发明授权
US5958904A Phosphonomethyl-imidazo�1,2-A! pyrimidine-2-carboxylic acid compounds
for treatment of neurotoxic injury
失效
用于治疗神经毒性损伤的膦酰基甲基 - 咪唑并[1,2-A]嘧啶-2-羧酸化合物
- 专利标题: Phosphonomethyl-imidazo�1,2-A! pyrimidine-2-carboxylic acid compounds for treatment of neurotoxic injury
- 专利标题(中): 用于治疗神经毒性损伤的膦酰基甲基 - 咪唑并[1,2-A]嘧啶-2-羧酸化合物
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申请号: US46885申请日: 1998-03-24
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公开(公告)号: US5958904A公开(公告)日: 1999-09-28
- 发明人: Alexis A. Cordi , Eric T. Sun
- 申请人: Alexis A. Cordi , Eric T. Sun
- 申请人地址: IL Chicago
- 专利权人: G.D. Searle & Co.
- 当前专利权人: G.D. Searle & Co.
- 当前专利权人地址: IL Chicago
- 主分类号: C07F9/6561
- IPC分类号: C07F9/6561 ; A61K31/675 ; A61K31/505
摘要:
A method is described to prevent neural cell injury by use of a compound from a class of phosphonometyl-imidazo�1,2-a!pyrimidine-2-carboxylic acid compounds. The treatment includes administration of a compound of this class alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula: ##STR1## wherein Y.sub.m is --CH.sub.2 -- or --CH.sub.2 --CH.sub.2 --; where m is one; wherein X is one or more groups attachable at one or more of the 5-, 6- and 7-ring positions of the imidazo�1,2-a!pyrimidine ring system; wherein each X and T is independently selected from hydrido, halo, alkyl, cycloalkyl, cycloalkylalkyl, haloalkyl, alkenyl, alkynyl, phenyl, benzyl, hydroxy, hydroxyalkyl, alkoxy, phenoxy, alkoxyalkyl, benzyloxy, cyano, alkanoyl, alkylthio, arylthio and amino; wherein each of R.sup.1, R.sup.2 and R.sup.6 is independently selected from hydrido, alkyl, allyl, cycloalkyl, cycloalkylalkyl, phenyl and benzyl; or a pharmaceutically-acceptable salt thereof.
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