PYRIMIDINE DERIVATIVES AND THEIR APPLICATION IN TREATMENT OF RESPIRATORY DISEASES SUCH AS COPD

摘要

1. The compound of formula (I): wherein A is C-R or N; R and R are selected from hydrogen, halogen, nitro, cyano, —S (O) R, amino, mono- or di-CC-alkylamino, —NHCOR, - NH (C = O) NHR, —NHSOR, CC-alkyl, CC-alkenyl, CC-alkynyl, hydroxyl, CC-alkoxy or CC-alkenyloxy, where CC-alkyl and CC-alkoxy may be further substituted with one to three identical or different radicals selected from the group consisting of halogen, hydroxy and CC-alkoxy; n is 0, 1 or 2; R is hydrogen; R and R are independently selected from hydrogen, halogen and CC-alkyl, which may be further substituted by loghene; R is selected from hydrogen, nitrile (-CN), -COOH, -COOR, -COR, -SOR, -CONH, -SONH, -CONHR, -SONHR, -CONRR, -SONRR and heteroaryl, where R and R are independently optionally substituted (CC) alkyl, phenyl or monocyclic heteroaryl having 5 or 6 atoms in the ring, or R and R, when they are attached to the same nitrogen atom, form a cyclic amine ring; R is selected from CC-alkyl, hydroxy-CC-alkyl, CC-alkoxy, amino, mono- or di-CC-alkylamino, hydroxycarbonyl, aminocarbonyl, CC-cycloalkyl, phenyl or CC-alkenyl, where C-C-cycloalkyl may be substituted with one or more CC-alkyl ohm, hydroxyl and CC-alkoxy, and phenyl may be substituted with one or more halogen, cyano, CC-alkyl, difluoromethyl, trifluoromethyl, difluoromethoxy, trifluoromethoxy and CC-alkoxy; R and R are independently selected from hydrogen and CC-alkyl, and R is CC -alkyl; -XX- represents -CR = N- or -NR-CO-; R and R, each independently, represent a radical of the formula - [Y] - [Alk] - [Q] - [Alk] -Z, where Y represents -O-, -S-, -NR-, - (С = O) -, -S (O) -, -С (= O) O-, - (C = O) NR-, -NR ( C = O) -, -NR-CC-alkyl- or -C-C-alkyl-NR-, -S (O) NR-, -NRS (O) -, where R is hydrogen, CC-alkyl; m, p, q and t independently mean 0 or 1; Alk and Alk, each not