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Page 1
Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Allosteric and Mutant Specific Inhibitors of IDH1.
Levell JR, Caferro T, Chenail G, Dix I, Dooley J, Firestone B, Fortin PD, Giraldes J, Gould T, Growney JD, Jones MD, Kulathila R, Lin F, Liu G, Mueller A, van der Plas S, Slocum K, Smith T, Terranova R, Touré BB, Tyagi V, Wagner T, Xie X, Xu M, Yang FS, Zhou LX, Pagliarini R, Cho YS. Levell JR, et al. Among authors: wagner t. ACS Med Chem Lett. 2016 Dec 16;8(2):151-156. doi: 10.1021/acsmedchemlett.6b00334. eCollection 2017 Feb 9. ACS Med Chem Lett. 2016. PMID: 28197303 Free PMC article.
Conformational refinement of hydroxamate-based histone deacetylase inhibitors and exploration of 3-piperidin-3-ylindole analogues of dacinostat (LAQ824).
Cho YS, Whitehead L, Li J, Chen CH, Jiang L, Vögtle M, Francotte E, Richert P, Wagner T, Traebert M, Lu Q, Cao X, Dumotier B, Fejzo J, Rajan S, Wang P, Yan-Neale Y, Shao W, Atadja P, Shultz M. Cho YS, et al. Among authors: wagner t. J Med Chem. 2010 Apr 8;53(7):2952-63. doi: 10.1021/jm100007m. J Med Chem. 2010. PMID: 20205394
Solubility-driven optimization of phosphodiesterase-4 inhibitors leading to a clinical candidate.
Press NJ, Taylor RJ, Fullerton JD, Tranter P, McCarthy C, Keller TH, Arnold N, Beer D, Brown L, Cheung R, Christie J, Denholm A, Haberthuer S, Hatto JD, Keenan M, Mercer MK, Oakman H, Sahri H, Tuffnell AR, Tweed M, Tyler JW, Wagner T, Fozard JR, Trifilieff A. Press NJ, et al. Among authors: wagner t. J Med Chem. 2012 Sep 13;55(17):7472-9. doi: 10.1021/jm300459a. Epub 2012 Aug 30. J Med Chem. 2012. PMID: 22889281
A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore.
Ostermann N, Ruedisser S, Ehrhardt C, Breitenstein W, Marzinzik A, Jacoby E, Vangrevelinghe E, Ottl J, Klumpp M, Hartwieg JC, Cumin F, Hassiepen U, Trappe J, Sedrani R, Geisse S, Gerhartz B, Richert P, Francotte E, Wagner T, Krömer M, Kosaka T, Webb RL, Rigel DF, Maibaum J, Baeschlin DK. Ostermann N, et al. Among authors: wagner t. J Med Chem. 2013 Mar 28;56(6):2196-206. doi: 10.1021/jm301706j. Epub 2013 Mar 15. J Med Chem. 2013. PMID: 23360239
The discovery of novel potent trans-3,4-disubstituted pyrrolidine inhibitors of the human aspartic protease renin from in silico three-dimensional (3D) pharmacophore searches.
Lorthiois E, Breitenstein W, Cumin F, Ehrhardt C, Francotte E, Jacoby E, Ostermann N, Sellner H, Kosaka T, Webb RL, Rigel DF, Hassiepen U, Richert P, Wagner T, Maibaum J. Lorthiois E, et al. Among authors: wagner t. J Med Chem. 2013 Mar 28;56(6):2207-17. doi: 10.1021/jm3017078. Epub 2013 Mar 15. J Med Chem. 2013. PMID: 23425156
Discovery of tetrahydropyrazolopyrimidine carboxamide derivatives as potent and orally active antitubercular agents.
Yokokawa F, Wang G, Chan WL, Ang SH, Wong J, Ma I, Rao SP, Manjunatha U, Lakshminarayana SB, Herve M, Kounde C, Tan BH, Thayalan P, Ng SH, Nanjundappa M, Ravindran S, Gee P, Tan M, Wei L, Goh A, Chen PY, Lee KS, Zhong C, Wagner T, Dix I, Chatterjee AK, Pethe K, Kuhen K, Glynne R, Smith P, Bifani P, Jiricek J. Yokokawa F, et al. Among authors: wagner t. ACS Med Chem Lett. 2013 Apr 1;4(5):451-5. doi: 10.1021/ml400071a. eCollection 2013 May 9. ACS Med Chem Lett. 2013. PMID: 24900693 Free PMC article.
Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors.
Ehara T, Irie O, Kosaka T, Kanazawa T, Breitenstein W, Grosche P, Ostermann N, Suzuki M, Kawakami S, Konishi K, Hitomi Y, Toyao A, Gunji H, Cumin F, Schiering N, Wagner T, Rigel DF, Webb RL, Maibaum J, Yokokawa F. Ehara T, et al. Among authors: wagner t. ACS Med Chem Lett. 2014 Apr 21;5(7):787-92. doi: 10.1021/ml500137b. eCollection 2014 Jul 10. ACS Med Chem Lett. 2014. PMID: 25050166 Free PMC article.
Lead optimization of spiropyrazolopyridones: a new and potent class of dengue virus inhibitors.
Zou B, Chan WL, Ding M, Leong SY, Nilar S, Seah PG, Liu W, Karuna R, Blasco F, Yip A, Chao A, Susila A, Dong H, Wang QY, Xu HY, Chan K, Wan KF, Gu F, Diagana TT, Wagner T, Dix I, Shi PY, Smith PW. Zou B, et al. Among authors: wagner t. ACS Med Chem Lett. 2015 Feb 2;6(3):344-8. doi: 10.1021/ml500521r. eCollection 2015 Mar 12. ACS Med Chem Lett. 2015. PMID: 25878766 Free PMC article.
Discovery of 1H-pyrazolo[3,4-b]pyridines as potent dual orexin receptor antagonists (DORAs).
Behnke D, Cotesta S, Hintermann S, Fendt M, Gee CE, Jacobson LH, Laue G, Meyer A, Wagner T, Badiger S, Chaudhari V, Chebrolu M, Pandit C, Hoyer D, Betschart C. Behnke D, et al. Among authors: wagner t. Bioorg Med Chem Lett. 2015 Dec 1;25(23):5555-60. doi: 10.1016/j.bmcl.2015.10.055. Epub 2015 Oct 19. Bioorg Med Chem Lett. 2015. PMID: 26522950
2,179 results