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Page 1
Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.
Gellibert F, de Gouville AC, Woolven J, Mathews N, Nguyen VL, Bertho-Ruault C, Patikis A, Grygielko ET, Laping NJ, Huet S. Gellibert F, et al. Among authors: patikis a. J Med Chem. 2006 Apr 6;49(7):2210-21. doi: 10.1021/jm0509905. J Med Chem. 2006. PMID: 16570917
Design and synthesis of pyrrolidine-5,5'-trans-lactams (5-oxo-hexahydropyrrolo[3,2-b]pyrroles) as novel mechanism-based inhibitors of human cytomegalovirus protease. 4. Antiviral activity and plasma stability.
Borthwick AD, Davies DE, Ertl PF, Exall AM, Haley TM, Hart GJ, Jackson DL, Parry NR, Patikis A, Trivedi N, Weingarten GG, Woolven JM. Borthwick AD, et al. Among authors: patikis a. J Med Chem. 2003 Oct 9;46(21):4428-49. doi: 10.1021/jm030810w. J Med Chem. 2003. PMID: 14521407
The design of potent, non-peptidic inhibitors of hepatitis C protease.
Andrews DM, Chaignot HM, Coomber BA, Dowle MD, Hind SL, Johnson MR, Jones PS, Mills G, Patikis A, Pateman TJ, Robinson JE, Slater MJ, Trivedi N. Andrews DM, et al. Among authors: patikis a. Eur J Med Chem. 2003 Apr;38(4):339-43. doi: 10.1016/s0223-5234(03)00050-3. Eur J Med Chem. 2003. PMID: 12750019
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: patikis a. 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: patikis a. 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: 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: patikis an. 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
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: patikis an. 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
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: patikis an. 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
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: patikis an. 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 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: patikis an. 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
12 results