CRYSTALLINE FORMS OF 3-(2,6-DICHLORO-3,5-DIMETHOXYPHENYL)-1-{ 6-[4-(4-ETHYLPIPERAZIN-1-YL)-PHENYLAMINO]-PYRIMIDIN-4-YL} -1-METHYLUREA AND ITS FRACTIONS Russian patent published in 2016 - IPC C07D239/48 C07D403/10 A61P35/00 

Abstract RU 2572848 C2

FIELD: chemistry.

SUBSTANCE: invention relates to novel hydrated and anhydrous crystalline forms, as well as to amorphous form of 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-{6-[4-(4-ethylpiperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methylurea of formula (I) and its monophosphoric and hydrochloride salt. Compounds possess properties of inhibitors of activity of kinase, selected from the group, including FGFR1, FGFR2, FGFR3, FGFR4, KDR, HER1, HER2, Bcr-Abl, Tie2 and Ret, and can be used in treatment of diseases, mediated by activity of said kinases. Diseases are selected from the group, including carcinoma of kidneys, liver, adrenal glands, urinary bladder, mammary gland, stomach, ovaries, large intestine, rectum, prostate, pancreas, lungs, vagina or thyroid gland; sarcoma, glioblastoma, leukaemia; tumours of head or neck; psoriasis; prostate gland hyperplasia or neoplasia In particular invention relates to anhydrous crystalline form of formula (I) compound and its monohydrate; to salt of phosphoric acid of formula (I) compound, its anhydrous crystalline forms A and B and its amorphous form; crystalline hydrochloride dehydrate. Crystalline form s are characterised by respective data of powder radiograph, indices of thermogram of differential scanning calorimetry, characteristic peaks of Raman scattering Invention also relates to method for obtaining anhydrous crystalline form A of monophosphoric acid salt.

EFFECT: amorphous form of monophosphoric acid salt does not contain characteristic peaks on powder radiogram, does not demonstrate vitrification in DSC determination and has decomposition temperature 115°C, determined by TGA.

34 cl, 9 dwg, 10 tbl, 21 ex

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RU 2 572 848 C2

Authors

Jerg Bergkhauzen

Prasad Kotesvara Kapa

Dzhozef Makkenna

Dzhoehl Slejd

Rejann Vu

Chzhehnmin Du

Frank Shtovasser

Dates

2016-01-20Published

2010-12-06Filed