Method for the stereoselective synthesis of cyclic amino acids

Organic compounds -- part of the class 532-570 series – Organic compounds – Carboxylic acids and salts thereof

Reexamination Certificate

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C562S503000, C562S504000

Reexamination Certificate

active

06864390

ABSTRACT:
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®) of Formulas (I), (II), (III) and (IV) wherein R is C1-C10alkyl or C3-C10cycloalkyl and pharmaceutically acceptable salts thereof.

REFERENCES:
patent: 9921824 (1999-05-01), None
PCT Search Report, PCT/US00/32570.
Herz, “Azulenes. VII. A Novel Rearrangement in the Synthesis of Azulenes”,Journal of the American Chemical Society, vol. 78, No. 7, pp. 1485-1494, 1956.

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