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
US-2015051222-A1 · Feb 19, 2015 · US
Unsolvated crystalline form 1 of N-[5-(3, 5-difluoro-benzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide and methods of use thereof
US9382235B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9382235-B2 |
| Application number | US-201514716986-A |
| Country | US |
| Kind code | B2 |
| Filing date | May 20, 2015 |
| Priority date | May 23, 2012 |
| Publication date | Jul 5, 2016 |
| Grant date | Jul 5, 2016 |
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- Title
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Abstract
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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.
First claim
Opening claim text (preview).
What is claimed is: 1. An unsolvated crystalline form 1 of N-[(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 4.8±0.5 degrees. 2. An unsolvated crystalline form according to claim 1 , wherein said x-ray powder diffraction pattern further comprises a peak at a 2-theta value of about 16.2±0.5 degrees. 3. An unsolvated crystalline form according to claim 1 , wherein said x-ray powder diffraction pattern further comprises a peak at a 2-theta value of about 17.4±0.5 degrees. 4. An unsolvated crystalline form according to claim 1 , wherein said x-ray powder diffraction pattern further comprises a peak at a 2-theta value of about 18.7±0.5 degrees. 5. An unsolvated crystalline form according to claim 1 , wherein said x-ray powder diffraction pattern further comprises a peak at a 2-theta value of about 20.1±0.5 degrees. 6. An unsolvated crystalline form according to claim 1 , wherein said x-ray powder diffraction pattern further comprises a peak at a 2-theta value of about 22.3±0.5 degrees. 7. An unsolvated crystalline form according to claim 1 , wherein said x-ray powder diffraction pattern further comprises peaks at 2-theta values of about 16.2 ±0.5 degrees, 17.4±0.5 degrees, 18.7±0.5 degrees, 20.1±0.5 degrees and 22.3±0.5 degrees. 8. An unsolvated crystalline form according to claim 1 , wherein said crystalline form is further characterized by exhibiting a peak in a differential scanning calorimetry scan of from about 188° C. to about 196° C. 9. A pharmaceutical composition, comprising an unsolvated crystalline form of N- [5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-l-yl)-2-(tetrahydro -pyran-4-ylamino)-benzamide according to claim 1 and at least one pharmaceutically acceptable excipient, carrier or diluent. 10. A pharmaceutical composition according to claim 9 , wherein said composition is in the form of a tablet, a capsule, a suspension, an emulsion, a dispersible powder, or granules. 11. A pharmaceutical composition according to claim 9 , wherein said composition comprises from about 10 mg to about 1 g of said N-[5-(3,5-difluorobenzyl)-1H -indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide per dose.
Assignees
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Classifications
- C07D405/12Primary
linked by a chain containing hetero atoms as chain links · CPC title
Crystalline forms, e.g. polymorphs · CPC title
- A61K31/496Primary
Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin · CPC title
containing further heterocyclic rings · CPC title
Antineoplastic agents · CPC title
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- What does patent US9382235B2 cover?
- 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.
- Who is the assignee on this patent?
- Nerviano Medical Sciences Srl
- What technology area does this patent fall under?
- Primary CPC classification C07D405/12. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Jul 05 2016 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 1 related publication on this page (citations in our corpus or others sharing the same primary CPC).