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    17B-hydroxysteroid dehydrogenase inhibitors
    1.
    发明授权
    17B-hydroxysteroid dehydrogenase inhibitors 失效
    17B-羟类固醇脱氢酶抑制剂

    公开(公告)号：US08003783B2

    公开(公告)日：2011-08-23

    申请号：US11234868

    申请日：2005-09-23

    申请人： Nigel Vicker ,  Harshani Rithma Ruchiranani Lawrence ,  Gillian Margaret Allan ,  Christian Bubert ,  Delphine Sophie Marion Fischer ,  Atul Purohit ,  Michael John Reed ,  Barry Victor Lloyd Potter

    发明人： Nigel Vicker ,  Harshani Rithma Ruchiranani Lawrence ,  Gillian Margaret Allan ,  Christian Bubert ,  Delphine Sophie Marion Fischer ,  Atul Purohit ,  Michael John Reed ,  Barry Victor Lloyd Potter

    IPC分类号： A61K31/58 ,  C07J71/00

    CPC分类号： C07J71/00 ,  C07J41/00

    摘要： There is provided a compound of Formula (III) wherein R1 is a selected from an alkyloxyalkyl group, a nitrile group, alkylaryl group, alkenylaryl group, alkylheteroaryl group, alkenylheteroaryl group, ═N—O—alkyl or ═N—O—H group, branched alkenyl, alkyl-alcohol group, amide or alkylamide or —CHO so that R1 together with R3 provide the enol tautomer or R1 together with R3 form a pyrazole, wherein (a) R4 is ═N—O-alkyl or ═N—O—H group, (b) the pyrazole is substituted with one of alkyl-OH group, alkyl ester group, alkyloxyalkyl group, branched alkyl group, and an amide and/or (c) the 2-position is substituted with a group selected from —OH and —O-hydrocarbyl or a heteroaryl ring; R2 is selected from —OH and a sulphamate group; and R3 is selected from —OH or ═O; wherein the ring system may be further substituted with one or more hydroxyl, alkyl, alkoxy, alkinyl or halo substituents.

    摘要翻译： 提供式（III）的化合物，其中R 1选自烷氧基烷基，腈基，烷基芳基，链烯基芳基，烷基杂芳基，烯基杂芳基，N-O-烷基或= N-O-H基 ，支链烯基，烷基醇基，酰胺或烷基酰胺或-CHO，使得R 1与R 3一起提供烯醇互变异构体或R 1与R 3一起形成吡唑，其中（a）R 4是= N-O-烷基或= O-H基，（b）吡唑被烷基-OH基，烷基酯基，烷氧基烷基，支链烷基和酰胺中的一个取代，和/或（c）2-位被选定的基团取代 从-OH和-O-烃基或杂芳基环; R2选自-OH和氨基磺酸酯基; 并且R 3选自-OH或= O; 其中所述环系可以进一步被一个或多个羟基，烷基，烷氧基，炔基或卤素取代基取代。

    11β-hydroxysteroid dehydrogenase inhibitors
    8.
    发明授权
    11β-hydroxysteroid dehydrogenase inhibitors 失效
    11beta-羟类固醇脱氢酶抑制剂

    公开(公告)号：US07230020B2

    公开(公告)日：2007-06-12

    申请号：US10970064

    申请日：2004-10-22

    申请人： Nigel Vicker ,  Su Xiangdong ,  Dharshini Ganeshapillai ,  Atul Purohit ,  Michael John Reed ,  Barry Victor Lloyd Potter

    发明人： Nigel Vicker ,  Su Xiangdong ,  Dharshini Ganeshapillai ,  Atul Purohit ,  Michael John Reed ,  Barry Victor Lloyd Potter

    IPC分类号： A61K31/423 ,  A61K31/426 ,  C07D263/56 ,  C07D277/64

    CPC分类号： C07D209/48 ,  C07D211/28 ,  C07D213/76 ,  C07D215/38 ,  C07D231/56 ,  C07D241/42 ,  C07D261/16 ,  C07D261/20 ,  C07D275/04 ,  C07D277/64 ,  C07D295/135 ,  C07D307/79 ,  C07D311/18 ,  C07D319/18 ,  C07D333/54 ,  C07D333/70 ,  C07D495/04

    摘要： A compound having Formula I R1—Z—R2Formula I wherein R1 is an optionally substituted phenyl ring; R2 is or comprises an optionally substituted aromatic ring; and Z is —X—Y—L— or —Y—X—L— wherein either X is selected from —S(═O)(═O)— and —C(═O)—; and Y is —NR3—; or X is selected from —S(═O)(═O)— and —S—, and Y is —C(R4)(R5)—; L is an optional linker; and R3, R4 and R5 are each independently selected from H and hydrocarbyl; and wherein when R2 comprises the following structural moiety wherein Q is an atom selected from the group consisting of S, O, N and C; the compound is selected from compounds of the formulae R1—C(═O)—NR3—L—R2; R1—S(═O)(═O)—C(R4)(R5)—L—R2; R1—S—C(R4)(R5)—L—R2; R1—NR3—S(═O)(═O)—L—R2; R1—NR3—C(═O)—L—R2; R1—C(R4)(R5)—S(═O)(═O)—L—R2; and R1—C(R4)(R5)—S—L—R2.

    摘要翻译： 具有式I的化合物<？in-line-formula description =“In-line Formulas”end =“lead”？> R 1 -ZR 2式I < in-line-formula description =“In-line formula”end =“tail”？>其中R 1是任选取代的苯环; R 2是或包含任选取代的芳环; Z是-X-Y-L-或-Y-X-L-，其中X选自-S（-O）（ - O） - 和-C（-O） - ; 和Y是-NR 3 - ; 或者X选自-S（-O）（ - O） - 和-S-，Y是-C（R 4a）（R 5） - ; L是可选的接头; 和R 3，R 4和R 5各自独立地选自H和烃基; 并且其中当R 2包含以下结构部分时，其中Q是选自S，O，N和C的原子; 该化合物选自式R 1 -C（-O）-NR 3 -L-R 2的化合物; R 1 -S（-O）（ - O）-C（R 4）（R 5） - R L 2 / SUB>; R 1 -S-C（R 4）（R 5） - L-R 2; R 1 -SO 2 -S（-O）（ - O）-L-R 2; R 1 -NR 3 -C（-O）-L-R 2; R 1 -C（R 4）（R 5）-S（-O）（ - O）-LR 2， / SUB>; 和R 1 -C（R 4）（R 5）-S-L-R 2。

    COMPOUND CAPABLE OF INHIBITING 17-BETA HYDROXYSTERIOD DEHYDROGENASE
    9.
    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。

    Compound capable of inhibiting 17-beta hydroxysteriod dehydrogenase
    10.
    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。