Methods and compositions for treating ophthalmic conditions with retinyl derivatives
AssigneeAcucela Inc.
InventorsKenneth Widder, Jay Lichter, Nathan L. Mata
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Abstract
Compounds that cause reversible night blindness may be used to treat ophthalmic conditions associated with the overproduction of waste products that accumulate during the course of the visual cycle. We describe methods and compositions using such compounds and their derivatives to treat, for example, the macular degenerations and dystrophies or to alleviate symptoms associated with such ophthalmic conditions. Such compounds and their derivatives may be used as single agent therapy or in combination with other agents or therapies.
Claims12
A method for treating macular degeneration in a mammal comprising administering to the mammal at least once an effective amount of a first compound having the following structure:
- wherein X1 is selected from the group consisting of NR2, O, S, CHR2;
- R1 is (CHR2)x-L1-R3, wherein x is 0, 1, 2, or 3;
- L1 is a single bond or —C(O)—;
- R2 is a moiety selected from the group consisting of H, (C1-C4)alkyl, F, (C1-C4)fluoroalkyl, (C1-C4)alkoxy, —C(O)OH, —C(O)—NH2, —(C1-C4)alkylamine, —C(O)—(C1-C4)alkyl, —C(O)—(C1-C4)fluoroalkyl, —C(O)—(C1-C4)alkylamine, and —C(O)—(C1-C4)alkoxy;
- and R3 is H or a moiety selected from the group consisting of (C2-C7) alkenyl, (C2-C7)alkynyl, aryl, (C3-C7)cycloalkyl, (C5-C7)cycloalkenyl, and a heterocycle, wherein the moiety is optionally substituted with 1-3 substituents independently selected from the group consisting of halogen, OH, O(C1-C4)alkyl, NH(C1-C4)alkyl, O(C1-C4)fluoroalkyl, and N[(C1-C4)alkyl]2;
- or a pharmaceutically acceptable salt or solvate thereof;
- provided that R3 is not H when both x is 0 and L1 is a single bond.
Dependencies are inferred from the claim text.