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Details for Patent: 8,343,984

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Details for Patent: 8,343,984

Title:Crystalline forms of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyr- idin-3-yl-pyrimidin-2-ylamino)-benzamide
Abstract: Polymorphic forms of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyr- idin-3-yl-pyrimidin-2-ylamino)-benzamide free base and salts thereof are prepared by various processes.
Inventor(s): Manley; Paul W (Arlesheim, CH), Shieh; Wen-Chung (Berkeley Heights, NJ), Sutton; Paul Allen (Parsippany, NJ), Karpinski; Piotr "Peter" H (Lincoln Park, NJ), Wu; Raeann (Pine Brook, NJ), Monnier; Stephanie M. (Raedersheim, FR), Brozio; Jorg (Basel, CH)
Assignee: Novartis AG (Basel, CH) Novartis Pharma GmbH (Vienna, AT)
Filing Date:Jul 18, 2006
Application Number:11/995,906
Claims:1. A crystalline form A of the hydrochloride salt of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyr- idin-3-yl-pyrimidin-2-ylamino)-benzenearmide, characterized by an X-ray powder diffraction pattern as shown in FIG. 2.

2. The crystalline form of claim 1, wherein form A is a dihydrate.

3. The crystalline form of claim 1, the crystalline form is characterized by an X-ray powder diffraction pattern having a least one maxima selected from about 8.5.degree., 11.0.degree., 11.5.degree., 17.2.degree., 18.8.degree., 19.2.degree., 20.8.degree., 22.1.degree. and 26.0.degree. (2.theta..degree. degrees).

4. The crystalline form of claim 1, wherein the crystalline form is isolated and characterized in more than 50% of the crystalline form A.

5. A crystalline form A' of the hydrochloride salt of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyr- idin-3-yl-pyrimidin-2-ylamino)-benzeneamide, characterized by an X-ray powder diffraction pattern as shown: in FIG. 6.

6. The crystalline form of claim 5, wherein form A' is a monohydrate.

7. The crystalline form of claim 5, the crystalline form is characterized by an X-ray powder diffraction pattern having a least one maxima selected from about 4.3.degree., 8.6.degree., 11.6.degree., 12.1.degree., 17.1.degree., 20.6.degree., 24.5.degree., 25.3.degree., 25.8.degree., 27.3.degree.and 31.6.degree. (2.theta..degree. degrees).

8. The crystalline form of claim 5, wherein the crystalline form is isolated and characterized in more than 50% of the crystalline form A'.

9. A crystalline form A' of the hydrochloride salt of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyr- idin-3-yl-pyrimidin-2-ylamino)-benzeneamide, characterized by en X-ray powder diffraction pattern as shown in FIG. 7.

10. The crystalline form of claim 9, wherein form A'' is anhydrous.

11. The crystalline form of claim 9, the crystalline form is characterized by an X-ray powder diffraction pattern having a least one maxima selected from about 4.5.degree., 8.8.degree., 11.5.degree., 11.9.degree., 13.0.degree., 14.4.degree., 14.8.degree., 15.3.degree., 16.9.degree., 17.6.degree., 19.2.degree., 19.5.degree., 19.9.degree., 21.3.degree., 24.6.degree., 25.4.degree., 26.4.degree., 27.9.degree. and 31.5.degree. (2.theta..degree. degrees).

12. The crystalline form of claim 9, wherein the crystalline form is isolated and characterized in more than 50% of the crystalline form A''.

13. A pharmaceutical composition comprising: (a) a therapeutically effective amount of a crystalline form of 4-methyl-N-[3-(4-methyl-imidazol-1-yl-5-trifluoromethyl-phenyl]-3-(4-pyri- din-3-yl-pyrimidin-2-ylamino)-benzeneamide hydrochloride salt thereof as a monohydrate according to claim 12; and (b) at least one pharmaceutically acceptable carrier, diluent or excipient.

14. A method of treating chronic myelogenous leukemia comprising the step of administering to a subject in need of such treatment, a therapeutically effective amount of a crystalline form of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyr- idin-3-yl-pyrimidin-2-ylamino)-benzeneamide hydrochloride salt thereof as a monohydrate according to claim 6.
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