发明名称 SUBSTITUTED 4-PHENYL-4-(1H-IMIDAZOL-2-YL)-PIPERIDINE DERIVATIVES FOR REDUCING ISCHAEMIC DAMAGE
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 R 1 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.
申请公布号 KR20050035120(A) 申请公布日期 2005.04.15
申请号 KR20047002380 申请日期 2002.10.10
申请人 JANSSEN PHARMACEUTICA N. V 发明人 BORGERS, MARCEL J.M.;FLAMENG, WILLEM;HERIJGERS, PAUL JOANNES LUDOVICUS;JANSSENS, FRANS EDUARD;LEENAERTS, JOSEPH ELISABETH;MEERT, THEO FRANS;FERNANDEZ-GADEA, FRANCISCO JAVIER;GOMEZ-SANCHEZ, ANTONIO
分类号 C07D401/04;A61K31/454;A61K31/4545;A61K31/506;A61P9/00;A61P9/10;A61P43/00;C07D401/14;C07D413/14;C07D417/14;(IPC1-7):A61K31/454 主分类号 C07D401/04
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