Merck + Co., Inc.

Other

Methylgene, Inc.

Milton L Hammond

Robert A Zambias

James M Balkovec

Dennis D Keith

Sherman Tim Waddell

Michael N Chang

John F Finn

Milana M Maletic

Michael Morytko

Gina M Santorelli

Aaron H Leeman

Lovji D Cama

Norman P Jensen

Mary F Sasor

Frank P DiNinno

Siya Ram

Robert E Schwartz

John McDonald

Jason J Hill

Kathleen M Rupprecht

Charles G Caldwell

Ihor E Kopka

Kevin D Dykstra

Mark L Greenlee

Arkadii Vaisburg

James V Heck

Helen Y Chen

David J Mathre

Frances A Bouffard

Timothy A Blizzard

Stephane Raeppel

Michael Mannion

Jubrail Rahil

Katherine Young

Frederic Gaudette

Kathryn L Thompson

Jeffrey Donald Hermes

Jerry Dwain Morgan, Ii

Qiang Tan

Stanley H Wright

Ralph Troy Mosley

Seongkon Kim

Nancy Z Zhou

Nafsika Georgopapadakou

Frank Dininno

Kevin Dykstra

Jubrail Rahl

This invention provides novel &#x3b2;-lactamase inhibitors of the aryl- and heteroaryl-sulfonamidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammomium groups. The compounds inhibit three classes of &#x3b2;-lactamases and synergize the antibacterial effects of &#x3b2;-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the &#x3b2;-lactam antibiotics as a result of the presence of the &#x3b2;-lactamases.

Inhibitors of beta-lactamase

The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

Estrogen receptor modulators

Prolines as antimicrobial agents

Catechols as antimicrobial agents

Transfer ribonucleic acid (tRNA) synthetase inhibitors, salts, and pharmaceutically acceptable compositions thereof of the general formula:

Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment

Certain propanolamine compounds are described which have a cyclohexapeptidyl nucleus and which possess antibiotic activity with physical properties suitable for direct use in therapeutic compositions. A process for their preparation is also described.

Cyclohexapeptidyl propanolamine compounds

Certain propanolamine compounds which have a cyclohexapeptidyl nucleus and which are found to have extremely active antibiotic activity with physical properties suitable for direct use in therapeutic compositions are described. A novel process for their preparation is also described.

Compounds represented by the formula (Seq ID Nos. 1-6) ##STR1## wherein all substituents are fully defined, are disclosed. These compounds exhibit utilities as antibiotic and antifungal agents and for the treatment and prevention of Pneumocystis infections.

Aza cyclohexapeptide compounds

1-Carba-1-dethiacephalosporin compounds of the formula I ##STR1## are disclosed. The compounds are useful against MRSA/MRCNS. Compositions and methods of use are also included.

3-thioheteroaryl 1-carba-1-dethiacephalosporin compounds, compositions

Cephalosporin compounds of the formula I ##STR1## are disclosed. The compounds are useful against MRSA/MRCNS. Compositions and methods of use are also included.

3-thioheteroaryl cephalosporin compounds, compositions and methods of use

Growing community of inventors

Somerville, NJ, United States of America

Milton L Hammond