Ophthamological drugs
AssigneeDuke University
InventorsEric Toone, David Epstein, Pratap Challa, Phillip Snyder, Xin Chen, Mitchell deLong
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Abstract
The present invention relates generally to ophthamological drugs. More specifically, the inventon relates to a method of modifying (derivatizing) ophthamological drugs so as to increase their penetration through the cornea. The invention also relates to drugs modified (derivatized) in accordance with the instant method and to the use of same in treating conditions associated with elevated intraocular pressure, particularly, glaucoma.
Claims48
A composition comprising:
- a compound derived from the esterification of a carboxylate functionality of a drug moiety with a sugar alcohol, the drug moiety comprising at least one of a phenoxyacetic acid, a cinnamic acid, and a mixture thereof.
A composition comprising:
- a compound derived from the esterification of a carboxylate functionality of a drug moiety thereof, with the proviso that the drug moiety is not a prostaglandin.
A compound selected from the group consisting of:
- 5-O-Ribitol[2,3-dichloro-4-(thiophene-2-carbonyl)]phenoxyacetate;
- 5-O-Xylitol 4-(2-phenylacryloyl)cinnamate;
- 5-O-{(9α,11α,15R)-15-[2-Benzo[b]thiophen-2-yl]-16,17,18,19,20-pentanor-5,6,13,14-tetrahydro-9,11,15-trihydroxyprostanoyl}xylitol;
- 11-Hydroxy-3,6,9-trioxaundecyl 4-(2-phenylacryloyl)cinnamate;
- 5-O-{(9α,11α,15R)-15-[2-Benzo[b]thiophen-2-yl]-16,17,18,19,20-pentanor-5,6,13,14-tetrahydro-9,11,15-trihydroxyprostanoyl}xylitol;
- 5-O-{(9α,11α,15R)-15-[2-Benzo[b]thiophen-2-yl]-16,17,18,19,20-pentanor-5,6,13,14-tetrahydro-9,11,15-trihydroxyprostanoyl}-D-ribitol;
- 4-O-{(9α,11α,15R)-15-[2-benzo[b]thiophen-2-yl]-16,17,18,19,20-pentanor-5,6,13,14-tetrahydro-9,11,15-trihydroxyprostanoyl}-L-threitol;
- 5-O-Xylitol 4-(2-phenylacryloyl)cinnamate;
- 1-O-D-Sorbitol 4-(2-phenylacryloyl)cinnamate;
- 1-O-D-Arabitol 4-(2-phenylacryloyl)cinnamate;
- 1-O-Glycerol[2,3-dichloro-4-(2-methylenebutyryl)]phenoxyacetate;
- 1-O-Erythritol[2,3-dichloro-4-(2-methylenebutyryl)]phenoxyacetate;
- 1-O-Ribitol[2,3-dichloro-4-(2-methylenebutyryl)]phenoxyacetate;
- 5-O-Ribitol[2,3-dichloro-4-(thiophene-2-carbonyl)]phenoxyacetate;
- 2-O-D-Sorbitol 4-(2-phenylacryloyl)cinnamate;
- and
- 2-O-Ribitol[2,3-dichloro-4-(2-methylenebutyryl)]phenoxyacetate.
A method of treating an ophthamological disorder, said method comprising administering to a human or other animal a safe and effective amount of a compound derived from the esterification of a carboxylate functionality of a drug moiety with a sugar alcohol, the drug moiety comprising at least one of a phenoxyacetic acid, a cinnamic acid, and a mixture thereof.
A method of determining the suitability of a compound for treating an ophthamological disorder, said method comprising
- providing a compound derived from the esterification of a carboxylate functionality of a drug moiety with a sugar alcohol;
- determining whether the compound releases its carboxcylic acid, in an assay under conditions mimicking conditions in an eye, within a predetermined half life;
- and
- selecting the compound for treatment of an ophthamological disorder if the compound releases its carboxcylic acid within the predetermined half life.
A compound derived from the esterification of a carboxylate functionality of a drug moiety with a sugar alcohol, the drug moiety being at least one of travaprost, latanoprost, and bimatoprost and mixtures thereof.
Dependencies are inferred from the claim text.