IP Library Granted Patent US 12,049,463
Granted Patent B2
US 12,049,463 · App. 17/818,846 · Granted Jul 30, 2024

Crystalline form of Tolebrutinib

Inventors: Minhua Chen (Suzhou, CN); Jiaming Shi (Suzhou, CN)
Assignee: Genzyme Corporation
C07D471/04A61P25/00A61P37/06C07B2200/13
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Quick Facts
Patent No.
US 12,049,463
App. No.
17/818,846
Granted
Jul 30, 2024
Kind
B2
Abstract

The present disclosure relates to a novel crystalline form of Tolebrutinib (hereinafter referred to as “Compound I”) and preparation methods thereof, pharmaceutical compositions containing the crystalline form, and uses of the crystalline form for preparing BTK inhibitor drugs and drugs for treating multiple sclerosis.

Claims (4)

1. A crystalline form of Compound I, wherein an X-ray powder diffraction pattern comprises characteristic peaks at 2theta values of 7.7°±0.2°, 11.0°±0.2°, 22.8°±0.2°, 12.0°±0.2°, 16.1°±0.2°, and 18.5°±0.2° using CuKα radiation

2. The crystalline form of Compound I according to claim 1 , wherein the X-ray powder diffraction pattern comprises at least one characteristic peak at 2theta values of 13.6°±0.2°, 20.1°±0.2°, and 24.8°±0.2° using CuKα radiation.

3. The crystalline form of Compound I according to claim 1 , wherein the X-ray powder diffraction pattern is as depicted in FIG. 2 using CuKα radiation.

4. A pharmaceutical composition, wherein said pharmaceutical composition comprises a therapeutically effective amount of the crystalline form according to claim 1 , and pharmaceutically acceptable excipients.

Assignments (4)
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 Jun 11, 2024
From: GENZYME CORPORATION
To: PRINCIPIA BIOPHARMA INC.
Reel/Frame 067694/0242 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 14, 2023
From: CRYSTAL PHARMACEUTICAL (SUZHOU) CO., LTD.
To: GENZYME CORPORATION
Reel/Frame 063945/0802 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 10, 2022
From: CHEN, MINHUA; SHI, JIAMING
To: CRYSTAL PHARMACEUTICAL (SUZHOU) CO., LTD.
Reel/Frame 060770/0972 →
Priority Claims (1)
CN 202011455573.5 · Dec 10, 2020 · national
Continuity (2)
Continuation PCTCN2021132028 · Nov 22, 2021
Related Publication 20220389011A1 · Dec 8, 2022
Cited By (2)
US 12,624,030 US 12,636,280