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    Substituted 4-phenyl-4-[1h-imidazol-2-yl]-piperidine derivatives for reducing ischaemic damage
    7.
    发明申请
    Substituted 4-phenyl-4-[1h-imidazol-2-yl]-piperidine derivatives for reducing ischaemic damage 有权
    取代的4-苯基-4- [1,5-咪唑-2-基] - 哌啶衍生物，用于减少缺血性损伤

    公开(公告)号：US20050004170A1

    公开(公告)日：2005-01-06

    申请号：US10492778

    申请日：2002-10-10

    申请人： Frans Janssens ,  Joseph Leenaerts ,  Francisco Javier Fernandez-Gadea ,  Paul Johannes Herijgers ,  Theo Meert ,  Antonio Gomez-Sanchez ,  William Flameng ,  Marcel Borgers

    发明人： Frans Janssens ,  Joseph Leenaerts ,  Francisco Javier Fernandez-Gadea ,  Paul Johannes Herijgers ,  Theo Meert ,  Antonio Gomez-Sanchez ,  William Flameng ,  Marcel Borgers

    IPC分类号： C07D401/04 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/506 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

    CPC分类号： A61K31/454

    摘要： The present invention relates to an agent for reducing ischaemic damage to an organ, in particular to a heart and a brain, pharmaceutical compositions comprising said agent and the use of said agent for the treatment of ischaemic diseases to the heart and the brain. The agent comprises a substituted 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivative according to Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof, the N-oxide forms thereof and the prodrugs thereof. In particular are claimed the compounds according to Formula (I) in which A=B is C═O or SO2, X is a covalent bond, R1 is alkyloxy, alkyloxyalkyl, Ar or NR9R10, wherein R9 and R10 each independently are hydrogen or Ar; or A=B and R1 together form a benzoxazolyl radical; p is zero, R3 is benzyl optionally substituted with hydroxy, alkyl or alkyloxycarbonyl and R4 and R5 each are hydrogen. The use of said agents has important clinical ramifications with regard to the reduction of ischaemic damage to an organ in a mammal, in particular to a heart and/or a brain, the prevention of coronary artery diseases in a mammal by inducing a cardioprotective effect and the treatment and prevention of stroke.

    摘要翻译： 本发明涉及用于减轻对器官特别是心脏和脑的缺血性损伤的药剂，包含所述药物的药物组合物和所述药物用于治疗心脏和脑部的缺血性疾病的用途。 该试剂包含根据式（I）的取代的4-苯基-4- [1H-咪唑-2-基] - 哌啶衍生物，其药学上可接受的酸或碱加成盐，其立体化学异构形式，其互变异构形式， 其N-氧化物形式及其前药。 特别是根据式（I）的化合物，其中A = B为C = O或SO 2，X为共价键，R 1为烷氧基，烷氧基烷基，Ar或NR 9 R 10， 其中R 9和R 10各自独立地是氢或Ar; 或A = B和R 1一起形成苯并恶唑基; p为0，R 3为任选被羟基，烷基或烷氧基羰基取代的苄基，R 4和R 5各自为氢。 所述试剂的使用对于减少对哺乳动物，特别是心脏和/或脑的器官的缺血损伤，通过诱导心脏保护作用来预防哺乳动物的冠状动脉疾病，具有重要的临床后果，以及 治疗和预防中风。