IP Library › Granted Patent US 10,316,016
Granted Patent B2
US 10,316,016 · App. 16/032,002 · Granted Jun 11, 2019

Compositions comprising an inhibitor of lysine specific demethylase-1

Inventors: Young K. Chen (San Marcos, CA); Toufike Kanouni (Rancho Santa Fe, CA); Stephen W. Kaldor (San Diego, CA); Jeffrey Alan Stafford (San Diego, CA); James Marvin Veal (Apex, NC); Paula Alessandra Tavares-Greco (Parsippany, NJ); Matthew Michael Kreilein (Hillsborough, NJ)
Assignee: CELGENE QUANTICEL RESEARCH, INC.
C07D401/04A61K31/4545A61K31/506C07D239/36
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Quick Facts
Patent No.
US 10,316,016
App. No.
16/032,002
Granted
Jun 11, 2019
Kind
B2
Abstract

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.

Claims (8)

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.

Continuity (4)
Continuation 15793512 · Oct 25, 2017
Continuation 15344426 · Nov 4, 2016
Provisional Application 62251507 · Nov 5, 2015
Related Publication 20180319767A1 · Nov 8, 2018