# US 10,369,144 B2 · Methods and compositions for treatment of disorders ameliorated by muscarinic receptor activation

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 10,369,144 B2
- Document ID: US10369144B2
- Status: Granted
- Kind: B2
- Application number: 16/289,165
- Filed: 2019-02-28
- Published: 2019-06-27
- Granted: 2019-08-06
- Earliest claimed: 2009-07-22
- Assignees: PureTech Health LLC
- Applicants: PureTech Health LLC
- Inventors: Eric Elenko; Philip E. Murray, III; Andrew C. Miller
- Web page: https://patentgrep.com/patent/US10369144B2

## CPC

- A61K 31/46: 8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
- A61K 9/20: Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)}
- A61K 9/48: Preparations in capsules, e.g. of gelatin, of chocolate {(A61K9/0004 takes precedence; bite capsules A61K9/0056)}
- A61K 9/4825: {Proteins, e.g. gelatin (gelatin capsule shells with substantial amounts of other macromolecular substances A61K9/4816)}
- A61K 9/485: {Inorganic compounds}
- A61K 9/4858: {Organic compounds}
- A61K 9/4866: {Organic macromolecular compounds}
- A61K 9/4891: {Coated capsules; Multilayered drug free capsule shells (with drug coating for immediate release A61K9/4808; osmotic devices A61K9/0004)}
- A61K 31/138: Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine (atenolol A61K31/165; pindolol A61K31/404; timolol A61K31/5377)
- A61K 31/222: with compounds having aromatic groups, e.g. dipivefrine, ibopamine
- A61K 31/4025: not condensed and containing further heterocyclic rings, e.g. cromakalim
- A61K 31/4178: not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
- A61K 31/438: The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
- A61K 31/44: Non condensed pyridines; Hydrogenated derivatives thereof
- A61K 31/4439: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465)
- A61K 31/4725: containing further heterocyclic rings
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61K 47/38: Cellulose; Derivatives thereof
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/14: for treating abnormal movements, e.g. chorea, dyskinesia
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A61P 25/24: Antidepressants
- A61P 25/26: Psychostimulants, e.g. nicotine, cocaine
- 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
- A61P 25/30: for treating abuse or dependence
- 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 disclosure provides a method of treating a central nervous system disorder in a patient in need thereof. The method comprises orally administering between 75 mg and 300 mg xanomeline and between 20 mg and 200 mg trospium chloride to the patient during a 24-hour period. The central nervous system disorder is selected from schizophrenia, Alzheimer's disease, Huntington's disease, Parkinson's disease, and Lewy Body dementia, wherein use of the trospium chloride alleviates a side effect associated with use of the xanomeline.

## Claims

### Claim 1

A single capsule formulation for oral administration comprising xanomeline and/or a salt thereof in an amount to cause a side effect chosen from nausea, vomiting, diarrhea, sweating and excess salivation; and trospium chloride in an amount effective to reduce the side effect associated with the oral administration of the xanomeline and/or the salt thereof.

### Claim 2 (depends on 1)

The formulation of claim 1, which is formulated as an immediate release formulation.

### Claim 3 (depends on 1)

The formulation of claim 1, which is formulated as a controlled release formulation.

### Claim 4 (depends on 1)

The formulation of claim 1, wherein the xanomeline and/or the salt thereof is formulated as a controlled release formulation and the trospium chloride is formulated as an immediate release formulation.

### Claim 5 (depends on 1)

The formulation of claim 1, wherein the formulation contains from 1 milligram to 1 gram of xanomeline and/or the salt thereof.

### Claim 6 (depends on 1)

The formulation of claim 1, wherein the formulation contains from five milligrams to 700 milligrams of xanomeline and/or the salt thereof.

### Claim 7 (depends on 1)

The formulation of claim 1, wherein the formulation contains from five milligrams to 500 milligrams of xanomeline and/or the salt thereof.

### Claim 8 (depends on 1)

The formulation of claim 1, wherein the formulation contains from 25 milligrams to 300 milligrams of xanomeline and/or the salt thereof.

### Claim 9 (depends on 1)

The formulation of claim 1, wherein the formulation contains from one milligram to 400 milligrams of trospium chloride.

### Claim 10 (depends on 1)

The formulation of claim 1, wherein the formulation contains from 6.5 milligrams to 200 milligrams of trospium chloride.

### Claim 11 (depends on 1)

The formulation of claim 1, wherein the formulation contains 20 milligrams of trospium chloride.

### Claim 12 (depends on 1)

A method of treating schizophrenia in a patient in need thereof, the method comprising:
orally administering a single capsule formulation of claim 1 twice daily.

### Claim 13 (depends on 12)

The method of claim 12, wherein the formulation contains 20 milligrams of trospium chloride.

### Claim 14 (depends on 12)

The method of claim 12, wherein the formulation contains from 25 milligrams to 300 milligrams of xanomeline and/or the salt thereof.

### Claim 15 (depends on 1)

The formulation of claim 1, wherein the salt of xanomeline is the salt of tartaric acid.

### Claim 16 (depends on 1)

The formulation of claim 1, wherein the amount of the xanomeline and/or the salt thereof is effective to treat a central nervous system disorder chosen from Alzheimer's disease, Huntington's disease, Parkinson's disease, and Lewy Body dementia.