# US 11,298,361 B2 · Fused benzazepines for treatment of Tourette's Syndrome

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- Number: US 11,298,361 B2
- Document ID: US11298361B2
- Status: Granted
- Kind: B2
- Application number: 14/414,368
- Filed: 2013-07-12
- Published: 2015-06-18
- Granted: 2022-04-12
- Earliest claimed: 2012-07-12
- Assignees: Emalex Biosciences, Inc.
- Applicants: Emalex Biosciences, Inc.
- Inventors: Richard E. Chipkin; Rudolf Kwan
- Web page: https://patentgrep.com/patent/US11298361B2

## CPC

- A61K 31/55: having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/14: for treating abnormal movements, e.g. chorea, dyskinesia
- A61P 25/22: Anxiolytics
- A61P 25/24: Antidepressants
- A61P 31/04: Antibacterial agents
- A61P 37/02: Immunomodulators
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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 encompasses methods of treating a subject who has been diagnosed as having a tic disorder or a movement disorder. The tic disorder can be Tourette's Syndrome, and the methods can include the steps of: (a) identifying a subject in need of treatment; and (b) administering to the subject a therapeutically effective amount of a composition comprising a D1/D5 receptor antagonist, a D1/D5 receptor partial agonist, or a mixture thereof. For example, the D1/D5 receptor antagonist can be ecopipam or a pharmaceutically acceptable salt, solvate, hydrate, prodrug, structural analog, metabolite, or polymorph thereof.

## Claims

### Claim 1

A method of treating Tourette's disorder in a human patient in need thereof, the method comprising:
administering to the patient 0.01 mg/kg to 500 mg/kg per day of ecopipam or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The method of claim 1, wherein the patient is not older than 18 years.

### Claim 3 (depends on 1)

The method of claim 1, wherein the patient is considered to be free from attention-deficit-hyperactivity disorder, depression, and obsessive-compulsive disorder.

### Claim 4

A method of treating Tourette's Disorder in a human patient in need thereof, the method comprising
administering to the patient about 0.1 mg to about 500 mg per day of ecopipam or a pharmaceutically acceptable salt thereof.

### Claim 5 (depends on 4)

The method of claim 4, comprising administering ecopipam hydrochloride.

### Claim 6 (depends on 5)

The method of claim 5, wherein the ecopipam is formulated for oral delivery.

### Claim 7 (depends on 6)

The method of claim 6, wherein the ecopipam is administered at a daily dose in a range of about 0.01 mg/kg to about 50 mg/kg.

### Claim 8 (depends on 7)

The method of claim 7, wherein ecopipam is administered at a daily dose in a range of about 0.1 mg/kg to about 5 mg/kg.

### Claim 9 (depends on 7)

The method of claim 7, wherein the ecopipam is administered at a dose of 50-100 mg/day.

### Claim 10 (depends on 4)

The method of claim 4, wherein the ecopipam is administered once, twice, or three times daily.

### Claim 11 (depends on 1)

The method of claim 1, further comprising a step of administering a second treatment for treating the tic disorder.

### Claim 12 (depends on 11)

The method of claim 11, wherein the second treatment is a behavioral, surgical, or pharmaceutical therapy.

### Claim 13 (depends on 1)

The method of claim 1, further comprising a step of administering to the subject a therapeutically effective amount of a second composition for the treatment of attention-deficit-hyperactivity disorder, depression, or obsessive-compulsive disorder.

### Claim 14 (depends on 1)

The method of claim 1, wherein the composition is formulated in a unit dosage form.

### Claim 15 (depends on 1)

The method of claim 1, wherein the composition is formulated as a capsule, tablet, pill, powder, or syrup.

### Claim 16 (depends on 1)

The method of claim 1, comprising administering 0.01 mg/kg to 50 mg/kg per day of ecopipam or a pharmaceutically acceptable salt thereof.

### Claim 17 (depends on 16)

The method of claim 16, comprising administering ecopipam hydrochloride.

### Claim 18 (depends on 1)

The method of claim 1, comprising administering 0.1 mg/kg to 5 mg/kg per day of ecopipam or a pharamaceutically acceptable salt thereof.

### Claim 19 (depends on 18)

The method of claim 18, comprising administering ecopipam hydrochloride.

### Claim 20

A method of treating Tourette's Disorder in a human patient in need thereof and not older than 18 years, comprising administering to the patient once daily oral dosages of ecopipam or a pharmaceutically acceptable salt thereof in a unit dosage form comprising 10 mg to 200 mg ecopipam or a pharmaceutically acceptable salt thereof.

### Claim 21

A method of treating Tourette's Disorder in a human patient in need thereof and not older than 18 years, comprising administering to the patient once daily oral dosages of ecopipam or a pharmaceutically acceptable salt thereof at a daily dose in a range of about 0.1 mg/kg to about 5 mg/kg.
