Warner-Lambert Company

Pfizer Corporation

Sophie Caroline Williams

Justin Stephen Bryans

David Clive Blakemore

The instant invention is a route to stereospecific 3-substituted 5-membered ring isomers of Formula (A). The final products are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), inflammation especially arthritis, sleep disorders, premenstrual syndrome, and hot flashes. The invention provides novel routes to synthesize steroselectively analogs of gabapentin (Neurontin&#xae;) of Formulas (I), (II), (III) and (IV) wherein R is C-Calkyl or C-Ccycloalkyl and pharmaceutically acceptable salts thereof.

Method for the stereoselective synthesis of cyclic amino acids

Alkyl amino acid derivatives useful as pharmaceutical agents

The compounds of the instant invention are bicyclic or tricyclic amino acids useful in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, arthritis, neuropathological disorders, sleep disorders, visceral pain disorders, and gastrointestinal disorders. Processes for the preparation of the final products and intermediates useful in the process are included. Pharmaceutical compositions containing one or more of the compounds are also included.

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Cambridge, United Kingdom

Sophie Caroline Williams