Effective delivery of cross-species a3 adenosine-receptor...

A - Human Necessities – 61 – K

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A61K 31/52 (2006.01) A61P 27/06 (2006.01)

Patent

CA 2665616

Provided are methods for reducing intraocular pressure in an individual having an ocular disorder causing elevated intraocular pressure, such as glaucoma. The method comprises administering to the individual an effective intraocular pressure-reducing amount of a pharmaceutical composition comprising an A3 subtype adenosine receptor (A3AR) antagonist, including dihydropyridine, pyridine, pyridinium salt or triazoloquinazoline, and derivatives thereof expressly having A3AR antagonist activity, including, e.g., the nucleoside- based A3AR antagonist, MRS-3820. Further provided is a method for ensuring the delivery of a topically administered therapeutic composition for reducing intraocular pressure, wherein the method expressly requires physically opening a channel through the corneal barrier of the patient's eye by a microneedle or micropipette to permit transport of the topical composition to the anterior chamber of the eye.

L'invention concerne des procédés pour réduire une pression intraoculaire chez un individu souffrant d'un trouble oculaire provoquant une pression intraoculaire élevée, comme un glaucome. Le procédé comporte l'administration au patient d'une quantité de réduction de pression intraoculaire efficace d'une composition pharmaceutique comprenant un antagoniste du récepteur d'adénosine du sous-type A3 (A3AR) comme la dihydropyridine, la pyridine, un sel de pyridium ou de la triazoloquinazoline et leurs dérivés ayant expressément une activité antagoniste A3AR, y compris, par exemple, l'antagoniste A3AR basé sur un nucléoside, MRS-3820. En outre, un procédé est fourni pour garantir la délivrance d'une composition thérapeutique administrée de manière topique pour réduire la pression intraoculaire. Ledit procédé nécessite expressément l'ouverture physique d'un canal à travers la barrière cornéenne de l'AEil du patient avec une micro-aiguille ou une micropipette afin de permettre le transport de la composition topique vers la chambre intérieure de l'AEil.

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