Amelioration of cataracts, macular degeneration and other...

A - Human Necessities – 61 – K

Patent

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Details

A61K 31/45 (2006.01) A61K 8/49 (2006.01) A61K 31/445 (2006.01) A61P 27/02 (2006.01) A61Q 5/00 (2006.01)

Patent

CA 2546053

Ophthalmically acceptable compositions used in arresting the development of cataract, presbyopia, macular degeneration and other retinopathies, glaucoma, uveitis and various corneal disorders are disclosed. The compositions are also useful as a prophylactic treatment to prevent or delay development of age- related ocular disorders, which include cataracts, presbyopia, glaucoma and macular degeneration. The compositions comprise a pharmaceutically acceptable carrier or diluent and at least one compound having the formula where R1 and R2 are, independently, H or C1 to C3 alkyl ; R3 and R4 are, independently C1 to C3 alkyl; and where R1 and R2, taken together, or R3 and R4, taken together, or both may be cycloalkyl; R5 is H, OH, or C1 to C6 alkyl ; R6 is or C1 to C6 alkyl, alkenyl, alkynyl, or substituted alkyl or alkenyl ; R7 is C1 to C6 alkyl, alkenyl, alkynyl, or substituted alkyl or alkenyl or where R6 and R7, or R5, R6 and R7, taken together, form a carbocycle or heterocycle having from 3 to 7 atoms in the ring.

L'invention concerne des compositions acceptables du point de vue ophtalmique, permettant de stopper le développement de la cataracte, de la presbytie, de la dégénérescence maculaire et autres rétinopathies, du glaucome, de l'uvéite et de divers troubles de la cornée. Les compositions sont utiles pour la prévention ou le ralentissement de troubles oculaires liés au vieillissement, par exemple la cataracte, la presbytie, le glaucome et la dégénérescence maculaire. Elles comprennent un vecteur ou diluant pharmaceutiquement acceptable et au moins un composé de formule ci-après. R¿1? et R¿2? sont, indépendamment, H ou alkyle C¿1? à C¿3?; R¿3? et R¿4? sont, indépendamment alkyle C¿1? à C¿3?; et R¿1? et R¿2?, ensemble, ou R¿3? et R¿4?, ensemble, ou les deux, peuvent être cycloalkyle; R¿5? est H, OH, ou alkyle C¿1? à C¿6?; R¿6? est alkyle C¿1? à C¿6?, alcényle, alkynyle, ou alkyle ou alcényle substitué; R¿7? est alkyle C¿1? à C¿6?, alcényle, alkynyle, ou alkyle ou alcényle substitué ou bien lorsque R¿6? et R¿7?, ou R¿5?, R¿6? et R¿7?, ensemble, forment un carbocycle ou un hétérocycle ayant entre 3 et 7 atomes dans la chaîne.

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