# US 12,005,035 B1 · Compositions and methods for treatment of chronic pain and depression

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- Number: US 12,005,035 B1
- Document ID: US12005035B1
- Status: Granted
- Kind: B1
- Application number: 18/448,990
- Filed: 2023-08-14
- Granted: 2024-06-11
- Earliest claimed: 2023-08-14
- Applicants: Daniel C. Javitt
- Inventors: Daniel C. Javitt
- Web page: https://patentgrep.com/patent/US12005035B1

## CPC

- A61K 31/135: having aromatic rings {, e.g. ketamine, nortriptyline (methadone A61K31/137)}
- A61K 31/167: having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
- A61K 33/00: Medicinal preparations containing inorganic active ingredients
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- 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

Described herein is a composition that includes an N-methyl-D-aspartate receptor (NMDAR) antagonist and a TAS2R receptor response mediating agent for treating neuropathic pain and depression. Methods for treating chronic pain with the described composition are also described.

## Claims

### Claim 1

A pharmaceutical formulation comprising ketamine and a bitter taste receptor (TAS2R) response mediating agent, wherein the ketamine is racemic ketamine, S-ketamine, or R-ketamine, and is provided at a concentration between 100 μM and 1 mM, inclusive, the TAS2R response mediating agent is NaOH, and wherein the molar ratio of ketamine to NaOH is from 2:1 to 1:1.

### Claim 2 (depends on 1)

The pharmaceutical formulation of claim 1, wherein the molar ratio of ketamine to NaOH is 2:1.

### Claim 3 (depends on 1)

The pharmaceutical formulation of claim 1, wherein the formulation is formulated for parenteral administration.

### Claim 4 (depends on 3)

The pharmaceutical formulation of claim 3, wherein the formulation is formulated for subcutaneous, intramuscular, intravenous, intraarticular, intraperitoneal, or intrathecal administration.

### Claim 5 (depends on 1)

A method for treatment of chronic pain or chronic pain associated with depression, comprising administering to a subject in need thereof an effective amount of the pharmaceutical formulation of claim 1, thereby treating the chronic pain or chronic pain associated with depression.

### Claim 6 (depends on 5)

The method of claim 5, wherein the molar ratio of ketamine to NaOH is 2:1.

### Claim 7 (depends on 5)

The method of claim 5, wherein the formulation is administered parenterally.

### Claim 8 (depends on 7)

The method of claim 7, wherein the formulation is administered subcutaneously, intramuscularly, intravenously, intraarticularly, intraperitoneally, or intrathecally.

### Claim 9 (depends on 5)

The method of claim 5, wherein the formulation is administered as a single bolus, a gradual infusion, or a combination thereof.

### Claim 10 (depends on 5)

The method of claim 5, wherein the depression is major depression or bipolar depression.

### Claim 11 (depends on 1)

The pharmaceutical formulation of claim 1, wherein the ketamine is provided at a concentration of 1 mM, and the molar ratio of ketamine to NaOH is 2:1.

### Claim 12 (depends on 1)

The pharmaceutical formulation of claim 1, wherein the ketamine is provided at a concentration of 1 mM, and the molar ratio of ketamine to NaOH is 3:2.

### Claim 13 (depends on 1)

The pharmaceutical formulation of claim 1, wherein the ketamine is provided at a concentration of 1 mM, and the molar ratio of ketamine to NaOH is 1:1.

### Claim 14 (depends on 1)

The pharmaceutical formulation of claim 1, wherein the ketamine is provided at a concentration of 500 nM, and the molar ratio of ketamine to NaOH is 2:1.

### Claim 15 (depends on 1)

The pharmaceutical formulation of claim 1, wherein the ketamine is provided at a concentration of 500 nM, and the molar ratio of ketamine to NaOH is 3:2.

### Claim 16 (depends on 1)

The pharmaceutical formulation of claim 1, wherein the ketamine is provided at a concentration of 500 nM, and the molar ratio of ketamine to NaOH is 1:1.

### Claim 17 (depends on 5)

The method of claim 5, wherein treating the chronic pain or chronic pain associated with depression is associated with psychic pain.

### Claim 18 (depends on 9)

The method of claim 9, wherein the gradual infusion is over 5-120 minutes.

### Claim 19 (depends on 9)

The method of claim 9, wherein the gradual infusion is over 20, 30, or 40 minutes.

### Claim 20 (depends on 9)

The method of claim 9, wherein the molar ratio of ketamine to NaOH is 2:1, and the formulation is administered intravenously over 10-120 minutes.