NOVEL SALT OF 3-[(3-{[4-(4-MORPHOLINYLMETHYL)-1H-PYRROL-2-YL]METHYLENE}-2-OXO-2,3-DIHYDRO-1H-INDOL-5-YL)METHYL]1,3-THIAZOLIDINE-2,4-DIONE, PREPARATION THEREOF AND FORMULATIONS CONTAINING SAME Russian patent published in 2019 - IPC C07D417/14 A61K31/5377 A61K31/4025 A61K31/403 A61K31/427 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to methanesulphonate of 3-[(3-{[4(4-morpholinylmethyl)-1H-pyrrol-2-yl]methylene}-2-oxo-2,3-dihydro-1H-indole-5-yl)methyl]-1,3-thiazolidine-2,4-dione of formula (II), where the notation means that the double bond has the configuration Z or E. Said compound according to the invention, which is the Z-isomer of methanesulphonate of 3-[(3-{[4-(4-morpholinylmethyl)-1H-pyrrol-2-yl]methylene}-2-oxo-2,3-dihydro-1H-indole-5-yl)methyl]-1,3-thiazolidin-2,4-dione, is characterized by an x-ray powder diffractogram with Bragg angles of 2 theta (expressed in °±0.2) 12.86; 15.13; 15.50; 17.70; 18.25; 18.71; 20.11; 21.46; 21.67; 21.89; 22.29; 22.58; 24.57; 25.82; 26.33. Said compounds of formula (II) are obtained by using as a starting material 3-[(3-{[4-(4-morpholinylmethyl)-1H-pyrrol-2-yl]methylene}-2-oxo-2,3-dihydro-1H-indole-5-yl)methyl]-1,3-thiazolidin-2,4-dione, which is dissolved in a binary solvent / water system, and then from 1 to 2 molar equivalents of methanesulphonic acid are added, stirred until methanesulphonate is precipitated, which is then filtered off.

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EFFECT: methanesulphonate of 3-[(3-{[4-(4-morpholinylmethyl)-1H-pyrrol-2-yl]methylene}-2-oxo-2,3-dihydro-1H-indole-5-yl)methyl]-1,3-thiazolidin-2,4-dione of formula (II) is intended for use in the manufacture of drugs for use in treatment of cancer and has improved solubility.

8 cl, 2 dwg, 2 tbl, 5 ex