IP Library › Granted Patent US 12,390,462
Granted Patent B2
US 12,390,462 · App. 18/225,992 · Granted Aug 19, 2025

Muscarinic acetylcholine M1 receptor antagonists

Inventors: Yifeng Xiong (San Diego, CA); Jeffrey Roppe (Temecula, CA); Austin Chih-Yu Chen (San Diego, CA); Yalda Bravo (San Diego, CA); Thomas Schrader (San Diego, CA); Jill Melissa Baccei (San Diego, CA)
Assignee: Contineum Therapeutics, Inc.
A61K31/4995A61K31/501A61K45/06C07D487/08
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Quick Facts
Patent No.
US 12,390,462
App. No.
18/225,992
Granted
Aug 19, 2025
Kind
B2
Abstract

Provided herein are compounds which are useful as antagonists of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

Claims (10)

1. A method of treating multiple sclerosis in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , further comprising the administration of one or more immunomodulatory agents.

3. The method of claim 2 , wherein the one or more immunomodulatory agents are selected from the group consisting of: an IFN-β 1 molecule; a corticosteroid; a polymer of glutamic acid, lysine, alanine and tyrosine or glatiramer; an antibody or fragment thereof against alpha-4 integrin or natalizumab; an anthracenedione molecule or mitoxantrone; a fingolimod or FTY720 or other S1P1 functional modulator; a dimethyl fumarate or other NRF2 functional modulator; an antibody to the alpha subunit of the IL-2 receptor of T cells (CD25) or daclizumab; an antibody against CD52 or alemtuzumab; an antibody against CD20 or ocrelizumab; and an inhibitor of a dihydroorotate dehydrogenase or teriflunomide.

4. A method of modulating muscarinic acetylcholine receptor M1 activity in a subject, the method comprising administering to the subject a compound a therapeutically effective amount of a compound selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

5. The method of claim 1 , wherein the compound or the pharmaceutically acceptable salt thereof is

or a pharmaceutically acceptable salt thereof.

6. The method of claim 4 , wherein the compound or the pharmaceutically acceptable salt thereof is

or a pharmaceutically acceptable salt thereof.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 18, 2024
From: XIONG, YIFENG; ROPPE, JEFFREY; CHEN, AUSTIN CHIH-YU; BRAVO, YALDA; SCHRADER, THOMAS; BACCEI, JILL MELISSA
To: PIPELINE THERAPEUTICS, INC.
Reel/Frame 066170/0993 →
CHANGE OF NAME Recorded Jan 18, 2024
From: PIPELINE THERAPEUTICS, INC.
To: CONTINEUM THERAPEUTICS, INC.
Reel/Frame 066353/0070 →
Continuity (3)
Division 17103455 · Nov 24, 2020
Provisional Application 62942665 · Dec 2, 2019
Related Publication 20230364082A1 · Nov 16, 2023
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