848141-14-0Relevant academic research and scientific papers
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.
supporting information, 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.
HETEROCYCLIC COMPOUNDS WITH AN ROR(GAMMA)T MODULATING ACTIVITY
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Paragraph 0646, (2018/03/06)
The present invention relates to a compound that may have an ROR(gamma)t modulating activity and can thus be useful in the treatment of cancer.
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.
PYRAZINEDIHYDROPYRIMIDINONE OR PYRIDAZINEDIHYDROPYRIMIDINONE COMPOUNDS AS MODULATORS OF ROR GAMMA
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, (2018/01/17)
The present invention encompasses compounds of the 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.
COMPOUNDS AS MODULATORS OF ROR GAMMA
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, (2015/11/09)
The present invention encompasses compounds of the 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.
NOVEL SALT 628
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Page/Page column 22, (2010/09/05)
6-Methyl-5-(1-methyl-1H-pyrazol-5-yl)-N-{[5-(methylsulfonyl)pyridin-2-yl]methyl}-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2-dihydropyridine-3-carboxamide 4-methylbenzenesulfonate and a novel crystalline form thereof are disclosed together with processes for preparing such salt and form, pharmaceutical compositions comprising such a salt and form, and the methods of treatment using such a salt and form.
2-PYRIDONE DERIVATIVES AS NETROPHIL ELASTASE INHIBITORS AND THEIR USE
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Page/Page column 102, (2008/06/13)
There are provided novel compounds of formula (I), wherein R1, R2, R4, R5, G1, G2, L, Y and n are as defined in the Specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes
2-PYRIDONE DERIVATIVES AS NEUTROPHIL ELASTASE INHIBITORS AND THEIR USE
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Page/Page column 86, (2010/02/11)
There are provided novel compounds of formula (I), wherein R1, R2, R4, R5, G1, G2, L, Y and n are as defined in the Specification and optical isomers, racemates and tautomers thereof, and p
