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Page 1
Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors.
Powell NA, Ciske FL, Cai C, Holsworth DD, Mennen K, Van Huis CA, Jalaie M, Day J, Mastronardi M, McConnell P, Mochalkin I, Zhang E, Ryan MJ, Bryant J, Collard W, Ferreira S, Gu C, Collins R, Edmunds JJ. Powell NA, et al. Among authors: van huis ca. Bioorg Med Chem. 2007 Sep 1;15(17):5912-49. doi: 10.1016/j.bmc.2007.05.069. Epub 2007 Jun 2. Bioorg Med Chem. 2007. PMID: 17574423
The discovery of fluoropyridine-based inhibitors of the Factor VIIa/TF complex.
Kohrt JT, Filipski KJ, Cody WL, Cai C, Dudley DA, Van Huis CA, Willardsen JA, Rapundalo ST, Saiya-Cork K, Leadley RJ, Narasimhan L, Zhang E, Whitlow M, Adler M, McLean K, Chou YL, McKnight C, Arnaiz DO, Shaw KJ, Light DR, Edmunds JJ. Kohrt JT, et al. Among authors: van huis ca. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4752-6. doi: 10.1016/j.bmcl.2005.07.059. Bioorg Med Chem Lett. 2005. PMID: 16125385
The discovery of fluoropyridine-based inhibitors of the factor VIIa/TF complex--Part 2.
Kohrt JT, Filipski KJ, Cody WL, Cai C, Dudley DA, Van Huis CA, Willardsen JA, Narasimhan LS, Zhang E, Rapundalo ST, Saiya-Cork K, Leadley RJ, Edmunds JJ. Kohrt JT, et al. Among authors: van huis ca. Bioorg Med Chem Lett. 2006 Feb 15;16(4):1060-4. doi: 10.1016/j.bmcl.2005.10.076. Epub 2005 Nov 11. Bioorg Med Chem Lett. 2006. PMID: 16289811
Binding thermodynamics of substituted diaminopyrimidine renin inhibitors.
Sarver RW, Peevers J, Cody WL, Ciske FL, Dyer J, Emerson SD, Hagadorn JC, Holsworth DD, Jalaie M, Kaufman M, Mastronardi M, McConnell P, Powell NA, Quin J 3rd, Van Huis CA, Zhang E, Mochalkin I. Sarver RW, et al. Among authors: van huis ca. Anal Biochem. 2007 Jan 1;360(1):30-40. doi: 10.1016/j.ab.2006.10.017. Epub 2006 Oct 30. Anal Biochem. 2007. PMID: 17113558
Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action.
Van Huis CA, Casimiro-Garcia A, Bigge CF, Cody WL, Dudley DA, Filipski KJ, Heemstra RJ, Kohrt JT, Leadley RJ Jr, Narasimhan LS, McClanahan T, Mochalkin I, Pamment M, Peterson JT, Sahasrabudhe V, Schaum RP, Edmunds JJ. Van Huis CA, et al. Bioorg Med Chem. 2009 Mar 15;17(6):2501-11. doi: 10.1016/j.bmc.2009.01.063. Epub 2009 Feb 3. Bioorg Med Chem. 2009. PMID: 19231206
The discovery of (2R,4R)-N-(4-chlorophenyl)-N- (2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl)-4-methoxypyrrolidine-1,2-dicarboxamide (PD 0348292), an orally efficacious factor Xa inhibitor.
Kohrt JT, Bigge CF, Bryant JW, Casimiro-Garcia A, Chi L, Cody WL, Dahring T, Dudley DA, Filipski KJ, Haarer S, Heemstra R, Janiczek N, Narasimhan L, McClanahan T, Peterson JT, Sahasrabudhe V, Schaum R, Van Huis CA, Welch KM, Zhang E, Leadley RJ, Edmunds JJ. Kohrt JT, et al. Among authors: van huis ca. Chem Biol Drug Des. 2007 Aug;70(2):100-12. doi: 10.1111/j.1747-0285.2007.00539.x. Chem Biol Drug Des. 2007. PMID: 17683371
The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 2.
Cody WL, Augelli-Szafran CE, Berryman KA, Cai C, Doherty AM, Edmunds JJ, He JX, Narasimhan LS, Penvose-Yi J, Plummer JS, Rapundalo ST, Rubin JR, Van Huis CA, Leblond L, Winocour PD, Siddiqui MA. Cody WL, et al. Among authors: van huis ca. Bioorg Med Chem Lett. 1999 Sep 6;9(17):2503-8. doi: 10.1016/s0960-894x(99)00419-9. Bioorg Med Chem Lett. 1999. PMID: 10498197
Structure-based drug design of pyrrolidine-1, 2-dicarboxamides as a novel series of orally bioavailable factor Xa inhibitors.
Van Huis CA, Bigge CF, Casimiro-Garcia A, Cody WL, Dudley DA, Filipski KJ, Heemstra RJ, Kohrt JT, Narasimhan LS, Schaum RP, Zhang E, Bryant JW, Haarer S, Janiczek N, Leadley RJ Jr, McClanahan T, Thomas Peterson J, Welch KM, Edmunds JJ. Van Huis CA, et al. Chem Biol Drug Des. 2007 Jun;69(6):444-50. doi: 10.1111/j.1747-0285.2007.00520.x. Chem Biol Drug Des. 2007. PMID: 17581239
14 results