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Discovery of BI-2545: A Novel Autotaxin Inhibitor That Significantly Reduces LPA Levels in Vivo

Autor: Helmut Romig, Sandra Handschuh, Tom Bretschneider, Bernd Nosse, Marco Ferrara, Paul Nicklin, Stefan Hoerer, Gerald Juergen Roth, Christian A. Kuttruff

Publikováno v: ACS medicinal chemistry letters. 8(12)

In an effort to find new therapeutic interventions addressing the unmet medical need of patients with idiopathic pulmonary fibrosis, we initiated a program to identify new autotaxin (ATX) inhibitors. Starting from a recently published compound (PF-83

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f11c130fd0b7a31871762c9d13a92903
https://pubmed.ncbi.nlm.nih.gov/29259743

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Synthesis and Anti-implantation Activity of New Stilbene Derivatives

Autor: Rakeshwar Bandichhor, Bernd Nosse, Vishnu K. Tandon, Kunwar A. Singh

Publikováno v: Arzneimittelforschung. 54:452-455

New stilbene (CAS 56-53-1) derivatives have been synthesized by reductive elimination of desoxybenzoin analogs which were obtained by Fries rearrangement of the corresponding phenolic esters. The chemical structures of the compounds obtained were con

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::982f8437483cd95c7b1a0123b38fd04d
https://doi.org/10.1055/s-0031-1296998

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Tumortherapien im Umbruch. Zielen lernen!

Autor: Bernd Nosse

Publikováno v: Chemie in unserer Zeit. 40:164-172

Bei der Entwicklung moderner Therapien zur Bekampfung von Krebs versucht man, Wirkstoffe spezifisch auf entartete Zellen zu richten und gezielt in molekulare Vorgange einzugreifen, um eine Wechselwirkung mit gesundem Gewebe zu vermeiden. Dieser Artik

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::539ffa1ddb6c449417cfdfbbd49240dc
https://doi.org/10.1002/ciuz.200600368

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Optimization of Ring-Closing Metathesis: Inert Gas Sparging and Microwave Irradiation

Autor: Won Boo Jeong, Bernd Nosse, Andreas Schall, Oliver Reiser

Publikováno v: Advanced Synthesis & Catalysis. 347:1869-1874

A systematic study of a ring-closing metathesis towards a tetrasubstituted double bond as part of a seven-membered ring in a 5.7.5-tricyclic guaianolide system is described. By combining two techniques, namely sparging an inert gas through the soluti

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::204c0f18684ef34ad4f9e77abce5244d
https://doi.org/10.1002/adsc.200505137

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Enantioselective Synthesis of Paraconic Acids

Autor: Michael Seitz, Oliver Reiser, Bernd Nosse, Sebastian Soergel, Rakeshwar B. Chhor, Claudius Boehm

Publikováno v: Chemistry - A European Journal. 9:260-270

The development of a new method for the enantioselective synthesis of disubstituted gamma-butyrolactones is reported. Based on this strategy, the total synthesis of three paraconic acids, that is (-)-roccellaric acid, (-)-nephrosteranic acid and (-)-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fbd002be53dc2ab6906c01d4be80101c
https://doi.org/10.1002/chem.200390019

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Identification of new potent GPR119 agonists by combining virtual screening and combinatorial chemistry

Autor: Bernd Wellenzohn, Uta Lessel, Christoph Hoenke, Bernd Nosse, Timo Isambert, Andreas Beller

Publikováno v: Journal of medicinal chemistry. 55(24)

Virtual screening in a huge collection of virtual combinatorial libraries has led to the identification of two new structural classes of GPR119 agonists with submicromolar in vitro potencies. Herein, we describe the virtual screening process involvin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::80cb329e336b3f0bc3948187e679d17c
https://pubmed.ncbi.nlm.nih.gov/23211099

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Novel 6,7,8,9-tetrahydro-5H-1,4,7,10a-tetraaza-cyclohepta[f]indene analogues as potent and selective 5-HT(2C) agonists for the treatment of metabolic disorders

Autor: Stephan Georg Mueller, Anna Pedret-Dunn, Natacha Prevost, Clemens Moeller, Christopher Brown, Juergen Prestle, Bernd Nosse, Stefan Scheuerer, Marcus Schindler, Mark Whittaker, Alexander Heifetz, Heather Tye

Publikováno v: Bioorganicmedicinal chemistry letters. 21(1)

The discovery of a novel series of 5-HT2C agonists based on a tricyclic pyrazolopyrimidine scaffold is described. Compounds with good levels of in vitro potency and moderate to good levels of selectivity with respect to the 5-HT2A and 5-HT2B receptor

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1fd92bc11aa8c6120cabf535e40752d2
https://pubmed.ncbi.nlm.nih.gov/21146986

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