# US 9,572,821 B2 · Pharmaceutical compositions for preventing and treating eye pathologies

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- Number: US 9,572,821 B2
- Document ID: US9572821B2
- Status: Granted
- Kind: B2
- Application number: 14/163,193
- Filed: 2014-01-24
- Published: 2014-05-22
- Granted: 2017-02-21
- Earliest claimed: 2014-01-24
- Assignees: Mitotech SA
- Applicants: Mitotech SA
- Inventors: Vladimir P. Skulachev; Maxim V. Skulachev
- Web page: https://patentgrep.com/patent/US9572821B2

## CPC

- A61K 31/66: Phosphorus compounds
- A61K 31/122: having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
- A61P 27/02: Ophthalmic agents
- A61P 27/06: Antiglaucoma agents or miotics
- A61P 27/12: for cataracts
- A61P 39/06: Free radical scavengers or antioxidants
- 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

## Abstract

The present invention relates to pharmacology, medicine, ophthalmology, and, in particular, concerns a class of chemical compounds of structure (I) and also their solvates, isomers or prodrugs applicable when incorporated into pharmaceutical compositions also containing pharmaceutically acceptable carrier which can be useful for prophylaxis and treatment of different eye pathologies such as cataract and macular dystrophy.

## Claims

### Claim 1

An ophthalmologic solution comprising:
NaCl; and
a therapeutically effective amount of a compound of Structure (I):
wherein:
A is an effector—antioxidant of structure:
and/or reduced form thereof, wherein:
m=2; and
Y is methyl;
L is a linker group, comprising:
a) a straight or branched hydrocarbon chain which can be optionally substituted by one or more substituents and optionally contains one or more double or triple bonds; or
b) a natural isoprene chain;
n is an integer from 1 to 20; and
B is a targeting group, comprising Sk+Z−, wherein:
Sk is a lipophilic cation; and
Z is a pharmacologically acceptable anion; and
a pharmaceutically acceptable carrier thereof.

### Claim 2 (depends on 1)

The solution of claim 1, wherein the compound of Structure (I) is SkQ1:

### Claim 3 (depends on 1)

The solution of claim 1, wherein NaCl is present at 0.9%.

### Claim 4 (depends on 1)

The solution of claim 1, further comprising sodium phosphate buffer with pH 6.5.

### Claim 5 (depends on 4)

The solution of claim 4, wherein the sodium phosphate buffer is present at 10 mM.

### Claim 6 (depends on 1)

The solution of claim 1, wherein the compound of Structure (I) is SkQ1 which is present at 250 nM.

### Claim 7 (depends on 4)

The solution of claim 4, wherein:
the compound of Structure (I) is SkQ1 which is present at 250 nM;
the sodium phosphate buffer is 10 mM, pH 6.5; and
the NaCl is present at 0.9%.