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US 9,808,531 B2Granted
Compounds and compositions for the treatment of ocular disorders
AssigneeGraybug Vision, Inc.
InventorsJeffrey L. Cleland, Ming Yang, John G. Bauman, Nu Hoang, Emmett Cunningham
Life of this patent
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Abstract
The disclosure describes prodrugs and derivatives of prostaglandins, carbonic anhydrase inhibitors, kinase inhibitors, beta-adrenergic receptor antagonists and other drugs, as well as controlled delivery formulations containing such prodrugs and derivatives, for the treatment of ocular disorders.
Claims27
A compound of Formula:
- or a pharmaceutically acceptable salt thereof;
- wherein:
- L1 is selected from:
- L2 is selected from:
- A is selected from:
- H, alkyl, cycloalkyl, cycloalkylalkyl, heterocycle, heterocycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, aryloxy, and alkyloxy;
- R1, R2, and R3 are selected from:
- —C(O)R4, C(O)A, and hydrogen wherein either R1 or R2 cannot be hydrogen and wherein R1, R2, and R3 can be further optionally substituted with R5;
- R4 is selected from:
- (i) —C10-C30alkylR5, —C10-C30alkenylR5, —C10-C30alkynylR5, —C10-C30alkenylalkynylR5, —C10-C30alkyl, —C10-C30alkenyl, —C10-C30alkynyl, and —C10-C30alkenylalkynyl;
- or
- (ii) an unsaturated fatty acid residue selected from linoleic acid, docosahexaenoic acid, eicosapentaenoic acid, alpha-linolenic acid, stearidonic acid, y-linolenic acid, arachidonic acid, docosatetraenoic acid, palmitoleic acid, vaccenic acid, paullinic acid, oleic acid, elaidic acid, gondoic acid, nervonic acid and mead acid;
- and
- R5 is selected from:
- halogen, hydroxyl, cyano, mercapto, amino, aryl, alkyl, alkoxy, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, aryloxy, —S(O)2alkyl, —S(O)alkyl, —P(O)(Oalkyl)2, B(OH)2, —Si(CH3)3, —COOH, —COOalkyl, —CONH2.
12 more elements
A compound of formula
- or a pharmaceutically acceptable salt thereof.
A compound of formula
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.