M
Michael Bös
Researcher at Boehringer Ingelheim
Publications - 24
Citations - 1993
Michael Bös is an academic researcher from Boehringer Ingelheim. The author has contributed to research in topics: Hepatitis C virus & NS3. The author has an hindex of 15, co-authored 24 publications receiving 1898 citations.
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Journal ArticleDOI
An NS3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus.
Daniel Lamarre,Paul C. Anderson,Murray D. Bailey,Pierre L. Beaulieu,Gordon Bolger,Pierre R. Bonneau,Michael Bös,Dale R. Cameron,Mireille Cartier,Michael G. Cordingley,Anne-Marie Faucher,Nathalie Goudreau,Stephen H. Kawai,George Kukolj,Lisette Lagacé,Steven R. LaPlante,Hans Narjes,Marc-André Poupart,Jean Rancourt,Roel E. Sentjens,Roger St. George,Bruno Simoneau,Gerhard G. Steinmann,Diane Thibeault,Youla S. Tsantrizos,Steven M. Weldon,Chan-Loi Yong,Montse Llinas-Brunet +27 more
TL;DR: Administration of BILN 2061 to patients infected with HCV genotype 1 for 2 days resulted in an impressive reduction of HCV RNA plasma levels, and established proof-of-concept in humans for an HCV NS3 protease inhibitor, illustrating the potential of the viral-enzyme-targeted drug discovery approach for the development of new HCV therapeutics.
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Influence of the 5-HT6 receptor on acetylcholine release in the cortex: pharmacological characterization of 4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine, a potent and selective 5-HT6 receptor antagonist.
Claus Riemer,Edilio Borroni,Bernard Levet-Trafit,James R. Martin,Sonia Poli,Porter Richard Hugh Phillip,Michael Bös +6 more
TL;DR: A functional correlation between 5-HT(6) receptors and cholinergic neurotransmission could be shown, supporting the therapeutic potential of 5- HT( 6) receptors in the treatment of cognitive deficits.
Journal ArticleDOI
Discovery of BI 224436, a Noncatalytic Site Integrase Inhibitor (NCINI) of HIV-1.
Lee Fader,Eric Malenfant,Mathieu Parisien,Rebekah J. Carson,François Bilodeau,Serge Landry,Marc Pesant,Christian Brochu,Sébastien Morin,Catherine Chabot,Ted Halmos,Yves Bousquet,Murray D. Bailey,Stephen H. Kawai,René Coulombe,Steven R. LaPlante,Araz Jakalian,Punit Bhardwaj,Dominik Wernic,Patricia Schroeder,Ma’an Amad,Paul J. Edwards,Michel Garneau,Jianmin Duan,Michael G. Cordingley,Richard Bethell,Stephen W. Mason,Michael Bös,Pierre R. Bonneau,Marc-André Poupart,Anne-Marie Faucher,Bruno Simoneau,Craig Fenwick,Christiane Yoakim,Youla S. Tsantrizos +34 more
TL;DR: An assay recapitulating the 3' processing activity of HIV-1 integrase (IN) was used to screen the Boehringer Ingelheim compound collection, leading to the discovery of compound 26 (BI 224436), the first NCINI to advance into a phase Ia clinical trial.
Journal ArticleDOI
Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: discovery and preliminary SAR of benzimidazole derivatives
Pierre L. Beaulieu,Michael Bös,Yves Bousquet,Gulrez Fazal,Jean Gauthier,James Gillard,Sylvie Goulet,Steven R. LaPlante,Marc-André Poupart,Sylvain Lefebvre,Ginette McKercher,Charles Pellerin,Volkhard Austel,George Kukolj +13 more
TL;DR: Potent analogues in this series inhibit the polymerase at low micromolar concentrations and provide an attractive "drug-like" lead structure for further optimization and the development of potential HCV therapeutics.
Journal ArticleDOI
Preclinical Profile of BI 224436, a Novel HIV-1 Non-Catalytic-Site Integrase Inhibitor
Craig Fenwick,Ma’an Amad,Murray D. Bailey,Richard Bethell,Michael Bös,Pierre R. Bonneau,Michael G. Cordingley,René Coulombe,Jianmin Duan,Paul J. Edwards,Lee Fader,Anne-Marie Faucher,Michel Garneau,Araz Jakalian,Stephen H. Kawai,Louie Lamorte,Steven R. LaPlante,Laibin Luo,Steve Mason,Marc-André Poupart,Nathalie Rioux,Patricia Schroeder,Bruno Simoneau,Sonia Tremblay,Youla S. Tsantrizos,Myriam Witvrouw,Christiane Yoakim +26 more
TL;DR: BI 224436 has drug-like in vitro absorption, distribution, metabolism, and excretion properties, including Caco-2 cell permeability, solubility, and low cytochrome P450 inhibition, and has an additive effect in combination with most approved antiretrovirals, including INSTIs.