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US 10,485,876 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.
Claims34
A compound of Formula III′:
- or a pharmaceutically acceptable salt thereof;
- wherein:
- R42 is selected from
- (i) —N═CH—C3-C30alkenylR5, —N═CH—C3-C30alkynylR5, —N═CH—C3-C30alkenylalkynylR5, —N═C1-C30alkylR5, —N═CH—C3-C30alkenyl, —N═CH—C3-C30alkynyl, —N═CH—C3-C30alkenylalkynyl, —N═C1-C30alkyl, —NHC3-C30alkenylR5, —NH—C3-C30alkynylR5, —NH—C5-C30alkenylalkynylR5, —NHC3-C30alkenylR16, —NH—C3-C30alkynylR16, and —NH—C5—C30alkenylalkynylR16,
- (ii) an amine linked polypropylene glycol, an amine or amide linked polypropylene oxide, an amine or amide linked polylactic acid, an amine or amide linked poly(lactic-co-glycolic acid),
- an amine or amide linked polyglycolic acid, a polyester, and a polyamide;
- R15 is R17;
- R16 is selected from:
- (i) —C(O)C3-C30alkylR5, —C(O)C3-C30alkenylR5, —C(O)C3-C30alkynylR5, —C(O)C3-C30alkenylalkynylR5, —C(O)C3-C30alkyl, —C(O)C3-C30alkenyl, —C(O)C3-C30alkynyl, and —C(O)C3-C30alkenylalkynyl;
- (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, euric acid, nervonic acid and mead acid;
- and
- (iii) polypropylene glycol, polypropylene oxide, polylactic acid, poly(lactic-co-glycolic acid),
- and polyglycolic acid;
- R17 is H or —C(O)A;
- A is selected from H, alkyl, cycloalkyl, cycloalkylalkyl, heterocycle, heterocycloalkyl, aryl, arylalkyl, heteroaryl, and heteroarylalkyl;
- R5 is selected from halogen, hydroxyl, cyano, mercapto, amino, 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, and —CONH2;
- and
- x and y are selected from an integer selected from 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29 and 30.
15 more elements
Dependencies are inferred from the claim text.