# US 12,594,262 B2 · CAI nanoemulsions

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- Number: US 12,594,262 B2
- Document ID: US12594262B2
- Status: Granted
- Kind: B2
- Application number: 17/785,842
- Filed: 2020-12-18
- Published: 2023-01-26
- Granted: 2026-04-07
- Earliest claimed: 2019-12-18
- Assignees: ForwardVue Pharma, Inc.
- Applicants: ForwardVue Pharma, Inc.
- Inventors: Alan J. Franklin; Laurent Balenci; Srikanth Kakamanu; Robert Dempsey
- Web page: https://patentgrep.com/patent/US12594262B2

## CPC

- A61K 9/1075: {Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers (A61K9/0026 takes precedence)}
- A61K 31/4192: 1,2,3-Triazoles
- 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 9/14: Particulate form, e.g. powders, {Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles (microspheres A61K9/16; microcapsules A61K9/50; nanocapsules, nanoparticles of the matrix type A61K9/51)}
- A61K 31/765: Polymers containing oxygen
- A61K 47/34: Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence)
- A61K 47/593: {Polyesters, e.g. PLGA or polylactide-co-glycolide}
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

The present disclosure relates to nanoemulsions of 5-amino-[4-(4-chlorobenzoyl)-3,5-dichlorobenzyl]-1,2,3-triazole-4-carboxamide (carboxy-amido-triazole or CAI), methods of preparing thereof, and their use in the treatment of inflammatory optic neuropathies.

## Claims

### Claim 1

A nanoemulsion formulation comprising 5-amino-[4-(4-chlorobenzoyl)-3,5-dichlorobenzyl]-1,2,3-triazole-4-carboxamide (CAI) and poly(D,L-lactic-co-glycolic acid) (PLGA), wherein the average particle size is less than 300 nm, and an ocular therapeutic substance selected from the group consisting of: a VEGF binding molecule and a tyrosine receptor kinase inhibitor.

### Claim 2 (depends on 1)

The nanoemulsion formulation according to claim 1, wherein the average particle size is less than 220 nm.

### Claim 3 (depends on 1)

The nanoemulsion formulation according to claim 1, wherein the average particle size is less than 150 nm.

### Claim 4 (depends on 1)

The nanoemulsion formulation according to claim 1, wherein the average particle size is 50 to 250 nm.

### Claim 5 (depends on 1)

The nanoemulsion formulation according to claim 1 further comprising 1% polyethylene glycol sorbitan monolaurate.

### Claim 6 (depends on 1)

The nanoemulsion formulation according to claim 1, wherein said VEGF binding molecule is selected from the group consisting of ranibizumab (Lucentis) and pegatanib (Macugen).

### Claim 7 (depends on 1)

The nanoemulsion formulation according to claim 1, wherein said PLGA is from 7 kDa to 17 kDa and/or 66 kDa to 106 kD.

### Claim 8 (depends on 1)

The nanoemulsion formulation according to claim 1, wherein said PLGA is from 7 kDa to 17 kDa.

### Claim 9 (depends on 1)

The nanoemulsion formulation according to claim 1, wherein said PLGA is from 66 kDa to 106 kD.

### Claim 10 (depends on 1)

A method of treating a patient suffering from inflammatory optic neuropathies comprising: local ocularly administering to said patient a therapeutically effective amount of the nanoemulsion formulation according to claim 1.

### Claim 11 (depends on 10)

The method according to claim 10, further comprising diagnosing inflammatory optic neuropathies in said patient.

### Claim 12 (depends on 10)

The method according to claim 10, wherein said local ocular administration is by topical administration or ocular injection.

### Claim 13 (depends on 12)

The method according to claim 12, wherein said ocular injection is any one or combination of routes selected from the group consisting of periocular injection, sub-Tenon's injection, juxtascleral injection, intravitreal injection, subconjunctival injection, subretinal injection, and retrobulbar injection.

### Claim 14 (depends on 13)

The method according to claim 13, wherein said local ocular administration is assisted by sonophoresis or iontophoresis.

### Claim 15 (depends on 10)

The method according to claim 10, wherein the therapeutically effective amount of CAI is from 0.1 mg/mL to 100 mg/mL.

### Claim 16 (depends on 1)

A method of preparing the nanoemulsion formulation according to claim 1, comprising: (i) dissolving PLGA and CAI in acetonitrile; (ii) adding the acetonitrile solution from step (i) gradually over a first predetermined time to an aqueous buffered salt solution (BSS) containing 1% polyethylene glycol sorbitan monolaurate while said BSS is agitated via high-speed vortexing; (iii) after step (ii) is complete, further agitating the resulting mixture via high-speed vortexing for a second pre-determined time; and (iv) removing the acetonitrile via evaporation to produce a nanoemulsion.