Výsledky vyhledávání - "Kurt Hilpert"

Identification of 2-(2-(1-Naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic Acid (Setipiprant/ACT-129968), a Potent, Selective, and Orally Bioavailable Chemoattractant Receptor-Homologous Molecule Expressed on Th2 Cells (CRTH2) Antagonist

Autor: Heinz Fretz, Xavier Leroy, Carmela Gnerre, Kurt Hilpert, Julien Pothier, Markus A. Riederer, Anja Valdenaire, Oliver Peter

Publikováno v: Journal of Medicinal Chemistry. 56:4899-4911

Herein we describe the discovery of the novel CRTh2 antagonist 2-(2-(1-naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic acid 28 (setipiprant/ACT-129968), a clinical development candidate for the treatment of asthma and seasonal a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::cb4a02fb1da7aa0fe9fa9c3373a09ecd
https://doi.org/10.1021/jm400122f

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Discovery of novel bridged tetrahydronaphthalene derivatives as potent T/L-type calcium channel blockers

Autor: Patrick Hess, Stephane Delahaye, Markus Rey, Marc Iglarz, John Gatfield, Kurt Hilpert, Dorte Renneberg, Francis Hubler

Publikováno v: Bioorganicmedicinal chemistry letters. 25(18)

Chemical evolution of mibefradil resulted in the identification of novel bridged tetrahydronaphthalene derivatives as potent T/L-type calcium channel blockers. A SAR study, in vitro and in vivo DMPK properties as well as the in vivo antihypertensive

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::380ada0fbd905ad8961360411708c767
https://pubmed.ncbi.nlm.nih.gov/26231163

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Selective and orally bioavailable phenylglycine tissue factor/factor VIIa inhibitors

Autor: Thierry Lavé, Hans-Joachim Böhm, Ulrike Obst-Sander, David Banner, Lutz Weber, Martin Stahl, Markus A. Riederer, Kurt Hilpert, Hans Peter Wessel, Thomas B. Tschopp, Katrin Groebke Zbinden, Holger Kühne, Leo Alig, Jean Ackermann

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 15:5344-5352

We describe the structure-based design and synthesis of highly potent, orally bioavailable tissue factor/factor VIIa inhibitors which interfere with the coagulation cascade by selective inhibition of the extrinsic pathway.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6032880aca0a8668a787f6fa99dc00cb
https://doi.org/10.1016/j.bmcl.2005.04.079

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Discovery and optimization of 4,5-diarylisoxazoles as potent dual inhibitors of pyruvate dehydrogenase kinase and heat shock protein 90

Autor: Min Huang, Jingkang Shen, Ting Yu, Urs Regenass, Kurt Hilpert, Dadong Zhang, Meiyu Geng, Shuchao Wu, Lorenza Wyder, Zuoquan Xie, Tao Meng

Publikováno v: Journal of medicinal chemistry. 57(23)

Upregulation of pyruvate dehydrogenase kinase (PDHK) has been observed in a variety of cancers. Inhibition of PDHK offers an attractive opportunity for the development of novel cancer therapies. To obtain novel PDHK inhibitors, we took advantage of t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6f27e1d294f68221855e797e6d29781a
https://pubmed.ncbi.nlm.nih.gov/31769671

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Optimization of 2-phenyl-pyrimidine-4-carboxamides towards potent, orally bioavailable and selective P2Y(12) antagonists for inhibition of platelet aggregation

Autor: Emmanuel Meyer, Markus A. Riederer, Eva Caroff, Alexander Treiber, Kurt Hilpert

Publikováno v: Bioorganicmedicinal chemistry letters. 24(17)

2-Phenyl-pyrimidine-4-carboxamide analogs were identified as P2Y12 antagonists. Optimization of the carbon-linked or nitrogen-linked substituent at the 6-position of the pyrimidine ring provided compounds with excellent ex vivo potency in the platele

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e9f7c38e0dbfd27846e50c9b57452c8c
https://pubmed.ncbi.nlm.nih.gov/25113932

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Identification of 2-(2-(1-naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic acid (setipiprant/ACT-129968), a potent, selective, and orally bioavailable chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2) antagonist

Autor: Heinz, Fretz, Anja, Valdenaire, Julien, Pothier, Kurt, Hilpert, Carmela, Gnerre, Oliver, Peter, Xavier, Leroy, Markus A, Riederer

Publikováno v: Journal of medicinal chemistry. 56(12)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::979036e264a84296502af4190aa6c2ae
https://pubmed.ncbi.nlm.nih.gov/23721423

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Assessing the predictive power of unsupervised visualization techniques to improve the identification of GPCR-focused compound libraries

Autor: Modest von Korff, Kurt Hilpert

Publikováno v: Journal of chemical information and modeling. 46(4)

Principal component analysis and self-organizing maps (SOMs) were compared to cluster and visualize the chemical space of a large and diverse data set. The data set comprised about 3000 G-protein-coupled receptor (GPCR) ligands for about 130 receptor

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5db20ba2b8e8fd366c972b5a3c253a63
https://pubmed.ncbi.nlm.nih.gov/16859289

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