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6 条记录 (耗时 0.019 秒)

    5-MORPHOLINYLMETHYLTHIOPHENYL PHARMACEUTIAL COMPOUNDS AS P38 MAP KINASE MODULATORS
    2.
    发明公开
    5-MORPHOLINYLMETHYLTHIOPHENYL PHARMACEUTIAL COMPOUNDS AS P38 MAP KINASE MODULATORS 审中-公开
    作为P38 MAP激酶调节剂的5-吗啉基甲基噻吩基药物化合物

    公开(公告)号：EP1756082A1

    公开(公告)日：2007-02-28

    申请号：EP05732791.8

    申请日：2005-04-13

    申请人： Astex Therapeutics Limited

    发明人： GILL, Adrian Liam ,  CARR, Maria Grazia ,  LYONS, John Francis ,  THOMPSON, Neil Thomas ,  REES, David Charles

    IPC分类号： C07D333/36 ,  C07D409/12 ,  C07D417/12 ,  A61K31/381 ,  A61P35/04

    CPC分类号： C07D333/36 ,  C07D409/12 ,  C07D417/12

    摘要： The invention provides compounds of the formula (I) or a salt, solvate or N-oxide thereof, wherein:R1 and R2 are the same or different and each is selected from hydrogen, saturated C1-3 hydrocarbyl, halogen and cyano; X is selected from C=O, C=S, C(=O)NH, C(=S)NH, C(=O)O, C(=O)S, C(=S)O and C(=S)S; R3 is selected from aryl and heteroaryl groups each having from 5 t0 12 ring members and being unsubstituted or substituted by one or more substituent groups R10 as defined in the claims; R4 and R5 are the same or different and are selected from hydrogen and methyl; or one of R4 and R5 is selected from hydroxymethyl and ethyl and the other is hydrogen; and R6 and R7 are the same or different and are selected from hydrogen and methyl. The compounds of the formula (I) hayed activity as p38 MAP kinase and Taf kinase inhibitors.

    摘要翻译： 本发明提供了式（I）化合物或其盐，溶剂化物或N-氧化物，其中：R 1和R 2相同或不同，并且各自选自氢，饱和C 1-3烃基，卤素和氰基; X选自C = O，C = S，C（= O）NH，C（= S）NH，C（= O）O，C（= O）S，C（= S）O和C S）S; R3选自各自具有5至10个环成员且未被取代或被一个或多个如权利要求所定义的取代基R10取代的芳基和杂芳基; R4和R5相同或不同，选自氢和甲基; 或者R 4和R 5中的一个选自羟甲基和乙基，另一个是氢; R6和R7相同或不同，选自氢和甲基。 式（I）化合物具有p38 MAP激酶和Taf激酶抑制剂的活性。

    HYDROXYBENZAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF HSP90
    4.
    发明公开
    HYDROXYBENZAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF HSP90 审中-公开
    羟基苯甲酰胺衍生物及其作为HSP90抑制剂的用途

    公开(公告)号：EP1883402A2

    公开(公告)日：2008-02-06

    申请号：EP06726757.5

    申请日：2006-04-13

    申请人： Astex Therapeutics Limited

    发明人： CHESSARI, Gianni ,  CONGREVE, Miles Stuart ,  NAVARRO, Eva Figueroa ,  FREDERICKSON, Martyn ,  MURRAY, Christopher ,  WOOLFORD, Alison Jo-Anne ,  CARR, Maria Grazia ,  O'BRIEN,Michael Alistair ,  WOODHEAD, Andrew James

    IPC分类号： A61K31/401 ,  A61K31/445 ,  A61K31/5375 ,  A61K31/166 ,  C07C233/65 ,  C07C233/66 ,  C07D207/10 ,  C07D211/34 ,  C07D295/02 ,  C07D309/14 ,  C07D265/30 ,  C07D295/18 ,  C07D211/42 ,  C07D211/22 ,  C07D211/56

    CPC分类号： C07D401/12 ,  C07C65/21 ,  C07D209/08 ,  C07D209/44 ,  C07D215/08 ,  C07D217/06 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D471/10 ,  C07D491/08 ,  C07D491/10

    摘要： The invention provides a compound for use as an inhibitor of Hsp90, the compound having the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; C 1-5 hydrocarbyl and C 1-5 hydrocarbyloxy; wherein the C 1-5 hydrocarbyl and C 1-5 hydrocarbyloxy moieties are each optionally substituted by one or more substituents selected from hydroxy, halogen, C 1-2 alkoxy, amino, mono- and di-C 1-2 alkylamino, and aryl and heteroaryl groups of 5 to 12 ring members; R4 is selected from hydrogen; a group -(O)n-R7 where n is 0 or 1 and R7 is an acyclic C 1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and mono- or di-C 1-5 hydrocarbyl-amino, wherein the acyclic Ci-5 hydrocarbyl group and the mono and di-C 1-5 hydrocarbylamino moieties in each instance are optionally substituted by one or more substituents selected from hydroxy, halogen, C 1-2 alkoxy, amino, mono- and di-C 1-2 alkylamino, and aryl and heteroaryl groups of 5 to 12 ring members; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and R5 and R6 are as defined in the claims.

    摘要翻译： 本发明提供了用作Hsp90抑制剂的化合物，具有式（I）的化合物：或其盐，互变异构体，溶剂化物和N-氧化物; 其中R1是羟基或氢; R2是羟基; 甲氧基或氢; 条件是R1和R2中的至少一个是羟基; R3选自氢; 卤素; 氰基; C 1-5烃基和C 1-5烃氧基; 其中C 1-5烃基和C 1-5烃氧基部分各自任选被一个或多个选自以下的取代基取代：羟基，卤素，C 1-2烷氧基，氨基，单 - 和二-C 1-2烷基氨基和芳基 和5至12个环成员的杂芳基; R4选自氢; 基团 - （O）n -R 7，其中n是0或1并且R 7是无环C 1-5烃基或具有3-7个环成员的单环碳环或杂环基团; 卤素; 氰基; 羟基; 氨基; 和单-C 1 -C 5烃基 - 氨基，其中无环C 1-5烃基和单和二-C 1-5烃氨基部分在每种情况下任选被一个或多个选自以下的取代基取代：羟基，卤素 ，C 1-2烷氧基，氨基，单 - 和二-C 1-2烷基氨基和5-12个环成员的芳基和杂芳基; 或R3和R4一起形成5至7个环成员的单环碳环或杂环; R5和R6如权利要求中所定义。