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Items: 26

1.

Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies.

Bezençon O, Heidmann B, Siegrist R, Stamm S, Richard S, Pozzi D, Corminboeuf O, Roch C, Kessler M, Ertel EA, Reymond I, Pfeifer T, de Kanter R, Toeroek-Schafroth M, Moccia LG, Mawet J, Moon R, Rey M, Capeleto B, Fournier E.

J Med Chem. 2017 Dec 14;60(23):9769-9789. doi: 10.1021/acs.jmedchem.7b01236. Epub 2017 Nov 20.

PMID:
29116786
2.

Discovery and evaluation of Cav3.2-selective T-type calcium channel blockers.

Bezençon O, Remeň L, Richard S, Roch C, Kessler M, Ertel EA, Moon R, Mawet J, Pfeifer T, Capeleto B.

Bioorg Med Chem Lett. 2017 Dec 1;27(23):5326-5331. doi: 10.1016/j.bmcl.2017.09.062. Epub 2017 Sep 30.

PMID:
29074257
3.

Milestones to the Discovery of T-type Calcium Channel Blockers for the Treatment of Generalized Epilepsies.

Bezençon O, Siegrist R, Heidmann B, Pozzi D, Stamm S, Remeň L, Richard S, Simons L, Gaston R, Downing D, Grisostomi C, Roch C, Kessler M, Gatfield J, Moon R, Pfeifer T, Mosbacher J, Reymond I, Ertel EA, de Kanter R, Capeleto B, Fournier E, Rey M, Moccia L, Toeroek-Schafroth M, Roscher R, Schindelholz B.

Chimia (Aarau). 2017 Oct 25;71(10):722-729. doi: 10.2533/chimia.2017.722.

PMID:
29070417
4.

Discovery and evaluation of Cav3.1-selective T-type calcium channel blockers.

Bezençon O, Remeň L, Richard S, Roch C, Kessler M, Moon R, Mawet J, Ertel EA, Pfeifer T, Capeleto B.

Bioorg Med Chem Lett. 2017 Dec 1;27(23):5322-5325. doi: 10.1016/j.bmcl.2017.09.063. Epub 2017 Oct 3.

PMID:
29066309
5.

The Use of Physiology-Based Pharmacokinetic and Pharmacodynamic Modeling in the Discovery of the Dual Orexin Receptor Antagonist ACT-541468.

Treiber A, de Kanter R, Roch C, Gatfield J, Boss C, von Raumer M, Schindelholz B, Muehlan C, van Gerven J, Jenck F.

J Pharmacol Exp Ther. 2017 Sep;362(3):489-503. doi: 10.1124/jpet.117.241596. Epub 2017 Jun 29.

PMID:
28663311
6.

Orexin research: patent news from 2016.

Boss C, Roch C.

Expert Opin Ther Pat. 2017 Oct;27(10):1123-1133. doi: 10.1080/13543776.2017.1344221. Epub 2017 Jun 28. Review.

PMID:
28631980
7.

Correction to Structure-Activity Relationship, Drug Metabolism and Pharmacokinetics Properties Optimization, and in Vivo Studies of New Brain Penetrant Triple T-Type Calcium Channel Blockers.

Siegrist R, Pozzi D, Jacob G, Torrisi C, Colas K, Braibant B, Mawet J, Pfeifer T, de Kanter R, Roch C, Kessler M, Moon R, Corminboeuf O, Bezençon O.

J Med Chem. 2017 Mar 9;60(5):2163. doi: 10.1021/acs.jmedchem.7b00219. Epub 2017 Feb 24. No abstract available.

PMID:
28234473
8.

Structure-Activity Relationship, Drug Metabolism and Pharmacokinetics Properties Optimization, and in Vivo Studies of New Brain Penetrant Triple T-Type Calcium Channel Blockers.

Siegrist R, Pozzi D, Jacob G, Torrisi C, Colas K, Braibant B, Mawet J, Pfeifer T, de Kanter R, Roch C, Kessler M, Corminboeuf O, Bezençon O.

J Med Chem. 2016 Dec 8;59(23):10661-10675. Epub 2016 Nov 23.

PMID:
27933950
9.

Preparation, Antiepileptic Activity, and Cardiovascular Safety of Dihydropyrazoles as Brain-Penetrant T-Type Calcium Channel Blockers.

Remen L, Bezençon O, Simons L, Gaston R, Downing D, Gatfield J, Roch C, Kessler M, Mosbacher J, Pfeifer T, Grisostomi C, Rey M, Ertel EA, Moon R.

J Med Chem. 2016 Sep 22;59(18):8398-411. doi: 10.1021/acs.jmedchem.6b00756. Epub 2016 Sep 12.

