Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1987-11-13
1989-04-18
Schwartz, Richard A.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514375, 514395, 548178, 548180, 548217, 548330, A61K 31425, C07D27764
Patent
active
048228095
ABSTRACT:
Compounds of the formula: ##STR1## wherein R.sub.1 is (1) hydrogen, (2) C.sub.1 to C.sub.4 alkyl, (3) C.sub.2 to C.sub.4 alkenyl, or (4) NR.sub.2 R.sub.3, wherein R.sub.2 and R.sub.3 are independently selected from (1) hydrogen, (2) C.sub.1 to C.sub.4 alkyl and (3) hydroxyl, but R.sub.2 and R.sub.3 are not simultaneously hydroxyl;
X is (1) oxygen, (2) sulfur, (3) SO.sub.2, or (4) NR.sub.4, wherein R.sub.4 is (1) hydrogen, (2) C.sub.1 to C.sub.6 alkyl, (3) C.sub.1 to C.sub.6 alkyl or (4) aroyl;
A is selected from C.sub.1 to C.sub.6 alkylene and C.sub.2 to C.sub.6 alkenylene; n is 0-4;
Y is selected independently at each occurrence from (1) hydrogen, (2) halogen, (3) hydroxy, (4) cyano, (5) halosubstituted alkyl, (6) C.sub.1 to C.sub.12 alkyl, (7) C.sub.2 to C.sub.12 alkenyl, (8) C.sub.1 to C.sub.12 alkoxy, (9) C.sub.3 to C.sub.8 cycloalkyl, (10) aryl, (11) aryloxy, (12) aroyl, (13) C.sub.1 to C.sub.12 arylalkyl, (14) C.sub.2 to C.sub.12 arylalkenyl, (15) C.sub.1 to C.sub.12 arylalkoxy, (16) C.sub.1 to C.sub.12 arylthioalkoxy, and substituted derivatives of (17) aryl, (18) aryloxy, (19) aroyl, (20) C.sub.1 to C.sub.12 arylalkyl, (21) C.sub.2 to C.sub.12 arylalkenyl, (22) C.sub.1 to C.sub.12 arylalkoxy, or (23) C.sub.1 to C.sub.12 arylthioalkoxy, wherein substituents are selected from halo, nitro, cyano, C.sub.1 to C.sub.12 alkyl, alkoxy, and halosubstituted alkyl;
and M is hydrogen, a pharmaceutically acceptable cation, aroyl, or C.sub.1 to C.sub.12 alkoyl, are potent inhibitors of 5- and/or 12-lipoxygenase enzymes. Also disclosed are lipoxygenase inhibiting compositions and a method for inhibiting lipoxygenase.
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patent: 4112186 (1978-10-01), Lafon
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patent: 4604407 (1986-08-01), Haslanger et al.
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patent: 4665206 (1987-05-01), Redpath et al.
Stewart Andrew O.
Summers James B.
Abbott Laboratories
Crowley Steven R.
Katz Martin L.
Schwartz Richard A.
Weinstock Steven F.
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