IP Library › Granted Patent US 9,637,500
Granted Patent B2
US 9,637,500 · App. 14/898,582 · Granted May 2, 2017

Solid forms of a macrocyclic kinase inhibitor

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Quick Facts
Patent No.
US 9,637,500
App. No.
14/898,582
Granted
May 2, 2017
Kind
B2
Abstract

This invention relates to crystalline solvates of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benz- oxadiazacyclotetradecine-3-carbonitrile, useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to pharmaceutical compositions comprising such crystalline solvates, and to methods of using such solvates and compositions in the treatment of abnormal cell growth in mammals, especially humans.

Claims (11)

1. A crystalline acetic acid solvate of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiaza-cyclotetradecine-3-carbonitrile, having a powder X-ray diffraction pattern comprising a peak at a 2θ value of: 12.9° 2θ±0.2° 2θ.

2. The crystalline solvate of claim 1 , having a powder X-ray diffraction pattern comprising peaks at 2θ values of: 12.9 and 14.5° 2θ±0.2° 2θ.

3. The crystalline solvate of claim 1 , having a powder X-ray diffraction pattern comprising peaks at 2θ values of: 11.4, 12.9 and 14.5° 2θ±0.2° 2θ.

4. The crystalline solvate of claim 1 , having a powder X-ray diffraction pattern comprising peaks at 2θ values of: 10.5, 11.4, 12.9 and 14.5° 2θ±0.2° 2θ.

5. The crystalline solvate of claim 1 , having a powder X-ray diffraction pattern comprising peaks at 2θ values of: 10.5, 11.4, 12.9, 14.5 and 15.3° 2θ±0.2° 2θ.

6. The crystalline solvate of claim 1 , having a Raman spectrum comprising wavenumber (cm −1 ) values of: 2234 cm −1 +2 cm −1 .

7. The crystalline solvate of claim 1 , having a Raman spectrum comprising wavenumber (cm −1 ) values of: 809 and 2234 cm −1 ±2 cm −1 .

8. The crystalline solvate of claim 1 , having a Raman spectrum comprising wavenumber (cm −1 ) values of: 809, 2234 and 3055 cm −1 +2 cm −1 .

9. The crystalline solvate of claim 1 , having: (a) a 19 F solid state NMR spectrum comprising the resonance (ppm) value of: −107.2 ppm±0.2 ppm; (b) a 13 C solid state NMR spectrum comprising the resonance (ppm) value of: 140.7 ppm±0.2 ppm; or (c) both (a) and (b).

10. The crystalline solvate of claim 1 , having a 13 C solid state NMR spectrum comprising resonance (ppm) values of: 22.8, 140.7 and 170.3 ppm±0.2 ppm.

11. A pharmaceutical composition comprising a crystalline acetic acid solvate of claim 1 , and a pharmaceutically acceptable excipient.

Assignments (1)
ASSIGNEE ADDRESS CORRECTION Recorded Mar 20, 2023
From: PFIZER INC.
To: PFIZER INC.
Reel/Frame 063119/0087 →