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Page 1
The discovery and preclinical characterization of 6-chloro-N-(2-(4,4-difluoropiperidin-1-yl)-2-(2-(trifluoromethyl)pyrimidin-5-yl)ethyl)quinoline-5-carboxamide based P2X7 antagonists.
Rech JC, Bhattacharya A, Branstetter BJ, Love CJ, Leenaerts JE, Cooymans LP, Eckert WA 3rd, Ao H, Wang Q, Chaplan SR, Wickenden AD, Lebsack AD, Breitenbucher JG. Rech JC, et al. Among authors: eckert wa 3rd. Bioorg Med Chem Lett. 2016 Oct 1;26(19):4781-4784. doi: 10.1016/j.bmcl.2016.08.029. Epub 2016 Aug 20. Bioorg Med Chem Lett. 2016. PMID: 27595421
Discovery of a novel series of selective HCN1 blockers.
McClure KJ, Maher M, Wu N, Chaplan SR, Eckert WA 3rd, Lee DH, Wickenden AD, Hermann M, Allison B, Hawryluk N, Breitenbucher JG, Grice CA. McClure KJ, et al. Among authors: eckert wa 3rd. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5197-201. doi: 10.1016/j.bmcl.2011.07.051. Epub 2011 Jul 23. Bioorg Med Chem Lett. 2011. PMID: 21824780
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. Among authors: eckert wa 3rd. 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
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