Discovery and SAR of 6-alkyl-2, 4-diaminopyrimidines as histamine H4 receptor antagonists

BM Savall, F Chavez, K Tays, PJ Dunford…

文献索引：Savall, Brad M.; Chavez, Frank; Tays, Kevin; Dunford, Paul J.; Cowden, Jeffery M.; Hack, Michael D.; Wolin, Ronald L.; Thurmond, Robin L.; Edwards, James P. Journal of Medicinal Chemistry, 2014 , vol. 57, # 6 p. 2429 - 2439

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被引用次数: 18

摘要

This report discloses the discovery and SAR of a series of 6-alkyl-2-aminopyrimidine derived histamine H4 antagonists that led to the development of JNJ 39758979, which has been studied in phase II clinical trials in asthma and atopic dermatitis. Building on our SAR studies of saturated derivatives from the indole carboxamide series, typified by JNJ 7777120, and incorporating knowledge from the tricyclic pyrimidines led us to the 6-alkyl-2, 4- ...