# US 12,178,811 B2 · Methods of treating depressive disorders

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- Number: US 12,178,811 B2
- Document ID: US12178811B2
- Status: Granted
- Kind: B2
- Application number: 17/093,183
- Filed: 2020-11-09
- Published: 2021-06-03
- Granted: 2024-12-31
- Earliest claimed: 2019-11-08
- Assignees: Xenon Pharmaceuticals Inc.
- Applicants: Xenon Pharmaceuticals Inc.
- Inventors: Cynthia Louise Harden; Gregory N. Beatch
- Web page: https://patentgrep.com/patent/US12178811B2

## CPC

- A61K 31/472: Non-condensed isoquinolines, e.g. papaverine
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61P 25/24: Antidepressants
- 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

In certain embodiments, the present disclosure is directed to methods for treating depressive disorders in a human, wherein the methods comprise orally administering a therapeutically effective amount of N-[4-(6-fluoro-3,4-dihydro-1H-isoquinolin-2-yl)-2,6-dimethylphenyl]-3,3-dimethylbutanamide (Compound A), to the human in need thereof. The present disclosure is further directed to various improved methods of therapy and administration of Compound A.

## Claims

### Claim 1

A method of treating a depressive disorder in a human in need thereof, comprising administering a therapeutically effective amount of Compound A to the human;
wherein Compound A is N-[4-(6-fluoro-3,4-dihydro-1H-isoquinolin-2-yl)-2,6-dimethylphenyl]-3,3-dimethylbutanamide;
wherein Compound A is orally administered to the human under fed conditions.

### Claim 2 (depends on 1)

The method of claim 1, wherein Compound A is orally administered to the human between about 30 minutes prior to about 2 hours after eating a meal.

### Claim 3 (depends on 2)

The method of claim 2, wherein Compound A is orally administered to the human during a meal or within 15 minutes after eating a meal.

### Claim 4 (depends on 1)

The method of claim 1, wherein the method comprises enhancing the opening of a Kv7 potassium channel in the humam.

### Claim 5 (depends on 4)

The method of claim 4, wherein the Kv7 potassium channel is one or more of Kv7.2, Kv7.3, Kv7.4, or Kv7.5.

### Claim 6 (depends on 5)

The method of claim 5, wherein the method is selective for enhancing the opening of one or more of Kv7.2, Kv7.3, Kv7.4, or Kv7.5over Kv7.1.

### Claim 7 (depends on 4)

The method of claim 4, wherein the method comprises opening of the Kv7.2/Kv7.3 (KCNQ2/3) potassium channel.

### Claim 8 (depends on 1)

The method of claim 1, wherein the depressive disorder is major depressive disorder (MDD), disruptive mood dysregulation disorder, persistent depressive disorder, bipolar spectrum disorder, postpartum depression, premenstrual dysphoric disorder (PMDD), season affective disorder (SAD), atypical depression, treatment-resistant depression (TRD), depression associated with agitation or anxiety, adjustment disorder with depressed mood, prolonged depressive reaction, or a combinatioin thereof.

### Claim 9 (depends on 8)

The method of claim 8, wherein the depressive disorder is major depressive disorder (MDD).

### Claim 10 (depends on 1)

The method of claim 1, wherein Compound A is administered a dose of 2 to 200 mg to the human.

### Claim 11 (depends on 10)

The method of claim 10, wherein Compound A is administered at a dose of 5 to 50 mg to the human.

### Claim 12 (depends on 10)

The method of claim 10, wherein Compound A is administered at a dose of 10, 15, 20, or 25 mg to the human.

### Claim 13 (depends on 1)

The method of claim 1, wherein Compound A is administered at a dose of at least 20 mg to the human.

### Claim 14 (depends on 1)

The method of claim 1, wherein Compound A is administered at a dose of 25 mg per day to the human.

### Claim 15 (depends on 1)

The method of claim 1, wherein Compound A is administered at a dose of 30 mg per day to the human.

### Claim 16 (depends on 1)

The method of claim 1, wherein Compound A is administered at a dose of 20-150 mg per day to the human.

### Claim 17 (depends on 1)

The method of claim 1, wherein Compound A is administered at a dose of 100 mg per day to the human.

### Claim 18 (depends on 1)

The method of claim 1, wherein Compound A is administered at a dose of 0.05-2.0 mg/kg to the human.

### Claim 19 (depends on 18)

The method of claim 18, wherein Compound A is administered at a dose of 0.1-1.0 mg/kg to the human.

### Claim 20 (depends on 19)

The method of claim 19, wherein Compound A is administered at a dose of 0.2-0.5 mg/kg to the human.

### Claim 21 (depends on 1)

The method of claim 1, wherein Compound A is orally administered as a single dose of 10-30 mg per day.