IP Library › Granted Patent US 12,281,110
Granted Patent B2
US 12,281,110 · App. 17/155,726 · Granted Apr 22, 2025

Processes for preparing an FGFR inhibitor

Inventors: Jiang Zhu (San Ramon, CA); Mohammad Masjedizadeh (San Jose, CA)
Assignee: Principia Biopharma, Inc.
C07D471/04A61P35/00C07B35/02C07B35/06C07B39/00C07B43/04C07B43/06C07B45/04C07B2200/13
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Quick Facts
Patent No.
US 12,281,110
App. No.
17/155,726
Granted
Apr 22, 2025
Kind
B2
Abstract

Disclosed herein are processes for preparing 8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one and FGFR inhibitor, as well as polymorphs and/or salt forms thereof.

Claims (19)

1. A crystalline free base of a compound of formula:

2. The crystalline free base according to claim 1 , characterized by an X-ray powder diffraction (XRPD) pattern comprising a characteristic peak at about 22° 2Θ.

3. The crystalline free base according to claim 1 , wherein the free base is in a substantially anhydrous form.

4. The crystalline free base according to claim 1 , wherein the free base is in a hydrate form.

5. The crystalline free base according to claim 4 , characterized by an X-ray powder diffraction (XRPD) pattern comprising a characteristic peak at about 6° 2Θ.

6. The crystalline free base according to claim 1 , wherein the free base is in a solvate form.

7. The crystalline free base according to claim 6 , wherein the solvate is at least one of an acetonitrile solvate, an acetone solvate, and a dichloromethane solvate.

8. The crystalline free base according to claim 6 , characterized by an X-ray powder diffraction (XRPD) pattern comprising a characteristic peak at about 14° 2Θ.

9. An amorphous free base of a compound of formula:

10. The amorphous free base according to claim 9 , characterized by an X-ray powder diffraction (XRPD) pattern comprising a characteristic disordered halo at about 23° 2Θ.

11. A crystalline hydrochloride salt or a crystalline maleate salt of a compound of formula:

12. The crystalline salt according to claim 11 , wherein the crystalline salt is a crystalline hydrochloride salt.

13. The crystalline hydrochloride salt according to claim 12 , characterized by an X-ray powder diffraction (XRPD) pattern comprising a characteristic peak at about 11° 2Θ.

14. The crystalline salt according to claim 11 , wherein the crystalline salt is a crystalline maleate salt.

15. The crystalline maleate salt according to claim 14 , characterized by an X-ray powder diffraction (XRPD) pattern comprising a characteristic peak at about 22.5° 2Θ.

16. A pharmaceutical composition comprising the crystalline free base of claim 1 , and a pharmaceutically acceptable carrier and/or excipient.

17. A pharmaceutical composition comprising the amorphous free base of claim 9 , and a pharmaceutically acceptable carrier and/or excipient.

18. A pharmaceutical composition comprising the crystalline hydrochloride salt of claim 12 , and a pharmaceutically acceptable carrier and/or excipient.

19. A pharmaceutical composition comprising the crystalline maleate salt of claim 14 , and a pharmaceutically acceptable carrier and/or excipient.

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 Jan 22, 2021
From: ZHU, JIANG; MASJEDIZADEH, MOHAMMAD
To: PRINCIPIA BIOPHARMA, INC.
Reel/Frame 055000/0967 →
Continuity (4)
Division 16745418 · Jan 17, 2020
Continuation 15748212
Provisional Application 62203498 · Aug 11, 2015
Related Publication 20210147417A1 · May 20, 2021
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