Isoxazolo-pyridine derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 413/12 (2006.01) A61K 31/4439 (2006.01) A61P 25/28 (2006.01) C07D 413/14 (2006.01) C07D 417/14 (2006.01) C07D 487/04 (2006.01) C07D 491/08 (2006.01) C07D 491/10 (2006.01)

Patent

CA 2707648

The present invention is concerned with isoxazole-pyridine derivatives of formula (I) wherein: X is O or NH; R1 is phenyl, pyridinyl, or pyrimidinyl, each optionally substituted with 1, 2 or 3 halo, R2 is H or CH3 or CF3; R3 , R4 , R5 , and R6 are each independently H optionally substituted C1-7alkyl optionally substituted C1- 7alkoxy CN, halo, NO2, S-C1-7alkyl, S(O)-C1-7alkyl optionally substituted benzyloxy -C(O)-R a, -C(O)- NR b R c, or a pharmaceutically acceptable salt thereof. The compounds are active on the GABA A .alpha.5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.

Cette invention concerne des dérivés isoxazolo-pyridine représentés par la formule (I), dans laquelle X représente O ou NH; R1 représente phényle, pyridinyle, ou pyrimidinyle, chacun éventuellement substitué avec 1, 2 ou 3 halo, R2 représente H ou CH3 ou CF3; R3, R4, R5, et R6 représentent indépendamment les uns des autres H, C1-7alkyle éventuellement substitué, C1-7alkoxy éventuellement substitué, CN, halo, NO2, S-C1-7alkyle, S(O)-C1-7alkyle, benzyloxy éventuellement substitué, -C(O)-Ra, -C(O)-NRb Rc, ou un sel pharmaceutiquement acceptable de ceux-ci. Les composés sont actifs sur le site de liaison aux récepteurs GABA A a5 et ils sont utilisés pour le traitement de troubles cognitifs, tels que la maladie d'Alzheimer.

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