Inhibitors of lysine specific demethylase-1
US-9573930-B2 · Feb 21, 2017 · US
US10047069B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10047069-B2 |
| Application number | US-201715793512-A |
| Country | US |
| Kind code | B2 |
| Filing date | Oct 25, 2017 |
| Priority date | Nov 5, 2015 |
| Publication date | Aug 14, 2018 |
| Grant date | Aug 14, 2018 |
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Official abstract text for this publication.
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. Amorphous phase of 4-[2-(4-aminopiperidin-1-yl)-5-(3-fluoro-4-methoxyphenyl)-1-methyl-6-oxo-1,6-dihydropyrimidin-4-yl]-2-fluorobenzonitrile besylate salt has an XRPD pattern showing a lack of crystallinity. 2. Amorphous crystalline 4-[2-(4-aminopiperidin-1-yl)-5-(3-fluoro-4-methoxyphenyl)-1-methyl-6-oxo-1,6-dihydropyrimidin-4-yl]-2-fluorobenzonitrile besylate salt exhibits a characteristic XRPD pattern substantially the same as shown in FIG. 3 . 3. Amorphous 4-[2-(4-aminopiperidin-1-yl)-5-(3-fluoro-4-methoxyphenyl)-1-methyl-6-oxo-1,6-dihydropyrimidin-4-yl]-2-fluorobenzonitrile besylate was prepared by ball milling Form 1 crystalline 4-[2-(4-aminopiperidin-1-yl)-5-(3-fluoro-4-methoxyphenyl)-1-methyl-6-oxo-1,6-dihydropyrimidin-4-yl]-2-fluorobenzonitrile besylate.
directly linked by a ring-member-to-ring-member bond · CPC title
Antineoplastic agents · CPC title
not condensed and containing further heterocyclic rings · CPC title
containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine · CPC title
as doubly bound oxygen atom or as unsubstituted hydroxy radical · CPC title
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