Fluoroquinolone derivatives for ophthalmic applications

Details Fluoroquinolone derivatives for ophthalmic applications Fluoroquinolone derivatives for ophthalmic applications

A - Human Necessities

61

K

A61K 31/4709 (2006.01) A61K 45/06 (2006.01) A61P 27/02 (2006.01) A61P 31/04 (2006.01)

Patent

CA 2714580

The present invention relates to fluoroquinolone derivatives having enhanced ocular penetration characteristics and/or antimicrobial activity, and to compositions comprising such derivatives. The derivatives and compositions are particularly well suited for treating ophthalmic bacterial infections. The present invention more particularly relates to the discovery that a 2-methyl substitution on a diazabicyclo group attached to a fluoroquinolone ring system produces improved permeability characteristics, and that a 5-amino substitution on a fluoroquinolone ring system results in improved anti-microbial activity.

Linvention concerne des dérivés de fluoroquinolone ayant des caractéristiques de pénétration oculaire amplifiées et/ou une activité antimicrobienne amplifiée, et des compositions contenant de tels dérivés. Les dérivés et compositions sont particulièrement bien appropriés pour traiter des infections bactériennes ophtalmiques. La présente invention concerne plus particulièrement la découverte selon laquelle une substitution 2-méthyle sur un groupe diazabicyclo attaché à un système de cycle fluoroquinolone produit des caractéristiques de perméabilité améliorées, et quune substitution 5-amino sur un système de cycle fluoroquinolone conduit à une activité antimicrobienne améliorée.

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