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    Pyridyl derivatives and their use as mGlu5 antagonists
    1.
    发明授权
    Pyridyl derivatives and their use as mGlu5 antagonists 失效
    吡啶衍生物及其作为mGlu5拮抗剂的用途

    公开(公告)号：US07915424B2

    公开(公告)日：2011-03-29

    申请号：US10598512

    申请日：2005-03-09

    申请人： Francisco Javier Agejas-Chicharro ,  Bruce Anthony Dressman ,  Jose Antonio Martinez Perez ,  James Allen Monn ,  Mohammad Sadegh Zia-Ebrahimi ,  Sonia Gutierrez Sanfeliciano ,  Steven Marc Massey ,  Steven Scott Henry

    发明人： Francisco Javier Agejas-Chicharro ,  Bruce Anthony Dressman ,  Jose Antonio Martinez Perez ,  James Allen Monn ,  Mohammad Sadegh Zia-Ebrahimi ,  Sonia Gutierrez Sanfeliciano ,  Steven Marc Massey ,  Steven Scott Henry

    IPC分类号： C07D211/78

    CPC分类号： C07D213/89 ,  C07D213/16 ,  C07D213/26 ,  C07D213/48 ,  C07D213/55 ,  C07D213/57 ,  C07D213/61 ,  C07D213/65 ,  C07D213/73 ,  C07D213/75 ,  C07D213/78 ,  C07D213/80 ,  C07D213/85

    摘要： The present invention is directed toward pyridyl derivatives of formula (I) as antagonists of the mGlu5 receptor. As such the compounds may be useful for treatment or prevention of disorders remedied by antagonism of the mGlu5 receptor, wherein Ar is phenyl or napthyl each of which may be substituted by one or more C1-C4 alkyl, C1-C4 alkoxy, C1-C5 acyl, halo, amino, nitro, cyano, hydroxy, C1-C5 acylamino, C1-C4 alkylsulfonylamino, mono-, di- or trifluorinated C1-C3 alkyl, substituents which may be the same or different and may bear a CONH2, CONHCH3, CON(CH3)2, CO2H, CO2CH3, OCF3, CH2NHCOCH3, CH2NH2, CH2N(CH3)2, CH2CN, CH2OH, CH2NHSO2CH3, CH2N(CH3)(CH2)2 CN, CH2N(CH3)CH(CH3)2, CH2NHCH(CH3)2, CH2NH(CH2)2CH3, CH2NHCO2R4, CH2NHCH2CH3, CH2NHCH3 NHCOC(CH3)2, or N(S(O)2CH3)2 substituent; R1 is hydrogen, halo, R4, CN, C(NOH)R3, C(NO—R4)R3, (CH)2CO2R4, (CH2)n OR3, COR3, CF3, SR4, S(O)R4, S(O)2R4, COCH2CO2R3, NHSO2R4, NHCOR3, C(NOR3)NH2, CH2OCOR3, (CH2)nNH2, CON(CH3)2 (CH2)nNHCO2R4, CO2R3, CONH2, CSNH2, C(NH)NHOR3, (CH2)nN(CH3)2, or CONHNHCOR3; R2 is 1,2-ethenediyl or 1,2-ethynediyl; R3 is hydrogen or C1-C4 alkyl; R4 is C1-C4 alkyl; and n is 0, 1, 2, 3 or 4; or a pharmaceutically acceptable salt thereof, or an N-oxide thereof.

    摘要翻译： 本发明涉及式（I）的吡啶基衍生物作为mGlu5受体的拮抗剂。 因此，这些化合物可用于治疗或预防通过拮抗mGlu5受体治疗的病症，其中Ar是苯基或萘基，其各自可被一个或多个C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 5 酰基，卤素，氨基，硝基，氰基，羟基，C 1 -C 5酰基氨基，C 1 -C 4烷基磺酰基氨基，单 - ，二 - 或三氟化的C 1 -C 3烷基，可以相同或不同并且可以具有CONH 2，CONHCH 3， CON（CH 3）2，CO 2 H，CO 2 CH 3，OCF 3，CH 2 NHCOCH 3，CH 2 NH 2，CH 2 N（CH 3）2，CH 2 CN，CH 2 OH，CH 2 NHSO 2 CH 3，CH 2 N（CH 3）（CH 2）2 CN，CH 2 N（CH 3）CH（CH 3） CH3）2，CH2NH（CH2）2CH3，CH2NHCO2R4，CH2NHCH2CH3，CH2NHCH3 NHCOC（CH3）2或N（S（O）2CH3）2取代基; R1是氢，卤素，R4，CN，C（NOH）R3，C（NO-R4）R3，（CH）2CO2R4，（CH2）n OR3，COR3，CF3，SR4，S（O）R4，S ）NH 2，NHCOR 3，C（NOR 3）NH 2，CH 2 OCOR 3，（CH 2）n NH 2，CON（CH 3）2（CH 2）n NHCO 2 R 4，CO 2 R 3，CONH 2，CSNH 2，C（NH）NHOR 3，（CH 2）n N ）2或CONHNHCOR3; R2是1,2-乙烯二基或1,2-亚乙炔基; R3是氢或C1-C4烷基; R4是C1-C4烷基; 且n为0,1,2,3或4; 或其药学上可接受的盐或其N-氧化物。