Pfizer Corporation

Akemi Ando

Rodney W Stevens

N-hydroxyureas as antiinflammatory agents

Certain novel isoxazoline compounds having the ability to inhibit the 5-lipoxygenase enzyme and having formula (I), ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.4 alkyl or --NR.sub.3 R.sub.4 ; R.sub.3 and R.sub.4 are each independently H or C.sub.1 -C.sub.4 alkyl; M is H or a pharmaceutically acceptable cation; A is C.sub.1 -C.sub.6 alkylene, C.sub.2 -C.sub.6 alkenylene or C.sub.2 -C.sub.6 alkynylene; Ar is phenylene or mono-, di- or tri-substituted phenylene wherein the substituents are each independently selected from halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy; n is an integer of 0 or 1; Y is H or C.sub.1 -C.sub.4 alkyl; R.sub.2 is C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.4 arylalkyl or C.sub.2 -C.sub.4 arylalkenyl; and said aryl and each aryl moiety in said arylalkyl and arylalkenyl may be substituted by from one to three substituents independently selected from halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halosubstituted C.sub.1 -C.sub.4 alkyl, halosubstituted C.sub.1 -C.sub.4 alkoxy, aryl-C.sub.1 -C.sub.4 alkoxy, phenoxy and mono-, di- and tri-substituted phenoxy wherein the substituents are each independently selected from halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and halosubstituted C.sub.1 -C.sub.4 alkyl. These compounds are useful in the treatment or alleviation of inflammatory diseases, allergy and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.

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Handa, Japan

Akemi Ando