Phenylmethyl derivatives having lipoxygenase inhibitory activity

Details Phenylmethyl derivatives having lipoxygenase inhibitory activity Phenylmethyl derivatives having lipoxygenase inhibitory activity

1992-09-10

1994-10-11

Ivy, C. Warren

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

544105, 5483047, C07D23526, C07D215227, C07D26536

Patent

active

053548655

ABSTRACT:
Compounds of the structure ##STR1## where Ar is optionally substituted carbocyclic aryl, 5- or 6-membered heterocyclic aryl, 10-membered bicyclic heterocyclic aryl containing one or two nitrogen atoms, 9- or 10-membered heterocyclic containing one or two nitrogen atoms and optionally containing a further nitrogen or oxygen atom and one oxo or thioxo substituent, benzo[b]furyl, benzo[b]thienyl, A.sub.1 is propynylene, methylene, or a valence bond, X is O, S, SO.sub.2, or NR.sub.2, Y is selected from alkyl, haloalkyl, alkoxy, halogen, and hydrogen, A.sub.2 is selected from ##STR2## and methylene where Z is OR.sub.5 or NHR.sub.5 where R.sub.5 is hydrogen or alkyl, R.sub.1 is hydrogen, alkyl, or OR.sub.5, and m and n are integers having a value of 1 or 2 are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.

REFERENCES:
patent: 5179115 (1993-01-01), Bruneau
patent: 5217969 (1993-06-01), Bruneau
patent: 5217977 (1993-06-01), Crawley
patent: 5217978 (1993-06-01), Bird
patent: 5240941 (1993-08-01), Bruneau
patent: 5250690 (1993-10-01), Turner et al.

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