Carcache DA - Search Results

1

Optimizing a Weakly Binding Fragment into a Potent RORγt Inverse Agonist with Efficacy in an in Vivo Inflammation Model.

Carcache DA, Vulpetti A, Kallen J, Mattes H, Orain D, Stringer R, Vangrevelinghe E, Wolf RM, Kaupmann K, Ottl J, Dawson J, Cooke NG, Hoegenauer K, Billich A, Wagner J, Guntermann C, Hintermann S. Carcache DA, et al. J Med Chem. 2018 Aug 9;61(15):6724-6735. doi: 10.1021/acs.jmedchem.8b00529. Epub 2018 Jul 24. J Med Chem. 2018. PMID: 29990434

2

Synthesis and Biological Evaluation of New Triazolo- and Imidazolopyridine RORγt Inverse Agonists.

Hintermann S, Guntermann C, Mattes H, Carcache DA, Wagner J, Vulpetti A, Billich A, Dawson J, Kaupmann K, Kallen J, Stringer R, Orain D. Hintermann S, et al. Among authors: carcache da. ChemMedChem. 2016 Dec 16;11(24):2640-2648. doi: 10.1002/cmdc.201600500. Epub 2016 Nov 30. ChemMedChem. 2016. PMID: 27902884

3

alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.

Mattes H, Carcache D, Kalkman HO, Koller M. Mattes H, et al. J Med Chem. 2010 Aug 12;53(15):5367-82. doi: 10.1021/jm901688m. J Med Chem. 2010. PMID: 20356304 No abstract available.

4

Quinazolinedione sulfonamides: a novel class of competitive AMPA receptor antagonists with oral activity.

Koller M, Lingenhoehl K, Schmutz M, Vranesic IT, Kallen J, Auberson YP, Carcache DA, Mattes H, Ofner S, Orain D, Urwyler S. Koller M, et al. Among authors: carcache da. Bioorg Med Chem Lett. 2011 Jun 1;21(11):3358-61. doi: 10.1016/j.bmcl.2011.04.017. Epub 2011 Apr 8. Bioorg Med Chem Lett. 2011. PMID: 21531559

5

6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists.

Orain D, Ofner S, Koller M, Carcache DA, Froestl W, Allgeier H, Rasetti V, Nozulak J, Mattes H, Soldermann N, Floersheim P, Desrayaud S, Kallen J, Lingenhoehl K, Urwyler S. Orain D, et al. Among authors: carcache da. Bioorg Med Chem Lett. 2012 Jan 15;22(2):996-9. doi: 10.1016/j.bmcl.2011.12.009. Epub 2011 Dec 8. Bioorg Med Chem Lett. 2012. PMID: 22197388

6

Discovery of 1H-pyrrolo[2,3-c]pyridine-7-carboxamides as novel, allosteric mGluR5 antagonists.

Koller M, Carcache DA, Orain D, Ertl P, Behnke D, Desrayaud S, Laue G, Vranesic I. Koller M, et al. Among authors: carcache da. Bioorg Med Chem Lett. 2012 Oct 15;22(20):6454-9. doi: 10.1016/j.bmcl.2012.08.053. Epub 2012 Aug 21. Bioorg Med Chem Lett. 2012. PMID: 22963764

7

Design and Synthesis of Selurampanel, a Novel Orally Active and Competitive AMPA Receptor Antagonist.

Orain D, Tasdelen E, Haessig S, Koller M, Picard A, Dubois C, Lingenhoehl K, Desrayaud S, Floersheim P, Carcache D, Urwyler S, Kallen J, Mattes H. Orain D, et al. ChemMedChem. 2017 Feb 3;12(3):197-201. doi: 10.1002/cmdc.201600467. Epub 2016 Nov 15. ChemMedChem. 2017. PMID: 27863026

8

Compound Property Optimization in Drug Discovery Using Quantitative Surface Sampling Micro Liquid Chromatography with Tandem Mass Spectrometry.

Chen X, Hatsis P, Judge J, Argikar UA, Ren X, Sarber J, Mansfield K, Liang G, Amaral A, Catoire A, Bentley A, Ramos L, Moench P, Hintermann S, Carcache D, Glick J, Flarakos J. Chen X, et al. Anal Chem. 2016 Dec 6;88(23):11813-11820. doi: 10.1021/acs.analchem.6b03449. Epub 2016 Nov 16. Anal Chem. 2016. PMID: 27797491

9

Benzimidazoles as Potent and Orally Active mGlu5 Receptor Antagonists with an Improved PK Profile.

Carcache D, Vranesic I, Blanz J, Desrayaud S, Fendt M, Glatthar R. Carcache D, et al. ACS Med Chem Lett. 2010 Nov 2;2(1):58-62. doi: 10.1021/ml100215b. eCollection 2011 Jan 13. ACS Med Chem Lett. 2010. PMID: 24900255 Free PMC article.

10

Metabolism and disposition of the metabotropic glutamate receptor 5 antagonist (mGluR5) mavoglurant (AFQ056) in healthy subjects.

Walles M, Wolf T, Jin Y, Ritzau M, Leuthold LA, Krauser J, Gschwind HP, Carcache D, Kittelmann M, Ocwieja M, Ufer M, Woessner R, Chakraborty A, Swart P. Walles M, et al. Drug Metab Dispos. 2013 Sep;41(9):1626-41. doi: 10.1124/dmd.112.050716. Epub 2013 Jun 17. Drug Metab Dispos. 2013. PMID: 23775850

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