# US 11,433,057 B2 · Method for improving or enhancing cognition

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- Number: US 11,433,057 B2
- Document ID: US11433057B2
- Status: Granted
- Kind: B2
- Application number: 16/097,750
- Filed: 2017-05-19
- Published: 2020-12-24
- Granted: 2022-09-06
- Earliest claimed: 2016-05-20
- Assignees: Vanda Pharmaceuticals Inc.
- Applicants: Vanda Pharmaceuticals Inc.
- Inventors: Mihael H. Polymeropoulos
- Web page: https://patentgrep.com/patent/US11433057B2

## CPC

- A61K 31/439: the ring forming part of a bridged ring system, e.g. quinuclidine (8-azabicyclo [3.2.1] octanes A61K31/46)
- A61K 9/4825: {Proteins, e.g. gelatin (gelatin capsule shells with substantial amounts of other macromolecular substances A61K9/4816)}
- 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
- 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

Disclosed herein are a method for improving cognition in an individual having findings consistent with a cognitive impairment, and a method of enhancing cognition in an individual. The methods include administering a therapeutically effective amount of (R)-3-(6-p-tolyl-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane or a metabolite or a pharmaceutically acceptable salt thereof to the individual.

## Claims

### Claim 1

A method for improving cognition in a human individual having findings consistent with a cognitive impairment, the method comprising:
administering a therapeutically effective amount of 13.5 to 16.5 mg/day of (R)-3-(6-p-tolyl-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane- or a pharmaceutically acceptable salt thereof to the human individual, and
achieving a statistically significant improvement in a cognitive function measurement obtained in the human individual, after the human individual is administered the (R)-3-(6-p-tolyl-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane,
wherein the cognitive impairment is Mild Cognitive Impairment amnestic mild cognitive impairment.

### Claim 2

A method of enhancing cognition in a human individual, the method comprising:
administering a therapeutically effective amount 13.5 to 16.5 mg/day of (R)-3-(6-p-tolyl-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane or a pharmaceutically acceptable salt thereof to the human individual, and
achieving a statistically significant improvement in a cognitive function measurement obtained in the human individual, after the human individual is administered (R)-3-(6-p-tolyl-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane,
wherein the human individual has findings consistent with a cognitive impairment.

### Claim 3 (depends on 1)

The method of claim 1, wherein the pharmaceutically acceptable salt thereof comprises a fumarate salt of (R)-3-(6-p-tolyl-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane.

### Claim 4 (depends on 3)

The method of claim 3, wherein the pharmaceutically acceptable salt thereof comprises a mono-fumarate salt of (R)-3-(6-p-tolyl-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane.

### Claim 5 (depends on 1)

The method of claim 1, wherein the therapeutically effective amount of (R)-3-(6-p-tolyl-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane or a pharmaceutically acceptable salt thereof is in the form of one or more capsules.

### Claim 6 (depends on 5)

The method of claim 5, wherein each of the one or more capsules contains a unit dose of 4.5 to 5.5-mg of (R)-3-(6-p-tolyl-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane or a pharmaceutically acceptable salt thereof.

### Claim 7 (depends on 1)

The method of claim 1, wherein the therapeutically effective amount of (R)-3-(6-p-tolyl-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane or a pharmaceutically acceptable salt thereof is administered after a meal.

### Claim 8 (depends on 2)

The method of claim 2, wherein the pharmaceutically acceptable salt thereof comprises a fumarate salt of (R)-3-(6-p-tolyl-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane.

### Claim 9 (depends on 8)

The method of claim 8, wherein the pharmaceutically acceptable salt thereof comprises a mono-fumarate salt of (R)-3-(6-p-tolyl-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane.

### Claim 10 (depends on 2)

The method of claim 2, wherein the therapeutically effective amount of (R)-3-(6-p-tolyl-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane or the pharmaceutically acceptable salt thereof is in the form of one or more capsules.

### Claim 11 (depends on 10)

The method of claim 10, wherein each of the one or more capsules contains a unit dose of 4.5 to 5.5 mg of (R)-3-(6-p-tolyl-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane or the pharmaceutically acceptable salt thereof.

### Claim 12 (depends on 2)

The method of claim 2, wherein the therapeutically effective amount of (R)-3-(6-p-tolyl-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane or the pharmaceutically acceptable salt thereof is administered after a meal.