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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. 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
Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor.
Swanson DM, Savall BM, Coe KJ, Schoetens F, Koudriakova T, Skaptason J, Wall J, Rech J, Deng X, De Angelis M, Everson A, Lord B, Wang Q, Ao H, Scott B, Sepassi K, Lovenberg TW, Carruthers NI, Bhattacharya A, Letavic MA. Swanson DM, et al. J Med Chem. 2016 Sep 22;59(18):8535-48. doi: 10.1021/acs.jmedchem.6b00989. Epub 2016 Sep 8. J Med Chem. 2016. PMID: 27548392
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: rech jc. 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
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: rech jc. 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
Synthesis and Pharmacological Characterization of Two Novel, Brain Penetrating P2X7 Antagonists.
Letavic MA, Lord B, Bischoff F, Hawryluk NA, Pieters S, Rech JC, Sales Z, Velter AI, Ao H, Bonaventure P, Contreras V, Jiang X, Morton KL, Scott B, Wang Q, Wickenden AD, Carruthers NI, Bhattacharya A. Letavic MA, et al. Among authors: rech jc. ACS Med Chem Lett. 2013 Mar 12;4(4):419-22. doi: 10.1021/ml400040v. eCollection 2013 Apr 11. ACS Med Chem Lett. 2013. PMID: 24900687 Free PMC article.
Novel methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones are P2X7 antagonists.
Rudolph DA, Alcazar J, Ameriks MK, Anton AB, Ao H, Bonaventure P, Carruthers NI, Chrovian CC, De Angelis M, Lord B, Rech JC, Wang Q, Bhattacharya A, Andres JI, Letavic MA. Rudolph DA, et al. Among authors: rech jc. Bioorg Med Chem Lett. 2015 Aug 15;25(16):3157-63. doi: 10.1016/j.bmcl.2015.06.004. Epub 2015 Jun 9. Bioorg Med Chem Lett. 2015. PMID: 26099534
27 results