Granted Patent
B2
US 12,410,176 · App. 18/482,278 · Granted Sep 9, 2025
Crystalline forms of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
Inventors:
Pasit Phiasivongsa (Hillsborough, CA); Kolbot By (San Ramon, CA); Jean Baum (San Bruno, CA)
Assignee:
Principia Biopharma Inc.
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Abstract
Crystalline forms of Compound (I): are disclosed. Pharmaceutical compositions comprising the same, methods of treating disorders and conditions mediated by BTK activity using the same, and methods for making Compound (I) and crystalline forms thereof are also disclosed.
Claims (6)
1. A process of preparing crystalline Form C of Compound (I):
wherein C* is a stereochemical center and
wherein crystalline Form C is characterized by an X-ray powder diffractogram having a signal at at least three two-theta values chosen from 9.8±0.2, 10.2±0.2, 15.6±0.2, 16.6±0.2, 18.6±0.2, 18.9±0.2, 19.6±0.2, and 21.6±0.2, the process comprising:
adding acetonitrile to amorphous (R)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile to form a solution;
seeding the solution with crystalline Form B of Compound (I) to form a mixture and stirring the mixture to obtain a slurry, wherein the crystalline Form B is characterized by an X-ray powder diffractogram having a signal at at least three two-theta values chosen from 10.8±0.2, 15.3±0.2, 16.3±0.2, 17.9±0.2, 18.4±0.2, 18.7±0.2, 22.0±0.2, and 22.9±0.2; and
isolating crystalline Form C by filtering the slurry.
Assignments (2)
ASSIGNEE CHANGE OF ADDRESS
Recorded Sep 16, 2025
From: PRINCIPIA BIOPHARMA INC.
To: PRINCIPIA BIOPHARMA INC.
Reel/Frame 072881/0270 →
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded Nov 8, 2023
From: BAUM, JEAN; BY, KOLBOT; PHIASIVONGSA, PASIT
To: PRINCIPIA BIOPHARMA INC.
Reel/Frame 065495/0170 →
Continuity (3)
Provisional Application
62964378
· Jan 22, 2020
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