التفاصيل البيبلوغرافية
| العنوان: |
Discovery and Characterization of CD12681, a Potent RORγ Inverse Agonist, Preclinical Candidate for the Topical Treatment of Psoriasis |
| المؤلفون: |
Ouvry, Gilles, Atrux‐Tallau, Nicolas, Bihl, Franck, Bondu, Aline, Bouix‐Peter, Claire, Carlavan, Isabelle, Christin, Olivier, Cuadrado, Marie‐Josée, Defoin‐Platel, Claire, Deret, Sophie, Duvert, Denis, Feret, Christophe, Forissier, Mathieu, Fournier, Jean‐François, Froude, David, Hacini‐Rachinel, Fériel, Harris, Craig Steven, Hervouet, Catherine, Huguet, Hélène, Lafitte, Guillaume, Luzy, Anne‐Pascale, Musicki, Branislav, Orfila, Danielle, Ozello, Benjamin, Pascau, Coralie, Pascau, Jonathan, Parnet, Véronique, Peluchon, Guillaume, Pierre, Romain, Piwnica, David, Raffin, Catherine, Rossio, Patricia, Spiesse, Delphine, Taquet, Nathalie, Thoreau, Etienne, Vatinel, Rodolphe, Vial, Emmanuel, Hennequin, Laurent François |
| المصدر: |
ChemMedChem ; volume 13, issue 4, page 321-337 ; ISSN 1860-7179 1860-7187 |
| بيانات النشر: |
Wiley |
| سنة النشر: |
2018 |
| المجموعة: |
Wiley Online Library (Open Access Articles via Crossref) |
| الوصف: |
With possible implications in multiple autoimmune diseases, the retinoic acid receptor‐related orphan receptor RORγ has become a sought‐after target in the pharmaceutical industry. Herein are described the efforts to identify a potent RORγ inverse agonist compatible with topical application for the treatment of skin diseases. These efforts culminated in the discovery of N ‐(2,4‐dimethylphenyl)‐ N ‐isobutyl‐2‐oxo‐1‐[(tetrahydro‐2 H ‐pyran‐4‐yl)methyl]‐2,3‐dihydro‐1 H ‐benzo[ d ]imidazole‐5‐sulfonamide (CD12681), a potent inverse agonist with in vivo activity in an IL‐23‐induced mouse skin inflammation model. |
| نوع الوثيقة: |
article in journal/newspaper |
| اللغة: |
English |
| DOI: |
10.1002/cmdc.201700758 |
| الإتاحة: |
https://doi.org/10.1002/cmdc.201700758Test |
| حقوق: |
http://onlinelibrary.wiley.com/termsAndConditions#vorTest |
| رقم الانضمام: |
edsbas.59C9C539 |
| قاعدة البيانات: |
BASE |
