POLYCRYSTALLINE FORM OF FREE BASE OR ACID ADDITION SALT OF INHIBITOR EGFR, METHOD OF ITS PRODUCTION AND APPLICATION Russian patent published in 2020 - IPC C07D403/04 A61K31/506 A61P35/00 

Abstract RU 2733412 C2

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to polymorph of N-(5-((4-(1-cyclopropyl-1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide (compound of formula I) in form of mesylate salt, selected from a group consisting of crystalline form I–VI of mesylate salt, wherein said crystalline forms are characterized by X-ray powder diffraction patterns such as given in the claim. Invention also relates to a method of producing crystalline forms of I–VI mesylate salt of a compound of formula I and use thereof.

EFFECT: technical result is crystalline forms of I–VI mesylate salt N-(5-((4-(1-cyclopropyl-1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide, having improved physical and chemical properties, such as degree of crystallinity, solubility, hygroscopicity and chemical stability, and suitable for preparing a drug for treating a disease mediated by EGFR mutant activity or a deletion-activated mutant in exon 19.

12 cl, 22 tbl, 22 ex, 22 dwg

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RU 2 733 412 C2

Authors

Chen Chzhunke

Lyu Fupin

Lyu Lej

Bao Rudi

Dates

2020-10-01Published

2016-12-23Filed