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Page 1
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: rigel df. 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: rigel df. J Med Chem. 2013 Mar 28;56(6):2207-17. doi: 10.1021/jm3017078. Epub 2013 Mar 15. J Med Chem. 2013. PMID: 23425156
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: rigel df. 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.
Structure-Guided Design of Substituted Biphenyl Butanoic Acid Derivatives as Neprilysin Inhibitors.
Kawanami T, Karki RG, Cody E, Liu Q, Liang G, Ksander GM, Rigel DF, Schiering N, Gong Y, Coppola GM, Iwaki Y, Sun R, Neubert A, Fan L, Ingles S, D'Arcy A, Villard F, Ramage P, Jeng AY, Leung-Chu J, Liu J, Beil M, Fu F, Chen W, Cumin F, Wiesmann C, Mogi M. Kawanami T, et al. Among authors: rigel df. ACS Med Chem Lett. 2020 Jan 27;11(2):188-194. doi: 10.1021/acsmedchemlett.9b00578. eCollection 2020 Feb 13. ACS Med Chem Lett. 2020. PMID: 32071687 Free PMC article.
Discovery of a Novel Piperidine-Based Inhibitor of Cholesteryl Ester Transfer Protein (CETP) That Retains Activity in Hypertriglyceridemic Plasma.
Yamada K, Brousseau M, Honma W, Iimura A, Imase H, Iwaki Y, Kawanami T, LaSala D, Liang G, Mitani H, Nonomura K, Ohmori O, Pan M, Rigel DF, Umemura I, Yasoshima K, Zhu G, Mogi M. Yamada K, et al. Among authors: rigel df. J Med Chem. 2017 Oct 26;60(20):8466-8481. doi: 10.1021/acs.jmedchem.7b00900. Epub 2017 Oct 16. J Med Chem. 2017. PMID: 29035537
Structure-Activity Relationships, Pharmacokinetics, and in Vivo Activity of CYP11B2 and CYP11B1 Inhibitors.
Papillon JP, Adams CM, Hu QY, Lou C, Singh AK, Zhang C, Carvalho J, Rajan S, Amaral A, Beil ME, Fu F, Gangl E, Hu CW, Jeng AY, LaSala D, Liang G, Logman M, Maniara WM, Rigel DF, Smith SA, Ksander GM. Papillon JP, et al. Among authors: rigel df. J Med Chem. 2015 Jun 11;58(11):4749-70. doi: 10.1021/acs.jmedchem.5b00407. Epub 2015 May 21. J Med Chem. 2015. PMID: 25953419
Optimization of Allosteric With-No-Lysine (WNK) Kinase Inhibitors and Efficacy in Rodent Hypertension Models.
Yamada K, Levell J, Yoon T, Kohls D, Yowe D, Rigel DF, Imase H, Yuan J, Yasoshima K, DiPetrillo K, Monovich L, Xu L, Zhu M, Kato M, Jain M, Idamakanti N, Taslimi P, Kawanami T, Argikar UA, Kunjathoor V, Xie X, Yagi YI, Iwaki Y, Robinson Z, Park HM. Yamada K, et al. Among authors: rigel df. J Med Chem. 2017 Aug 24;60(16):7099-7107. doi: 10.1021/acs.jmedchem.7b00708. Epub 2017 Aug 3. J Med Chem. 2017. PMID: 28771350
Discovery of N-[5-(6-Chloro-3-cyano-1-methyl-1H-indol-2-yl)-pyridin-3-ylmethyl]-ethanesulfonamide, a Cortisol-Sparing CYP11B2 Inhibitor that Lowers Aldosterone in Human Subjects.
Papillon JP, Lou C, Singh AK, Adams CM, Ksander GM, Beil ME, Chen W, Leung-Chu J, Fu F, Gan L, Hu CW, Jeng AY, LaSala D, Liang G, Rigel DF, Russell KS, Vest JA, Watson C. Papillon JP, et al. Among authors: rigel df. J Med Chem. 2015 Dec 10;58(23):9382-94. doi: 10.1021/acs.jmedchem.5b01545. Epub 2015 Nov 18. J Med Chem. 2015. PMID: 26540564
48 results