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
Title | Year | Author | Number |
---|---|---|---|
SALT OF MONOCYCLIC DERIVATIVE OF PYRIDINE AND CRYSTAL THEREOF | 2015 |
|
RU2658821C1 |
UREA DERIVATIVE | 2017 |
|
RU2768587C2 |
INDAZOLE DERIVATIVE SALTS AND THEIR CRYSTALS | 2017 |
|
RU2747399C2 |
METHOD OF PRODUCING NITROGEN-CONTAINING HETEROCYCLIC COMPOUND AND INTERMEDIATE COMPOUND THEREOF | 2016 |
|
RU2717830C2 |
METHOD FOR PRODUCTION OF 7H-PYRROLO[2,3-D]PYRIMIDINE DERIVATIVES AND THEIR COCRYSTALS | 2017 |
|
RU2779212C2 |
PHARMACEUTICAL COMPOSITION CONTAINING OPTICALLY ACTIVE COMPOUND POSSESSING ACTIVITY OF THROMBOPOIETIN RECEPTOR AGONIST, AND INTERMEDIATE COMPOUND THEREFOR | 2008 |
|
RU2476429C2 |
CRYSTAL OF AZOLE BENZENE DERIVATIVE | 2015 |
|
RU2675854C2 |
SALT OF PYRAZOLOQUINOLINE DERIVATIVE AND CRYSTAL THEREOF | 2014 |
|
RU2655171C2 |
PYRIDONE DERIVATIVE HAVING TETRAHYDROPYRANYLMETHYL GROUP | 2015 |
|
RU2707953C2 |
METHOD FOR OBTAINING A DERIVATIVE OF 7H-PYRROLO[2,3-D] PYRIMIDINE AND ITS INTERMEDIATE | 2016 |
|
RU2755618C2 |
Authors
Dates
2018-01-16—Published
2014-10-15—Filed