# US 10,307,409 B2 · Muscarinic combinations and their use for combating hypocholinergic disorders of the central nervous system

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- Number: US 10,307,409 B2
- Document ID: US10307409B2
- Status: Granted
- Kind: B2
- Application number: 15/260,996
- Filed: 2016-09-09
- Published: 2016-12-29
- Granted: 2019-06-04
- Earliest claimed: 2015-03-06
- Assignees: Chase Pharmaceuticals Corporation
- Applicants: Chase Pharmaceuticals Corporation
- Inventors: Thomas N. Chase; Kathleen E. Clarence-Smith
- Web page: https://patentgrep.com/patent/US10307409B2

## CPC

- A61K 31/4439: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465)
- A61K 9/0056: {Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals}
- A61K 9/7023: {Transdermal patches and similar drug-containing composite devices, e.g. cataplasms (galenical aspects of iontophoretic devices A61K9/0009; microneedle arrays A61K9/0021; buccal patches A61K9/006)}
- A61K 31/166: having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
- A61K 31/216: of acids having aromatic rings, e.g. benactizyne, clofibrate
- A61K 31/4178: not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
- A61K 31/439: the ring forming part of a bridged ring system, e.g. quinuclidine (8-azabicyclo [3.2.1] octanes A61K31/46)
- A61K 31/44: Non condensed pyridines; Hydrogenated derivatives thereof
- A61K 31/454: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
- A61K 31/4725: containing further heterocyclic rings
- A61K 31/517: ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- 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)

## Abstract

A combination of a muscarinic cholinergic receptor agonist, a non-anticholinergic antiemetic agent and a non-selective, peripheral anticholinergic agent for the treatment of hypocholinergic disorders of the central nervous system.

## Claims

### Claim 1

A pharmaceutical combination comprising as Components:
(a) a muscarinic cholinergic receptor agonist (MCRA)
(b) a non-anticholinergic antiemetic agent (naAEA); and
(c) a muscarinic receptor antagonist selected from the group consisting of the non-selective, peripheral anticholinergic agents (nsPAChAs);
wherein said MCRA Component (a) is selected from the group consisting of cevimeline and pharmaceutically acceptable salts thereof, milameline and pharmaceutically acceptable salts thereof; xanomeline and pharmaceutically acceptable salts thereof, and MK-7622 and pharmaceutically acceptable salts thereof; said naAEA Component (b) is selected from the group consisting of ondansetron and pharmaceutically acceptable salts and solvates thereof, domperidone and pharmaceutically acceptable salts and solvates thereof and metoclopramide and pharmaceutically acceptable salt and solvates thereof; and said nsPAChA Component (c) is oxybutynin in a transdermal patch.

### Claim 2 (depends on 1)

The combination of claim 1, wherein said MCRA Component (a) is selected from the group consisting of cevimeline and pharmaceutically acceptable salts thereof, in an amount (in cevimeline) of from 34.5 mg to 180 mg; milameline and pharmaceutically acceptable salts thereof, in an amount (in milameline) of from 2.4 mg to 12 mg; xanomeline and pharmaceutically acceptable salts thereof, in an amount (in xanomeline) of from 90 mg to 450 mg; and MK-7622 and pharmaceutically acceptable salts thereof, in an amount (in MK-7622) of from from 5 mg to 270 mg; in a pharmaceutical composition in admixture with a pharmaceutical carrier; said naAEA Component (b) is selected from the group consisting of ondansetron and pharmaceutically acceptable salts and solvates thereof, in an amount (in ondansetron) of from 4 mg to 64 mg, domperidone and pharmaceutically acceptable salts and solvates thereof, in an amount, in domperidone of from 5 mg to 30 mg; and metoclopramide and pharmaceutically acceptable salts and solvates thereof, in an amount (in metoclopramide) of from 5 mg to 30 mg; in a pharmaceutical composition in admixture with a pharmaceutical carrier; and said nsPAChA Component (c) is oxybutynin in admixture with a pharmaceutical carrier or vehicle in a transdermal patch releasing from 3.9 mg/24 h to 7.8 mg/24 h oxybutynin.

### Claim 3 (depends on 2)

The combination of claim 2, wherein said MCRA Component (a) is cevimeline or a pharmaceutically acceptable salt thereof; said naAEA Component (b) is ondansetron or a pharmaceutically acceptable salt thereof; and (c) said nsPAChA is oxybutynin in a transdermal patch releasing 3.9 mg/24 h oxybutynin.