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15 条记录 (耗时 0.034 秒)

    COMPOUND
    4.
    发明申请
    COMPOUND 审中-公开
    复合

    公开(公告)号：US20070225256A1

    公开(公告)日：2007-09-27

    申请号：US11689936

    申请日：2007-03-22

    申请人： Matthew Leese ,  Atul Purohit ,  Michael Reed ,  Fabrice Jourdan ,  Barry Victor Potter ,  Christian Bubert

    发明人： Matthew Leese ,  Atul Purohit ,  Michael Reed ,  Fabrice Jourdan ,  Barry Victor Potter ,  Christian Bubert

    IPC分类号： A61K31/675 ,  A61K31/58 ,  C07J43/00 ,  C07J41/00

    CPC分类号： C07J43/003 ,  C07J3/00 ,  C07J7/0005 ,  C07J31/006 ,  C07J41/0005 ,  C07J41/0072

    摘要： The present invention provides a compound comprising a steroidal ring system and an optional group R1 selected from any one of —OH, a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein the A ring of the steroidal ring system is optionally substituted at position 2 or 4 with a group R4 which may be a suitable subtituent, wherein the D ring of the steroidal ring system is substituted by a group R2 of the formula -L-R3, wherein L is an optional linker group and R3 is selected from groups which are or which comprise one of (i) —SO2R5, wherein R5 is H, a hydrocarbyl group or a bond or group attached to the D ring; (ii) —NO2; (iii) —SOR6, wherein R6 is H or a hydrocarbyl group; (iv) —R7, wherein R7 is a halogen; (v) -alkyl; (vi) —C(═O)R3, wherein R3 is H or hydrocarbyl; (vii) —C≡CR9, wherein R9 is H or hydrocarbyl; (viii) —OC(═O)NR10R11 wherein R10 and R11 are independently selected from H and hydrocarbyl; (ix), (x), (xi), (xii) and (xiii) are formulae wherein when R3 is -alkyl, R4 is present as a hydrocarbon group, when R3 is —NO2R4 is present and/or R1 is present as a sulphamate group, and when R3 is —C(═O)R3R4 is present and R1 is present as a sulphamate group.

    摘要翻译： 本发明提供了包含甾族环系统和选自-OH，氨基磺酸盐基团，膦酸盐基团，硫代膦酸盐基团，磺酸盐基团或磺酰胺基团中的任何一个的任选基团R1的化合物; 其中所述甾族环系统的A环任选在位置2或4处被基团R 4取代，所述基团R 4可以是合适的取代基，其中所述甾族环系统的D环被基团 R L 3，其中L是任选的连接基团，R 3选自以下基团，或其中包含一个 的（i）-SO 2 R 5，其中R 5是H，连接到D环上的烃基或键或基团 ; （ii）-NO 2 2; （iii）-SOR 6，其中R 6是H或烃基; （iv）-R 7，其中R 7为卤素; （v） - 烷基; （vi）-C（-O）R 3，其中R 3是H或烃基; （vii）-C≡CR9，其中R 9是H或烃基; （viii）-OC（-O）NR 10 R 11，其中R 10和R 11独立地选自 由H和烃基组成; （ix），（x），（xi），（xii）和（xiii）是其中当R 3为 - 烷基时，R 4为烃， 当R 3为-NO 2 R 4存在时，和/或R 1存在作为 并且当R 3为-C（-O）R 3 3 R 4时，存在R 1和R 2 >以氨基磺酸盐基团存在。

    17B-hydroxysteroid dehydrogenase inhibitors
    7.
    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。

    Compound
    9.
    发明申请
    Compound 失效
    复合

    公开(公告)号：US20060074060A1

    公开(公告)日：2006-04-06

    申请号：US11234868

    申请日：2005-09-23

    申请人： Nigel Vicker ,  Harshani Lawrence ,  Gillian Allan ,  Christian Bubert ,  Delphine Sophie Fischer ,  Alan Purohit ,  Michael Reed ,  Barry Victor Potter

    发明人： Nigel Vicker ,  Harshani Lawrence ,  Gillian Allan ,  Christian Bubert ,  Delphine Sophie Fischer ,  Alan Purohit ,  Michael Reed ,  Barry Victor 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 (I) wherein (I) R2 is selected from (i) an alkyloxyalkyl group (ii) a nitrile group, and wherein R2 is capable of forming a hydrogen bond (iii) alkylaryl group, wherein the aryl group is substituted by other than a C1-10 group (iv) alkenylaryl group wherein the aryl group is substituted (v) alkylheteroaryl group, wherein when heteroaryl group comprises only C and N in the ring, the aryl group is substituted by other than a methyl group (vi) alkenylheteroaryl group, (vii) ═N—O-alkyl or ═N—O—H group (viii) branched alkenyl (ix) alkyl-alcohol group (x) amide or alkylamide wherein (a) the alkyl of the alkylamide is —CH2— or —Ch2Ch2—, (b) the amide is di-substituted and/or (c) the amide is substituted with at least one of alkyl heterocycle group, alkenyl heterocycle group, alkylheteroaryl group, alkenylheteroaryl group, heteroaryl group, alkylamine group, alkyloxyalkyl group, alkylaryl group, straight or branched alkyl group, (xi) —CHO so that R1 together with R3 provide the enol tautomer (a); OR R2 together with R3 form (xii) 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 (xiii) a heteroaryl ring to provide a compound of the formula (b); (II) R2 is selected from groups capable of forming a hydrogen bond, a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group and a sulphonamide group; and (III) R3 is selected from —OH, ═O, or a C(═O)—mimetic.

    摘要翻译： 提供式（I）化合物，其中（I）R 2选自（ⅰ）烷氧基烷基（ⅱ）腈基，其中R2能够形成氢键（ⅲ）烷基芳基，其中芳基 基团被取代的芳基（ⅴ）烷基杂芳基以外的C 1-10基团（ⅳ）链烯基芳基取代，其中当杂芳基仅在环中仅包含C和N时，芳基被除了 甲基（vi）烯基杂芳基，（vii）-NO-烷基或-NOH基（viii）支链烯基（ix）烷基 - 醇基（x）酰胺或烷基酰胺，其中（a）烷基酰胺的烷基是-CH2- 或-C 2 -C 12 - ，（b）酰胺是二取代的和/或（c）酰胺被烷基杂环基，烯基杂环基，烷基杂芳基，烯基杂芳基，杂芳基，烷基胺基，烷氧基烷基中的至少一个 基团，烷基芳基，直链或支链烷基，（xi）-CHO，使得R1起始 与R3提供烯醇互变异构体（a）; OR 2与R 3一起形成（xii）吡唑，其中（a）R4是-NO-烷基或-NOH基，（b）吡唑被烷基-OH基，烷基酯基，烷氧基烷基，支链烷基 基团和酰胺和/或（c）2位被选自-OH和-O-烃基（xiii）杂芳基环的基团取代，以提供式（b）的化合物; （II）R2选自能够形成氢键的基团，氨基磺酸酯基，膦酸酯基，硫代膦酸酯基，磺酸酯基和磺酰胺基; 和（III）R 3选自-OH，-O或C（-O） - 模仿物。