Thiazole derivatives as lipoxygenase inhibitors

Details Thiazole derivatives as lipoxygenase inhibitors Thiazole derivatives as lipoxygenase inhibitors

C - Chemistry, Metallurgy

07

D

C07D 417/14 (2006.01) A61K 31/47 (2006.01)

Patent

CA 2168252

The invention concerns a thiazole derivative of formula (I) wherein Q is 2-oxo-1,2,3,4-tetrahydroquinolin-6-yl or 2-oxo-1,2-dihydroquinolin-6-yl which bears on the nitrogen atom at the 1-position a (1-4C)alkyl substituent; X1 is thio, sulphinyl or sulphony: Ar is thiazolediyl; R1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; and R2 and R3 together form a group of the formula -A2-X2-A3- which together with the carbon atom to which A2 and A3 are attached define a ring having 5 or 6 ring atoms, wherein A2 and A3, which may be the same or different, each is (1-3C)alkylene and X2 is oxy, and which ring may bear one or two (1-4C)alkyl substituents or a pharmaceutically-acceptable salt thereof; processes for their preparation; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.

Dérivé de thiazole répondant à la formule (I), dans laquelle Q représente 2-oxo-1,2,3,4-tétrahydroquinoléin-6-yle ou 2-oxo-1,2-dihydroquinoléin-6-yle portant un substituant alkyle C1-4 en position 1 sur l'atome d'azote; X<1> représente thio, sulfinyle ou sulfonyle; Ar représente thiazolediyle; R<1> représente alkyle C1-4, alcényle C3-4 ou alcynyle C3-4; et R<2> et R<3> forment ensemble un groupe répondant à la formule -A<2>-X<2>-A<3>- et formant, conjointement avec l'atome de carbone auquel sont rattachés A<2> et A<3>, un cycle à 5 ou 6 atomes, A<2> et A<3>, identiques ou différents, représentant alkylène C1-3, tandis que X<2> représente oxy, et ledit cycle pouvant porter un ou deux substituants alkyle C1-4; ou son sel pharmaceutiquement acceptable; leurs procédés de préparation; compositions pharmaceutiques les contenant, et leur utilisation comme inhibiteurs de 5-lipoxydase.

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