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Page 1
1H-Pyrrolo[3,2-b]pyridine GluN2B-Selective Negative Allosteric Modulators.
Chrovian CC, Soyode-Johnson A, Wall JL, Rech JC, Schoellerman J, Lord B, Coe KJ, Carruthers NI, Nguyen L, Jiang X, Koudriakova T, Balana B, Letavic MA. Chrovian CC, et al. Among authors: coe kj. ACS Med Chem Lett. 2019 Jan 10;10(3):261-266. doi: 10.1021/acsmedchemlett.8b00542. eCollection 2019 Mar 14. ACS Med Chem Lett. 2019. PMID: 30891123 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: coe kj. 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: coe kj. 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
A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate.
Chrovian CC, Soyode-Johnson A, Peterson AA, Gelin CF, Deng X, Dvorak CA, Carruthers NI, Lord B, Fraser I, Aluisio L, Coe KJ, Scott B, Koudriakova T, Schoetens F, Sepassi K, Gallacher DJ, Bhattacharya A, Letavic MA. Chrovian CC, et al. Among authors: coe kj. J Med Chem. 2018 Jan 11;61(1):207-223. doi: 10.1021/acs.jmedchem.7b01279. Epub 2017 Dec 20. J Med Chem. 2018. PMID: 29211470
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. 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 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.
Optimization and biological evaluation of thiazole-bis-amide inverse agonists of RORγt.
Gege C, Albers M, Kinzel O, Kleymann G, Schlüter T, Steeneck C, Hoffmann T, Xue X, Cummings MD, Spurlino J, Milligan C, Fourie AM, Edwards JP, Leonard K, Coe K, Scott B, Pippel D, Goldberg SD. Gege C, et al. Bioorg Med Chem Lett. 2020 Jun 15;30(12):127205. doi: 10.1016/j.bmcl.2020.127205. Epub 2020 Apr 21. Bioorg Med Chem Lett. 2020. PMID: 32336498
Design, Synthesis, and Preclinical Evaluation of 3-Methyl-6-(5-thiophenyl)-1,3-dihydro-imidazo[4,5-b]pyridin-2-ones as Selective GluN2B Negative Allosteric Modulators for the Treatment of Mood Disorders.
Chrovian CC, Soyode-Johnson A, Stenne B, Pippel DJ, Schoellerman J, Lord B, Needham AS, Xia C, Coe KJ, Sepassi K, Schoetens F, Scott B, Nguyen L, Jiang X, Koudriakova T, Balana B, Letavic MA. Chrovian CC, et al. Among authors: coe kj. J Med Chem. 2020 Sep 10;63(17):9181-9196. doi: 10.1021/acs.jmedchem.9b02113. Epub 2020 Aug 28. J Med Chem. 2020. PMID: 32787105
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: coe kj. 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.
Discovery of a Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase with Oral Anti-Inflammatory Activity.
Tichenor MS, Wiener JJM, Rao NL, Pooley Deckhut C, Barbay JK, Kreutter KD, Bacani GM, Wei J, Chang L, Murrey HE, Wang W, Ahn K, Huber M, Rex E, Coe KJ, Wu J, Seierstad M, Bembenek SD, Leonard KA, Lebsack AD, Venable JD, Edwards JP. Tichenor MS, et al. Among authors: coe kj. ACS Med Chem Lett. 2021 Apr 5;12(5):782-790. doi: 10.1021/acsmedchemlett.1c00044. eCollection 2021 May 13. ACS Med Chem Lett. 2021. PMID: 34055226 Free PMC article.
23 results