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    • 75. 发明申请
      WO2010023448A1 NOVEL POTASSIUM CHANNEL BLOCKERS 审中-公开
    • NOVEL POTASSIUM CHANNEL BLOCKERS
    • 新型钾通道阻塞剂
    • WO2010023448A1
    • 2010-03-04
    • PCT/GB2009/002078
    • 2009-08-27
    • XENTION LIMITED , JOHN, Derek, Edward , MULLA, Mushtaq , HAMLYN, Richard, John , GARRETT, Sarah, Louise , HARTZOULAKIS, Basil , MADGE, David , FORD, John
    • JOHN, Derek, Edward , MULLA, Mushtaq , HAMLYN, Richard, John , GARRETT, Sarah, Louise , HARTZOULAKIS, Basil , MADGE, David , FORD, John
    • C07C311/21 , C07D205/04 , C07D211/08 , C07D213/04 , C07D231/00 , C07D233/54 , C07D265/28 , C07D271/12 , C07D277/32 , C07D307/79 , C07D311/70 , C07D317/62 , C07D319/18 , A61K31/18 , A61P29/00
    • C07C311/21 , C07C311/46 , C07C317/32 , C07C317/40 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D207/12 , C07D209/08 , C07D211/16 , C07D211/34 , C07D211/44 , C07D213/36 , C07D213/40 , C07D213/71 , C07D231/12 , C07D231/18 , C07D231/56 , C07D233/61 , C07D233/64 , C07D233/84 , C07D265/30 , C07D265/36 , C07D271/08 , C07D277/28 , C07D277/36 , C07D277/46 , C07D285/12 , C07D285/135 , C07D307/79 , C07D311/70 , C07D317/62 , C07D319/18 , C07D401/12 , C07D403/12 , C07D413/12
    • The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof wherein; X 1 is selected from a group consisting of CH 2 , C(=O), C(=NH), NC(=O), R 1 is selected from the group consisting of optionally substituted arylalkyl, and optionally substituted heteroarylalkyl R 2 is selected from the group consisting of optionally substituted alkyl, optionally substituted aryl or heteroaryl or NR 24 R 25 , R 3 is selected from the group consisting of hydrogen, halogen, hydroxyl, alkoxy, aryloxy, optionally substituted alkyl, optionally substituted amino, optionally substituted amino sulfonyl or nitrile; R 4 is selected from the group consisting of optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted acyl, optionally substituted sulfonyl, optionally substituted sulfamoyl, optionally substituted aryl, optionally substituted arylalkyl, and optionally substituted heteroaryl R 5 may be hydrogen, an optionally substituted alkyl, preferably CH 3 or, NR 4 R 5 may form an optionally substituted saturated or partially saturated 4-7 membered ring with the general formula (II). Wherein; X 2 is C(=O), CH 2 , CH(R 6 ) or C(R 6 )(R 6 ), X 3 is CH 2 , CH(R 7 ), C(R 7 )(R 7 ), NH, N(R 8 ), O or S Each R 6 independently represents optionally substituted amino, optionally substituted amino carbonyl, hydroxyl, optionally substituted acyl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalky, optionally substituted aryl or optionally substituted heteroaryl; Each R 7 independently represents optionally substituted amino, optionally substituted amino carbonyl, hydroxyl, optionally substituted acyl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalky, optionally substituted aryl or optionally substituted heteroaryl R 8 is optionally substituted acyl, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalkyl, optionally substituted aryl or optionally substituted heteroaryl; R 24 and R 25 are the same or different and each represents hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalkyl, optionally substituted aryl or optionally substituted heteroaryl, n = 1 or 2 m = 1, 2 or 3 With the proviso that when X 1 is C=O and R 5 is H then R 4 is not (a) or (b) or (c). Where R 4 a, R 5 a and R 6 a are each independently H, C 1-6 alkyl, aryl, heteroaryl, cycloalkyl, or aryl-C 1-6 alkyl; R 10 a is H or C 1-6 alkyl; and R 11 a is C 1-6 alkyl or aryl-C 1-6 alkyl and when X 1 is C=O or CH 2 and R 5 is H then R 4 is not (d) Where q is 0 to 5, R 3 b is H, OH or alkoxy and R 4 b is NH 2 , phenyl or a C 3-10 heterocycle. The compounds are useful as potassium ion channel inhibitors.
