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1. 发明授权

US08558028B2 Compound capable of inhibiting 17-beta hydroxysteriod dehydrogenase 失效
标题翻译：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。

2. 发明授权

US08119627B2 Heterocyclic compounds as inhibitors of 17beta-HSD3 有权
标题翻译：杂环化合物作为17β-HSD3的抑制剂
公开(公告)号：US08119627B2
公开(公告)日：2012-02-21
申请号：US11968436
申请日：2008-01-02
申请人： Nigel Vicker , Joanna Mary Day , Helen Victoria Bailey , Wesley Heaton , Ana Maria Ramos Gonzalez , Christopher Mark Sharland , Michael John Reed , Atul Purohit , Barry Victor Lloyd Potter
发明人： Nigel Vicker , Joanna Mary Day , Helen Victoria Bailey , Wesley Heaton , Ana Maria Ramos Gonzalez , Christopher Mark Sharland , Michael John Reed , Atul Purohit , Barry Victor Lloyd Potter
IPC分类号： A61K31/55
CPC分类号： C07C237/22 , C07C233/36 , C07D209/20 , C07D211/56 , C07D211/58 , C07D211/62 , C07D211/96 , C07D215/38 , C07D215/44 , C07D223/12 , C07D223/16 , C07D239/42 , C07D401/12 , C07D401/14 , C07D405/06 , C07D409/06 , C07D409/12 , C07D451/04
摘要： There is provided a compound having Formula (I) wherein each of rings A and B is selected from 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; X is an optional group selected from O, S, —S═O, —S(═O)2, —C═O, —S(═O)2NR8, —C═ONR9, and —NR10, wherein n and p are independently selected from 0 and 1; Y is (R11)1-3 wherein each R11 is independently selected from —NR12, —CR13R14, —S(═O)2 and —C═O; Z is selected from (i) six or seven membered ring containing carbon and at least one nitrogen, which may be optionally substituted wherein the substituents may together form further ring fused thereto; and (ii) a —R15—NR16— group.
摘要翻译：提供了具有式（I）的化合物，其中环A和B各自选自5或6元碳环，任选地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; X是选自O，S，-S = O，-S（= O）2，-C = O，-S（= O）2 NR 8，-CONONR 9和-NR 10的任选基团，其中n和p 独立地选自0和1; Y是（R 11）1-3，其中每个R 11独立地选自-NR 12，-CR 13 R 14，-S（= O）2和-C≡O; Z选自（i）含有六元或七元环的碳和至少一个氮，其可以是任选取代的，其中取代基可以一起形成稠合的另外的环; 和（ii）-R 15 -NR 16 - 基团。

3. 发明申请

US20100286204A1 COMPOUND CAPABLE OF INHIBITING 17-BETA HYDROXYSTERIOD DEHYDROGENASE 失效
标题翻译：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。

4. 发明申请

US20090023710A1 Compound 有权
公开(公告)号：US20090023710A1
公开(公告)日：2009-01-22
申请号：US11968436
申请日：2008-01-02
申请人： Nigel Vicker , Joanna Mary Day , Helen Victoria Bailey , Wesley Heaton , Ana Maria Ramos Gonzalez , Christopher Mark Sharland , Michael John Reed , Atul Purohit , Barry Victor Lloyd Potter
发明人： Nigel Vicker , Joanna Mary Day , Helen Victoria Bailey , Wesley Heaton , Ana Maria Ramos Gonzalez , Christopher Mark Sharland , Michael John Reed , Atul Purohit , Barry Victor Lloyd Potter
IPC分类号： A61K31/55 , C07D211/58 , C07C233/22 , A61P35/00 , C07D223/12 , A61K31/167
CPC分类号： C07C237/22 , C07C233/36 , C07D209/20 , C07D211/56 , C07D211/58 , C07D211/62 , C07D211/96 , C07D215/38 , C07D215/44 , C07D223/12 , C07D223/16 , C07D239/42 , C07D401/12 , C07D401/14 , C07D405/06 , C07D409/06 , C07D409/12 , C07D451/04
摘要： There is provided a compound having Formula (I) wherein each of R1, R2, R3, R4, R5, R6 and R7 are independently selected from (a) H, (b) R17, —OC(R17)3, —OCH(R17)2, —OCH2R17, —C(R17)3, —CH(R17)2, or —CH2R17 wherein R17 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(R11)C(O)R13; 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, alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl; each of rings A and B are selected from 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; X is an optional group selected from O, S, S═O, S(═O)2, C═O, S(═O)2NR8, C═ONR9, NR10, wherein R8, R9 and R10 are independently selected from H and hydrocarbyl, wherein n and p are independently selected from 0 and 1; Y is (R11)1-3 wherein each R11 is independently selected from NR12, CR13R14, S(═O)2 and C═O, wherein R12, R13 and R14 are independently selected from Hand hydrocarbyl; Z is selected from (i) six or seven membered ring containing carbon and at least one nitrogen, which may be optionally substituted wherein the substituents may together form further ring fused thereto; and (ii) a —R15—NR16— group wherein R15 is an optionally substituted C1-6 alkyl chain and R16 is selected from H and hydrocarbyl; and R3 is selected from Formula (A).

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