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Page 1
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. 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 of N-{N-[(3-cyanobenzene) sulfonyl]-4(R)-(3,3-difluoropiperidin-1-yl)-(l)-prolyl}-4-[(3',5'-dichloro-isonicotinoyl) amino]-(l)-phenylalanine (MK-0617), a highly potent and orally active VLA-4 antagonist.
Venkatraman S, Lebsack AD, Alves K, Gardner MF, James J, Lingham RB, Maniar S, Mumford RA, Si Q, Stock N, Treonze KM, Wang B, Zunic J, Munoz B. Venkatraman S, et al. Among authors: lebsack ad. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5803-6. doi: 10.1016/j.bmcl.2009.07.111. Epub 2009 Jul 28. Bioorg Med Chem Lett. 2009. PMID: 19713111
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. 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
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: lebsack ad. 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
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: lebsack ad. 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 JNJ-64264681: A Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
Tichenor MS, Wiener JJM, Rao NL, Bacani GM, Wei J, Pooley Deckhut C, Barbay JK, Kreutter KD, Chang L, Clancy KW, Murrey HE, Wang W, Ahn K, Huber M, Rex E, Coe KJ, Wu J, Rui H, Sepassi K, Gaudiano M, Bekkers M, Cornelissen I, Packman K, Seierstad M, Xiouras C, Bembenek SD, Alexander R, Milligan C, Balasubramanian S, Lebsack AD, Venable JD, Philippar U, Edwards JP, Hirst G. Tichenor MS, et al. Among authors: lebsack ad. J Med Chem. 2022 Nov 10;65(21):14326-14336. doi: 10.1021/acs.jmedchem.2c01026. Epub 2022 Oct 31. J Med Chem. 2022. PMID: 36314537
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: lebsack ad. 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
A Single Amino Acid Difference between Mouse and Human 5-Lipoxygenase Activating Protein (FLAP) Explains the Speciation and Differential Pharmacology of Novel FLAP Inhibitors.
Blevitt JM, Hack MD, Herman K, Chang L, Keith JM, Mirzadegan T, Rao NL, Lebsack AD, Milla ME. Blevitt JM, et al. Among authors: lebsack ad. J Biol Chem. 2016 Jun 10;291(24):12724-12731. doi: 10.1074/jbc.M116.725325. Epub 2016 Apr 16. J Biol Chem. 2016. PMID: 27129215 Free PMC article.
16 results