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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: wang t. 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.
Biphenyl Acid Derivatives as APJ Receptor Agonists.
Su S, Clarke A, Han Y, Chao HJ, Bostwick J, Schumacher W, Wang T, Yan M, Hsu MY, Simmons E, Luk C, Xu C, Dabros M, Galella M, Onorato J, Gordon D, Wexler R, Gargalovic PS, Lawrence RM. Su S, et al. Among authors: wang t. J Med Chem. 2019 Nov 27;62(22):10456-10465. doi: 10.1021/acs.jmedchem.9b01513. Epub 2019 Nov 14. J Med Chem. 2019. PMID: 31724863
Discovery and SAR of aryl hydroxy pyrimidinones as potent small molecule agonists of the GPCR APJ.
Myers MC, Bilder DM, Cavallaro CL, Chao HJ, Su S, Burford NT, Nayeem A, Wang T, Yan M, Langish RA, Dabros M, Li YX, Rose AV, Behnia K, Onorato JM, Gargalovic PS, Wexler RR, Lawrence RM. Myers MC, et al. Among authors: wang t. Bioorg Med Chem Lett. 2020 Apr 1;30(7):126955. doi: 10.1016/j.bmcl.2020.126955. Epub 2020 Jan 22. Bioorg Med Chem Lett. 2020. PMID: 32035698
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: wang t. 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
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: wang t. 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: wang t. 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 an Oxycyclohexyl Acid Lysophosphatidic Acid Receptor 1 (LPA1) Antagonist BMS-986278 for the Treatment of Pulmonary Fibrotic Diseases.
Cheng PTW, Kaltenbach RF 3rd, Zhang H, Shi J, Tao S, Li J, Kennedy LJ, Walker SJ, Shi Y, Wang Y, Dhanusu S, Reddigunta R, Kumaravel S, Jusuf S, Smith D, Krishnananthan S, Li J, Wang T, Heiry R, Sum CS, Kalinowski SS, Hung CP, Chu CH, Azzara AV, Ziegler M, Burns L, Zinker BA, Boehm S, Taylor J, Sapuppo J, Mosure K, Everlof G, Guarino V, Zhang L, Yang Y, Ruan Q, Xu C, Apedo A, Traeger SC, Cvijic ME, Lentz KA, Tirucherai G, Sivaraman L, Robl J, Ellsworth BA, Rosen G, Gordon DA, Soars MG, Gill M, Murphy BJ. Cheng PTW, et al. Among authors: wang y, wang t. J Med Chem. 2021 Nov 11;64(21):15549-15581. doi: 10.1021/acs.jmedchem.1c01256. Epub 2021 Oct 28. J Med Chem. 2021. PMID: 34709814
Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists.
Shi J, Gu Z, Jurica EA, Wu X, Haque LE, Williams KN, Hernandez AS, Hong Z, Gao Q, Dabros M, Davulcu AH, Mathur A, Rampulla RA, Gupta AK, Jayaram R, Apedo A, Moore DB, Liu H, Kunselman LK, Brady EJ, Wilkes JJ, Zinker BA, Cai H, Shu YZ, Sun Q, Dierks EA, Foster KA, Xu C, Wang T, Panemangalore R, Cvijic ME, Xie C, Cao GG, Zhou M, Krupinski J, Whaley JM, Robl JA, Ewing WR, Ellsworth BA. Shi J, et al. Among authors: wang t. J Med Chem. 2018 Feb 8;61(3):681-694. doi: 10.1021/acs.jmedchem.7b00982. Epub 2018 Jan 27. J Med Chem. 2018. PMID: 29316397
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