# US 11,110,184 B2 · Methods for treating and diagnosing blinding eye diseases

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- Number: US 11,110,184 B2
- Document ID: US11110184B2
- Status: Granted
- Kind: B2
- Application number: 16/695,918
- Filed: 2019-11-26
- Published: 2020-03-26
- Granted: 2021-09-07
- Earliest claimed: 2012-05-01
- Assignees: Translatum Medicus Inc.
- Applicants: Translatum Medicus Inc.
- Inventors: Shelley Romayne Boyd
- Web page: https://patentgrep.com/patent/US11110184B2

## CPC

- A61K 49/0034: {Indocyanine green, i.e. ICG, cardiogreen}
- A61B 3/102: {for optical coherence tomography [OCT]}
- A61B 3/1025: {for confocal scanning}
- A61B 3/1233: {for measuring blood flow, e.g. at the retina}
- A61B 3/1241: {specially adapted for observation of ocular blood flow, e.g. by fluorescein angiography}
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 31/415: 1,2-Diazoles
- A61K 31/416: condensed with carbocyclic ring systems, e.g. indazole
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 49/0008: {Screening agents using (non-human) animal models or transgenic animal models or chimeric hosts, e.g. Alzheimer disease animal model, transgenic model for heart failure}
- A61B 2503/40: Animals
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61B: DIAGNOSIS; SURGERY; IDENTIFICATION (usefulness limited to only animals A61D)

## Abstract

This invention relates to, in part, methods and compositions that are useful for the diagnosis, treatment, or prevention of a blinding eye disease, including in the discovery of drugs that are efficacious against these diseases. Diseases include, for example, age related macular degeneration and reticular pseudodrusen disease, and the methods described herein include, for example, the method named delayed near infrared analysis (DNIRA).

## Claims

### Claim 1

A method for modulating polarization of macrophages associated with a retinal pigment epithelium (RPE) cell layer in the eye of a subject in need thereof, comprising administering to said subject an effective amount of a compound of Formula I:
or a pharmaceutically acceptable salt thereof, wherein:
each of R1 and R2 is independently H or a C1-C6 alkyl and
R3 is H or a C1-C6 alkyl;
wherein the macrophage polarization is M1 and M2 or between M1 and M2, and the macrophages are Iba1+.

### Claim 2 (depends on 1)

The method of claim 1, wherein the compound of Formula I is bindarit.

### Claim 3 (depends on 1)

The method of claim 1, wherein the compound is formulated for sustained release.

### Claim 4 (depends on 1)

The method of claim 1, wherein the compound is formulated for ophthalmic administration.

### Claim 5 (depends on 1)

The method of claim 1, wherein the ophthalmic administration is intravitreal administration, intraocular administration, or effected to the ocular surface.

### Claim 6 (depends on 1)

The method of claim 1, wherein the subject is a human.

### Claim 7 (depends on 6)

The method of claim 6, wherein the human subject is afflicted with a blinding eye disease.

### Claim 8 (depends on 7)

The method of claim 7, wherein the blinding eye disease is characterized by an influx of macrophages across the subject's RPE cell layer relative to a subject not afflicted with the blinding eye disease.

### Claim 9 (depends on 1)

The method of claim 1, wherein the M1 macrophage polarization results in a macrophage-mediated inflammatory response.

### Claim 10 (depends on 9)

The method of claim 9, wherein the macrophage-mediated inflammatory response is decreased.

### Claim 11 (depends on 1)

The method of claim 1, wherein the RPE cell layer comprises a monolayer structure.

### Claim 12 (depends on 11)

The method of claim 11, wherein the RPE cell layer monolayer structure is preserved.

### Claim 13 (depends on 1)

The method of claim 1, wherein the method further comprises administering an additional therapeutic agent.

### Claim 14 (depends on 13)

The method of claim 13, wherein the additional therapeutic agent is one or more of an anti-vascular endothelial growth factor (VEGF) agent, an angiotensin-converting enzyme (ACE) inhibitor, a peroxisome proliferator-activated receptor (PPAR)-gamma agonist, a renin inhibitor, a steroid, an agent that modulates autophagy, semapimod, a MIF inhibitor, a CCR2 inhibitor, CKR-2B, a 2-thioimidazole, CAS 445479-97-0, CCX140, clodronate, a clodonate-liposome preparation and gadolinium chloride.