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Identification of 6-Hydroxypyrimidin-4(1H)-one-3-carboxamides as Potent and Orally Active APJ Receptor Agonists.
Pi Z, Johnson JA, Meng W, Phillips M, Schumacher WA, Bostwick JS, Gargalovic PS, Onorato JM, Generaux CN, Wang T, He Y, Gordon DA, Wexler RR, Finlay HJ. Pi Z, et al. Among authors: generaux cn. ACS Med Chem Lett. 2021 Oct 22;12(11):1766-1772. doi: 10.1021/acsmedchemlett.1c00385. eCollection 2021 Nov 11. ACS Med Chem Lett. 2021. PMID: 34795866 Free PMC article.
Design and preparation of N-linked hydroxypyridine-based APJ agonists.
Richter JM, Alex Bates J, Gargalovic P, Onorato JM, Generaux C, Wang T, Gordon DA, Wexler RR, Finlay HJ. Richter JM, et al. Among authors: generaux c. Bioorg Med Chem Lett. 2022 Oct 1;73:128882. doi: 10.1016/j.bmcl.2022.128882. Epub 2022 Jul 8. Bioorg Med Chem Lett. 2022. PMID: 35817293
In Vitro and In Vivo Evaluation of a Small-Molecule APJ (Apelin Receptor) Agonist, BMS-986224, as a Potential Treatment for Heart Failure.
Gargalovic P, Wong P, Onorato J, Finlay H, Wang T, Yan M, Crain E, St-Onge S, Héroux M, Bouvier M, Xu C, Chen XQ, Generaux C, Lawrence M, Wexler R, Gordon D. Gargalovic P, et al. Among authors: generaux c. Circ Heart Fail. 2021 Mar;14(3):e007351. doi: 10.1161/CIRCHEARTFAILURE.120.007351. Epub 2021 Mar 5. Circ Heart Fail. 2021. PMID: 33663236 Free PMC article.
Discovery of a Hydroxypyridinone APJ Receptor Agonist as a Clinical Candidate.
Johnson JA, Kim SH, Jiang J, Phillips M, Schumacher WA, Bostwick JS, Gargalovic PS, Onorato JM, Luk CE, Generaux C, He Y, Chen XQ, Xu C, Galella MA, Wang T, Gordon DA, Wexler RR, Finlay HJ. Johnson JA, et al. Among authors: generaux c. J Med Chem. 2021 Mar 25;64(6):3086-3099. doi: 10.1021/acs.jmedchem.0c01878. Epub 2021 Mar 9. J Med Chem. 2021. PMID: 33689340
Linking (Pyr)1apelin-13 pharmacokinetics to efficacy: Stabilization and measurement of a high clearance peptide in rodents.
Onorato JM, Xu C, Chen XQ, Rose AV, Generaux C, Lentz K, Shipkova P, Arthur S, Hennan JK, Haskell R, Myers MC, Lawrence RM, Finlay HJ, Basso M, Bostwick J, Fernando G, Garcia R, Hellings S, Hsu MY, Zhang R, Zhao L, Gargalovic P. Onorato JM, et al. Among authors: generaux c. Anal Biochem. 2019 Mar 1;568:41-50. doi: 10.1016/j.ab.2018.12.022. Epub 2018 Dec 31. Anal Biochem. 2019. PMID: 30605634
18 results