Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1989-02-22
1990-10-16
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514212, 5142342, 5142345, 514258, A61K 31505, A61K 31535
Patent
active
049635417
ABSTRACT:
Compounds of the formula: ##STR1## wherein A is selected from NR.sub.1 R.sub.2 and N(OR.sub.6)R.sub.2 ; and B and C are chloro when A is N(OR.sub.6)R.sub.2 or are independently selected from NHR.sub.3 and NR.sub.4 R.sub.5 where R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are independently selected from the group consisting of alkyl, cycloalkyl and alkylaryl each of which may be unsubstituted or substituted with one or more substituents selected from the group consisting of hydroxy, OR, NRR, OCOR, OCONRR, NRCOR and NRCONRR where R is selected from the group consisting of hydrogen, alkyl, aryl, alkylaryl, alkoxy and hydroxy or R.sub.1 and R.sub.2 or R.sub.4 and R.sub.5 together can form a heteroaryl group and R.sub.6 is a member selected from the group consisting of hydrogen, alkyl, alkylaryl and trialkylsilyl; and the pharmaceutically acceptable salts thereof.
These compounds are useful as inhibitors of lipoxygenase enzymes.
REFERENCES:
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Corey et al., J. Am. Chem. Soc. 1984, 106, 1503-1504 "Rationally Designed Potent Competitive Inhibitors of Leukotriene Biosynthesis".
Radmark et al., FEBS Lett., 110, 213 (1980), "The Inhibitory Effects of BW 755C on Arachidonic Acid Metabolism in Human Polymorphonuclear Leukocytes".
Morris et al., Prostaglandins, 10, (1980), "The Role of Arachidonate Lipoxygenase in the Release of SRS-A from Guinea-pig Chopped Lung".
Coutts, Meeting Abstract 70, Prostaglandins and Leukotrienes, '84, "Arylmethyl Phenyl Esthers: A New Class of Specific Inhibitors of 5-Lipoxygenase".
Walker et al., Pharm. Pharmacol., 31, 778, (1979), "Inhibition of Rabbit PMN Lipoxygenase Activity by Benoxaprofen".
Carter et al., Federation Proceedings, 44(4):904, 1985, "Dipyrodamole: A Potent and Specific 5-Lipoxygenase Inhibitor".
Pichler et al., Drugs of the Future, 8, 1023, 1983, "RA-642".
Basha Anwer
Brooks Dee W.
Abbott Laboratories
Janssen Jerry F.
Shah Mukund J.
Ward Edward C.
Weinstock Steven F.
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