Macrocyclic polymorphs, compositions comprising such...

C - Chemistry – Metallurgy – 07 – H

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C07H 17/08 (2006.01) A61K 31/7048 (2006.01) A61P 31/04 (2006.01)

Patent

CA 2676061

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.

L'invention concerne de nouvelles formes de composés présentant une activité antibiotique à large spectre, en particulier des formes polymorphes cristallines et des formes amorphes de tels composés, des compositions comprenant de telles formes polymorphes cristallines et formes amorphes de tels composés et des procédés pour la fabrication et l'utilisation de celles-ci. Les composés et compositions de l'invention sont utiles dans l'industrie pharmaceutique, par exemple dans le traitement ou la prévention de maladies ou troubles associés à l'utilisation d'antibiotiques, de chimiothérapies ou de thérapies antivirales, dont, mais ils ne sont pas limités à ceux-ci, la colite, par exemple la colite pseudo-membraneuse ; la diarrhée associée à des antibiotiques ; et des infections dues à Clostridium difficile (C. difficile), à Clostridium perfringens (C. perfringens), à l'espèce des staphylocoques, par exemple au staphylocoque résistant à la méthicilline, ou aux entérocoques dont les entérocoques résistants à la vancomycine.

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