PMID:
27579577
10.

Discovery of Highly Potent Dual Orexin Receptor Antagonists via a Scaffold-Hopping Approach.

Heidmann B, Gatfield J, Roch C, Treiber A, Tortoioli S, Brotschi C, Williams JT, Bolli MH, Abele S, Sifferlen T, Jenck F, Boss C.

ChemMedChem. 2016 Oct 6;11(19):2132-2146. doi: 10.1002/cmdc.201600175. Epub 2016 Jul 8.

PMID:
27390287
11.
12.

Recent trends in orexin research--2010 to 2015.

Boss C, Roch C.

Bioorg Med Chem Lett. 2015 Aug 1;25(15):2875-87. doi: 10.1016/j.bmcl.2015.05.012. Epub 2015 May 15. Review.

PMID:
26045032
13.

Substituted pyrrolidin-2-ones: Centrally acting orexin receptor antagonists promoting sleep. Part 2.

Sifferlen T, Boller A, Chardonneau A, Cottreel E, Gatfield J, Treiber A, Roch C, Jenck F, Aissaoui H, Williams JT, Brotschi C, Heidmann B, Siegrist R, Boss C.

Bioorg Med Chem Lett. 2015 May 1;25(9):1884-91. doi: 10.1016/j.bmcl.2015.03.035. Epub 2015 Mar 21.

PMID:
25838147
14.

[Chronic pain and artificial diseases].

Roch C, Knöchlein C, Albrecht J.

Schmerz. 2014 Oct;28(5):528-31. doi: 10.1007/s00482-014-1477-4. German.

PMID:
25190610
15.

Human xylosyltransferase-I - a new marker for myofibroblast differentiation in skin fibrosis.

Faust I, Roch C, Kuhn J, Prante C, Knabbe C, Hendig D.

Biochem Biophys Res Commun. 2013 Jul 5;436(3):449-54. doi: 10.1016/j.bbrc.2013.05.125. Epub 2013 Jun 6.

PMID:
23747722
16.

[Shortage of physicians in anaesthesiology and intensive care medicine - Causes, consequences and solutions].

Papenfuß T, Roch C.

Anasthesiol Intensivmed Notfallmed Schmerzther. 2012 May;47(5):352-7. doi: 10.1055/s-0032-1313574. Epub 2012 May 24. German.

PMID:
22628032
17.

Differences in gene expression of human xylosyltransferases and determination of acceptor specificities for various proteoglycans.

Roch C, Kuhn J, Kleesiek K, Götting C.

Biochem Biophys Res Commun. 2010 Jan 1;391(1):685-91. doi: 10.1016/j.bbrc.2009.11.121. Epub 2009 Nov 26.

PMID:
19944077
18.

[Regional anesthesia as a useful alternative to general anesthesia? Overview of the current data].

Papenfuss T, Roch C, Schwemmer U.

Anasthesiol Intensivmed Notfallmed Schmerzther. 2009 Nov;44(11-12):766-71; quiz 773-6. doi: 10.1055/s-0029-1242129. Epub 2009 Nov 16. Review. German.

PMID:
19918709
19.

First in-gel detection and purification of human xylosyltransferase II.

Casanova JC, Roch C, Kuhn J, Kleesiek K, Götting C.

Biochem Biophys Res Commun. 2009 Feb 6;379(2):243-8. doi: 10.1016/j.bbrc.2008.12.033. Epub 2008 Dec 25.

PMID:
19100717
20.

Pathogenesis and pharmacology of epilepsy in the lithium-pilocarpine model.

André V, Dubé C, François J, Leroy C, Rigoulot MA, Roch C, Namer IJ, Nehlig A.

Epilepsia. 2007;48 Suppl 5:41-7. Erratum in: Epilepsia. 2007 Dec;48(12):2379.

22.

Detection of late epilepsy by the texture analysis of MR brain images in the lithium-pilocarpine rat model.

Yu O, Roch C, Namer IJ, Chambron J, Mauss Y.

Magn Reson Imaging. 2002 Dec;20(10):771-5.

PMID:
12591572
24.
25.

Automatic learning strategies and their application to electrophoresis analysis.

Roch C, Pun T, Hochstrasser DF, Pellegrini C.

Comput Med Imaging Graph. 1989 Sep-Oct;13(5):383-91.

PMID:
2804944
26.

Automatic classification of two-dimensional gel electrophoresis pictures by heuristic clustering analysis: a step toward machine learning.

Appel R, Hochstrasser D, Roch C, Funk M, Muller AF, Pellegrini C.

Electrophoresis. 1988 Mar;9(3):136-42.

PMID:
3234347

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