    • 本发明提供式（I）化合物或其盐或其药学上可接受的衍生物，其中： X 1选自CH 2，C（= O），C（= NH），NC（= O），R 1选自任选取代的芳烷基和任选取代的杂芳基烷基R 2选自基团 由任选取代的烷基，任选取代的芳基或杂芳基或NR 24 R 25组成，R 3选自氢，卤素，羟基，烷氧基，芳氧基，任选取代的烷基，任选取代的氨基，任选取代的氨基磺酰基或腈; R 4选自任选取代的烷基，任选取代的环烷基，任选取代的杂环烷基，任选取代的酰基，任选取代的磺酰基，任选取代的氨磺酰基，任选取代的芳基，任选取代的芳基烷基和任选取代的杂芳基R 5可以是氢， 任选取代的烷基，优选CH 3或NR 4 R 5可以形成具有通式（II）的任选取代的饱和或部分饱和的4-7元环。 其中： X2是C（= O），CH2，CH（R6）或C（R6）（R6），X3是CH2，CH（R7），C（R7）（R7），NH，N（R8） 每个R 6独立地表示任选取代的氨基，任选取代的氨基羰基，羟基，任选取代的酰基，任选取代的烷氧基，任选取代的芳氧基，任选取代的烷基，任选取代的环烷基，任选取代的芳基烷基，任选取代的芳基或任选取代的杂芳基; 每个R 7独立地表示任选取代的氨基，任选取代的氨基羰基，羟基，任选取代的酰基，任选取代的烷氧基，任选取代的芳氧基，任选取代的烷基，任选取代的环烷基，任选取代的芳基烷基，任选取代的芳基或任选取代的杂芳基R 8是任选取代的 酰基，任选取代的烷基，任选取代的环烷基，任选取代的芳基烷基，任选取代的芳基或任选取代的杂芳基; R 24和R 25相同或不同，各自表示氢，任选取代的烷基，任选取代的环烷基，任选取代的芳基烷基，任选取代的芳基或任选取代的杂芳基，n = 1或2 m = 1,2或3，条件是当 X1为C = O，R5为H，R4不为（a）或（b）或（c）。 其中R 4a，R 5a和R 6a各自独立地为H，C 1-6烷基，芳基，杂芳基，环烷基或芳基-C 1-6烷基; R10a是H或C1-6烷基; R 11a为C 1-6烷基或芳基-C 1-6烷基，当X 1为C = O或CH 2且R 5为H时，R 4不为（d）其中q为0至5，R 3b为H，OH或烷氧基，R 4b为NH 2 ，苯基或C 3-10杂环。 该化合物可用作钾离子通道抑制剂。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 79. 发明申请
      WO2009052440A1 INHIBITORS OF ANTI-APOPTOTIC PROTEINS 审中-公开
    • INHIBITORS OF ANTI-APOPTOTIC PROTEINS
    • 抗微生物蛋白的抑制剂
    • WO2009052440A1
    • 2009-04-23
    • PCT/US2008/080383
    • 2008-10-17
    • BURNHAM INSTITUTE FOR MEDICAL RESEARCH , PELLECCHIA, Maurizio
    • PELLECCHIA, Maurizio
    • A61K31/535
    • C07D277/36
    • Various compounds comprising a thiazolidine ring are described as well as the use of such compounds to inhibit at least one BCL-2 protein family member. One of the compounds described has the structure the structure A, wherein each of R 1 and R 2 comprises hydrogen, a substituted or unsubstituted straightchained aliphatic group, a halogen, an alkoxyl, a halogen-substituted alkyl, a halogensubstituted alkoxyl, hydroxyl, carboxyl, cyano group, an amido group, a substituted or unsubstituted cycloaliphatic group, a substituted or unsubstituted aromatic group, or a substituted or unsubstituted heterocyclic group; X comprises oxygen, sulfur, or imino group; and Z comprises a moiety such as naphthaline or dehydronaphthaline, among others.
    • 描述了包含噻唑烷环的各种化合物以及这些化合物用于抑制至少一种BCL-2蛋白家族成员的用途。 所述化合物之一具有结构A，其中R 1和R 2各自包含氢，取代或未取代的直链脂族基，卤素，烷氧基，卤素取代的烷基，卤素取代的烷氧基，羟基，羧基，氰基 取代或未取代的脂环族基团，取代或未取代的芳基，或取代或未取代的杂环基; X包括氧，硫或亚氨基; Z包括诸如萘或脱氢萘等部分。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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