SALT OF NITROGEN-CONTAINING HETEROCYCLIC COMPOUND OR ITS CRYSTALLINE FORM, PHARMACEUTICAL COMPOSITION AND FLT3 INHIBITOR Russian patent published in 2018 - IPC C07D239/48 A61K31/505 A61P35/02 

Abstract RU 2641106 C2

FIELD: pharmacology.

SUBSTANCE: invention relates to new salts 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 selected from succinate, fumarate, pamoate, hydrochloride, phosphate, sulfate and hydrobromide, as well as crystalline salt forms. The compounds possess the properties of FLT3 (Fms-like tyrosine kinase 3) inhibitor and can be used to treat blood carcinoma including various forms of leukemia, for example acute lymphatic leukemia (ALL), acute myeloid leukemia (AML), acute promyelocytic leukemia (APL), chronic lymphocytic leukemia (CLL), and others. Crystalline α 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 on a powder X-ray diffractogram shows diffraction peaks at diffraction angles of (2θ) 10.5, 17.1, 19.1 and 22.4°; crystalline β succinate of this compound demonstrates diffraction peaks at diffraction angles of (2θ) 12.8, 16.1, 21.4 and 28.0°. Crystalline fumarate of the said compound on a powder X-ray diffractogram shows diffraction peaks at diffraction angles of (2θ) 8.6, 13.7, 17.8 and 23.0°.

EFFECT: salts have storage stability or high solubility.

9 cl, 6 dwg, 10 tbl, 13 ex

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RU 2 641 106 C2

Authors

Midzumoto Sinsuke

Matsumoto Takuya

Dates

2018-01-16Published

2014-10-15Filed