Oxazoloquinolinone derivatives, their preparation and their...

Details Oxazoloquinolinone derivatives, their preparation and their... Oxazoloquinolinone derivatives, their preparation and their...

C - Chemistry, Metallurgy

12

P

C12P 41/00 (2006.01) A61K 31/435 (2006.01) C07D 498/04 (2006.01)

Patent

CA 2157427

3,3a,4,5-Tetrahydro-1H-oxazolo[3,4-a]quinolin-1-one derivatives of formula (I) (see formula I) in which: n is 0 or 1, R1 represents a hydrogen atom or an ethenyl, methyl, ethyl, phenyl, hydroxymethyl or methoxymethyl group, and (i) R2 is a methyl, trifluoromethyl or cyano group, R3 is a hydrogen atom or a hydroxyl or benzyloxy group and R4 and R5 are hydrogen atoms, or (ii) R2 and R4 together form a - (CH2)4- group, R3 is a hydroxyl group and R5 is a hydrogen atom, or (iii) R2 and R5 together form an -O- (CH2) 3- group, and R3 and R4 are hydrogen atoms, or (iv) R2 and R5 together form a -(CH2) 4 group, R3 is a hydroxyl group and R4 is a hydrogen atom, are useful as selective inhibitors of MAO-A or as mixed inhibitors of MAO-A and MAO-B.

Divulgation de dérivés de 3,3a,4,5-tétrahydro-1H-oxazolo¬3,4-a|quinolin-1-one de formule I (voir la formule I) dans laquelle : n est égal à 0 ou 1, R1 est un atome d'hydrogène ou un groupe vinyle, méthyle, éthyle, phényle, hydroxyméthyle ou méthoxyméthyle et (i) R2 est un groupe méthyle, trifluorométhyle ou cyano, R3 est un atome d'hydrogène ou groupe hydroxyle ou benzyloxy, R4 et R5 sont des atomes d'hydrogène, ou bien (ii) R2 et R4 forment ensemble un groupe -(CH2)4-, R3 est un groupe hydroxyle et R5 est un atome d'hydrogène, ou bien (iii) R2 et R5 forment ensemble un groupe -O-(CH2)3- et R3 et R4 sont des atomes d'hydrogène, ou bien (iv) R2 et R5 forment ensemble un groupe -(CH2)4-, R3 est un groupe hydroxyle et R4 est un atome d'hydrogène. Ces dérivés sont utiles comme inhibiteurs sélectifs de MAO-A ou comme inhibiteurs mixtes de MAO-A et de MAO-B.

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