Neurotherapeutic clavulanate composition and method

Details Neurotherapeutic clavulanate composition and method Neurotherapeutic clavulanate composition and method

A - Human Necessities

61

K

A61K 31/423 (2006.01) A61K 31/00 (2006.01) A61K 31/197 (2006.01) A61K 31/198 (2006.01) A61K 31/395 (2006.01) A61K 31/424 (2006.01) A61K 31/43 (2006.01) A61K 31/431 (2006.01) A61K 31/4353 (2006.01) A61K 31/5365 (2006.01) A61K 31/5383 (2006.01) A61K 31/545 (2006.01) A61K 31/546 (2006.01) A61K 38/08 (2006.01) A61K 45/06 (2006.01) A61P 3/06 (2006.01) A61P 25/00 (2006.01) A61P 25/16 (2006.01) A61P 25/24 (2006.01) A61P 25/28 (2006.01)

Patent

CA 2380820

Administration of certain .beta.-lactam compounds, has been found to provide significant neurotropic effects in warm-blooded vertebrates evidenced inter alia by anxiolytic and anti-aggressive behavior and enhanced cognition believed to be mediated by inhibition of neurogenic NAALADase and related neurogenic enzyme activity. The .beta.-lactamase inhibitor, clavulanic acid exhibits potent NAALADase inhibition, and it exhibits good blood brain barrier transport to provide effective inhibition of neurogenic NAALADase with significant neuro-therapeutic effects. Clavulanate acid and related compounds are useful, for example, for treatment of anxiety, anti-aggressive disorders, memory impairment, and disease states characterized by glutamate abnormalities. Therapeutic methods for using such compounds and their pharmaceutical formulations are described.

L'administration de certains composés .beta.-lactam permet d'obtenir des effets neurotropes importants sur les vertébrés à sang chaud, démontrés entre autres choses par un comportement anxiolytique et anti-agressif et une activité mentale renforcée, connue pour être transmise par l'inhibition de la NAALADase neurogène et l'activité enzymatique neurogène associée. L'inhibiteur .beta.-lactamase, l'acide clavulanique, démontre une inhibition de NAALADase efficace, et présente un bon transport à travers la barrière cervicale sanguine, afin de produire une inhibition efficace de NAALADase neurogène avec des effets neuro-thérapeutiques importants. L'acide clavulanique et ses composés associés peuvent être utilisés en vue de, traiter l'anxiété, par exemple, les troubles anti-agressifs, la perte de mémoire, et les états maladifs caractérisés par des anomalies en glutamate. L'invention concerne également des procédés thérapeutiques, afin d'utiliser ces composés ainsi que leurs préparations pharmaceutiques.

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