Neurotherapeutic composition and method

A - Human Necessities – 61 – K

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A61K 31/5365 (2006.01) A61K 31/43 (2006.01) A61K 31/431 (2006.01) A61K 31/545 (2006.01) A61K 31/546 (2006.01) A61K 45/06 (2006.01) A61P 9/10 (2006.01) A61P 25/00 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2383522

Administration .beta.-lactam compounds, including of inhibitors of certain bacterial peptidases have been found to provide significant neurotropic effects in warm-blooded vertebrates evidencedinter alia by anxiolytic and anti- aggressive behavior and enhanced cognition believed to be mediated by inbibition of neurogenic NAALADase and related enzyme activity. .beta.-Lactam antibiotics and .beta.-lactamase inhibitors have been found to exhibit potent NAALADase inhibition, and those compounds with blood brain barrier transport are effective inhibitors of neurogenic NAALADase with significant neuro- therapeutic effects. .beta.-Lactam compounds are useful for treatment of numerous disease states associated with glutamate abnormalities. Therapeutic methods for using such compounds and their pharmaceutical formulations are described.

On a trouvé que l'administration de composés à base de .beta.-lactame, notamment des inhibiteurs de certaines peptidases bactériennes, pouvait produire des effets neurotropes importants chez des vertébrés à sang chaud, ces effets étant mis en relief, entre autres, par une attitude anxiolytique et anti-aggressive et une activité cognitive accrue, lesquelles sont supposées être induites par l'inhibition de la NAALADase neurogène et de l'activité enzymatique associée. On a trouvé que les antibiotiques à base de .beta.-lactame et les inhibiteurs de la .beta.-lactamase possédaient un pouvoir d'inhibition de la NAALADase, et que ces composés, capables de transport à travers la barrière hémato-encéphalique, constituaient des inhibiteurs efficaces de la NAALADase neurogène et possédaient des effets neuro-thérapeutiques importants. On peut utiliser les composés à base de .beta.-lactame dans le traitement de nombreuses pathologies associées aux anomalies du glutamate. L'invention concerne encore des procédés thérapeutiques d'utilisation de tels composés, ainsi que les formulations pharmaceutiques de ces composés.

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