Merck + Co., Inc.

Laszlo R Treiber

Byron H Arison

Georgette Dezeny

Lawrence F Colwell, Jr

Russell B Lingham

Shieh-Shung T Chen

Wayne J Thompson

Robert T Goegelman

Leeyuan Huang

George A Doss

Ali Shafiee

Robert A Reamer

Suresh K Balani

Francis J Dumont

John G MacConnell

Vincent P Gullo

Nancy E Kohl

Doss, George A

There is disclosed a dual compartment solid phase extraction cartridge comprising a container divided into a top volume and a bottom volume by a porous filter or frit, the top and bottom volumes having a quantity of sorbent. The cartridge is useful in the separation of components of a liquid and solid mixture.

Dual compartment solid phase extraction cartridge

New cholesterol lowering compounds are formed from the photochemical treatment of the zaragozic acids.

Cholesterol lowering compounds

Zaragozic acids isolated from a culture of MF5465 have been subjected to photoreaction, then derivatized at the 4-keto position. The resulting derivatives are active as squalene synthetase inhibitors and are useful in the treatment of hypercholesterolemia.

This invention relates to compounds of structural formula ##STR1## which are inhibitors of squalene synthase and useful as cholesterol lowering agents.

Described is a process for producing a new FK-506 antagonist agent, a C-21 hydroxylated analog of FR-900520 under novel fermentation conditions utilizing the novel microorganism, Streptomyces hygroscopicus (Merck Culture Collection MA 6832) ATCC No. 55166. The macrolide antagonist is useful in preventing and/or counteracting accidental or inadvertent FK-506 overdosage in an FK-506 therapeutic program designed to prevent autoimmune diseases or human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.

C-21 hydroxylated FK-506 antagonist

A dipeptide isostere is the biotransformed product after incubation with a culture of Streptomyces. It inhibits HIV protease, and is useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as a compound, pharmaceutically acceptable salt, pharmaceutical composition ingredient, whether or not as a prodrug or as a 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.

Synthesis of protease inhibitor

A novel dipeptide isostere is the biotransformed product after incubation with a culture of Streptomyces. It inhibits HIV protease, and is useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as a compound, pharmaceutically acceptable salt, pharmaceutical composition ingredient, whether or not as a prodrug or as a 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.

Method of hydroxylation with ATCC 55086

A process for the lactonization of mevinic acid HMG-CoA reductase inhibitors and analogs thereof is disclosed.

Process for the lactonization of mevinic acids and analogs thereof

Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents are represented by the following structural formulae (I) and (II): ##STR1## are disclosed.

Antihypercholesterolemic agents

Non-ionic, lipophilic substances are isolated from aqueous or aqueous-organic solution by treatment with a macroreticular polymeric absorbent followed by elution with additional or a different organic solvent.

Isolation of non-ionic lipophilic materials on macroreticular polymeric

Fermentation broths or impure solutions containing thienamycin, a substance having antibiotic activity against gram-negative and gram-positive microorganisms, are purified using a sequence of ion exchange resins, starting with an anion exchange resin of the polystyrene-trimethylammonium type in the HCO.sub.3 -cycle, and ending with absorption on and elution from a polymeric cross-linked polystyrene-type resin adsorbent. Variations in the intermediate steps, e.g. different resins and eluates are possible and are illustrated within.

Growing community of inventors

Gillette, NJ, United States of America

Laszlo R Treiber