848141-13-9Relevant articles and documents
Discovery of a Series of Pyrazinone RORγAntagonists and Identification of the Clinical Candidate BI 730357
Harcken, Christian,Csengery, Johanna,Turner, Michael,Wu, Lifen,Liang, Shuang,Sibley, Robert,Brunette, Steven,Labadia, Mark,Hoyt, Kathleen,Wayne, Anita,Wieckowski, Thomas,Davis, Gregg,Panzenbeck, Mark,Souza, Donald,Kugler, Stanley,Terenzio, Donna,Collin, Delphine,Smith, Dustin,Fryer, Ryan M.,Tseng, Yin-Chao,Hehn, J?rg P.,Fletcher, Kim,Hughes, Robert O.
, p. 143 - 154 (2021/01/26)
The interleukin (IL)-23/T helper (Th)17 axis plays a critical role in autoimmune diseases, and there is an increasing number of biologic therapies that target IL-23 and IL-17. The transcription factor retinoic acid receptor-related orphan nuclear receptor γt (RORγt) is important for the activation and differentiation of Th17 cells and thus is an attractive pharmacologic target for the treatment of Th17-mediated diseases. A novel series of pyrazinone RORγantagonists was discovered through hybridization of two distinct screening hits and scaffold hopping. The series offers attractive potency and selectivity in combination with favorable druglike properties, such as metabolic stability and aqueous solubility. Lead optimization identified a clinical candidate, compound (S)-11 (BI 730357), for the treatment of autoimmune diseases.
COMPOUNDS AS MODULATORS OF ROR GAMMA
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, (2019/03/28)
The present invention encompasses compounds of the formula (I)(I) wherein the variables are defined herein which are suitable for the modulation of RORγ and the treatment of diseases related to the modulation of RORγ. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.
PTERIDINE DERIVATIVES AS MODULATORS OF ROR GAMMA
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, (2017/08/01)
The present invention encompasses compounds of formula (I) wherein the variables are defined herein which are suitable for the modulation of RORγ and the treatment of diseases related to the modulation of RORγ. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.