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    Compound
    2.
    发明申请
    Compound 审中-公开
    复合

    公开(公告)号：US20100120789A1

    公开(公告)日：2010-05-13

    申请号：US12554943

    申请日：2009-09-07

    申请人： Nigel Vicker ,  Xiangdong Su ,  Fabienne Praduax ,  Michael John Reed ,  Barry Victor Lloyd Potter

    发明人： Nigel Vicker ,  Xiangdong Su ,  Fabienne Praduax ,  Michael John Reed ,  Barry Victor Lloyd Potter

    IPC分类号： A61K31/497 ,  C07C233/00 ,  A61K31/165 ,  A61K31/4365 ,  C07D495/04 ,  C07D405/02 ,  C12Q1/32

    CPC分类号： C11D3/0073 ,  C11D3/2086 ,  C11D3/33 ,  C11D7/265 ,  C11D7/3245 ,  C11D11/0041

    摘要： There is provided a compound having Formula I R1—Z—R2   Formula I wherein R1 is a group selected from optionally substituted fused polycyclic groups, substituted alkyl groups, branched alkyl groups, and optionally substituted cycloalkyl groups Z is a linker which is or comprises a carbonyl group or a isostere of a carbonyl group R2 is selected from optionally substituted aromatic rings and optionally substituted heterocyclic rings wherein (a) R2 is a 2-substituted thiophene group, and/or (b) Z is a group of the formula —C(═O)—CR3R4—X—(CR5R6)n-, wherein X is selected from NR7, S, O, S═O, and S(═O)2, wherein n is 0 or 1 and/or (c) R1 is an adamantyl group and Z is or comprises an amide group, and/or (d) R1 is an adamantyl group and Z is or comprises a group of the formula —(CR8R9)p- NR10—S(═O)2—(CR11R12)q-, wherein p is 0 or 1 and q is 0 or 1 and/or (e) R1 is an adamantyl group and Z is or comprises a group of the formula —(CR13R14)v-Y—(CR15R16)w- where Y is a heteroaryl group in which a bond in the heteroaryl ring is a isostere of a carbonyl group, wherein v is o or 1 and w is 0 or 1; wherein each of R3, R4, R5, R6, R8, R9, R11, R12, R13, R14, R15 and R16, are independently selected from H, hydrocarbyl and halogen, wherein each of R7 and R10 are independently selected from H and hydrocarbyl.

    摘要翻译： 提供了具有式I的化合物R1-Z-R2式Ⅰ其中R1是选自任选取代的稠合多环基团，取代的烷基，支链烷基和任选取代的环烷基的基团Z是一种或多种 羰基或羰基的等排基团选自任选取代的芳环和任选取代的杂环，其中（a）R 2是2-取代的噻吩基团，和/或（b）Z是式-C （= O）-CR 3 R 4 -X-（CR 5 R 6）n - ，其中X选自NR 7，S，O，S = O和S（= O）2，其中n为0或1和/或（c） R1是金刚烷基，Z是或包含酰胺基，和/或（d）R1是金刚烷基，Z是或包含式 - （CR8R9）对NR10-S（= O）2- （CR11R12）q-，其中p为0或1，q为0或1，和/或（e）R1为金刚烷基，Z为或包含式 - （CR13R14）vY-（CR15R16）w- 在哪里 Y是杂芳基环中的键是羰基的等离子体的杂芳基，其中v是0或1，w是0或1; 其中R 3，R 4，R 5，R 6，R 8，R 9，R 11，R 12，R 13，R 14，R 15和R 16各自独立地选自H，烃基和卤素，其中R 7和R 10各自独立地选自H和烃基 。

    17B-hydroxysteroid dehydrogenase inhibitors
    4.
    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
    10.
    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。