PYRROPHYRIMIDINE COMPOUNDS RELATED TO A2b-SELECTIVE ANTAGONISTS, THEIR SYNTHESIS AND APPLICATION

摘要

The present invention relates to compounds of the structure where R is a substituted or unsubstituted alkyl, where the substituent is hydroxyl, dihydroxy, carboxyl, -C (= O) NRR, -NRR, -NRC (= O) NRR, -NRC (= O) OR, -OC (= O) NRR or -NHC (= O) R; R5 is hydrogen, or substituted or unsubstituted alkyl, where the substituent is hydroxyl, dihydroxy, carboxyl, -C (= O) NRR, -NRR, -NRC (= O) NRR, -NRC (= O) OR, -OC ( = O) NRR or -NHC (= O) R, or R, R and N together form a substituted piperazine, a substituted azetidine ring or a pyrrolidine ring, substituted with - (CH) OH or -CHC (= O) OH; R4 is a substituted or unsubstituted phenyl, or a 5-6 membered heteroaryl ring, where the substituent is a halogen, hydroxyl, cyano, (C-C) alkyl, (C-C) alkoxy, or -NRR; R 5 is hydrogen, or substituted or unsubstituted (C-C) alkyl; R5 is - (CH) OR, -CHNOR, -C (= O) NRR, - (CH) C (= O) OR, - (CH) C (= O) NRR; wherein R2 is a substituted or unsubstituted (C-C) alkyl, (C-C) cycloalkyl or aryl, heteroaryl or 4-8 membered heterocyclic ring; R 5 is hydrogen or substituted or unsubstituted (C-C) alkyl, (C-C) alkylaryl; each R and R independently is hydrogen or a substituted or unsubstituted (CC) alkyl, (CC) alkylaryl, (CC) alkylamino group, (CC) alkoxy group or saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic ring, or R, N and R together form substituted or unsubstituted 4-8 membered heterocyclic ring; R4 is hydrogen, or a substituted or unsubstituted (C-C) alkyl, (C-C) cycloalkyl, or aryl, heteroaryl or heterocyclic ring; R, N and R together form a 4-8 membered heterocyclic ring; each R and R independently is hydrogen or alkyl; m is 0, 1, 2 or 3; and k is 1, 2 or 3; or their specific