1002344-90-2Relevant articles and documents
3-PHOSPHOGLYCERATE DEHYDROGENASE INHIBITORS AND USES THEREOF
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Paragraph 00401-00403, (2017/10/06)
The present invention provides compounds, compositions thereof, and methods of using the same.
Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulators
Hemmerling, Martin,Edman, Karl,Lepist?, Matti,Eriksson, Anders,Ivanova, Svetlana,Dahmén, Jan,Rehwinkel, Hartmut,Berger, Markus,Hendrickx, Ramon,Dearman, Matthew,Jensen, Tina Jellesmark,Wissler, Lisa,Hansson, Thomas
supporting information, p. 5741 - 5748 (2016/11/28)
A structure-based design approach led to the identification of a novel class of indazole ether based, non-steroidal glucocorticoid receptor (GR) modulators. Several examples were identified that displayed cell potency in the picomolar range, inhibiting LPS-induced TNF-α release by primary peripheral blood mononuclear cells (PBMCs). Additionally, an improved steroid hormone receptor binding selectivity profile, compared to classical steroidal GR agonists, was demonstrated. The indazole ether core tolerated a broad range of substituents allowing for modulation of the physiochemical parameters. A small sub-set of indazole ethers, with pharmacokinetic properties suitable for oral administration, was investigated in a rat antigen-induced joint inflammation model and demonstrated excellent anti-inflammatory efficacy.
5-[(3,3,3-Trifluoro-2-hydroxy-1-arylpropyl)amino-1-arylquinolin-2-ones, a process for their production and their use as anti-inflammatory agents
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Page/Page column 20, (2010/03/02)
The present invention relates to compounds of formula I, processes and intermediates for their production and their use as antiinflammatory agents.