Neurotherapeutic composition and method therefor

Abstract

Neurotherapeutically effective pharmaceutical compositions are described that include carboxypeptidase E inhibitors. One class of carboxypeptidase E inhibitors found to exhibit significant neurotropic activity are β-lactam compounds, particularly penam and cephem β-lactam antibiotics and non-antibiotic derivatives thereof.

Description

[0001] This application is a continuation of U.S. patent application Ser. No. 09 / 783,201, filed Feb. 14, 2001, which is expressly incorporated by reference herein.FIELD OF INVENTION [0002] This invention relates to a novel mechanism of neuropsychiatric intervention. More particularly, this invention is directed to pharmaceutical formulations and methods for treatment of a variety of neurological disease states, including cognitive and behavioral disorders. BACKGROUND AND SUMMARY OF THE INVENTION [0003] The pharmaceutical industry has directed extensive research and development efforts toward discovery and commercialization of drugs for treatment of neurological disorders. Such disorders typically derive from chemical imbalances in the brain. Overproduction or underproduction of pertinent neurochemical species and / or receptor dysfunction has been identified with many disease states recognized by neurologists, psychiatrists, psychologists and other medical practitioners skilled in the...

AI Technical Summary

Benefits of technology

[0006] In a related embodiment there is provided method for treatment of cognitive and behavioral disorders in a patient in need of such treatment. The method comprises the step of inhibiting neurogenic peptidases, particularly, carboxypeptidase E and related neurogenic enzymes. Such neuropeptidase inhibition is effected by administering an effective amount of a β-lactam compound recognized for its capacity to bind to and inhibit a bacterial enzyme, for example, a β-lactamase or a bacterial protease involved in bacterial cell wall synthesis. Such bacterial proteases are known in the art as “penicillin binding proteins.” Exemplary of β-lactam compounds for use in this invention are moxalactam, its salts, esters and structurally related cephems and 1-oxa-1-dethia cephems. Effective inhibition of neurogenic-carboxypeptidase E and related neuro-peptidase activity in warm-blooded vertebrates in accordance with this invention has been found to produce marked enhancement in cognitive performance and behavioral management.

[0007] Exemplary of cognitive and behavioral disorders susceptible to treatment in accordance with this invention include aggressive disorder, obsessive compulsive disorder, anxiety, depression, ADHD, and memory impairment. Animal data suggest that the method and formulation of this invention have potential as an antiaggressive agent to control impulsivity and violence in autism, Tourette's syndrome, mental retardation, psychosis, mania, senile dementia and individuals with personality disorders and history of inappropriate aggression. Clinic applications extend to the treatment of children with ADHD and conduct disorder, as an anxiolytic, and as a cognition enhancer for the geriatric population to improve learning and memory and to ameliorate disorientation.

Problems solved by technology

Such disorders typically derive from chemical imbalances in the brain.

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