1003709-83-8Relevant articles and documents
Route scouting and optimization of a potent sulfoximine-based inverse agonist of RORγt
Lafitte, Guillaume,Parnet, Veronique,Pierre, Romain,Raffin, Catherine,Vatinel, Rodolphe,Musicki, Branislav,Tomas, Loic,Bouix-Peter, Claire,Ouvry, Gilles,Daver, Sebastien,Arlabosse, Jean-Marie,Boiteau, Jean-Guy,Gerfaud, Thibaud,Harris, Craig S.
, p. 5974 - 5986 (2018/09/11)
During our research looking for novel inverse agonists of RORγt, we identified a potent sulfoximine-based modulator as one of our pre-clinical candidates for the topical treatment for psoriasis. Herein, we describe the various routes we evaluated during the lead generation and optimization phases and the final route chosen for scale-up to deliver the first 100 g of API.