Methods and compositions for treating retina-associated disease using CCR3-inhibitors
AssigneeAlkahest, Inc.
InventorsLaura Corradini, Sam Jackson, Karoly Nikolich
Life of this patent
Estimating the term…
Abstract
Methods of improving visual endpoints related to retina-associated disease with CCR3 modulating agents are provided. An example of such an endpoint is visual acuity. Retina-associated diseases upon which visual acuity and other visual endpoints may be improved include retinopathy of prematurity, age-related macular degeneration, central retinal vein occlusion, and diabetic retinopathy.
Claims37
A method of improving visual acuity in a subject diagnosed with a retina-associated disease, the method comprising orally administering to the subject a therapeutically effective amount of a compound which is a co-crystal of Formula 2:
- wherein:
- R1 is C1-6-alkyl, C1-6-haloalkyl, O—C1-6-haloalkyl, halogen;
- m is 1, 2 or 3;
- R2a and R2b are each independently selected from H, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-6-cycloalkyl, COO—C1-6-alkyl, O—C1-6-alkyl, CONR2b.1R2b.2, or halogen;
- R2b.1 is H, C1-6-alkyl, C0-4-alkyl-C3-6-cycloalkyl, or C1-6-haloalkyl;
- R2b.2 is H, or C1-6-alkyl;
- or R2b.1 and R2b.2 are together a C3-6-alkylene group forming with the nitrogen atom a heterocyclic ring, wherein optionally one carbon atom of the ring is replaced by an oxygen atom
- R3 is H, or C1-6-alkyl;
- X is an anion selected from the group consisting of chloride, bromide, iodide, sulphate, phosphate, methanesulphonate, nitrate, maleate, acetate, benzoate, citrate, salicylate, fumarate, tartrate, dibenzoyltartrate, oxalate, succinate, benzoate and p-toluenesulphonate;
- j is 0, 0.5, 1, 1.5 or 2;
- with a co-crystal former selected from the group consisting of orotic acid, hippuric acid, L-pyroglutamic acid, D-pyroglutamic acid, nicotinic acid, L-(+)-ascorbic acid, saccharin, piperazine, 3-hydroxy-2-naphtoic acid, mucic (galactaric) acid, pamoic (embonic) acid, stearic acid, cholic acid, deoxycholic acid, nicotinamide, isonicotinamide, succinamide, uracil, L-lysine, L-proline, D-valine, L-arginine, glycine.
Dependencies are inferred from the claim text.