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Page 1
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: scott bp. 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
Novel ketooxazole based inhibitors of fatty acid amide hydrolase (FAAH).
Timmons A, Seierstad M, Apodaca R, Epperson M, Pippel D, Brown S, Chang L, Scott B, Webb M, Chaplan SR, Breitenbucher JG. Timmons A, et al. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2109-13. doi: 10.1016/j.bmcl.2008.01.091. Epub 2008 Jan 30. Bioorg Med Chem Lett. 2008. PMID: 18289847
Characterization of 2-(2,6-dichloro-benzyl)-thiazolo[5,4-d]pyrimidin-7-yl]-(4-trifluoromethyl-phenyl)-amine (JNJ-39729209) as a novel TRPV1 antagonist.
Maher MP, Bhattacharya A, Ao H, Swanson N, Wu NT, Freedman J, Kansagara M, Scott B, Li DH, Eckert WA 3rd, Liu Y, Sepassi K, Rizzolio M, Fitzgerald A, Liu J, Branstetter BJ, Rech JC, Lebsack AD, Breitenbucher JG, Wickenden AD, Chaplan SR. Maher MP, et al. Eur J Pharmacol. 2011 Aug 1;663(1-3):40-50. doi: 10.1016/j.ejphar.2011.05.001. Epub 2011 May 10. Eur J Pharmacol. 2011. PMID: 21575625
Identification and synthesis of 2,7-diamino-thiazolo[5,4-d]pyrimidine derivatives as TRPV1 antagonists.
Lebsack AD, Branstetter BJ, Hack MD, Xiao W, Peterson ML, Nasser N, Maher MP, Ao H, Bhattacharya A, Kansagara M, Scott BP, Luo L, Rynberg R, Rizzolio M, Chaplan SR, Wickenden AD, Guy Breitenbucher J. Lebsack AD, et al. Among authors: scott bp. Bioorg Med Chem Lett. 2009 Jan 1;19(1):40-6. doi: 10.1016/j.bmcl.2008.11.024. Epub 2008 Nov 13. Bioorg Med Chem Lett. 2009. PMID: 19038548
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: scott bp. 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
Heteroarylureas with spirocyclic diamine cores as inhibitors of fatty acid amide hydrolase.
Keith JM, Jones WM, Pierce JM, Seierstad M, Palmer JA, Webb M, Karbarz MJ, Scott BP, Wilson SJ, Luo L, Wennerholm ML, Chang L, Brown SM, Rizzolio M, Rynberg R, Chaplan SR, Breitenbucher JG. Keith JM, et al. Among authors: scott bp. Bioorg Med Chem Lett. 2014 Feb 1;24(3):737-41. doi: 10.1016/j.bmcl.2013.12.113. Epub 2014 Jan 6. Bioorg Med Chem Lett. 2014. PMID: 24433863
1-Aryl-2-((6-aryl)pyrimidin-4-yl)amino)ethanols as competitive inhibitors of fatty acid amide hydrolase.
Keith JM, Hawryluk N, Apodaca RL, Chambers A, Pierce JM, Seierstad M, Palmer JA, Webb M, Karbarz MJ, Scott BP, Wilson SJ, Luo L, Wennerholm ML, Chang L, Rizzolio M, Chaplan SR, Breitenbucher JG. Keith JM, et al. Among authors: scott bp. Bioorg Med Chem Lett. 2014 Mar 1;24(5):1280-4. doi: 10.1016/j.bmcl.2014.01.064. Epub 2014 Jan 31. Bioorg Med Chem Lett. 2014. PMID: 24513048
The SAR of brain penetration for a series of heteroaryl urea FAAH inhibitors.
Keith JM, Tichenor MS, Apodaca RL, Xiao W, Jones WM, Seierstad M, Pierce JM, Palmer JA, Webb M, Karbarz MJ, Scott BP, Wilson SJ, Wennerholm ML, Rizzolio M, Rynberg R, Chaplan SR, Breitenbucher JG. Keith JM, et al. Among authors: scott bp. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3109-3114. doi: 10.1016/j.bmcl.2016.05.001. Epub 2016 May 5. Bioorg Med Chem Lett. 2016. PMID: 27189675
Heteroarylureas with fused bicyclic diamine cores as inhibitors of fatty acid amide hydrolase.
Keith JM, Jones W, Pierce JM, Seierstad M, Palmer JA, Webb M, Karbarz M, Scott BP, Wilson SJ, Luo L, Wennerholm M, Chang L, Rizzolio M, Rynberg R, Chaplan S, Guy Breitenbucher J. Keith JM, et al. Among authors: scott bp. Bioorg Med Chem Lett. 2020 Oct 15;30(20):127463. doi: 10.1016/j.bmcl.2020.127463. Epub 2020 Aug 9. Bioorg Med Chem Lett. 2020. PMID: 32784090
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
Keith JM, Apodaca R, Xiao W, Seierstad M, Pattabiraman K, Wu J, Webb M, Karbarz MJ, Brown S, Wilson S, Scott B, Tham CS, Luo L, Palmer J, Wennerholm M, Chaplan S, Breitenbucher JG. Keith JM, et al. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4838-43. doi: 10.1016/j.bmcl.2008.07.081. Epub 2008 Jul 25. Bioorg Med Chem Lett. 2008. PMID: 18693015
33 results