Compositions comprising an inhibitor of lysine specific demethylase-1
US-10047069-B2 · Aug 14, 2018 · US
US10316016B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10316016-B2 |
| Application number | US-201816032002-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jul 10, 2018 |
| Priority date | Nov 5, 2015 |
| Publication date | Jun 11, 2019 |
| Grant date | Jun 11, 2019 |
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Described herein are amorphous and crystalline forms of pharmaceutically acceptable salts of the lysine specific demethylase-1 inhibitor 4-[2-(4-aminopiperidin-1-yl)-5-(3-fluoro-4-methoxy-phenyl)-1-methyl-6-oxo-1,6-dihydropyrimidin-4-yl]-2-fluorobenzonitrile. Also described are pharmaceutical compositions suitable for administration to a mammal that include the lysine specific demethylase-1 inhibitor, and methods of using the lysine specific demethylase-1 inhibitor for treating diseases or conditions that are associated with lysine specific demethylase-1 activity.
Opening claim text (preview).
What is claimed is: 1. A pharmaceutical composition comprising a crystalline form of a pharmaceutically acceptable salt of 4-[2-(4-amino-piperidin-1-yl)-5-(3-fluoro-4-methoxy-phenyl)-1-methyl-6-oxo-1,6-dihydro-pyrimidin-4-yl]-2-fluorobenzonitrile, wherein the crystalline form of 4-[2-(4-amino-piperidin-1-yl)-5-(3-fluoro-4-methoxy-phenyl)-1-methyl-6-oxo-1,6-dihydro-pyrimidin-4-yl]-2-fluorobenzonitrile can exist in unsolvated as well as solvated forms. 2. The pharmaceutical composition of claim 1 , wherein the pharmaceutically acceptable salt is 4-[2-(4-amino-piperidin-1-yl)-5-(3-fluoro-4-methoxy-phenyl)-1-methyl-6-oxo-1,6-dihydro-pyrimidin-4-yl]-2-fluorobenzonitrile besylate. 3. The pharmaceutical composition of claim 1 , wherein the solvated form comprises water or ethanol. 4. The pharmaceutical composition of claim 1 comprising about 0.5 mg to about 200 mg of crystalline 4-[2-(4-amino-piperidin-1-yl)-5-(3-fluoro-4-methoxy-phenyl)-1-methyl-6-oxo-1,6-dihydro-pyrimidin-4-yl]-2-fluorobenzonitrile besylate salt. 5. A pharmaceutical composition comprising a crystalline form of a pharmaceutically acceptable salt of 4-[2-(4-amino-piperidin-1-yl)-5-(3-fluoro-4-methoxy-phenyl)-1-methyl-6-oxo-1,6-dihydro-pyrimidin-4-yl]-2-fluorobenzonitrile and a residual amount of an organic solvent. 6. The pharmaceutical composition of claim 5 , wherein the pharmaceutically acceptable salt is 4-[2-(4-amino-piperidin-1-yl)-5-(3-fluoro-4-methoxy-phenyl)-1-methyl-6-oxo-1,6-dihydro-pyrimidin-4-yl]-2-fluorobenzonitrile besylate. 7. The pharmaceutical composition of claim 5 , wherein the organic solvent is a Class 3 solvent. 8. The pharmaceutical composition of claim 1 , wherein an appropriate daily dosage is from about 1 to about 30 mg/kg per body weight.
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directly linked by a ring-member-to-ring-member bond · CPC title
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