Discovery of phenoxyindazoles and phenylthioindazoles as RORγ inverse agonists

Autor: Romain Pierre, Etienne Thoreau, Catherine Raffin, Claire Bouix-Peter, Laurent Chantalat, Gaëlle Polge, Jonathan Pascau, Gilles Ouvry, Nathalie Taquet, Catherine Comino, Denis Duvert, Danielle Orfila, Agnès Perrin, Yves Rival, Laurent Francois Andre Hennequin, Laurent Lamy, Christophe Feret, Branislav Musicki, Veronique Parnet, Anne-Pascale Luzy, Olivier Christin, Fabrice Ciesielski, Craig S. Harris

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 26:5802-5808

Targeting the IL17 pathway and more specifically the nuclear receptor RORγ is thought to be beneficial in multiple skin disorders. The Letter describes the discovery of phenoxyindazoles and thiophenoxy indazoles as potent RORγ inverse agonists. Opt

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::af63284f22f668869fc68a5936ba38ec
https://doi.org/10.1016/j.bmcl.2016.10.023

Sulfoximines as potent RORγ inverse agonists

Autor: Etienne Thoreau, Craig S. Harris, David Froude, Franck Bihl, Gilles Ouvry, Delphine Spiesse, Patricia Rossio, Christophe Feret, Emmanuel Vial, Laurent F. Hennequin, Jonathan Pascau, Coralie Pascau, Romain Pierre, Claire Defoin-Platel, Nathalie Taquet, Catherine Hervouet, Veronique Parnet, Olivier Christin, Guillaume Lafitte, Sophie Deret, Catherine Raffin, Claire Bouix-Peter, Anne-Pascale Luzy, Feriel Hacini-Rachinel, Branislav Musicki, Danielle Orfila, Rodolphe Vatinel

Publikováno v: Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters, 2018, 28 (8), pp.1269-1273. ⟨10.1016/j.bmcl.2018.03.041⟩
Bioorganic and Medicinal Chemistry Letters, Elsevier, 2018, 28 (8), pp.1269-1273. ⟨10.1016/j.bmcl.2018.03.041⟩

Progress in the identification of suitable RORγ inverse agonists as clinical candidates has been hampered by the high lipophilicity that seems required for high potency on this nuclear receptor. In this context, we decided to focus on the replacemen

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::00fa57781e16cd4033a4b4d8d851561b
https://hal.science/hal-02526180

Novel 3-(4-piperidinylthio)-1 H -indoles as potent nonopioid orally active central analgesics

Autor: Dominique Potin, Veronique Parnet, Francoise Camborde, Alix Cloarec, Joelle Meignen, Francois Caussade, Daniel Provost, Jean-Marie Teulon

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 10:805-809

A series of 3-(4-piperidinylthio)-1H-indoles was synthesized and evaluated in mice in the phenylbenzoquinone(PBQ)-induced writhing and hot plate tests. Most of these compounds are good analgesics with activities comparable to that of morphine. Among

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dcade688672fc4695b0e866f5a9ef49f
https://doi.org/10.1016/s0960-894x(00)00102-5

'A la folie … pas du tout'.

Autor: Prescott, Judith

Publikováno v: Hollywood Reporter -- International Edition; 4/9/2002, Vol. 372 Issue 47, p20, 2p

Andrée Davanture, la passion du montage

Autor: Forest claude

L'ouvrage retrace le parcours de cette grande monteuse du cinéma, qui commença classiquement dans le cinéma populaire en 1952 en travaillant avec les réalisateurs français de renom de l'époque (Henri Verneuil, Robert Hossein), devint cheffe mon