Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Scynexis, Inc.

Seynix, Inc.

Seynexis, Inc.

Mark L Greenlee

Frank P DiNinno

Thomas N Salzmann

Thomas A Rano

Dongfang Meng

Kenneth J Wildonger

Lovji D Cama

James V Heck

Donald M Sperbeck

James M Balkovec

Robert R Wilkening

Dann LeRoy Parker, Jr

Ahmed Mamai

Amjad Ali

James M Apgar

Wendy Lee

Gayle E Taylor

Donald W Graham

Robert S Meissner

Milton L Hammond

Wanying Sun

James Francis Dropinski

Frances A Bouffard

Brian H Heasley

Bruno Tse

Weiming Fan

Michael Robert Peel

Steven H Olson

Carol A McVean

Gregory Pacofsky

Hao Liu

Gregory P Rouen

Keqaing Li

Kingsley Nelson

Frances Aileen Bouffard

James Apgar

Kenneth James Wildonger

Carol A Mcvean

Novel derivatives of enfumafungin are disclosed herein, along with' their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and method of using such compounds as antifungal agents and/or inhibitors of (1,3)-&#x3b2;-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.

Antifungal agents

Novel derivatives of enfumafungin are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-&#x3b2;-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.

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, metastatic bone disease, Paget's disease, periodontal disease, 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, inflammation, inflammatory bowel disease, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.

Estrogen receptor modulators

The present invention relates to novel enfumafungin derivatives of formula I and pharmaceutically acceptable salts thereof, their synthesis, and their use as inhibitors of (1,3)-&#x3b2;-D-glucan synthase. The present compounds and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising the present compounds and pharmaceutically acceptable salts thereof, are useful for treating or preventing antifungal infections and associated diseases and conditions.

The present invention is directed to D-homoandrosta-17-yl-carbamate derivatives as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.

D-homoandrosta-17-yl carbamate derivatives as selective glucocorticoid receptor ligands

The present invention encompasses compounds of Formula (I) or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included. 

17-carbamoyloxy cortisol derivatives as selective glucocorticoid receptor modulators

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, metastatic bone disease, Paget's disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, age-related mild cognitive impairment, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, irritable bowel syndrome, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.

Substituted succinic acid metallo-&bgr;-lactamase inhibitors and their use in treating bacterial infections

A carbapenem antibiotic of the formula I ##STR1## is disclosed. The variable X.sup..crclbar. represents a counterion. Pharmaceutical compositions and methods of use are also disclosed.

1-.beta.-methyl-carbapenem, compositions containing same and methods of

New antibacterial 6-amido-1-methyl-2-(substituted-thio)-carbapenems and process for their synthesis involving new azetidinone intermediates.

6-amido-1-methyl-2-(substituted-thio)carbapenems

Disclosed are carbapenems of the formula ##STR1## which are 2-(9-fluorenonyl)-carbapenems useful as antibacterial agents. Intermediates for preparation of these compounds is also disclosed.

2-(9-fluorenonyl)-carbapenem intermediates

The present invention relates to antibacterial agents of the carbapenem class, in which the 2-position sidechain is characterized by a phenanthridine moiety typically having a substituent attached to the nitrogen of the phenanthridine and substituted at other positions by various neutral substituents. When there is substitution on the nitrogen of the phenathridine moiety that nitrogen is a charged quaternary nitrogen.

2-phenanthridinyl carbaphenem antibacterial agent

The present invention relates to antibacterial agents of the carbapenem class, in which the 2-position sidechain is characterized by a phenanthridine moiety, substituted by various neutral substituents.

2-phenanthridinyl carbapenem antibacterial agents

Carbapenems having the formula: ##STR1## where X is O or S(O).sub.0-2 ; are useful antibacterial agents, especially with respect to activity against methicillin resistant Staphylococcus aureus (MRSA).

2-(substituted-dibenzofuranyl and dibenzothienyl) carbapenem

Growing community of inventors

Rahway, NJ, United States of America

Mark L Greenlee