Fluorine-containing amino acid derivatives

C - Chemistry – Metallurgy – 07 – C

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C07C 229/50 (2006.01) A61K 31/196 (2006.01) A61K 31/215 (2006.01)

Patent

CA 2318800

Fluorine-containing amino acid derivatives represented general formula (I), pharmaceutically acceptable salts thereof or hydrates of the same, wherein X1 represents hydrogen or fluorine; and R1 and R2 are the same or different and each represents hydrogen or lower C1-10 alkyl. These compounds are useful as drugs, in particular, group 2 metabotropic glutamate receptor agonists for treating and preventing psychiatric disorders such as schizophrenia, anxiety and associated diseases, depression, dipolar disturbance and epilepsy, and neurological diseases such as drug addiction, cognition disorder, Alzheimer's disease, Huntington's chorea, Parkinson's disease, motility disturbance associating muscular stiffness, cerebral ischemia, cerebral insufficiency, spinal cord lesion and head disturbance.

L'invention concerne des dérivés d'acides aminés renfermant du fluor représentés par la formule générale (I) ci-après, et des sels ou des hydrates pharmaceutiquement acceptables de ces dérivés. Dans ladite formule, X<1> représente hydrogène ou fluor; et R<1> et R<2>, qui sont identiques ou différents, représentent chacun hydrogène ou un alkyle C<1-10> inférieur. Ces composés sont utiles comme médicaments, notamment comme agonistes du récepteur du glutamate métabotropique du groupe 2, pour le traitement et la prévention de troubles psychiatriques tels que la schizophrénie, l'anxiété et les maladies associées, la dépression, les perturbations dipolaires et l'épilepsie, ainsi que les troubles neurologiques tels que la toxicomanie, les troubles cognitifs, la maladie d'Alzheimer, la chorée de Huntington, la maladie de Parkinson, les troubles de la motilité associés à la raideur musculaire, l'ischémie cérébrale, l'insuffisance cérébrale, les lésions de la moelle épinière et les troubles cérébraux.

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