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    5-MORPHOLINYLMETHYLTHIOPHENYL PHARMACEUTIAL COMPOUNDS AS P38 MAP KINASE MODULATORS
    1.
    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。

    5-AMINO-2-CARBONYLTHIOPHENE DERIVATIVES FOR USE AS P38 MAP KINASE INHIBITORS IN THE TREATMENT OF INFLAMMATORY DISEASES
    3.
    发明公开
    5-AMINO-2-CARBONYLTHIOPHENE DERIVATIVES FOR USE AS P38 MAP KINASE INHIBITORS IN THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
    5-氨基-2- CARBONYLTHIOPHEN衍生物及其AS p38 MAP激酶抑制剂炎症性疾病的治疗

    公开(公告)号：EP1615907A1

    公开(公告)日：2006-01-18

    申请号：EP04727048.3

    申请日：2004-04-13

    申请人： Astex Therapeutics Limited

    发明人： GILL, Adrian Liam ,  WOODHEAD, Steven ,  CARR, Maria

    IPC分类号： C07D333/38 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14 ,  A61K31/381 ,  A61K31/415 ,  A61K31/4196 ,  A61P29/00

    CPC分类号： C07D409/12 ,  C07D333/38 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14

    摘要： The invention provides the use of a compound for the manufacture of a medicament for the prophylaxis or treatment of a disease state or condition mediated by a p38 MAP kinase; the compound being defined by formula (I): wherein: R1 and R2 are the same or different and each is selected from hydrogen, C1-4 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 to 12 ring members, the aryl and heteroaryl groups each being unsubstituted or substituted by one or more substituent groups R7 selected from halogen, hydroxy, trifluoromethyl, cyano, nitro, carboxy, amino, carbocyclic and heterocyclic groups having from 3 to 12 ring members; a group Ra-Rb wherein Ra is a bond, 0, CO, X1C(X2), C(X2)X1, X1C(X2)X1, S, SO, SO2, NRc, SO2NRc or NRcSO2; and Rb is selected from hydrogen, carbocyclic and heterocyclic groups having from 3 to 7 ring members, and a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from hydroxy, oxo, halogen, cyano, nitro, amino, mono- or di-C1-4 hydrocarbylamino, carbocyclic and heterocyclic groups having from 3 to 12 ring members and wherein one or more carbon atoms of the C1-8 hydrocarbyl group may optionally be replaced by 0, S, SO, SO2, NRc, X1C(X2), C(X2)X1 or X1C(X2)X1; X1 is 0, S or NRc and X2 is =0, =S or =NRc; Rc is hydrogen or C1-4 hydrocarbyl; R4 is a group YR5 or a group R6; Y is is NH, 0 or S; R5 is selected from (a) carbocyclic and heterocyclic groups having from 3 to 12 ring members; and (b) C1-8 hydrocarbyl groups optionally substituted by one or more substituents selected from hydroxy, oxo, halogen, cyano, amino, mono- or di- C1-4 hydrocarbylamino, and carbocyclic and heterocyclic groups having from 3 to 12 ring members, wherein one or more carbon atoms of the C1-8 hydrocarbyl group may optionally be replaced by 0, S, SO, SO2, NRc, X1C(X2), C(X2)X1 or X1C(X2)X1, provided that when Y is 0, a carbon atom adjacent to the group Y is not replaced by 0; and R6 is a heterocyclic group having from 4 to 12 ring members and containing at least one ring nitrogen atom through which R6 is linked to the adjacent carbonyl group; wherein the carbocyclic and heterocyclic groups of substituents R5 and R6 are each unsubstituted or substituted by one or more substituent groups R7 as hereinbefore defined. Also provided are novel compounds, pharmaceutical compositions containing the compounds and methods for their preparation.