IP Library Granted Patent US 10,639,347
Granted Patent B2
US 10,639,347 · App. 16/420,068 · Granted May 5, 2020

Peptides useable for treatment of disorders of the eye

Inventors: Michael John Mackel (Portland, OR); John Park (Santa Ana, CA)
Assignee: Allegro Pharmaceuticals, LLC
A61K38/12A61K9/08A61K38/07A61K38/1709A61K47/64A61K51/065A61K51/082A61K51/088A61L27/227A61L31/043C07K7/00A61K9/06A61L2300/252
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Quick Facts
Patent No.
US 10,639,347
App. No.
16/420,068
Granted
May 5, 2020
Kind
B2
Abstract

Compounds comprising R-G-Cysteic Acid (i.e., R-G-NH—CH(CH 2 —SO 3 H)COOH or Arg-Gly-NH—CH(CH 2 —SO 3 H)COOH) and derivatives thereof, including pharmaceutically acceptable salts, hydrates, stereoisomers, multimers, cyclic forms, linear forms, drug-conjugates, pro-drugs and their derivatives. Also disclosed are methods for making and using such compounds including methods for inhibiting cellular adhesion to RGD binding sites or delivering other diagnostic or therapeutic agents to RGD binding sites in human or animal subjects.

Claims (18)

1. A method for treating a disorder selected from: retinopathy, diabetic retinopathy, macular hole, vitreomacular traction, age related macular degeneration, wet macular degeneration, retinal neovascularization; retinal neovascularization due to diabetic retinopathy and retinal neovascularization due to retinal vein occlusion, in an eye of a subject who suffers from said disorder, said method comprising administering to the subject an effective amount of a compound which comprises Glycinyl-Arginyl-Glycinyl-Cysteic acid-Threonyl-Proline-COOH (SEQ ID NO: 2) or which has the formula:

X1-R-G-Cysteic Acid-X

where X and X1 are selected from: Phe-Val-Ala, -Phe-Leu-Ala, -Phe-Val-Gly, -Phe-Leu-Gly, -Phe-Pro-Gly, -Phe-Pro-Ala, -Phe-Val; or from Arg, Gly, Cysteic acid, Phe, Val, Ala, Leu, Pro, Thr and salts, and any combinations of any D-isomers and L-isomers thereof.

2. A method according to claim 1 wherein the compound comprises SEQ ID NO: 2 and has the structural formula:

3. A method according to claim 1 wherein the compound comprises Glycinyl-Arginyl-Glycinyl-Cysteic acid-Threonyl-Proline-COOH (SEQ ID NO. 2).

4. A method according to claim 1 wherein the disorder causes vitreomacular traction and wherein the administration of the compound deters said vitreomacular traction.

5. A method according to claim 1 wherein the compound is injected into an eye of the subject.

6. A method according to claim 5 wherein the compound is injected intravitreally.

7. A method according to claim 1 wherein the compound is administered topically to an eye of the subject.

8. A method according to claim 7 wherein the compound is contained in a liquid or gel preparation for topical administration to said eye.

9. A method according to claim 1 wherein the compound is administered by intravitreal injection to induce posterior vitreal detachment and/or vitreolysis in the eye prior to performance of a vitrectomy and wherein the method further comprises the step of performing said vitrectomy after the compound has induced said posterior vitreal detachment and/or vitreolysis in the eye.

10. A method according to claim 1 wherein the disorder causes inflammation and wherein the administration of the compound reduces said inflammation.

11. A method according to claim 1 wherein the disorder causes abnormal cell adhesion and wherein the administration of the compound deters said abnormal cell adhesion.

12. A method according to claim 11 wherein the administration of the compound deters adhesion to a cell adhesion motif selected from: fibronectin, vitronectin, laminin, fibrinogen, thrombospondin, and von Willebrand factor.

13. A method according to claim 1 wherein the disorder causes abnormal cellular apoptosis and wherein the administration of the compound reduces said abnormal cellular apoptosis.

14. A method according to claim 1 wherein the disorder causes a pathological integrin-extracellular matrix interaction and wherein the administration of the compound deters said pathological integrin-extracellular matrix interaction.

15. A method according to claim 1 wherein the disorder causes a pathological interaction between fibroblasts and glycoprotein components of extracellular matrix and wherein the administration of the compound deters said pathological interaction between fibroblasts and glycoprotein components of extracellular matrix.

16. A method according to claim 1 wherein the disorder causes abnormal angiogenesis and wherein the administration of the compound reduces said abnormal angiogenesis.

Continuity (5)
Continuation 15867101 · Jan 10, 2018
Continuation 14696250 · Apr 24, 2015
Continuation 12943900 · Nov 10, 2010
Provisional Application 61259748 · Nov 10, 2009
Related Publication 20190343916A1 · Nov 14, 2019
Cited By (1)
US 12,454,549