609783-75-7Relevant academic research and scientific papers
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)
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.
BENZAMIDE DERIVATIVES
-
Page 40, (2010/02/10)
A compound represented by formula (1): wherein X is a single bond or a substituted or unsubstituted lower alkylene group; Z is a saturated or unsaturated monocyclic hydrocarbon ring group or the like; and each of R1, R2, R3 and R4, which may be the same or different, is a hydrogen atom, a halogen atom, a nitro group, a cyano group, a carboxyl group, a substituted or unsubstituted alkyl group, or the like, a prodrug of said compound, or a pharmaceutically acceptable salt of said compound or prodrug has inhibitory effect on Rho kinase and hence is useful for treating diseases which are such that morbidity due to them is expected to be improved by inhibition of Rho kinase and secondary effects such as inhibition of the Na+/H+ exchange transport system caused by the Rho kinase inhibition, for example, hypertension.
