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Page 1
Novel inhibitors of potassium ion channels on human T lymphocytes.
Michne WF, Guiles JW, Treasurywala AM, Castonguay LA, Weigelt CA, Oconnor B, Volberg WA, Grant AM, Chadwick CC, Krafte DS, et al. Michne WF, et al. Among authors: weigelt ca. J Med Chem. 1995 May 26;38(11):1877-83. doi: 10.1021/jm00011a007. J Med Chem. 1995. PMID: 7540207
Discovery of 6-(aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as potent, selective dipeptidyl peptidase-4 (DPP4) inhibitors.
Meng W, Brigance RP, Chao HJ, Fura A, Harrity T, Marcinkeviciene J, O'Connor SP, Tamura JK, Xie D, Zhang Y, Klei HE, Kish K, Weigelt CA, Turdi H, Wang A, Zahler R, Kirby MS, Hamann LG. Meng W, et al. J Med Chem. 2010 Aug 12;53(15):5620-8. doi: 10.1021/jm100634a. J Med Chem. 2010. PMID: 20684603
2-Arylbenzoxazoles as novel cholesteryl ester transfer protein inhibitors: optimization via array synthesis.
Harikrishnan LS, Kamau MG, Herpin TF, Morton GC, Liu Y, Cooper CB, Salvati ME, Qiao JX, Wang TC, Adam LP, Taylor DS, Chen AY, Yin X, Seethala R, Peterson TL, Nirschl DS, Miller AV, Weigelt CA, Appiah KK, O'Connell JC, Michael Lawrence R. Harikrishnan LS, et al. Among authors: weigelt ca. Bioorg Med Chem Lett. 2008 Apr 15;18(8):2640-4. doi: 10.1016/j.bmcl.2008.03.030. Epub 2008 Mar 14. Bioorg Med Chem Lett. 2008. PMID: 18374566
Identification of highly potent and selective PI3Kδ inhibitors.
Marcoux D, Qin LY, Ruan Z, Shi Q, Ruan Q, Weigelt C, Qiu H, Schieven G, Hynes J, Bhide R, Poss M, Tino J. Marcoux D, et al. Among authors: weigelt c. Bioorg Med Chem Lett. 2017 Jul 1;27(13):2849-2853. doi: 10.1016/j.bmcl.2017.01.077. Epub 2017 Feb 7. Bioorg Med Chem Lett. 2017. PMID: 28209465
Optimization of activity, selectivity, and liability profiles in 5-oxopyrrolopyridine DPP4 inhibitors leading to clinical candidate (Sa)-2-(3-(aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b]pyridin-6(7H)-yl)-N,N-dimethylacetamide (BMS-767778).
Devasthale P, Wang Y, Wang W, Fevig J, Feng J, Wang A, Harrity T, Egan D, Morgan N, Cap M, Fura A, Klei HE, Kish K, Weigelt C, Sun L, Levesque P, Moulin F, Li YX, Zahler R, Kirby MS, Hamann LG. Devasthale P, et al. Among authors: weigelt c. J Med Chem. 2013 Sep 26;56(18):7343-57. doi: 10.1021/jm4008906. Epub 2013 Sep 9. J Med Chem. 2013. PMID: 23964740
Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.
Marcoux D, Duan JJ, Shi Q, Cherney RJ, Srivastava AS, Cornelius L, Batt DG, Liu Q, Beaudoin-Bertrand M, Weigelt CA, Khandelwal P, Vishwakrishnan S, Selvakumar K, Karmakar A, Gupta AK, Basha M, Ramlingam S, Manjunath N, Vanteru S, Karmakar S, Maddala N, Vetrichelvan M, Gupta A, Rampulla RA, Mathur A, Yip S, Li P, Wu DR, Khan J, Ruzanov M, Sack JS, Wang J, Yarde M, Cvijic ME, Li S, Shuster DJ, Borowski V, Xie JH, McIntyre KW, Obermeier MT, Fura A, Stefanski K, Cornelius G, Hynes J Jr, Tino JA, Macor JE, Salter-Cid L, Denton R, Zhao Q, Carter PH, Dhar TGM. Marcoux D, et al. J Med Chem. 2019 Nov 14;62(21):9931-9946. doi: 10.1021/acs.jmedchem.9b01369. Epub 2019 Oct 31. J Med Chem. 2019. PMID: 31638797
Discovery of (3S,4S)-3-methyl-3-(4-fluorophenyl)-4-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxyprop-2-yl)phenyl)pyrrolidines as novel RORγt inverse agonists.
Jiang B, Duan JJ, Stachura S, Karmakar A, Hemagiri H, Raut DK, Gupta AK, Weigelt CA, Khan J, Sack JS, Wu DR, Yarde M, Shen DR, Galella MA, Mathur A, Zhao Q, Salter-Cid LM, Carter PH, Dhar TGM. Jiang B, et al. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127392. doi: 10.1016/j.bmcl.2020.127392. Epub 2020 Jul 10. Bioorg Med Chem Lett. 2020. PMID: 32738966
66 results