N-{3-3-CYCLOPROPYL-5-(2-FLUORO-4-IODOPHENYLAMINO)-6,8-DIMETHYL-2,4,7-TRIOXO-3,4,6,7-TETRAHYDRO-2H-PYRIDO4,3-DPYRIMIDINE-1-IL-PHENYL}-CYCLOPROPANECARBOXAMIDE DIMETHYLSULFOXIDE SOLVATE AS MEK1/2 INHIBITOR

摘要

FIELD: pharmacology.;SUBSTANCE: invention relates to a new compound, N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodophenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]-phenyl}-cyclopropanecarboxamide dimethylsulfoxide solvate of formula 1 ; , ;which is a MEK, in particular MEK1, MEK2 and MEK1/2, inhibitor. The compound can be used to prevent and/or treat malignant melanomas. The invention also relates to a process for preparation of a compound of formula 1. The method consists in reaction of a compound of formula 2 ; ;or a salt thereof with a cyclopropanecarboxylic acid or an activated derivative thereof, followed by obtaining a crystalline solvate of the desired product while cooling the hot saturated solution in dimethylsulfoxide.;EFFECT: compound has lower toxicity with prolonged dosing.;10 cl, 7 ex, 3 tbl, 2 dwg