Nitrogen-containing heterocyclic compound or salt thereof
US-9145415-B2 · Sep 29, 2015 · US
US9701644B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9701644-B2 |
| Application number | US-201615130168-A |
| Country | US |
| Kind code | B2 |
| Filing date | Apr 15, 2016 |
| Priority date | Oct 16, 2013 |
| Publication date | Jul 11, 2017 |
| Grant date | Jul 11, 2017 |
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An object of the present invention is to provide a compound and pharmaceutical composition showing superior stability and/or solubility, etc. and having superior FLT3 inhibitory activity. The present invention provides a salt of (S,E)-N-(1-((5-(2-((4-cyanophenyl)amino)-4-(propylamino)pyrimidin-5-yl)pent-4-yn-1-yl)amino)-1-oxopropan-2-yl)-4-(dimethylamino)-N-methylbut-2-enamide, or a crystal thereof. Since the salt or a crystal thereof has superior FLT3 inhibitory activity and shows superior physicochemical properties as drugs, such as storage stability, solubility, and so forth, it is useful for treatments of diseases or conditions relating to FLT3. The present invention also provides a pharmaceutical composition and FLT3 inhibitor containing the salt or a crystal thereof.
Opening claim text (preview).
The invention claimed is: 1. A crystal of succinate of (S,E)-N-(1-((5-(2-((4-cyanophenyl)amino)-4-(propylamino)pyrimidin-5-yl)pent-4-yn-1-yl)amino)-1-oxopropan-2-yl)-4-(dimethylamino)-N-methylbut-2-enamide, which shows diffraction peaks at diffraction angles (2θ) of 10.5, 17.1, 19.1, and 22.4° in powder X-ray diffractometry, or a crystal of succinate of (S,E)-N-(1-((5-(2-((4-cyanophenyl)amino)-4-(propylamino)pyrimidin-5-yl)pent-4-yn-1-yl)amino)-1-oxopropan-2-yl)-4-(dimethylamino)-N-methylbut-2-enamide, which shows diffraction peaks at diffraction angles (2θ) of 12.8, 16.1, 21.4, and 28.0° in powder X-ray diffractometry, or a crystal of fumarate of (S,E)-N-(1-((5-(2-((4-cyanophenyl)amino)-4-(propylamino)pyrimidin-5-yl)pent-4-yn-1-yl)amino)-1-oxopropan-2-yl)-4-(dimethylamino)-N-methylbut-2-enamide, which shows diffraction peaks at diffraction angles (2θ) of 8.6, 13.7, 17.8, and 23.0° in powder X-ray diffractometry. 2. A pharmaceutical composition containing the crystal according to claim 1 .
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