Optimer Pharmaceuticals, Inc.

Merck Sharp + Dohme Corp.

Yu-Hung Chiu

Youe-Kong Shue

Alex Romero

Yoshi Ichikawa

Farah Kondori Babakhani

Tessie Mary Che

Chan-Kou Hwang

David Rabuka

Franklin W Okumu

Kenneth Marby

Sulan Yao

Pamela Sears

Steve Sucheck

Chang-Hsing Liang

Yoshitaka Ichikawa

Jonathan James Duffield

Jonathan Duffield

Yoshiaki Ichikawa

Described herein are novel macrolides, the preparation of novel macrolides, the use of novel macrolides for preventing, treating, or ameliorating various conditions, and the use of novel macrolides as antibacterial agents.

Antibacterial agents

The invention encompasses an active metabolite of the 18-membered macrocyclic antimicrobial agents, specifically, a metabolite of tiacumicin B and in certain embodiments, R-Tiacumicin B or and its related compounds. In particular, the invention encompasses a compound that acts as a potent antibiotic agent for the treatment of bacterial infections, specifically GI infections caused by toxin producing strains of() and().

Antibiotic macrocycle compounds and methods of manufacture and use thereof

The invention relates to novel forms of compounds displaying broad spectrum antibiotic activity, especially crystalline polymorphic forms and amorphous forms of such compounds, compositions comprising such crystalline polymorphic forms and amorphous forms of such compounds, processes for manufacture and use thereof. The compounds and compositions of the invention are useful in the pharmaceutical industry, for example, in the treatment or prevention of diseases or disorders associated with the use of antibiotics, chemotherapies, or antiviral therapies, including, but not limited to, colitis, for example, pseudo-membranous colitis; antibiotic associated diarrhea; and infections due to(''),(''),species, for example, methicillin-resistant, orincluding Vancomycin-resistant enterococci.

Macrolide polymorphs, compositions comprising such polymorphs, and methods of use and manufacture thereof

The invention relates to novel forms of compounds displaying broad spectrum antibiotic activity, especially crystalline polymorphic forms and amorphous forms of such compounds, compositions comprising such crystalline polymorphic forms and amorphous forms of such compounds, processes for manufacture and use thereof. The compounds and compositions of the invention are useful in the pharmaceutical industry, for example, in the treatment or prevention of diseases or disorders associated with the use of antibiotics, chemotherapies, or antiviral therapies, including, but not limited to, colitis, for example, pseudo-membranous colitis; antibiotic associated diarrhea; and infections due to(''),(''),species, for example, methicillin-resistant, orincluding Vancomycin-resistant

Macrocyclic polymorphs, compositions comprising such polymorphs, and methods of use and manufacture thereof

The present invention relates generally to the 18-membered macrocyclic antimicrobial agents called Tiacumicins, specifically, OPT-80 (which is composed almost entirely of the R-Tiacumicin B), pharmaceutical compositions comprising OPT-80, and methods using OPT-80. In particular, this compound is a potent drug for the treatment of bacterial infections, specificallyinfections.

18-membered macrocycles and analogs thereof

Macrocyclic polymorphs, compositions comprising such polymorphs and methods of use and manufacture thereof

Described herein are novel macrolides, the preparation of novel macrolides, to the use of novel macrolides for preventing, treating, or ameliorating various conditions, and the use of novel macrolides as antibacterial agents.

Polymorphic crystalline forms of tiacumicin B

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San Diego, CA, United States of America

Yu-Hung Chiu