Abstract: Fermentation of the microorganism Actinoplanacete sp. (MA6559), ATTC No. 53771, in the presence of the HIV reverse transcriptase inhibitor ##STR1## yields 3-[2-(benzoxazol-2-yl)ethyl]-5-(1-hydroxyethyl)-6-methyl-2(1H)-pyridinone and 3-[2-(benzoxazol-2-yl)ethyl]-5-ethyl-6-hydroxymethyl-2(1H)-pyridinone, both of which are useful in the prevention or treatment of infection by HIV and the treatment of AIDS.
Abstract: Incubation of ##STR1## with a preparation from mammalian organ yields as biotransformation products the 6-hydroxymethyl and 5-(1-hydroxy)ethyl anologs. These products are useful in the prevention or treatment of infection by HIV and the treatment of AIDS.
Type:
Grant
Filed:
June 7, 1991
Date of Patent:
December 8, 1992
Assignee:
Merck & Co., Inc.
Inventors:
Suresh K. Balani, Byron H. Arison, Harri G. Ramjit, Anthony D. Theoharides, Laura R. Kauffman
Abstract: An efficient process for stereoselective preparation of a medicinally significant hydroxyamide compound of structural formula: ##STR1## comprises the addition of metalated amide enolates to chiral .alpha.-amino metalated epoxides. The hydroxyamide reaction products are useful as inhibitors of the HIV protease or of renin, or as intermediates in the preparation of inhibitors of the HIV protease or renin.
Type:
Grant
Filed:
July 2, 1991
Date of Patent:
December 8, 1992
Assignee:
Merck & Co., Inc.
Inventors:
David Askin, Ralph Volante, Michael Wallace, Ichiro Shinkai
Abstract: Topical administration of a cholinomimetic agent, such as pilocarpine, in combination with a cholinergic M.sub.3 receptor antagonist, such as 4-diphenyl-acetoxy-N-methylpiperidine, to the eye of a mammal reduces intraocular pressure without the concommitant miotic effect that normally occurs with administration of a cholinomimetic agent along.
Abstract: Peptide analogues of human humoral hypercalcemic factor (hHCF) that contain a lactam bridge act as inhibitors of the naturally occurring peptide. A lactam bridge between Lys and Asp situated five residues (inclusive) apart confers rigidity to that region of the peptide, and enhances the helical nature and metabolic stability of the peptide analogue.
Abstract: Poly(diallylamine) blended with poly(N-methylolacrylamide) effectively detackifies over-sprayed paint in the circulating water of a wet paint spray booth operation. After detackification the dispersed paint is flocculated with hydrolyzed polyacrylamide, the paint waste is removed, and the clarified water is recirculated back into the paint spray booth operation.
Abstract: Novel indole compounds inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds or pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.