ACID ADDITION SALT OF TRK INHIBITING COMPOUND Russian patent published in 2019 - IPC C07D401/12 A61K31/506 A61P1/04 A61P11/02 A61P13/02 A61P17/04 A61P17/06 A61P25/02 A61P25/06 A61P29/00 A61P35/00 A61P37/08 A61P43/00 

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds - para-toluenesulphonate and di(p-toluenesulphonate 1-{2-[4-(2-amino-5-chloro-3-pyridinyl)phenoxy]-5-pyrimidinyl}-3-[2-(methylsulphonyl)-5-(trifluoromethyl)phenyl]urea and their crystalline forms. Compounds possess Trk inhibitory activity, stably inhibit increased vascular permeability NGF, are not characterized by interaction with drugs and have excellent solubility and absorption compared to free bases. Para-luoro-sulphonate 1-{2-[4-(2-amino-5-chloro-3-pyridinyl)phenoxy]-5-pyrimidinyl}-3-[2-(methylsulphonyl)-5-(trifluoromethyl)phenyl]urea can represent a crystal which is characterized by powder X-ray diffraction pattern, containing peaks at following values 2θ: 6.35; 7.74; 9.98; 11.08; 11.42; 12.68; 13.22; 14.83; 15.42; 15.98; 16.89; 17.33; 17.86; 18.29; 19.00; 19.46; 20.56; 20.92; 21.47; 22.04; 23.82 and 24.49. Di(p-toluenesulphonate) 1-{2-[4-(2-amino-5-fluoropyridin-3-yl)phenoxy]pyrimidin-5-yl}-3-[2-(pyridin-3-yl)-5-(trifluoromethyl)phenyl]urea can be a crystal and is characterized by powder X-ray diffraction pattern containing peaks at following values 2θ: 6.11; 6.29; 7.76; 9.65; 10.18; 12.30; 12.57; 13.23; 13.59; 14.05; 14.85; 15.47; 16.94; 17.98; 18.52; 18.79; 19.32; 20.58; 21.25; 21.55; 22.11; 22.73; 23.20 and 24.36.

EFFECT: compounds can be used in treating various diseases associated with Trk, such as pain, itching, lower urinary tract disorder, asthma, allergic rhinitis, inflammatory bowel disease, Chagas disease, malignant tumor, and so forth.

5 cl, 18 dwg, 17 tbl, 21 ex