参考标题:Discovery And Synthesis Of 6,7,8,9-Tetrahydro-5H-Pyrimido-[4,5-D]Azepines As Novel Trpv1 Antagonists 作者:Natalie A. Hawryluk,Jeffrey E. Merit,Alec D. Lebsack,Bryan J. Branstetter,Michael D. Hack,Nadia Swanson,Hong Ao,Michael P. Maher,Anindya Bhattacharya,Qi Wang,Jamie M. Freedman,Brian P. Scott,Alan D. Wickenden,Sandra R. Chaplan,J. Guy Breitenbucher |发布日期:2010.12 摘要:Utilization Of A Tetrahydro-Pyrimdoazepine Core As A Bioisosteric Replacement For A Piperazine-Urea Resulted In The Discovery A Novel Series Of Potent Antagonists Of Trpv1. The Tetrahydro-Pyrimdoazepines Have Been Identified As Having Good In Vitro And In Vivo Potency And Acceptable Physical Properties.