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    • 10. 发明申请
    • HETEROCYCLIC SUBSTITUTED 2- (4-PHENOXY) PYRIDINE DERIVATIVES AND RELATED COMPOUNDS AS SODIUM CHANNEL BLOCKERS FOR THE TREATMENT OF NEURONAL DAMAGE AND NEURODEGENERATIVE CONDITIONS
    • 杂环取代的2-(4-苯氧基)吡啶衍生物及相关化合物作为治疗神经损伤和神经营养因子的钠通道阻断剂
    • WO2003022285A1
    • 2003-03-20
    • PCT/US2002/028299
    • 2002-09-06
    • EURO-CELTIQUE S.A.SHAO, BinGOEHRING, R., Richard
    • SHAO, BinGOEHRING, R., Richard
    • A61K31/5377
    • C07D213/64C07D213/81
    • This invention relates to aryl substituted pyridines of Formula (I) or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein: Ar is selected from the group consisting of Ar 1 , Ar 2 , Ar 3 and Ar 4 , wherein Ar 1 is R 1 is 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, wherein Y is O, S or NR 11 , wherein R 11 is hydrogen or alkyl, Z is a saturated heterocyclic ring optionally substituted at one or more carbon atoms, m is 0 or 1, and n is 0-6; or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Ar and R 1 -R 4 are set in the specification. The invention is also directed to the use of 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 amyothrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, including diabetic neuropathy, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, and as antiarrhythmics.
    • 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,前药或溶剂合物,其中:Ar选自Ar1,Ar2,Ar3和Ar4,其中Ar1是R1选自 由任选取代的烷基,氨基,烷基硫醇,C(O)R 10,SO 2 R 10和OC(O)NH 2组成; R2是Ym-(CH2)nZ,其中Y是O,S或NR11,其中R11是氢或烷基,Z是在一个或多个碳原子上任意取代的饱和杂环,m是0或1,n是0 -6; 或其药学上可接受的盐,前药或溶剂合物,其中Ar和R 1 -R 4置于说明书中。 本发明还涉及式I化合物用于治疗全身和局部缺血后的神经元损伤,用于治疗或预防神经变性疾病如肌萎缩性侧索硬化(ALS)以及治疗,预防或改善 急性或慢性疼痛,包括糖尿病性神经病,作为抗惊厥药,抗惊厥药,抗抑郁药,作为局部麻醉剂,以及作为抗心律失常药。