IP Library Granted Patent US 10,294,242
Granted Patent B2
US 10,294,242 · App. 15/741,893 · Granted May 21, 2019

Diaryl macrocycle polymorph

Inventors: Jingrong J. Cui (San Diego, CA); Evan W. Rogers (San Diego, CA)
Assignee: TP Therapeutics, Inc.
C07D498/18A61P35/00C07C271/16C07B2200/07C07B2200/13
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Quick Facts
Patent No.
US 10,294,242
App. No.
15/741,893
Granted
May 21, 2019
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 (20)

1. 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 crystalline polymorph form 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.

3. The crystalline polymorph form 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.

4. The crystalline polymorph form 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.

5. The crystalline polymorph form 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.

6. The crystalline polymorph form 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.

7. The crystalline polymorph form 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.

8. The crystalline polymorph form 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.

9. The crystalline polymorph form 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.

10. The crystalline polymorph form 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.

11. The crystalline polymorph form 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.

12. The crystalline polymorph form 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.

13. The crystalline polymorph form 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.

14. The crystalline polymorph form 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.

15. The crystalline polymorph form 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.

16. The crystalline polymorph form 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.

17. The crystalline polymorph form 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.

18. The crystalline polymorph form 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.

19. The crystalline polymorph form 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.

20. The crystalline polymorph form 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.

Assignments (1)
CHANGE OF NAME Recorded Aug 19, 2019
From: TP THERAPEUTICS, INC.
To: TURNING POINT THERAPEUTICS, INC.
Reel/Frame 050084/0756 →
Continuity (3)
Provisional Application 62218672 · Sep 15, 2015
Provisional Application 62188846 · Jul 6, 2015
Related Publication 20180194777A1 · Jul 12, 2018
Cited By (7)
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