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Discovery of phenoxyindazoles and phenylthioindazoles as RORγ inverse agonists.
Ouvry, Gilles; Bouix-Peter, Claire; Ciesielski, Fabrice; Chantalat, Laurent; Christin, Olivier; Comino, Catherine; Duvert, Denis; Feret, Christophe; Harris, Craig S; Lamy, Laurent; Luzy, Anne-Pascale; Musicki, Branislav; Orfila, Danielle; Pascau, Jonathan; Parnet, Véronique; Perrin, Agnès; Pierre, Romain; Polge, Gaëlle; Raffin, Catherine; Rival, Yves; Taquet, Nathalie; Thoreau, Etienne; Hennequin, Laurent F.
Affiliation
  • Ouvry G; Galderma R&D, Les Templiers 2400 Route des Colles, 06410 Biot, France.
  • Bouix-Peter C; Galderma R&D, Les Templiers 2400 Route des Colles, 06410 Biot, France.
  • Ciesielski F; NovAliX, Bld Sébastien Brant, Bioparc, 67405 Illkirch Cedex, France.
  • Chantalat L; Galderma R&D, Les Templiers 2400 Route des Colles, 06410 Biot, France.
  • Christin O; Galderma R&D, Les Templiers 2400 Route des Colles, 06410 Biot, France.
  • Comino C; Galderma R&D, Les Templiers 2400 Route des Colles, 06410 Biot, France.
  • Duvert D; Galderma R&D, Les Templiers 2400 Route des Colles, 06410 Biot, France.
  • Feret C; Galderma R&D, Les Templiers 2400 Route des Colles, 06410 Biot, France.
  • Harris CS; Galderma R&D, Les Templiers 2400 Route des Colles, 06410 Biot, France.
  • Lamy L; Galderma R&D, Les Templiers 2400 Route des Colles, 06410 Biot, France.
  • Luzy AP; Galderma R&D, Les Templiers 2400 Route des Colles, 06410 Biot, France.
  • Musicki B; Galderma R&D, Les Templiers 2400 Route des Colles, 06410 Biot, France.
  • Orfila D; Galderma R&D, Les Templiers 2400 Route des Colles, 06410 Biot, France.
  • Pascau J; Galderma R&D, Les Templiers 2400 Route des Colles, 06410 Biot, France.
  • Parnet V; Galderma R&D, Les Templiers 2400 Route des Colles, 06410 Biot, France.
  • Perrin A; Galderma R&D, Les Templiers 2400 Route des Colles, 06410 Biot, France.
  • Pierre R; Galderma R&D, Les Templiers 2400 Route des Colles, 06410 Biot, France.
  • Polge G; Galderma R&D, Les Templiers 2400 Route des Colles, 06410 Biot, France.
  • Raffin C; Galderma R&D, Les Templiers 2400 Route des Colles, 06410 Biot, France.
  • Rival Y; Galderma R&D, Les Templiers 2400 Route des Colles, 06410 Biot, France.
  • Taquet N; Galderma R&D, Les Templiers 2400 Route des Colles, 06410 Biot, France.
  • Thoreau E; Galderma R&D, Les Templiers 2400 Route des Colles, 06410 Biot, France.
  • Hennequin LF; Galderma R&D, Les Templiers 2400 Route des Colles, 06410 Biot, France.
Bioorg Med Chem Lett ; 26(23): 5802-5808, 2016 12 01.
Article in En | MEDLINE | ID: mdl-27815118
ABSTRACT
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. Optimization of the potency and efforts to mitigate the phototoxic liability of the series are presented. Finally, crystallization of the lead compound revealed that the series bound to an allosteric site of the nuclear receptor. Such compounds could be useful as tool compounds for understanding the impact of topical treatment on skin disease models.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Nuclear Receptor Subfamily 1, Group F, Member 3 / Indazoles Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2016 Type: Article Affiliation country: France
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Nuclear Receptor Subfamily 1, Group F, Member 3 / Indazoles Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2016 Type: Article Affiliation country: France