发明公开
EP1568690A1 The use of carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones as sodium channel blockers
失效
通过碳环和杂环取代的缩氨基脲和缩氨基硫脲及它们作为钠通道阻断剂的使用
- 专利标题: The use of carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones as sodium channel blockers
- 专利标题(中): 通过碳环和杂环取代的缩氨基脲和缩氨基硫脲及它们作为钠通道阻断剂的使用
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申请号: EP04030775.3申请日: 1998-04-22
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公开(公告)号: EP1568690A1公开(公告)日: 2005-08-31
- 发明人: Wang, Yan , Cai, Sui Xiong , Lan, Nancy C. , Ilyin, Victor I. , Keana, John F. W. , Weber, Eckard
- 申请人: Euro-Celtique S.A.
- 申请人地址: 122 Boulevard de la Pétrusse 2330 Luxembourg LU
- 专利权人: Euro-Celtique S.A.
- 当前专利权人: Euro-Celtique S.A.
- 当前专利权人地址: 122 Boulevard de la Pétrusse 2330 Luxembourg LU
- 代理机构: Chapman, Paul William
- 优先权: US44530P 19970422; US62649P 19971022
- 主分类号: C07D211/06
- IPC分类号: C07D211/06 ; C07D213/02 ; C07D215/02 ; C07D239/02 ; C07D309/02 ; A61K31/35 ; A61K31/44 ; A61K31/445 ; A61K31/47 ; A61K31/505 ; C07D213/64
摘要:
This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by formula (I), or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R 1 , R 21 , R 22 and R 23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R 22 and R 23 , together with the N, form a heterocycle; A 1 and A 2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR 24 , CR 25 R 26 , C(O), NR 24 C(O), C(O)NR 24 , SO, SO 2 or a covalent bond; where R 24 , R 25 and R 26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl. The invention is also directed to the use of carbocycle and heterocycle substituted semicarbazones and thiosemicarbazones for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyiotrophic lateral sclerosis (ALS), for the treatment and prevention of otoneurotoxicity and eye diseases involving glutamate toxicity and for the treatment, prevention or amelioration of pain, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy and urinary incontinence.
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