j) hydroxy; (k) alkoxy; (l) aryloxy; (m) —SO2-alkyl; and (n) —N(R14)C(O)R15, wherein R14 and R15 are independently selected from H and hydrocarbyl, wherein the optional substituents of (d) (e) (f) (h) and (i) are selected from the group consisting of: C1-6 alkyl, halo, cyano, nitro, haloalkyl, hydroxy, C1-6 alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl; wherein n and p are independently selected from 0 and 1; X is an optional group selected from O, S, S=0, S(═O)2, C═O, S(═O)2NR16, C═ONR17, NR18, in which R16, R17, and R18 are independently selected from H and hydrocarbyl, R10 is selected from H and hydrocarbyl, R11 is selected from CR19R20 and C═O, in which R19 and R20 are independently selected from H and hydrocarbyl, R12 is selected from a substituted five or six membered carbon rings optionally containing one or more hetero atoms selected from N, S, and O and optionally having fused thereto a further ring, and wherein the one or more substituents are selected from hydrocarbyl groups.

    摘要翻译： 提供具有式I的化合物，其中R1，R2，R3，R4，R5，R6，R7，R8和R9各自独立地选自（a）H，（b）R13，-OC（R13）3， - OCH（R 13）2，-OCH 2 R 13，C（R 13）3，-CH（R 13）2或-CH 2 R 13，其中R 13是卤素; （c）-CN; （d）任选取代的烷基，（e）任选取代的杂烷基; （f）任选取代的芳基; （g）任选取代的杂芳基; （h）任选取代的芳基烷基; （i）任选取代的杂芳基烷基; （j）羟基; （k）烷氧基; （I）芳氧基; （m）-SO 2 - 烷基; 和（n）-N（R 14）C（O）R 15，其中R 14和R 15独立地选自H和烃基，其中选择（d）（e）（f）（h）和（i） 羟基，C 1-6烷氧基，羧基，羧基烷基，羧酰胺，巯基，氨基，烷基氨基，二烷基氨基，磺酰基，亚磺酰氨基，芳基和杂芳基; 其中n和p独立地选自0和1; X是选自O，S，S = 0，S（= O）2，C = O，S（= O）2 NR 16，C = CONR 17，NR 18的任选基团，其中R 16，R 17和R 18独立地选自 由H和烃基组成，R 10选自H和烃基，R 11选自CR 19 R 20和C = O，其中R 19和R 20独立地选自H和烃基，R 12选自取代的五或六元碳环，任选含有 一个或多个选自N，S和O的杂原子，并且任选地与另一个环稠合，并且其中一个或多个取代基选自烃基。