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Page 1
Optimization of the In Vivo Potency of Pyrazolopyrimidine MALT1 Protease Inhibitors by Reducing Metabolism and Increasing Potency in Whole Blood.
Quancard J, Simic O, Pissot Soldermann C, Aichholz R, Blatter M, Renatus M, Erbel P, Melkko S, Endres R, Sorge M, Kieffer L, Wagner T, Beltz K, Mcsheehy P, Wartmann M, Régnier CH, Calzascia T, Radimerski T, Bigaud M, Weiss A, Bornancin F, Schlapbach A. Quancard J, et al. Among authors: wagner t. J Med Chem. 2020 Dec 10;63(23):14594-14608. doi: 10.1021/acs.jmedchem.0c01246. Epub 2020 Nov 20. J Med Chem. 2020. PMID: 33216547
Orally bioavailable competitive CCR5 antagonists.
Thoma G, Nuninger F, Schaefer M, Akyel KG, Albert R, Beerli C, Bruns C, Francotte E, Luyten M, MacKenzie D, Oberer L, Streiff MB, Wagner T, Walter H, Weckbecker G, Zerwes HG. Thoma G, et al. Among authors: wagner t. J Med Chem. 2004 Apr 8;47(8):1939-55. doi: 10.1021/jm031046g. J Med Chem. 2004. PMID: 15055994
Novel 2,7-dialkyl-substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamide transition state peptidomimetics are potent and orally active inhibitors of human renin.
Göschke R, Stutz S, Rasetti V, Cohen NC, Rahuel J, Rigollier P, Baum HP, Forgiarini P, Schnell CR, Wagner T, Gruetter MG, Fuhrer W, Schilling W, Cumin F, Wood JM, Maibaum J. Göschke R, et al. Among authors: wagner t. J Med Chem. 2007 Oct 4;50(20):4818-31. doi: 10.1021/jm070314y. Epub 2007 Sep 8. J Med Chem. 2007. PMID: 17824679
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.
2,235 results