| abstract |
This invention relates to quinoline derivatives (I), their use in the treatment of hypersensitive ailments and a pharmaceutical composition containing the same. They are especially valuable as lipoxygenase inhibitors and/or leukotriene antagonists, typically antagonists of leukotriene D4, possessing anti-inflammatory and anti-allergic properties. <CHEM> a is 0-2; b is 0-1; c is 0-4; d is 0-5; e is 0-4; f is 0-5; n is 0-2; R is independently hydrogen, alkyl, hydroxy, alkoxy, carboxy, carbalkoxy, halo, nitro, haloalkyl, cyano or acyl; R min is independently hydrogen, alkyl, hydroxy, alkoxy, halo or haloalkyl; R1 is independently hydrogen, alkyl or aralkyl; R2 is -(CH2)x - X, where x is 0-3; X is hydrogen, alkyl, alkenyl, cycloalkyl, aryl aralkyl, hydroxy, alkoxy, aralkoxy, amino, mono-and di-alkylamino, aralkylamino, acylamino, carbamyl, carboxy, carbalkoxy, tetrazolyl, or acylsulfonamido; vicinal R2 groups together may be (CH2)y - where y is 1-4, thus forming a 3-6 membered ring; geminal R1 and R2 groups may together form a spiro substituent, -(CH2)z -, where z is 2 to 5; geminal R1 or R1 and R2 groups may together form an alkylidenyl substituent, =CHR1; Z is -COOR1, CN, - @NHSO2R3, -@N(R1)2, -OR1, tetrazolyl or substituted tetrazolyl where the substituent may be alkyl, carboxyalkyl or carbalkoxyalkyl; and R3 is hydrogen, alkyl, haloalkyl, phenyl or benzyl; or a pharmaceutically acceptable salt thereof. |