Indolinyl n-hydroxyurea and n-hydroxamic acid derivatives as lipoxygenase inhibitors.

摘要

Certain novel indoline derivatives having the ability to inhibit the 5-lipoxygenase enzyme and having formula (I) wherein R1 is C1-C4 alkyl or -NR2R3; R2 and R3 are each, independently, hydrogen or C1-C4 alkyl; R4 is C3-C6 cycloalkyl, C4-C7 cycloalkylalkyl, aryloxy C2-C4 alkyl, arylthio C2-C4 alkyl, arylamino C2-C4 alkyl, arylsulfinyl C2-C4 alkyl, aryl, aryl C1-C6 alkyl, aryloxyaryl C1-C6 alkyl or arylthioaryl C1-C6 alkyl, and the aryl groups in the said aryloxyalkyl, arylthioalkyl, arylaminoalkyl, arylsulfinylalkyl, aryl, arylalkyl, aryloxyarylalkyl and arylthioarylalkyl may be substituted up to the maximal number of substituents and the substituents are each independently, selected from the group consisting of halo, cyano, C1-C5 alkyl, C2-C6 alkenyl, C1-C5 alkoxy, C2-C6 alkenyloxy, C2-C6 alkoxyalkyl, halosubstituted C1-C4 alkyl, halosubstituted C1-C4 alkoxy, C2-C5 alkoxycarbonyl, aminocarbonyl and C1-C4 alkylthio; A is C1-C6 alkylene, C3-C6 alkenylene or -O-(CH2)m-; Y is each independently, halogen, halosubstituted C1-C6 alkyl, C1-C6 alkyl, C2-C6 alkenyl, C1-C6 alkoxy or C3-C8 alkenyloxy; m is 2, 3 or 4; n is 0, 1, 2 or 3; and provided that the substituent Y, if present, and the linking group A are attached to the aromatic ring. These compounds are useful in the treatment of alleviation of inflammatory diseases, allergic conditions and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.