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Last Updated: April 26, 2024

Claims for Patent: 8,217,057

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Summary for Patent: 8,217,057

Title:	Polymorphs of a c-MET/HGFR inhibitor
Abstract:	This invention relates to polymorphs of (R)-3-[1-(2,6-Dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-py- razol-4-yl)-pyridin-2-ylamine that are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to compositions including such salts and polymorphs, and to methods of using such compositions in the treatment of abnormal cell growth in mammals, especially humans.
Inventor(s):	Cui; Jingrong Jean (San Diego, CA), Tran-Dube; Michelle Bich (San Diego, CA)
Assignee:	Pfizer Inc. (New York, NY)
Application Number:	12/095,116
Patent Claims:	1. A crystalline form of free base of (R)-3-[1-(2,6-dichloro-3-fluoro-phenyl)ethoxy]-5-(1-piperidin-4-yl-1H-pyr- azol-4-yl)-pyridin-2-ylamine having a powder X-ray diffraction pattern substantially the same as shown in FIG. 1. 2. The crystalline form of claim 1, wherein the powder X-ray diffraction pattern has a peak at diffraction angle (2.theta.) of 19.7.+-.0.1. 3. The crystalline form of claim 1, wherein the powder X-ray diffraction pattern has peaks at diffraction angles (2.theta.) of 17.3.+-.0.1 and 19.7.+-.0.1. 4. The crystalline form of claim 1, wherein the powder X-ray diffraction pattern has peaks at diffraction angles (2.theta.) of 15.7.+-.0.1, 17.3.+-.0.1, and 19.7.+-.0.1. 5. The crystalline form of claim 1, wherein the powder X-ray diffraction pattern has peaks at diffraction angles (2.theta.) of 15.7.+-.0.1, 17.3.+-.0.1, 19.7.+-.0.1, and 26.8.+-.0.1. 6. A pharmaceutical composition comprising the crystalline form of claim 1. 7. A capsule comprising the pharmaceutical composition of claim 6. 8. The capsule of claim 7 comprising from 0.1 to 200 mg of the crystalline form of (R)-3-[1-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-py- razol-4-yl)-pyridin-2-ylamine. 9. The capsule of claim 7 comprising from 25 to 150 mg of the crystalline form of (R)-3-[1-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-- yl-1H-pyrazol-4-yl)-pyridin-2-ylamine. 10. The capsule of claim 7 comprising from 50 to 100 mg of the crystalline form of (R)-3-[1-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-py- razol-4-yl)-pyridin-2-ylamine.

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