首页> 外国专利> USE OF SUBSTITUTED 4-PHENYL-4-(1H-IMIDAZOL-2-YL)- PIPERIDINE DERIVATIVES FOR THE MANUFACTURE OF MEDICAMENTS FOR REDUCING ISCHAEMIC DAMAGE

USE OF SUBSTITUTED 4-PHENYL-4-(1H-IMIDAZOL-2-YL)- PIPERIDINE DERIVATIVES FOR THE MANUFACTURE OF MEDICAMENTS FOR REDUCING ISCHAEMIC DAMAGE

机译:取代的4-苯基-4-(1H-咪唑-2-基)-哌啶衍生物用于减少缺血性损伤的药物的生产

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.
机译:本发明涉及一种用于减少对器官,特别是对心脏和大脑的缺血性损伤的药剂,包括该药剂的药物组合物,以及该药剂在治疗对心脏和大脑的缺血性疾病中的用途。该药剂包含根据式(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。特别要求保护的是根据式(I)的化合物,其中A = B是C = O或SO 2,X是共价键,R 1是烷氧基,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为零,R 3为任选地被羟基,烷基或烷氧基羰基取代的苄基,并且R 4和R 5各自为氢。所述试剂的使用在减少对哺乳动物特别是对心脏和/或大脑的器官的缺血性损伤,通过诱导心脏保护作用和预防哺乳动物的冠状动脉疾病方面具有重要的临床意义。中风的治疗和预防。

著录项

  • 公开/公告号IL161347B

    专利类型

  • 公开/公告日2010-03-28

    原文格式PDF

  • 申请/专利权人 JANSSEN PHARMACEUTICA N.V.;

    申请/专利号IL161347

  • 发明设计人

    申请日2004-04-13

  • 分类号

  • 国家 IL

  • 入库时间 2022-08-21 18:46:43

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