210691-38-6Relevant articles and documents
Discovery and Characterization of CD12681, a Potent RORγ Inverse Agonist, Preclinical Candidate for the Topical Treatment of Psoriasis
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-Fran?ois,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 Fran?ois
, p. 321 - 337 (2018/02/12)
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-2H-pyran-4-yl)methyl]-2,3-dihydro-1H-benzo[d]imidazole-5-sulfonamide (CD12681), a potent inverse agonist with in vivo activity in an IL-23-induced mouse skin inflammation model.
A class of sulfonamide carbonic anhydrase inhibitors with neuropathic pain modulating effects
Carta, Fabrizio,Di Cesare Mannelli, Lorenzo,Pinard, Melissa,Ghelardini, Carla,Scozzafava, Andrea,McKenna, Robert,Supuran, Claudiu T.
, p. 1828 - 1840 (2015/03/14)
A series of benzene sulfonamide carbonic anhydrase (CA, EC 4.2.1.1) inhibitors which incorporate lipophilic 4-alkoxy- and 4-aryloxy moieties, together with several derivatives of ethoxzolamide and sulfanilamide are reported. These derivatives were investi
INDOLINE SCAFFOLD SHP-2 INHIBITORS AND CANCER TREATMENT METHOD
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Page/Page column 55; 57, (2010/04/03)
The subject invention concerns methods and compounds for inhibiting Shp2. In one embodiment, a compound of the invention has a chemical structure as shown in formula I or II: wherein X, Y, and Z are independently N or S; R1 is cycloalkyl, heter