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Last Updated: April 5, 2025

Claims for Patent: 9,649,306

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Summary for Patent: 9,649,306

Title:	Treatment of diseases through administration of N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2- -(tetrahydro-pyran-4-ylamino)-benzamide
Abstract:	The present invention relates to a process for the preparation of N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2- -(tetrahydro-pyran-4-ylamino)-benzamide. Novel solid forms of this compound, their utility in treating diseases caused by deregulated protein kinase activity and pharmaceutical compositions containing them are also object of the present invention.
Inventor(s):	Barbugian; Natale Alvaro (Milan, IT), Forino; Romualdo (Milan, IT), Fumagalli; Tiziano (Trezzano Rosa, IT), Orsini; Paolo (Legnano, IT)
Assignee:	NERVIANO MEDICAL SCIENCES S.R.L. (Nerivano (MI), IT)
Application Number:	15/172,478
Patent Claims:	1. A method of treating a disease in a mammal, comprising administering to said mammal a therapeutically effective amount of an unsolvated crystalline form 2 of N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-- (tetrahydro-pyran-4-ylamino)-benzamide, wherein said crystalline form is characterized by an x-ray powder diffraction pattern comprising a peak at a 2-theta value of about 10.5.+-.0.5 degrees, and wherein said disease is selected from the group consisting of non-small cell lung cancer (NSCLC), colorectal cancer (CRC), neuroblastoma, medulloblastoma and melanoma. 2. The method according to claim 1, wherein said x-ray powder diffraction pattern of said unsolvated crystalline form 2 of N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-- (tetrahydro-pyran-4-ylamino)-benzamide further comprises a peak at a 2-theta value of about 11.1.+-.0.5 degrees. 3. The method according to claim 2, wherein said x-ray powder diffraction pattern of said unsolvated crystalline form 2 of N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-- (tetrahydro-pyran-4-ylamino)-benzamide further comprises peaks at 2-theta values of about 14.3.+-.0.5 degrees, 18.4.+-.0.5 degrees, and 21.8.+-.0.5 degrees. 4. The method according to claim 1, wherein said unsolvated crystalline form 2 of N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazi- n-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide is further characterized by exhibiting a peak in a differential scanning calorimetry scan of from about 197.degree. C. to about 198.5.degree. C. 5. The method according to claim 1, wherein said mammal is a human. 6. A method of treating a disease in a mammal, comprising administering to said mammal a pharmaceutical composition comprising at least one pharmaceutically acceptable excipient and a therapeutically effective amount of an unsolvated crystalline form 2 of N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-- (tetrahydro-pyran-4-ylamino)-benzamide, wherein said crystalline form is characterized by an x-ray powder diffraction pattern comprising a peak at a 2-theta value of about 10.5.+-.0.5 degrees, and wherein said disease is selected from the group consisting of non-small cell lung cancer (NSCLC), colorectal cancer (CRC), neuroblastoma, medulloblastoma and melanoma. 7. The method according to claim 6, wherein said x-ray powder diffraction pattern of said unsolvated crystalline form 2 of N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-- (tetrahydro-pyran-4-ylamino)-benzamide further comprises a peak at a 2-theta value of about 11.1.+-.0.5 degrees. 8. The method according to claim 7, wherein said x-ray powder diffraction pattern of said unsolvated crystalline form 2 of N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-- (tetrahydro-pyran-4-ylamino)-benzamide further comprises peaks at 2-theta values of about 14.3.+-.0.5 degrees, 18.4.+-.0.5 degrees, and 21.8.+-.0.5 degrees. 9. The method according to claim 6, wherein said unsolvated crystalline form 2 of N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazi- n-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide is further characterized by exhibiting a peak in a differential scanning calorimetry scan of from about 197.degree. C. to about 198.5.degree. C. 10. The method according to claim 6, wherein said mammal is a human.

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