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Discovery of Imidazo[1,2-a]pyrazines and Pyrazolo[1,5-c]pyrimidines as TARP γ-8 Selective AMPAR Negative Modulators.
Savall BM, Wu D, Swanson DM, Seierstad M, Wu N, Vives Martinez J, García Olmos B, Lord B, Coe K, Koudriakova T, Lovenberg TW, Carruthers NI, Maher MP, Ameriks MK. Savall BM, et al. Among authors: lovenberg tw. ACS Med Chem Lett. 2018 Dec 26;10(3):267-272. doi: 10.1021/acsmedchemlett.8b00599. eCollection 2019 Mar 14. ACS Med Chem Lett. 2018. PMID: 30891124 Free PMC article.
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. Among authors: lovenberg tw. 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
4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate.
Letavic MA, Savall BM, Allison BD, Aluisio L, Andres JI, De Angelis M, Ao H, Beauchamp DA, Bonaventure P, Bryant S, Carruthers NI, Ceusters M, Coe KJ, Dvorak CA, Fraser IC, Gelin CF, Koudriakova T, Liang J, Lord B, Lovenberg TW, Otieno MA, Schoetens F, Swanson DM, Wang Q, Wickenden AD, Bhattacharya A. Letavic MA, et al. Among authors: lovenberg tw. J Med Chem. 2017 Jun 8;60(11):4559-4572. doi: 10.1021/acs.jmedchem.7b00408. Epub 2017 May 25. J Med Chem. 2017. PMID: 28493698
Lead Optimization of 5-Aryl Benzimidazolone- and Oxindole-Based AMPA Receptor Modulators Selective for TARP γ-8.
Ravula S, Savall BM, Wu N, Lord B, Coe K, Wang K, Seierstad M, Swanson DM, Ziff J, Nguyen M, Leung P, Rynberg R, La D, Pippel DJ, Koudriakova T, Lovenberg TW, Carruthers NI, Maher MP, Ameriks MK. Ravula S, et al. Among authors: lovenberg tw. ACS Med Chem Lett. 2018 Jul 13;9(8):821-826. doi: 10.1021/acsmedchemlett.8b00215. eCollection 2018 Aug 9. ACS Med Chem Lett. 2018. PMID: 30128074 Free PMC article.
Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793.
Préville C, Bonaventure P, Koudriakova T, Lord B, Nepomuceno D, Rizzolio M, Mani N, Coe KJ, Ndifor A, Dugovic C, Dvorak CA, Coate H, Pippel DJ, Fitzgerald A, Allison B, Lovenberg TW, Carruthers NI, Shireman BT. Préville C, et al. Among authors: lovenberg tw. ACS Med Chem Lett. 2020 Apr 27;11(10):2002-2009. doi: 10.1021/acsmedchemlett.0c00085. eCollection 2020 Oct 8. ACS Med Chem Lett. 2020. PMID: 33062185 Free PMC article.
Aplysamine-1 and related analogs as histamine H3 receptor antagonists.
Swanson DM, Wilson SJ, Boggs JD, Xiao W, Apodaca R, Barbier AJ, Lovenberg TW, Carruthers NI. Swanson DM, et al. Among authors: lovenberg tw. Bioorg Med Chem Lett. 2006 Feb 15;16(4):897-900. doi: 10.1016/j.bmcl.2005.11.003. Epub 2005 Nov 21. Bioorg Med Chem Lett. 2006. PMID: 16300945
The discovery and synthesis of JNJ 31020028, a small molecule antagonist of the Neuropeptide Y Y₂ receptor.
Swanson DM, Wong VD, Jablonowski JA, Shah C, Rudolph DA, Dvorak CA, Seierstad M, Dvorak LK, Morton K, Nepomuceno D, Atack JR, Bonaventure P, Lovenberg TW, Carruthers NI. Swanson DM, et al. Among authors: lovenberg tw. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5552-6. doi: 10.1016/j.bmcl.2011.06.136. Epub 2011 Jul 18. Bioorg Med Chem Lett. 2011. PMID: 21802951
The discovery of potent selective NPY Y(2) antagonists.
Chai W, Wong VD, Nepomuceno D, Bonaventure P, Lovenberg TW, Carruthers NI. Chai W, et al. Among authors: lovenberg tw. Bioorg Med Chem Lett. 2013 Jul 15;23(14):4141-4. doi: 10.1016/j.bmcl.2013.05.038. Epub 2013 May 22. Bioorg Med Chem Lett. 2013. PMID: 23756063
171 results