# US 10,188,669 B2 · Mitochondria-targeted antioxidants for treatment of age-related brain disorders

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- Number: US 10,188,669 B2
- Document ID: US10188669B2
- Status: Granted
- Kind: B2
- Application number: 15/058,903
- Filed: 2016-03-02
- Published: 2016-12-08
- Granted: 2019-01-29
- Earliest claimed: 2011-09-22
- Assignees: Mitotech SA
- Applicants: Mitotech S.A.
- Inventors: Maxim Vladimirovich Skulachev; Vladimir Petrovich Skulachev; Maxim Viktorovich Egorov; Nikolai Konstantinovich Isaev; Nadezhda Anatolievna Kapay; Dmitry Borisovich Zorov; Elena Viktorovna Stelmashuk; Fedor Fedorovich Severin
- Web page: https://patentgrep.com/patent/US10188669B2

## CPC

- A61K 31/66: Phosphorus compounds
- A61K 31/444: containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/54: the modifying agent being an organic compound
- A61K 47/545: {Heterocyclic compounds (A61K47/558 takes precedence)}
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- C09B 11/24: Phthaleins containing amino groups {; Phthalanes; Fluoranes; Phthalides; Rhodamine dyes; Phthaleins having heterocyclic aryl rings; Lactone or lactame forms of triarylmethane dyes}
- C09B 69/001: {Dyes containing an onium group attached to the dye skeleton via a bridge}
- 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
- C09B: ORGANIC DYES OR CLOSELY-RELATED COMPOUNDS FOR PRODUCING DYES {, e.g. PIGMENTS}; MORDANTS; LAKES (fermentation or enzyme using processes to synthesise a desired chemical compound C12P)

## Abstract

A method for providing to a mammal a neuroprotective effect against a brain pathology that is associated with reactive oxygen species originating from mitochondria (mROS). The method includes the step of administering to the mammal an SkQ mitochondria-targeted antioxidant in an amount effective to provide said neuroprotective effect. The SkQ mitochondria-targeted antioxidant may be administered either prophylactically or for treatment with respect to brain pathologies other than brain trauma or stroke, and may be administered for treatment of brain trauma or stroke.

## Claims

### Claim 1

A method for providing to a mammal a neuroprotective effect against a brain pathology that is mediated by reactive oxygen species originating from mitochondria (mROS), wherein the brain pathology is selected from the group consisting of alcohol intoxication, hyperhomocysteinemia, and brain trauma, the method comprising the step of administering to the mammal an SkQ mitochondria-targeted antioxidant in an amount effective to provide said neuroprotective effect, wherein the SkQ mitochondria-targeted antioxidant is administered either prophylactically to inhibit the course of the pathology or for treatment of the pathology after its onset with the exception that, where the pathology is brain trauma, the SkQ mitochondria-targeted antioxidant is administered only for treatment after onset of the pathology.

### Claim 2 (depends on 1)

The method according to claim 1, wherein the SkQ mitochondria-targeted antioxidant is selected from the group consisting of SkQ1 and SkQR1.

### Claim 3 (depends on 1)

The method according to claim 1, wherein the SkQ mitochondria-targeted antioxidant is administered to the mammal in an amount of about 1pmole to 1 mmole per kg of body weight of the mammal per day.

### Claim 4 (depends on 1)

The method according to claim 1, wherein the brain pathology comprises alcohol intoxication.

### Claim 5 (depends on 4)

The method according to claim 4, wherein the SkQ mitochondria-targeted antioxidant is administered to the mammal after the mammal has undergone alcohol narcosis.

### Claim 6 (depends on 1)

The method according to claim 1, wherein the brain pathology is hyperhomocysteinemia.

### Claim 7 (depends on 6)

The method according to claim 6, wherein the mammal is a pregnant human.

### Claim 8 (depends on 1)

The method according to claim 1, wherein the SkQ mitochondria-targeted antioxidant is administered to the mammal prior to an appearance in the subject of behavioral defects due to the brain pathology.

### Claim 9 (depends on 1)

The method according to claim 1, wherein the SkQ mitochondria-targeted antioxidant is administered to the mammal after the mammal has contracted the brain pathology or after an appearance in the subject of behavioral defects due to the brain pathology.

### Claim 10 (depends on 1)

The method according to claim 1, wherein the brain pathology is brain trauma.

### Claim 11 (depends on 10)

The method according to claim 10, wherein the SkQ mitochondria-targeted antioxidant is administered to the mammal daily after the mammal has experienced the brain trauma for a period of at least 4 days after the trauma.

### Claim 12 (depends on 1)

The method according to claim 1, wherein the SkQ mitochondria-targeted antioxidant is administered to the mammal by a mode of administration selected from the group consisting of intradermal, intramuscular, intraperitoneal, intravenous, subcutaneous, intranasal, epidural, oral, sublingual, intracerebral, intravaginal, transdermal, rectal, by inhalation and topical.

### Claim 13 (depends on 1)

The method according to claim 1, wherein the SkQ mitochondria-targeted antioxidant is administered to the mammal in combination with a glycolysis inhibitor.

### Claim 14

A method for providing to a mammal a neuroprotective effect against a brain pathology, wherein the brain pathology is brain trauma, the method comprising the step of administering to the mammal an SkQ mitochondria-targeted antioxidant in an amount effective to initiate an increased production of erythropoietin in the mammal.

### Claim 15

A method for providing to a mammal a neuroprotective effect against a brain pathology, wherein the brain pathology is brain trauma, the method comprising the step of administering to the mammal an SkQ mitochondria-targeted antioxidant in an amount effective to cause a decrease in activity of glycogen synthase kinase (GSK-3β) in the mammal.
