A New Potent Irreversible Inhibitor of y-Aminobutyric Acid Aminotransferase (21058/23058)

A promising new candidate inhibitor of the enzyme gamma-aminobutyric acid aminotransferase, critical to central nervous system disorders, has been prepared. Therapeutic potential in the treatment of epilepsy, drug addiction, pain control and neurological disorders is indicated.

ADVANTAGES: In vitro studies indicate enhanced inhibition and selectivity toward the GABA-AT enzyme than present day drugs.

SUMMARY: A low level of gamma-amino butyric acid (GABA) in the brain is associated with epilepsy, a central nervous system disease characterized by recurring convulsive seizures, and drug addiction. The enzyme gamma-aminobutyric acid aminotransferase (GABA-AT) degrades GABA in the brain and therefore is the target for inhibition. Vigabatrin (4-Amino-5-hexenoic acid) is a drug on the European market that irreversibly inhibits GABA-AT. Based on its structure, a new conformationally rigid compound was designed and synthesized. It inactivates GABA-AT presumably through a Michael addition pathway. In vitro enzyme studies indicate this new molecule binds ~ 90 times greater, inactivates ~ 2 times faster, and is overall ~ 200 times more effective at GABA-AT inactivation than vigabatrin. Continuing studies support the superior performance of this new GABA-AT inhibitor. Therapeutic potential exists for a range of neurological indications.

STATUS: U. S. Patent No. 6,794,413 and U. S. Patent No. 7,381,748 have issued.

Type of Offer: Licensing



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