Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Methylgene, Inc.

Seongkon Kim

Helen Y Chen

Jane Yang Wu

Jeffrey Donald Hermes

Frank P DiNinno

Milton L Hammond

Arkadii Vaisburg

Timothy A Blizzard

Sookhee Nicole Ha

Stephane Raeppel

Kevin D Dykstra

Michael Mannion

Timothy Allen Blizzard

Jubrail Rahil

Nelo R Rivera

Katherine Young

Frederic Gaudette

Jason Eugene Imbriglio

Ian Mangion

Candido Gude

Michael Shevlin

Qiang Tan

Nafsika Georgopapadakou

Nancy Z Zhou

Rebecca T Ruck

Frank Dininno

Christopher J Mortko

Kevin Dykstra

Jubrail Rahl

Substituted bicyclic beta-lactams of Formula I: (I), are &#x3b2;-lactamase inhibitors, wherein a, X, Rand Rare defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with &#x3b2;-lactam antibiotics. In particular, the compounds can be employed with a &#x3b2;-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to &#x3b2;-lactam antibiotics due to the presence of the &#x3b2;-lactamases.

&#x3b2;-lactamase inhibitors

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

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Holmdel, NJ, United States of America

Seongkon Kim