4, 5, 6, 7, - tetrasubstituted benzoxazolones

C - Chemistry – Metallurgy – 07 – D

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167/231, 167/235

C07D 263/58 (2006.01) A61K 31/42 (2006.01) A61K 31/44 (2006.01) C07D 413/12 (2006.01)

Patent

CA 2021421

72222-152 Abstract of the Disclosure Certain 6-aryl- or 6-heteroaryl- alkylaminobenzoxa- zolones of the formula (I) below, and their pharmaceutically- acceptable salts, are dual inhibitors of lipoxygenase and cyclo- oxygenase enzymes, and so are useful as antiallergy and antiinflammatory agents. Image (I) [wherein R1 is hydrogen or C1 - C3 alkyl; R2 is a group of the formula - (CH2)m - Ar or - (CH2)m - Het (wherein m is an integer of 1 to 6 and Ar is phenyl optionally substituted by one or more radicals selected from the class con- sisting of (C1-C3) alkyl, (C1-C3) alkoxy, (C1-C3) alkylthio, halo, (C1-C2) alkylamino and hydroxyl; and Het is selected from the class consisting of furyl, thienyl, pyridyl, pyrrolyl, imidazolyl, pyranyl, oxazolyl or indazolyl); and Y1, Y2 and Y3 are each independently hydrogen, (C1-C3) alkyl, halo or (C1-C3) alkoxy or trifluoromethyl; with the proviso that at least two of Y1, Y2 and Y3 are other than hydrogen].

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