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    Piperidine Derivatives as Cxcr3 Receptor Antagonists
    1.
    发明申请
    Piperidine Derivatives as Cxcr3 Receptor Antagonists 审中-公开
    哌啶衍生物作为Cxcr3受体拮抗剂

    公开(公告)号：US20090030039A1

    公开(公告)日：2009-01-29

    申请号：US12278719

    申请日：2007-02-06

    申请人： Erwin Coesemans ,  Jean-Pierre Andre Marc Bongartz ,  Guy Rosali Eugeen Van Lommen ,  Jean Pierre Frans Van Wauwe ,  Mieke Buntinx

    发明人： Erwin Coesemans ,  Jean-Pierre Andre Marc Bongartz ,  Guy Rosali Eugeen Van Lommen ,  Jean Pierre Frans Van Wauwe ,  Mieke Buntinx

    IPC分类号： A61K31/4545 ,  C07D401/04

    CPC分类号： C07D401/04 ,  C07D401/14

    摘要： The present invention relates to a compound of formula (I) a N-oxide thereof, a pharmaceutically acceptable salt thereof, a stereochemically isomeric form thereof or a solvate thereof, wherein X represents N or CH; Y and Z each independently represent C(═O) or CH2 provided that at least one of Y and Z represents C(═O); R1 represents CH(R4)-aryl or CH(R4)-heteroaryl; R2 represents aryl2 or heteroaryl; R3 represents hydrogen; C1-4alkylcarbonyl; C1-6alkyl optionally substituted with C1-6alkyloxy, C1-6alkylthio, C1-6alkyloxycarbonyl or aryl1; provided that when Y and Z each represent C(═O), X represents CH, R3 represents hydrogen, R4 represents hydrogen, and R2 represents unsubstituted pyridyl or phenyl optionally substituted with one halo or with one C1-4alkyloxy or with one or two C1-4alkyl, then aryl in the definition of R1 is other than phenyl substituted with one halo or with one or two C1-4alkyl; and provided that when Y and Z each represent C(═O), X represents CH, R3 represents hydrogen, and R2 represents unsubstituted pyridyl or phenyl optionally substituted with one halo or with one C1-4alkyloxy or with one or two C1-4alkyl, then heteroaryl in the definition of R1 is other than unsubstituted thienyl or unsubstituted pyridyl. The present invention also relates to the use of a compound of formula (I) for the manufacture of a medicament for preventing or treating a disease mediated through activation of the CXCR3 receptor; to processes for preparing the compounds of formula (I) and pharmaceutical compositions comprising them.

    摘要翻译： 本发明涉及式（I）的化合物，其N-氧化物，其药学上可接受的盐，其立体化学异构形式或其溶剂合物，其中X表示N或CH; Y和Z各自独立地表示C（-O）或CH 2，条件是Y和Z中的至少一个表示C（-O）; R 1表示CH（R 4） - 芳基或CH（R 4） - 杂芳基; R 2表示芳基2或杂芳基; R3表示氢; C 1-4烷基羰基; 任选被C 1-6烷氧基，C 1-6烷硫基，C 1-6烷氧基羰基或芳基取代的C 1-6烷基; 条件是当Y和Z各自表示C（-O）时，X表示CH，R 3表示氢，R 4表示氢，R 2表示未取代的吡啶基或任选被一个卤素或一个C 1-4烷氧基取代的苯基或与一个或两个C 1 -4-烷基，则R1定义中的芳基不同于被一个卤素或一个或两个C 1-4烷基取代的苯基; 并且条件是当Y和Z各自表示C（-O）时，X表示CH，R 3表示氢，R 2表示未取代的吡啶基或任选被一个卤素或一个C 1-4烷氧基取代或与一个或两个C 1-4烷基取代的苯基， 那么R1的定义中的杂芳基不是未取代的噻吩基或未取代的吡啶基。 本发明还涉及式（I）化合物在制备用于预防或治疗通过活化CXCR3受体介导的疾病的药物中的用途; 制备式（I）化合物的方法和包含它们的药物组合物。