SALT OF MU-OPIOID RECEPTOR (MOR) AGONIST, CRYSTAL FORM I OF ITS FUMARATE SALT, AND THEIR PRODUCTION METHOD Russian patent published in 2022 - IPC C07D405/04 A61K31/4433 A61P29/00 A61P9/00 A61P11/00 A61P13/00 A61P25/00 A61P37/00 

FIELD: medicine.

SUBSTANCE: invention relates to fumarate salt of (1S,4S)-4-ethoxy-N-(2-((R)-9-(pyridine-2-yl)-6-oxaspiro[4.5]deca-9-yl)ethyl)-1,2,3,4-tetrahydronaphthalene-1-amine, its crystal form I. The crystal form I of fumarate salt of (1S,4S)-4-ethoxy-N-(2-((R)-9-(pyridine-2-yl)-6-oxaspiro[4.5]deca-9-yl)ethyl)-1,2,3,4-tetrahydronaphthalene-1-amine is characterized by a powder X-ray diffractogram represented by means of a diffraction angle 2θ, obtained using Cu-Kα-radiation, and it shows characteristic peaks at diffraction angle 2θ values, which are 5.76, 10.82, 11.47, 12.69, 13.86, 14.77, 15.27, 15.74, 17.26, 17.61, 18.34, 22.39, 23.06, 23.75, and 24.23, while the error range for each of characteristic peaks of 2θ is ±0.2. A method for the production of fumarate salt, according to the invention, includes a stage of a reaction of (1S,4S)-4-ethoxy-N-(2-((R)-9-(pyridine-2-yl)-6-oxaspiro[4.5]deca-9-yl)ethyl)-1,2,3,4-tetrahydronaphthalene-1-amine with fumaric acid. A method for the production of the crystal form I of a compound, according to the invention, includes the dissolution of a compound represented by the formula (I) in a solvent, crystallization, filtration, and drying to obtain the target crystal form I; at the same time, the solvent is tetrahydrofuran; and crystallization is crystallization during cooling, while a colling temperature is a room temperature.

EFFECT: fumarate salt of (1S,4S)-4-ethoxy-N-(2-((R)-9-(pyridine-2-yl)-6-oxaspiro[4.5]deca-9-yl)ethyl)-1,2,3,4-tetrahydronaphthalene-1-amine, used in the manufacture of a drug for the treatment of corresponding diseases mediated by mu-opioid receptor (MOR) agonist, where the specified corresponding diseases mediated by mu-opioid receptor (MOR) agonist are pain.

16 cl, 3 dwg, 2 tbl