5-lipoxygenase inhibitors

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai

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Details

514570, A61U 3119, A61U 31235

Patent

active

048016110

ABSTRACT:
This invention encompasses compounds and methods for inhibiting lipoxygenase and includes a pharmaceutical composition comprising a pharmaceutical carrier and an effective lipoxygenase inhibiting amount of a compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different members of the group consisting of tert-alkyl of 4 to 10 carbon atoms; and R.sub.3 is ##STR2## wherein R.sub.4 is hydrogen or lower alkyl; ##STR3## wherein R.sub.6 and R.sub.7 may be the same or different and are alkyl of 1 to 4 carbon atoms; or ##STR4## and the pharmaceuticlaly acceptable salts thereof. The compounds and pharmaceutical formulations of the present invention are 5-lipoxygenase inhibitors and, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.

REFERENCES:
patent: 4012523 (1977-03-01), Wagner
patent: 4067998 (1978-01-01), Wagner
patent: 4108831 (1978-08-01), Cottman
patent: 4198425 (1980-04-01), Mitsui et al.
patent: 4262013 (1981-04-01), Mitsui et al.
Foegh et al. Improved Rat Cardiac Allograft Survival with Non-Steroidal Pharm Agents., Transplant Proc., 19,1297-1300 (Feb. 1987).
Foegh et al., Presentation at 6th Int Conf. On Prostaglandins and Related cpds., Florence, Italy, Jun. 3-6, 1987 (abstract attached).
Foegh, et al., Presentation at NIH Workshop, Potential Therapeutic use of Inhibitors of Leukotriene . . . , Jun. 23, 1986 (trip report attached).
Wagner, E. R. et al., "Hypolipidemic Arylthioalkanoic Acids", J. Med. Chem., 1977, vol. 20, No. 8, 1007-1013.

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