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Page 1
Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[d]thiazol-5-ylamino)-6-(tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl Dihydrogen Phosphate, for the Treatment of Inflammatory Diseases.
Haile PA, Casillas LN, Votta BJ, Wang GZ, Charnley AK, Dong X, Bury MJ, Romano JJ, Mehlmann JF, King BW, Erhard KF, Hanning CR, Lipshutz DB, Desai BM, Capriotti CA, Schaeffer MC, Berger SB, Mahajan MK, Reilly MA, Nagilla R, Rivera EJ, Sun HH, Kenna JK, Beal AM, Ouellette MT, Kelly M, Stemp G, Convery MA, Vossenkämper A, MacDonald TT, Gough PJ, Bertin J, Marquis RW. Haile PA, et al. Among authors: convery ma. J Med Chem. 2019 Jul 25;62(14):6482-6494. doi: 10.1021/acs.jmedchem.9b00575. Epub 2019 Jul 2. J Med Chem. 2019. PMID: 31265286
Design and synthesis of orally active pyrrolidin-2-one-based factor Xa inhibitors.
Watson NS, Brown D, Campbell M, Chan C, Chaudry L, Convery MA, Fenwick R, Hamblin JN, Haslam C, Kelly HA, King NP, Kurtis CL, Leach AR, Manchee GR, Mason AM, Mitchell C, Patel C, Patel VK, Senger S, Shah GP, Weston HE, Whitworth C, Young RJ. Watson NS, et al. Among authors: convery ma. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3784-8. doi: 10.1016/j.bmcl.2006.04.053. Epub 2006 May 11. Bioorg Med Chem Lett. 2006. PMID: 16697194
Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides.
Chan C, Borthwick AD, Brown D, Burns-Kurtis CL, Campbell M, Chaudry L, Chung CW, Convery MA, Hamblin JN, Johnstone L, Kelly HA, Kleanthous S, Patikis A, Patel C, Pateman AJ, Senger S, Shah GP, Toomey JR, Watson NS, Weston HE, Whitworth C, Young RJ, Zhou P. Chan C, et al. Among authors: convery ma. J Med Chem. 2007 Apr 5;50(7):1546-57. doi: 10.1021/jm060870c. Epub 2007 Mar 6. J Med Chem. 2007. PMID: 17338508
Selective and dual action orally active inhibitors of thrombin and factor Xa.
Young RJ, Brown D, Burns-Kurtis CL, Chan C, Convery MA, Hubbard JA, Kelly HA, Pateman AJ, Patikis A, Senger S, Shah GP, Toomey JR, Watson NS, Zhou P. Young RJ, et al. Among authors: convery ma. Bioorg Med Chem Lett. 2007 May 15;17(10):2927-30. doi: 10.1016/j.bmcl.2007.03.080. Epub 2007 Mar 30. Bioorg Med Chem Lett. 2007. PMID: 17420122
Structure and property based design of factor Xa inhibitors: biaryl pyrrolidin-2-ones incorporating basic heterocyclic motifs.
Young RJ, Borthwick AD, Brown D, Burns-Kurtis CL, Campbell M, Chan C, Charbaut M, Convery MA, Diallo H, Hortense E, Irving WR, Kelly HA, King NP, Kleanthous S, Mason AM, Pateman AJ, Patikis AN, Pinto IL, Pollard DR, Senger S, Shah GP, Toomey JR, Watson NS, Weston HE, Zhou P. Young RJ, et al. Among authors: convery ma. Bioorg Med Chem Lett. 2008 Jan 1;18(1):28-33. doi: 10.1016/j.bmcl.2007.11.019. Epub 2007 Nov 13. Bioorg Med Chem Lett. 2008. PMID: 18053714
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with biaryl P4 motifs.
Young RJ, Borthwick AD, Brown D, Burns-Kurtis CL, Campbell M, Chan C, Charbaut M, Chung CW, Convery MA, Kelly HA, Paul King N, Kleanthous S, Mason AM, Pateman AJ, Patikis AN, Pinto IL, Pollard DR, Senger S, Shah GP, Toomey JR, Watson NS, Weston HE. Young RJ, et al. Among authors: convery ma. Bioorg Med Chem Lett. 2008 Jan 1;18(1):23-7. doi: 10.1016/j.bmcl.2007.11.023. Epub 2007 Nov 17. Bioorg Med Chem Lett. 2008. PMID: 18054228
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with monoaryl P4 motifs.
Kleanthous S, Borthwick AD, Brown D, Burns-Kurtis CL, Campbell M, Chaudry L, Chan C, Clarte MO, Convery MA, Harling JD, Hortense E, Irving WR, Irvine S, Pateman AJ, Patikis AN, Pinto IL, Pollard DR, Roethka TJ, Senger S, Shah GP, Stelman GJ, Toomey JR, Watson NS, West RI, Whittaker C, Zhou P, Young RJ. Kleanthous S, et al. Among authors: convery ma. Bioorg Med Chem Lett. 2010 Jan 15;20(2):618-22. doi: 10.1016/j.bmcl.2009.11.077. Epub 2009 Nov 20. Bioorg Med Chem Lett. 2010. PMID: 20006499
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with aminoindane and phenylpyrrolidine P4 motifs.
Young RJ, Adams C, Blows M, Brown D, Burns-Kurtis CL, Chan C, Chaudry L, Convery MA, Davies DE, Exall AM, Foster G, Harling JD, Hortense E, Irvine S, Irving WR, Jackson S, Kleanthous S, Pateman AJ, Patikis AN, Roethka TJ, Senger S, Stelman GJ, Toomey JR, West RI, Whittaker C, Zhou P, Watson NS. Young RJ, et al. Among authors: convery ma. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1582-7. doi: 10.1016/j.bmcl.2011.01.131. Epub 2011 Feb 1. Bioorg Med Chem Lett. 2011. PMID: 21349710
The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs.
Watson NS, Adams C, Belton D, Brown D, Burns-Kurtis CL, Chaudry L, Chan C, Convery MA, Davies DE, Exall AM, Harling JD, Irvine S, Irving WR, Kleanthous S, McLay IM, Pateman AJ, Patikis AN, Roethke TJ, Senger S, Stelman GJ, Toomey JR, West RI, Whittaker C, Zhou P, Young RJ. Watson NS, et al. Among authors: convery ma. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1588-92. doi: 10.1016/j.bmcl.2011.01.129. Epub 2011 Feb 2. Bioorg Med Chem Lett. 2011. PMID: 21349711
Encoded library technology as a source of hits for the discovery and lead optimization of a potent and selective class of bactericidal direct inhibitors of Mycobacterium tuberculosis InhA.
Encinas L, O'Keefe H, Neu M, Remuiñán MJ, Patel AM, Guardia A, Davie CP, Pérez-Macías N, Yang H, Convery MA, Messer JA, Pérez-Herrán E, Centrella PA, Alvarez-Gómez D, Clark MA, Huss S, O'Donovan GK, Ortega-Muro F, McDowell W, Castañeda P, Arico-Muendel CC, Pajk S, Rullás J, Angulo-Barturen I, Alvarez-Ruíz E, Mendoza-Losana A, Ballell Pages L, Castro-Pichel J, Evindar G. Encinas L, et al. Among authors: convery ma. J Med Chem. 2014 Feb 27;57(4):1276-88. doi: 10.1021/jm401326j. Epub 2014 Feb 5. J Med Chem. 2014. PMID: 24450589
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