449804-09-5Relevant academic research and scientific papers
BICYCLIC ROR-GAMMA MODULATORS
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, (2019/10/04)
Described herein are retinoic acid related-related orphan nuclear receptor (ROR) modulators and methods of utilizing ROR-gamma modulators in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.
SPIROCYCLIC ROR-GAMMA MODULATORS
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, (2019/10/04)
Described herein are retinoic acid related-related orphan nuclear receptor (ROR) modulators and methods of utilizing ROR-gamma modulators in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.
Modulators of the nuclear hormone receptor ROR
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, (2017/03/28)
The invention provides small molecule modulators of retinoic acid receptor-related orphan receptors such as RORα, RORβ, or RORγ, of formula with the variable atoms as defined herein and R1 comprising a hydroxyl- or alkoxyl-substituted fluoroalkyl group. Compounds of the invention can be effective modulators at concentrations ineffective to act on LXR receptors, or on other nuclear receptors, or other biological targets. Methods of modulation the RORs and methods of treating metabolic disorders, immune disorders, cancer, and CNS disorders wherein modulation of an ROR is medically indicated are also provided.
Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis
Tamayo, Nuria A.,Norman, Mark H.,Bartberger, Michael D.,Hong, Fang-Tsao,Bo, Yunxin,Liu, Longbin,Nishimura, Nobuko,Yang, Kevin C.,Tadesse, Seifu,Fotsch, Christopher,Chen, Jie,Chmait, Samer,Cupples, Rod,Hale, Clarence,Jordan, Steven R.,Lloyd, David J.,Sivits, Glenn,Van, Gwyneth,St. Jean, David J.
supporting information, p. 4462 - 4482 (2015/06/25)
The glucokinase-glucokinase regulatory protein (GK-GKRP) complex plays an important role in controlling glucose homeostasis in the liver. We have recently disclosed a series of arylpiperazines as in vitro and in vivo disruptors of the GK-GKRP complex with
SULFONYLPIPERAZINE DERIVATIVES THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN FOR THE TREATMENT OF DIABETES
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Page/Page column 131; 132, (2012/03/26)
The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.
Design and synthesis of heterocyclic malonyl-CoA decarboxylase inhibitors
Cheng, Jie-Fei,Chen, Mi,Liu, Bin,Hou, Zheng,Arrhenius, Thomas,Nadzan, Alex M.
, p. 695 - 700 (2007/10/03)
We have previously reported the discovery of small molecule inhibitors of malonyl-CoA decarboxylase (MCD) as novel metabolic modulators, which inhibited fatty acid oxidation and consequently increased the glucose oxidation rates in the isolated working ra
