Synthesis and separation of optically active isomers of...

C - Chemistry – Metallurgy – 07 – H

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C07H 17/08 (2006.01)

Patent

CA 2430233

The present invention provides methods for purifying and using optically active isomers of erythromycin as well as compositions comprising such optically active isomers. Such optically active isomers having desired actions as an antibiotic substantially separable from undesirable effects on GI motility and the cardiac potassium channels such that the cardiac action potential is not prolonged and the QT interval on the surface EKG (electrocardiogram) is not increased, such that the erythromycin can be useful for more effective therapy of systemic infections. Also disclosed are methods for assaying the levels of such isomers present in the biological fluids.

L'invention concerne des procédés servant à purifier, identifier et utiliser des isomères optiques d'érythromycine, ainsi que des compositions contenant ces isomères optiques. Ces isomères exercent les effets désirés en tant qu'antibiotiques, pouvant être pratiquement séparés des effets indésirables sur la motilité gastro-intestinale et les canaux potassiques cardiaques, de façon à ne pas prolonger le potentiel d'action cardiaque et à ne pas augmenter l'intervalle QT sur l'électrocardiogramme de surface, ce qui permet d'utiliser l'érythromycine pour une thérapie plus efficace des infections systémiques. L'invention concerne également des procédés servant à contrôler les niveaux de ces isomères présents dans les fluides biologiques.

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