IP Library › Granted Patent US 12,187,739
Granted Patent B2
US 12,187,739 · App. 17/933,434 · Granted Jan 7, 2025

Diaryl macrocycle polymorph

Inventors: Jingrong J. Cui (San Diego, CA); Evan W. Rogers (San Diego, CA)
Assignee: TURNING POINT THERAPEUTICS, INC.
C07D498/18A61P35/00C07C271/16C07B2200/07C07B2200/13
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Quick Facts
Patent No.
US 12,187,739
App. No.
17/933,434
Granted
Jan 7, 2025
Kind
B2
Abstract

This disclosure relates to polymorphs of (7S,13R)-11-fluoro-7,13-dimethyl-6,7,13,14-tetrahydro-1,15-ethenopyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecin-4(5H)-one that are useful in the treatment of disease, such as cancer, in mammals. This disclosure also relates to compositions including such polymorphs, and to methods of using such compositions in the treatment of diseases, such as cancer, in mammals, especially in humans.

Claims (23)

1. A pharmaceutical composition comprising a crystalline polymorph form of (7S,13R)-11-fluoro-7,13-dimethyl-6,7,13,14-tetrahydro-1,15-ethenopyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecin-4 (5H)-one, wherein the crystalline polymorph form has a powder X-ray diffraction pattern comprising a peak at diffraction angle (2θ) of 27.4±0.1.

2. The pharmaceutical composition of claim 1 , wherein the crystalline polymorph form has a powder X-ray diffraction pattern comprising peaks at diffraction angles (2θ) of 27.4±0.1 and 22.8±0.1.

3. The pharmaceutical composition of claim 1 , wherein the crystalline polymorph form has a powder X-ray diffraction pattern comprising peaks at diffraction angles (2θ) of 27.4±0.1 and 21.2±0.1.

4. The pharmaceutical composition of claim 1 , wherein the crystalline polymorph form has a powder X-ray diffraction pattern comprising peaks at diffraction angles (2θ) of 27.4±0.1 and 18.8±0.1.

5. The pharmaceutical composition of claim 1 , wherein the crystalline polymorph form has a powder X-ray diffraction pattern comprising peaks at diffraction angles (2θ) of 27.4±0.1 and 16.5±0.1.

6. The pharmaceutical composition of claim 1 , wherein the crystalline polymorph form has a powder X-ray diffraction pattern comprising peaks at diffraction angles (2θ) of 27.4±0.1 and 16.1±0.1.

7. The pharmaceutical composition of claim 1 , wherein the crystalline polymorph form has a powder X-ray diffraction pattern comprising peaks at diffraction angles (2θ) of 27.4±0.1 and 9.4±0.1.

8. The pharmaceutical composition of claim 1 , wherein the crystalline polymorph form has a powder X-ray diffraction pattern comprising peaks at diffraction angles (2θ) of 27.4±0.1, 22.8±0.1, and 21.2±0.1.

9. The pharmaceutical composition of claim 1 , wherein the crystalline polymorph form has a powder X-ray diffraction pattern comprising peaks at diffraction angles (2θ) of 27.4±0.1, 22.8±0.1, and 18.8±0.1.

10. The pharmaceutical composition of claim 1 , wherein the crystalline polymorph form has a powder X-ray diffraction pattern comprising peaks at diffraction angles (2θ) of 27.4±0.1, 22.8±0.1, and 16.5±0.1.

11. The pharmaceutical composition of claim 1 , wherein the crystalline polymorph form has a powder X-ray diffraction pattern comprising peaks at diffraction angles (2θ) of 27.4±0.1, 22.8±0.1, and 16.1±0.1.

12. The pharmaceutical composition of claim 1 , wherein the crystalline polymorph form has a powder X-ray diffraction pattern comprising peaks at diffraction angles (2θ) of 27.4±0.1, 22.8±0.1, and 9.4±0.1.

13. The pharmaceutical composition of claim 1 , wherein the crystalline polymorph form has a powder X-ray diffraction pattern comprising peaks at diffraction angles (2θ) of 27.4±0.1, 21.2±0.1, and 18.8±0.1.

14. The pharmaceutical composition of claim 1 , wherein the crystalline polymorph form has a powder X-ray diffraction pattern comprising peaks at diffraction angles (2θ) of 27.4±0.1, 21.2±0.1, and 16.5±0.1.

15. The pharmaceutical composition of claim 1 , wherein the crystalline polymorph form has a powder X-ray diffraction pattern comprising peaks at diffraction angles (2θ) of 27.4±0.1, 21.2±0.1, and 16.1±0.1.

16. The pharmaceutical composition of claim 1 , wherein the crystalline polymorph form has a powder X-ray diffraction pattern comprising peaks at diffraction angles (2θ) of 27.4±0.1, 21.2±0.1, and 9.4±0.1.

17. The pharmaceutical composition of claim 1 , wherein the crystalline polymorph form has a powder X-ray diffraction pattern comprising peaks at diffraction angles (2θ) of 27.4±0.1, 18.8±0.1, and 16.5±0.1.

18. The pharmaceutical composition of claim 1 , wherein the crystalline polymorph form has a powder X-ray diffraction pattern comprising peaks at diffraction angles (2θ) of 27.4±0.1, 18.8±0.1, and 16.1±0.1.

19. The pharmaceutical composition of claim 1 , wherein the crystalline polymorph form has a powder X-ray diffraction pattern comprising peaks at diffraction angles (2θ) of 27.4±0.1, 18.8±0.1, and 9.4±0.1.

20. The pharmaceutical composition of claim 1 , wherein the crystalline polymorph form has a powder X-ray diffraction pattern comprising peaks at diffraction angles (2θ) of 9.4±0.1, 16.1±0.1, 16.5±0.1, 18.8±0.1, 21.2±0.1, 22.8±0.1, and 27.4±0.1.

21. The pharmaceutical composition of claim 1 , wherein the crystalline polymorph form has a powder X-ray diffraction pattern substantially as shown in FIG. 1 .

22. The pharmaceutical composition of claim 1 , wherein the crystalline polymorph form has a differential scanning calorimetry (DSC) thermogram showing a melting point at 345.5° C.

23. The pharmaceutical composition of claim 1 , wherein the crystalline polymorph form has a differential scanning calorimetry (DSC) thermogram as shown in FIG. 2 .

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 20, 2022
From: CUI, JINGRONG JEAN; ROGERS, EVAN W.
To: TP THERAPEUTICS
Reel/Frame 061154/0826 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 20, 2022
From: CUI, JINGRONG JEAN; ROGERS, EVAN
To: TP THERAPEUTICS, INC.
Reel/Frame 061155/0030 →
CHANGE OF NAME Recorded Sep 20, 2022
From: TP THERAPEUTICS, INC.
To: TURNING POINT THERAPEUTICS, INC.
Reel/Frame 061488/0674 →
Continuity (6)
Continuation 17071569 · Oct 15, 2020
Continuation 16378095 · Apr 8, 2019
Division 15741893
Provisional Application 62218672 · Sep 15, 2015
Provisional Application 62188846 · Jul 6, 2015
Related Publication 20230295184A1 · Sep 21, 2023
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