Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Jean-Yves Chiva"'
Autor:
Kathy F. K. Cheung, Jean-Yves Chiva, Satish Dayal, Darren Stead, Carly L. Nichols, Rob Webster, Lee R. Roberts, David Stonehouse, Felice Daverio, Iain Gardner, Andrew Pike, Michael Paradowski, David C. Blakemore, Gilles H. Goetz, Lesa Watson, Chris Pickford, Jared B.J. Milbank, Ye Che, Robert Wybrow, Florian Wakenhut, Keith Statham, Caroline Smith-Burchnell, Samuel Crook, Fiona M. Adam, David C. Pryde, David Leese, Mike Westby, Duncan Hay, Stephen M. Shaw, Tram T. Tran
Publikováno v:
ChemMedChem. 9:1378-1386
Nonstructural protein 5A (NS5A) represents a novel target for the treatment of hepatitis C virus (HCV). Daclatasvir, recently reported by Bristol-Myers-Squibb, is a potent NS5A inhibitor currently under investigation in phase 3 clinical trials. While
Publikováno v:
Synlett. 2011:1101-1104
Treatment of 4-amino-4-phenyl-butan-2-ol with mesyl chloride, followed by displacement with amine nucleophiles resulted in a 1,3 rearrangement via an azetidinium cation intermediate. This rearrangement has been proven to proceed via a double inversio
Autor:
Malcolm MacKenny, Andrews Mark David, Jean-Yves Chiva, Mark Ian Lansdell, Alan Daniel Brown, David W. Gordon, David Sebastien Fradet
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5893-5897
A second wave of potential SSRIs with high ease of synthetic accessibility were designed based on the reported selective serotonin re-uptake inhibitor litoxetine and our own previous work in this area. Preparation and subsequent optimisation yielded
Autor:
Rachel L. Eastwood, Kerry A. Paradowski, Donald Stuart Middleton, Jean-Yves Chiva, Barber Christopher Gordon, David C. Blakemore
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:1499-1503
Optimisation of a series of 4-piperidinyltriazoles led to the identification of compound 28a which showed good whole cell antiviral activity, excellent selectivity over the hERG ion channel and complete oral absorption.
Autor:
Rachel L. Eastwood, Barber Christopher Gordon, Kerry A. Paradowski, Michelle Y. Platts, David R. Fenwick, Jean-Yves Chiva, David C. Blakemore
Publikováno v:
Tetrahedron Letters. 52:512-514
An efficient route to dipyridone acid HIV integrase inhibitors is developed. The key steps include a one-pot three-step formation of the core template (containing one point of structural diversity) followed by a regioselective benzylation and in situ
Autor:
Florian Wakenhut, Thien Duc Tran, Chris Pickford, Stephen Shaw, Mike Westby, Caroline Smith-Burchnell, Lesa Watson, Michael Paradowski, Jared Milbank, David Stonehouse, Kathy Cheung, Robert Wybrow, Felice Daverio, Samuel Crook, Keith Statham, David Leese, Darren Stead, Fiona Adam, Duncan Hay, Lee R. Roberts, Jean-Yves Chiva, Carly Nichols, David C. Blakemore, Gilles H. Goetz, Ye Che, Iain Gardner, Satish Dayal, Andrew Pike, Rob Webster, David C. Pryde
Publikováno v:
ChemMedChem. 9(7)
In ongoing studies towards novel hepatitis C virus (HCV) therapeutics, inhibitors of nonstructural protein 5A (NS5A) were evaluated. Specifically, starting from previously reported lead compounds, peripheral substitution patterns of a series of biary
Autor:
Mark Andrews, Alan Brown, Jean-Yves Chiva, David Fradet, David Gordon, Mark Lansdell, Malcolm MacKenny
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(8)
The reported selective serotonin Re-uptake Inhibitor Litoxetine was used as the starting point in the design of a range of potential SSRIs with high ease of synthetic accessibility. Preparation and subsequent optimization yielded a range of potent an
Autor:
Rachel L. Eastwood, Donald Stuart Middleton, David C. Blakemore, Barber Christopher Gordon, Jean-Yves Chiva, Kerry A. Paradowski
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(4)
The development of a new class of CCR5 antagonist replacing the tropane core of maraviroc by piperidine with a branched N-substituent is described. Compound 15h shows good whole cell antiviral activity together with microsomal stability and only weak