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, R<1> is alkyloxy, alkyloxyalkyl, Ar or NR<9>R<10>, wherein R<9> and R<10> each independently are hydrogen or Ar ; or A=B and R<1> together form a benzoxazolyl radical ; p is zero, R<3> is benzyl optionally substituted with hydroxy, alkyl or alkyloxycarbonyl and R<4> and R<5> 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 WO03039440(A3) 申请公布日期 2003.12.18
申请号 WO2002EP11371 申请日期 2002.10.10
申请人 JANSSEN PHARMACEUTICA N.V.;JANSSENS, FRANS, EDUARD;LEENAERTS, JOSEPH, ELISABETH;FERNANDEZ-GADEA, FRANCISCO, JAVIER;GOMEZ-SANCHEZ, ANTONIO;FLAMENG, WILLEM;HERIJGERS, PAUL, JOANNES, LUDOVICUS;MEERT, THEO, FRANS;BORGERS, MARCEL, J., M. 发明人 JANSSENS, FRANS, EDUARD;LEENAERTS, JOSEPH, ELISABETH;FERNANDEZ-GADEA, FRANCISCO, JAVIER;GOMEZ-SANCHEZ, ANTONIO;FLAMENG, WILLEM;HERIJGERS, PAUL, JOANNES, LUDOVICUS;MEERT, THEO, FRANS;BORGERS, MARCEL, J., M.
分类号 C07D401/04;A61K31/454;A61K31/4545;A61K31/506;A61P9/00;A61P9/10;A61P43/00;C07D401/14;C07D413/14;C07D417/14 主分类号 C07D401/04
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