发明名称 SUBSTITUTED 4-PHENYL-4-(1H-IMIDAZOL-2YL)-PIPERIDINE 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 SO<SUB>2</SUB>, X is a covalent bond, R<SUP>1 </SUP>is alkyloxy, alkyloxyalkyl, Ar or NR<SUP>9</SUP>R<SUP>10</SUP>, wherein R<SUP>9 </SUP>and R<SUP>10 </SUP>each independently are hydrogen or Ar; or A=B and R<SUP>1 </SUP>together form a benzoxazolyl radical; p is zero, R<SUP>3 </SUP>is benzyl optionally substituted with hydroxy, alkyl or alkyloxycarbonyl and R<SUP>4 </SUP>and R<SUP>5 </SUP>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 ZA200402816(B) 申请公布日期 2005.06.29
申请号 ZA20040002816 申请日期 2004.04.13
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 FRANS EDUARD JANSSENS;FRANCISCO JAVIER FERNANDEZ-GADEA;WILLEM FLAMENG;THEO FRANS MEERT;JOSEPH ELISABETH LEENAERTS;ANTONIO GOMEZ-SANCHEZ;PAUL JOANNES LUDOVICUS HERJIGERS;MARCEL J. M. BORGERS
分类号 A61K;C07D401/04;A61K31/454;A61K31/4545;A61K31/506;A61P;A61P9/00;A61P9/10;A61P43/00;C07D401/14;C07D413/14;C07D417/14 主分类号 A61K
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