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Discovery of Potent and Orally Bioavailable Pyridine N-Oxide-Based Factor XIa Inhibitors through Exploiting Nonclassical Interactions.
Xu G, Liu Z, Wang X, Lu T, DesJarlais RL, Thieu T, Zhang J, Devine ZH, Du F, Li Q, Milligan CM, Shaffer P, Cedervall PE, Spurlino JC, Stratton CF, Pietrak B, Szewczuk LM, Wong V, Steele RA, Bruinzeel W, Chintala M, Silva J, Gaul MD, Macielag MJ, Nargund R. Xu G, et al. Among authors: spurlino jc. J Med Chem. 2022 Aug 11;65(15):10419-10440. doi: 10.1021/acs.jmedchem.2c00442. Epub 2022 Jul 21. J Med Chem. 2022. PMID: 35862732
Orally efficacious thrombin inhibitors with cyanofluorophenylacetamide as the P2 motif.
Kreutter KD, Lu T, Lee L, Giardino EC, Patel S, Huang H, Xu G, Fitzgerald M, Haertlein BJ, Mohan V, Crysler C, Eisennagel S, Dasgupta M, McMillan M, Spurlino JC, Huebert ND, Maryanoff BE, Tomczuk BE, Damiano BP, Player MR. Kreutter KD, et al. Among authors: spurlino jc. Bioorg Med Chem Lett. 2008 May 1;18(9):2865-70. doi: 10.1016/j.bmcl.2008.03.087. Epub 2008 Apr 8. Bioorg Med Chem Lett. 2008. PMID: 18420408
Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif.
Lu T, Markotan T, Ballentine SK, Giardino EC, Spurlino J, Crysler CS, Brown K, Maryanoff BE, Tomczuk BE, Damiano BP, Shukla U, End D, Andrade-Gordon P, Bone RF, Player MR. Lu T, et al. J Med Chem. 2010 Feb 25;53(4):1843-56. doi: 10.1021/jm901802n. J Med Chem. 2010. PMID: 20102150 Clinical Trial.
Identification and structure activity relationships of quinoline tertiary alcohol modulators of RORγt.
Kummer DA, Cummings MD, Abad M, Barbay J, Castro G, Wolin R, Kreutter KD, Maharoof U, Milligan C, Nishimura R, Pierce J, Schalk-Hihi C, Spurlino J, Urbanski M, Venkatesan H, Wang A, Woods C, Xue X, Edwards JP, Fourie AM, Leonard K. Kummer DA, et al. Bioorg Med Chem Lett. 2017 May 1;27(9):2047-2057. doi: 10.1016/j.bmcl.2017.02.044. Epub 2017 Feb 21. Bioorg Med Chem Lett. 2017. PMID: 28318945
Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors.
Qiao L, Baumann CA, Crysler CS, Ninan NS, Abad MC, Spurlino JC, Desjarlais RL, Kervinen J, Neeper MP, Bayoumy SS, Williams R, Deckman IC, Dasgupta M, Reed RL, Huebert ND, Tomczuk BE, Moriarty KJ. Qiao L, et al. Among authors: spurlino jc. Bioorg Med Chem Lett. 2006 Jan 1;16(1):123-8. doi: 10.1016/j.bmcl.2005.09.037. Epub 2005 Oct 19. Bioorg Med Chem Lett. 2006. PMID: 16236500
6-Substituted quinolines as RORγt inverse agonists.
Barbay JK, Cummings MD, Abad M, Castro G, Kreutter KD, Kummer DA, Maharoof U, Milligan C, Nishimura R, Pierce J, Schalk-Hihi C, Spurlino J, Tanis VM, Urbanski M, Venkatesan H, Wang A, Woods C, Wolin R, Xue X, Edwards JP, Fourie AM, Leonard K. Barbay JK, et al. Bioorg Med Chem Lett. 2017 Dec 1;27(23):5277-5283. doi: 10.1016/j.bmcl.2017.10.027. Epub 2017 Oct 16. Bioorg Med Chem Lett. 2017. PMID: 29079472
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
Potent, nonpeptide inhibitors of human mast cell tryptase. Synthesis and biological evaluation of novel spirocyclic piperidine amide derivatives.
Costanzo MJ, Yabut SC, Zhang HC, White KB, de Garavilla L, Wang Y, Minor LK, Tounge BA, Barnakov AN, Lewandowski F, Milligan C, Spurlino JC, Abraham WM, Boswell-Smith V, Page CP, Maryanoff BE. Costanzo MJ, et al. Among authors: spurlino jc. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2114-21. doi: 10.1016/j.bmcl.2008.01.093. Epub 2008 Jan 30. Bioorg Med Chem Lett. 2008. PMID: 18272363
44 results