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Page 1
The evolution of P2X7 antagonists with a focus on CNS indications.
Rech JC, Bhattacharya A, Letavic MA, Savall BM. Rech JC, et al. Among authors: savall bm. Bioorg Med Chem Lett. 2016 Aug 15;26(16):3838-45. doi: 10.1016/j.bmcl.2016.06.048. Epub 2016 Jun 30. Bioorg Med Chem Lett. 2016. PMID: 27426304 Review.
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: savall bm. 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: savall bm. 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: savall bm. 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.
Discovery and Characterization of AMPA Receptor Modulators Selective for TARP-γ8.
Maher MP, Wu N, Ravula S, Ameriks MK, Savall BM, Liu C, Lord B, Wyatt RM, Matta JA, Dugovic C, Yun S, Ver Donck L, Steckler T, Wickenden AD, Carruthers NI, Lovenberg TW. Maher MP, et al. Among authors: savall bm. J Pharmacol Exp Ther. 2016 May;357(2):394-414. doi: 10.1124/jpet.115.231712. Epub 2016 Mar 17. J Pharmacol Exp Ther. 2016. PMID: 26989142
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. 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.
Tricyclic aminopyrimidine histamine H4 receptor antagonists.
Savall BM, Gomez L, Chavez F, Curtis M, Meduna SP, Kearney A, Dunford P, Cowden J, Thurmond RL, Grice C, Edwards JP. Savall BM, et al. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6577-81. doi: 10.1016/j.bmcl.2011.08.014. Epub 2011 Aug 19. Bioorg Med Chem Lett. 2011. PMID: 21920744
25 results