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1,2-diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepines as TRPV1 antagonists with improved properties.
Lebsack AD, Rech JC, Branstetter BJ, Hawryluk NA, Merit JE, Allison B, Rynberg R, Buma J, Rizzolio M, Swanson N, Ao H, Maher MP, Herrmann M, Freedman J, Scott BP, Luo L, Bhattacharya A, Wang Q, Chaplan SR, Wickenden AD, Breitenbucher JG. Lebsack AD, et al. Among authors: merit je. Bioorg Med Chem Lett. 2010 Dec 1;20(23):7142-6. doi: 10.1016/j.bmcl.2010.09.006. Epub 2010 Sep 7. Bioorg Med Chem Lett. 2010. PMID: 20932750
Heteroaryl urea inhibitors of fatty acid amide hydrolase: structure-mutagenicity relationships for arylamine metabolites.
Tichenor MS, Keith JM, Jones WM, Pierce JM, Merit J, Hawryluk N, Seierstad M, Palmer JA, Webb M, Karbarz MJ, Wilson SJ, Wennerholm ML, Woestenborghs F, Beerens D, Luo L, Brown SM, Boeck MD, Chaplan SR, Breitenbucher JG. Tichenor MS, et al. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7357-62. doi: 10.1016/j.bmcl.2012.10.076. Epub 2012 Oct 22. Bioorg Med Chem Lett. 2012. PMID: 23141911
Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-[4,5-d]azepines as novel TRPV1 antagonists.
Hawryluk NA, Merit JE, Lebsack AD, Branstetter BJ, Hack MD, Swanson N, Ao H, Maher MP, Bhattacharya A, Wang Q, Freedman JM, Scott BP, Wickenden AD, Chaplan SR, Breitenbucher JG. Hawryluk NA, et al. Among authors: merit je. Bioorg Med Chem Lett. 2010 Dec 1;20(23):7137-41. doi: 10.1016/j.bmcl.2010.09.023. Epub 2010 Sep 17. Bioorg Med Chem Lett. 2010. PMID: 20947352