Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Francesca Blasco"'
Autor:
Peter Drueckes, Clive Mccarthy, Catherine H. Régnier, Giorgio Ottaviani, Janitha Reetz, Marc Gerspacher, Fabienne Baffert, Francesca Blasco, Philipp Holzer, Christoph Gaul, Julien Scesa, Eric Vangrevelinghe, Pascal Furet, Carole Pissot-Soldermann, Flavio Ossola, Gisele A. Tavares, Thomas Radimerski
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2609-2613
We have designed and synthesized a novel series of 2,8-diaryl-quinoxalines as Janus kinase 2 inhibitors. Many of the inhibitors show low nanomolar activity against JAK2 and potently suppress proliferation of SET-2 cells in vitro. In addition, compoun
Autor:
Raffaello Masciadri, Anke Kurt, Andreas Koblet, Theresa M. Ballard, Pierre-Emmanuel Broutin, Guido Achermann, Porter Richard Hugh Phillip, Francesca Blasco, Frédéric Knoflach, Heinz Stadler, Henner Knust, Peter Hilty, Bernd Büttelmann, Andrew Thomas, Maria-Clemencia Hernandez, Martin Graf, James R. Martin, Holger Fischer, Gerhard Trube, Jürgen Wichmann
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5746-5752
Through iterative design cycles we have discovered a number of novel new classes where the imidazo[1,5-a][1,2,4]-triazolo[1,5-d][1,4]benzodiazepine was deemed the most promising GABA(A) alpha5 inverse agonist class with potential for cognitive enhanc
Autor:
Daniel Guthy, Marc Gerspacher, Jasmin Wirth, Robin Alec Fairhurst, Joachim Blanz, Van Huy Luu, Patricia Imbach-Weese, Robert Mah, Christian Schnell, Esther Roehn-Carnemolla, Giorgio Caravatti, Christine Fritsch, Francesca Blasco, Sandrine Desrayaud, Pascal Furet, Dorothee Arz, Mark Knapp
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(17)
A cyclisation within a 4',5-bisthiazole (S)-proline-amide-urea series of selective PI3Kα inhibitors led to a novel 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole tricyclic sub-series. The synthesis and optimisation of this 4,5-dihydrobenzo[1,2-d:3,4-d]bis
Autor:
Patricia Imbach-Weese, Jacques Hamon, Doriano Fabbro, Reiner Aichholz, Vito Guagnano, Robin Alec Fairhurst, Ian N. Bruce, Christine Fritsch, Giorgio Caravatti, Joachim Blanz, Pascal Furet, Francesca Blasco, Mark Knapp
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(13)
Phosphatidylinositol-3-kinase α (PI3Kα) is a therapeutic target of high interest in anticancer drug research. On the basis of a binding model rationalizing the high selectivity and potency of a particular series of 2-aminothiazole compounds in inhi
Publikováno v:
Bioorganicmedicinal chemistry. 21(11)
There has recently been a burgeoning interest in impeding drug metabolism by replacing hydrogen atoms with deuterium to invoke a kinetic isotope effect. Imatinib, a front-line therapy for both chronic myeloid leukemia and of gastrointestinal stromal
Autor:
Christoph Gaul, Patrick Chène, Thomas Radimerski, Eric Vangrevelinghe, Carole Pissot-Soldermann, Alain De Pover, Marc Gerspacher, Ralf Endres, Dirk Erdmann, Fabienne Baffert, Francesco Hofmann, Jörg Trappe, Peter Drueckes, Marc Lang, Thomas Buhl, Reiner Aichholz, Catherine H. Régnier, Francesca Blasco, Philipp Holzer, Pascal Furet
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(5)
A series of novel benzoxazole derivatives has been designed and shown to exhibit attractive JAK2 inhibitory profiles in biochemical and cellular assays, capable of delivering compounds with favorable PK properties in rats. Synthesis and structure–a
Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation
Autor:
Lucinda Steward, Francesca Blasco, Jens-Uwe Peters, Thomas Lübbers, Alexander Alanine, Sabine Kolczewski
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(1)
The optimisation of affinity and selectivity in a novel series of dual 5-HT 5A /5-HT 7 receptor ligands is described. Brain penetrant 2-aminodihydroquinazolines with low nanomolar affinities were identified.
Autor:
Jens-Uwe Peters, Francesca Blasco, Thomas Lübbers, Sabine Kolczewski, Lucinda Steward, Alexander Alanine
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(1)
The optimisation of molecular properties within a series of 2-amino dihydroquinazoline 5-HT5A/5-HT7 receptor ligands resulted in a significantly improved brain-to-plasma ratio, enhancing the pharmacological utility of these compounds. By modulating t
Autor:
Patricia Imbach-Weese, Robin Alec Fairhurst, Doriano Fabbro, Pascal Furet, Joachim Blanz, Christine Fritsch, Giorgio Caravatti, Vito Guagnano, Ian N. Bruce, Mark Knapp, Jacques Hamon, Francesca Blasco, Reiner Aichholz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:4723