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Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases.
Jaeschke G, Kolczewski S, Spooren W, Vieira E, Bitter-Stoll N, Boissin P, Borroni E, Büttelmann B, Ceccarelli S, Clemann N, David B, Funk C, Guba W, Harrison A, Hartung T, Honer M, Huwyler J, Kuratli M, Niederhauser U, Pähler A, Peters JU, Petersen A, Prinssen E, Ricci A, Rueher D, Rueher M, Schneider M, Spurr P, Stoll T, Tännler D, Wichmann J, Porter RH, Wettstein JG, Lindemann L. Jaeschke G, et al. Among authors: petersen a. J Med Chem. 2015 Feb 12;58(3):1358-71. doi: 10.1021/jm501642c. Epub 2015 Feb 2. J Med Chem. 2015. PMID: 25565255
Scaffold hopping towards potent and selective JAK3 inhibitors: discovery of novel C-5 substituted pyrrolopyrazines.
de Vicente J, Lemoine R, Bartlett M, Hermann JC, Hekmat-Nejad M, Henningsen R, Jin S, Kuglstatter A, Li H, Lovey AJ, Menke J, Niu L, Patel V, Petersen A, Setti L, Shao A, Tivitmahaisoon P, Vu MD, Soth M. de Vicente J, et al. Among authors: petersen a. Bioorg Med Chem Lett. 2014 Nov 1;24(21):4969-75. doi: 10.1016/j.bmcl.2014.09.031. Epub 2014 Sep 21. Bioorg Med Chem Lett. 2014. PMID: 25262541
Fragment-Based Drug Design of Novel Pyranopyridones as Cell Active and Orally Bioavailable Tankyrase Inhibitors.
de Vicente J, Tivitmahaisoon P, Berry P, Bolin DR, Carvajal D, He W, Huang KS, Janson C, Liang L, Lukacs C, Petersen A, Qian H, Yi L, Zhuang Y, Hermann JC. de Vicente J, et al. Among authors: petersen a. ACS Med Chem Lett. 2015 Aug 4;6(9):1019-24. doi: 10.1021/acsmedchemlett.5b00251. eCollection 2015 Sep 10. ACS Med Chem Lett. 2015. PMID: 26396691 Free PMC article.
Novel hexahydropyrrolo[3,4-c]pyrrole CCR5 antagonists.
Rotstein DM, Melville CR, Padilla F, Cournoyer D, Lee EK, Lemoine R, Petersen AC, Setti LQ, Wanner J, Chen L, Filonova L, Loughhead DG, Manka J, Lin XF, Gleason S, Sankuratri S, Ji C, Derosier A, Dioszegi M, Heilek G, Jekle A, Berry P, Mau CI, Weller P. Rotstein DM, et al. Among authors: petersen ac. Bioorg Med Chem Lett. 2010 May 15;20(10):3116-9. doi: 10.1016/j.bmcl.2010.03.095. Epub 2010 Mar 30. Bioorg Med Chem Lett. 2010. PMID: 20417098
Evaluation of secondary amide replacements in a series of CCR5 antagonists as a means to increase intrinsic membrane permeability. Part 1: Optimization of gem-disubstituted azacycles.
Lemoine RC, Petersen AC, Setti L, Wanner J, Jekle A, Heilek G, deRosier A, Ji C, Berry P, Rotstein D. Lemoine RC, et al. Among authors: petersen ac. Bioorg Med Chem Lett. 2010 Jan 15;20(2):704-8. doi: 10.1016/j.bmcl.2009.11.072. Epub 2009 Dec 7. Bioorg Med Chem Lett. 2010. PMID: 20004099
1,823 results