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 with halogen; R selected from CC-alkyl, hydroxy-CC-alkyl, CC-alkoxy, amino, mono- or di-CC-alkylamino, hydroxycarbonyl, aminocarbonyl, CC-cycloalkyl, phenyl or CC-alkenyl, where CC-cycloalkyl may be substituted one or more CC-alkyl, 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; R is —COR, —CONRR or —COR; —X — X — represents —CR = N— or —NR — CO—; R 1 is hydrogen or C 1-6 alkyl; R, R, R 1 each independently represents a radical of the formula - [Alk] [Q] - [Alk] -Z, where p, q and t independently mean 0 or 1, provided that p, q and t simultaneously does not mean 0; Alk and Alk each independently represents a CC alkylene radical; Q represents a divalent mono- or bicyclic carbocyclic or heterocyclic radical having 3 to 9 members in the ring; Z represents (1) a monocyclic heterocyclic ring of 5 or 6 members in a ring or a bridging heterocyclic ring system of 7 or 8