Retinal derivatives and methods for the use thereof for the treatment of visual disorders
AssigneeUniversity of Washington
InventorsKrzysztof Palczewski, Matthew Batten
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Abstract
Compositions of and methods for using synthetic retinal derivatives as retinoid replacements and opsin agonists are provided.
Claims25
A method for treatment of an endogenous 11-cis-retinal deficiency in an eye of a human subject, the method comprising:
- administering to the human subject in need thereof a therapeutically effective amount of a synthetic retinyl ester that is a 9-cis-retinyl ester or an 11-cis-retinyl ester, wherein the 9-cis-retinyl ester has a structure as represented by Formula I or the 11-cis-retinyl ester has a structure as represented by Formula II, wherein A in each formula is CH2OR and R forms a retinyl ester, and the ester substituent of said retinyl ester comprises a carboxylate radical of a C1 to C10 monocarboxylic acid or a C2 to C22 polycarboxylic acid:
- wherein the ester substituent is selected from the group consisting of formate, acetate, propionate, butyrate, valerate, caproate, heptanoate, caprylate, pelargonate, caprate, oxalate, malonate, succinate, fumarate, malate, glutarate, adipate, pimelate, suberate, azelate, sebacate, citrate, oxaloacetate, and ketoglutarate.
A method for the treatment of Leber Congenital Amaurosis or Retinitis Pigmentosa in a human subject due to an endogenous 11-cis-retinal deficiency in an eye of a human subject due to an inherited mutation in RPE65 or LRAT, the method comprising administering to the human subject a synthetic retinyl ester that is a 9-cis-etinyl ester or an 11-cis-retinyl ester, wherein the 9-cis-retinyl ester has a structure as represented by Formula I or the 11-cis-retinyl ester has a structure as represented by Formula II, wherein A in each formula is CH2OR and R forms a retinyl ester, and the ester substituent of said retinyl ester comprises a carboxylate radical of a C1 to C10 monocarboxylic acid or a C2 to C22 polycarboxylic acid:
- wherein the ester substituent is selected from the group consisting of formate, acetate, propionate, butyrate, valerate, caproate, heptanoate, caprylate, pelargonate, caprate, oxalate, malonate, succinate, fumarate, malate, glutarate, adipate, pimelate, suberate, azelate, sebacate, citrate, oxaloacetate, and ketoglutarate.
Dependencies are inferred from the claim text.