5-lipoxygenase inhibitors

Details 5-lipoxygenase inhibitors 5-lipoxygenase inhibitors

1998-12-08

2000-05-16

Richter, Johann

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

5462711, 5462714, 5462721, 5462724, 5462734, 5462744, 5462751, 5462754, 5462761, 5462774, 5462777, 548146, 548186, 548206, 548214, 548255, 5482622, 5482658, 5482662, 5482668, 5482672, 5482678, 5482682, 5483047, 5483351, 5483731, 5483751, 5483761, 5483771, 5483611, 5483625, 548469, 548518, 548523, 548527, 549 59, 549 61, 549 62, 549 65, 549 74, 549 75, 549472, 549474, 549475, 549491, 549497, 549504, C07D207323, C07D20736, C07D23360, C07D23361, C07D40110, C07D40310, C07D40510, C07D23510, C07D23514

Patent

active

060639288

ABSTRACT:
Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having the following formula I: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Ar.sup.1 is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which is bonded to X.sup.1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C.sub.1-4 alkyl and the like; X.sup.1 is a direct bond or C.sub.1-4 alkylene; Ar.sup.2 is phenylene optionally substituted with halo, hydroxy, cyano, amino and the like; X.sup.2 is --A--X-- or --X--A-- wherein A is a direct bond or C.sub.1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar.sup.3 is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C.sub.1-4 alkyl and the like; R.sup.1 and R.sup.2 are each C.sub.1-4 alkyl, or together they form a group of formula --D.sup.1 --Z--D.sup.2 -- which together with the carbon atom to which it is attached defines a ring having 3 to 8 atoms, wherein D.sup.1 and D.sup.2 are C.sub.1-4 alkylene and Z is a direct bond or oxy, thio, sulfinyl, sulfonyl, or vinylene, and D.sup.1 and D.sup.2 may be substituted by C.sub.1-3 alkyl; and Y is CONR.sup.3 R.sup.4, CN, C(R.sup.3).dbd.N--OR.sup.4, COOR.sup.3, COR.sup.3 or CSNR.sup.3 R.sup.4, wherein R.sup.3 and R.sup.4 are each H or C.sub.1-4 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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