Salt of nitrogen-containing heterocyclic compound or crystal thereof, pharmaceutical composition, and FLT3 inhibitor

US9701644B2 · US · B2

Patent metadata
FieldValue
Publication numberUS-9701644-B2
Application numberUS-201615130168-A
CountryUS
Kind codeB2
Filing dateApr 15, 2016
Priority dateOct 16, 2013
Publication dateJul 11, 2017
Grant dateJul 11, 2017

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  1. Title

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  2. Abstract

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  3. Assignees and inventors

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  4. Key dates

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  5. First independent claim

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  6. CPC / IPC classifications

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Abstract

Official abstract text for this publication.

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.

First claim

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 .

Assignees

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Classifications

  • specific for leukemia · CPC title

  • Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

  • with carboxyl groups on a condensed ring system containing two rings · CPC title

  • Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim · CPC title

  • One nitrogen atom (nitro radicals C07D239/30) · CPC title

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What does patent US9701644B2 cover?
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 the…
Who is the assignee on this patent?
Fujifilm Corp
What technology area does this patent fall under?
Primary CPC classification C07D239/48. Mapped technology areas include Chemistry & Metallurgy.
When was this patent published?
Publication date Tue Jul 11 2017 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 2 related publications on this page (citations in our corpus or others sharing the same primary CPC).