首页> 外国专利> Heterocyclically substituted 2- (d-phenoxy) pyridine derivatives and related compounds as sodium channel blockers for the treatment of neuronal damage and neurodegenerative conditions

Heterocyclically substituted 2- (d-phenoxy) pyridine derivatives and related compounds as sodium channel blockers for the treatment of neuronal damage and neurodegenerative conditions

机译:杂环取代的2-(d-苯氧基)吡啶衍生物和相关化合物作为钠通道阻滞剂,用于治疗神经元损伤和神经退行性疾病

摘要

"HYPEROCYCLIC REPLACED 2- (4-PHENoxy) PYRIDINE DERIVATIVES AND RELATED COMPOUNDS AS SODIUM CHANNEL LOCKERS FOR NEURONAL DAMAGE TREATMENT AND NEURODEGENERATIVE CONDITIONS". This invention relates to the aryl substituted pyridines of formula (I) or a pharmaceutically acceptable salt, promedicate or solvate thereof, wherein: Ar is selected from the group consisting of Ar ~ 1 ~, Ar ~ 2 ~, Ar ~ 3 ~, and Ar ~ 4 ~, where Ar ~ 1 ~ is R ~ 1 ~ selected from the group consisting of an optionally substituted alkyl, amino, alkylthiol, C (O) R ~ 10 ~, SO ~ 2 ~ R ~ 10 ~ and OC ( O) NH 2 -; R ~ 2 ~ is -Y ~ m ~ - (CH ~ 2 ~) ~ n ~ -Z 'where: Y is O, S or NR ~ 11 ~, where R ~ 11 ~ is hydrogen or alkyl, Z is a ring saturated heterocyclic, optionally substituted on one or more carbon atoms, m is 0 or 1 and n is 0-6; or a pharmaceutically acceptable salt, promedicate or solvate thereof, wherein Ar and R 1 -R 4 are set forth in the description. The invention also relates to the use of the compounds of formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as lateral amyotrophic sclerosis (ALS) and for treatment, prevention or amelioration of both acute or chronic pain, including diabetic neuropathy and anti-tinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics and as antiarrhythmics.
机译:“取代2-(4-苯氧基)吡啶衍生物的高环化合物和相关化合物,作为钠离子通道封闭剂,用于神经损伤治疗和神经退行性疾病”。本发明涉及式(I)的芳基取代的吡啶或其药学上可接受的盐,药物或溶剂化物,其中:Ar选自由Ar〜1〜,Ar〜2〜,Ar〜3〜组成的组,和Ar〜4〜,其中Ar〜1〜为R〜1〜,选自任选取代的烷基,氨基,烷基硫醇,C(O)R〜10〜,SO〜2〜R〜10〜和OC( O)NH 2-; R〜2〜为-Y〜m〜-(CH〜2〜)〜n〜-Z'其中:Y为O,S或NR〜11〜,其中R〜11〜为氢或烷基,Z为环饱和杂环,可选地在一个或多个碳原子上取代,m为0或1,n为0-6;或其药学上可接受的盐,药物或溶剂化物,其中Ar和R 1 -R 4在说明书中列出。本发明还涉及式I化合物在治疗整体性和局灶性局部缺血后的神经元损伤,治疗或预防神经退行性疾病如侧肌萎缩性硬化症(ALS)以及治疗,预防或改善两者中的用途。急性或慢性疼痛,包括糖尿病性神经病变和抗耳鸣剂,作为抗惊厥药和抗躁狂抑郁药,作为局部麻醉药和抗心律不齐药物。

著录项

  • 公开/公告号BR0212327A

    专利类型

  • 公开/公告日2004-09-21

    原文格式PDF

  • 申请/专利权人 EURO-CELTIQUE S/A;

    申请/专利号BR20020212327

  • 发明设计人 BIN SHAO;R. RICHARD GOEHRING;

    申请日2002-09-06

  • 分类号A61K31/5377;A61K31/4545;C07D413/04;C07D213/68;C07D213/74;C07D213/79;C07D213/81;

  • 国家 BR

  • 入库时间 2022-08-21 23:12:01

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