1034148-00-9Relevant academic research and scientific papers
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
, 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.
INDAZOLYL ESTER AND AMIDE DERIVATIVES FOR THE TREATMENT OF GLUCOCORTICOID RECEPTOR MEDIATED DISORDERS
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Example 2, (2008/12/06)
Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments
