Claims for Patent: 11,453,656

Summary for Patent: 11,453,656

Title:	Salt of an aminopyridine derivative compound, a crystalline form thereof, and a process for preparing the same
Abstract:	The present invention relates to novel mesylate salt of N-(5-(4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yppyrimidine-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide, a novel crystalline form thereof, and a process for preparing the same. More specifically, the present invention relates to mesylate salt of N-(5-(4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yl)pyrimidine-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide, which is excellent in stability, solubility, and bioavailability when it is administered not only alone but also in combination with other drugs and which has a high purity, a crystalline form thereof, and a process for preparing the same.
Inventor(s):	Sang Ho Oh, Jong Gyun Kim, Se-Woong Oh, Tae Dong Han, Soo Yong Chung, Seong Ran LEE, Kyeong Bae Kim, Young Sung Lee, Woo Seob Shin, Hyun Ju, Jeong Ki Kang, Su Min Park, Dong Kyun Kim
Assignee:	Yuhan Corp
Application Number:	US16/605,944
Patent Claims:	1. Mesylate salt of N-(5-(4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yl)pyrimidine-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide, as represented by the following Formula 1: which is in a crystalline form (I) that has diffraction peaks in a PXRD (powder X-ray diffraction) graph present at 2θ (theta) angles of 5.614±0.2, 17.143±0.2, and 21.585±0.2 degrees. 2. The mesylate salt of claim 1, wherein the crystalline form (I) has diffraction peaks in a PXRD (powder X-ray diffraction) graph present at 2θ (theta) angles of 5.614±0.2, 12.394±0.2, 14.086±0.2, 17.143±0.2, 21.585±0.2, 22.131±0.2, and 22.487±0.2 degrees. 3. The mesylate salt of claim 1, wherein the crystalline form has diffraction peaks in a PXRD graph present at 20 angles of 5.614±0.2, 12.394±0.2, 14.086±0.2, 17.143±0.2, 18.020±0.2, 19.104±0.2, 21.585±0.2, 22.131±0.2, and 22.487±0.2 degrees. 4. Mesylate salt of N-(5-(4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yl)pyrimidine-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide, as represented by the following Formula 1: which is in a crystalline form (I) that has an endothermic transition peak value at 210 to 230° C. in a DSC (differential scanning calorimetry) graph. 5. The mesylate salt of claim 4, wherein the crystalline form has an endothermic transition peak value at 217±2° C. in a DSC graph. 6. A pharmaceutical composition for treating a protein kinase-mediated disorder, which comprises the mesylate salt of claim 1 and a pharmaceutically acceptable additive. 7. A pharmaceutical composition which comprises the mesylate salt of claim 2 and a pharmaceutically acceptable additive. 8. A pharmaceutical composition for treating a protein kinase-mediated disorder, which comprises the mesylate salt of claim 4 and a pharmaceutically acceptable additive. 9. A pharmaceutical composition for treating a protein kinase-mediated disorder, which comprises the mesylate salt of claim 5 and a pharmaceutically acceptable additive. 10. The mesylate salt of claim 1, wherein the crystalline form (I) has a water content of about 2.48% to about 3.19%. 11. The mesylate salt of claim 10, wherein the crystalline form (I) has a water content of about 2.70%. 12. The mesylate salt of claim 2, wherein the crystalline form (I) has a water content of about 2.48% to about 3.19%. 13. The mesylate salt of claim 12, wherein the crystalline form (I) has a water content of about 2.70%. 14. The mesylate salt of claim 3, wherein the crystalline form (I) has a water content of about 2.48% to about 3.19%. 15. The mesylate salt of claim 14, wherein the crystalline form (I) has a water content of about 2.70%.