Granted Patent
B2
US 12,486,250 · App. 17/756,888 · Granted Dec 2, 2025
Muscarinic receptor 4 antagonists and methods of use
Inventors:
Nicholas Pagano (San Diego, CA); Nicole Harriott (San Diego, CA); Brian M. Cochran (San Diego, CA); Scott Stirn (San Diego, CA); Christina Marie Costa (San Diego, CA)
Assignee:
Neurocrine Biosciences, Inc.
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Abstract
Provided herein are compounds of the following Formula (I): or a pharmaceutically acceptable salt thereof. Methods for treating a diseases, disorders, or symptom by antagonizing muscarinic receptors, including specifically antagonizing muscarinic receptor 4 (M4), are also provided.
Claims (2)
1 . A crystalline Form I of 2-(1-benzylpiperidin-4-yl)ethyl (2R,6S)-2,6-dimethyl-4-[5-(trifluoromethyl) pyrazin-2-yl]piperazine-1-carboxylate; having a Powder X-Ray Diffraction (PXRD) diffractogram with one or more peaks at two-theta angle selected from 6.3±0.2, 17.2±0.2, 18.0±0.2, 18.5±0.2, and 23.4±0.2 degrees; or having a Powder X-Ray Diffraction (PXRD) diffractogram with peaks at two-theta angle of 6.3=0.2, 17.2±0.2, 18.0±0.2, 18.5±0.2, and 23.4±0.2 degrees; and having a differential scanning calorimetry (DSC) thermogram comprising two peaks, one peak with an onset temperature of 91.6±3° C. and a second peak with an onset temperature of 116.0±3° C.; and having a thermal gravimetric analysis (TGA) thermogram with a weight loss of less than 1% up to about 120° C.
2 . A crystalline Form II of 2-(1-benzylpiperidin-4-yl)ethyl (2R,6S)-2,6-dimethyl-4-[5-(trifluoromethyl) pyrazin-2-yl]piperazine-1-carboxylate; having a Powder X-Ray Diffraction (PXRD) diffractogram with one or more peaks at two-theta angle selected from 10.8±0.2, 16.0±0.2, 20.8±0.2, 21.7±0.2, and 25.1±0.2 degrees; or having a Powder X-Ray Diffraction (PXRD) diffractogram with peaks at two-theta angle of 10.8=0.2, 16.0±0.2, 20.8±0.2, 21.7±0.2, and 25.1±0.2 degrees; and having a differential scanning calorimetry (DSC) thermogram comprising one peak with an onset temperature of 115.1±3° C. and substantially free of a peak with an onset temperature of 91.6±3° C.; and having a thermal gravimetric analysis (TGA) thermogram with a weight loss of less than 0.1% up to about 135° C.
Assignments (2)
CONFIRMATORY GRANT OF SECURITY INTEREST IN UNITED STATES PATENTS
Recorded May 26, 2026
From: NEUROCRINE BIOSCIENCES, INC.
To: JPMORGAN CHASE BANK, N.A.
Reel/Frame 075670/0001 →
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded Aug 29, 2022
From: PAGANO, NICHOLAS; HARRIOTT, NICOLE; COCHRAN, BRIAN M.; STIRN, SCOTT; COSTA, CHRISTINA MARIE
To: NEUROCRINE BIOSCIENCES, INC.
Reel/Frame 060921/0450 →
Continuity (3)
Provisional Application
63056090
· Jul 24, 2020
Provisional Application
62944647
· Dec 6, 2019
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