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

US7863249B2 · kind B2 · utility

Assignee

• Optimer Pharmaceuticals, Inc. · US

Inventors

• Yu-Hung Chiu · San Diego, US
• Tessie M. Che · Westfield, US
• Alex Romero · San Diego, US
• Yoshi Ichikawa · San Diego, US
• Youe-Kong Shue · Taipei, TW

Key dates

• Filing date: Apr 11, 2008
• Grant date: Jan 4, 2011
• Expiry date: May 7, 2029

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D407/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

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 Clostridium difficile (“C. difficile”), Clostridium perfringens (“C. perfringens”), Staphylococcus species, for example, methicillin-resistant Staphylococcus, or Enterococcus including Vancomycin-resistant enterococci.