700835-81-0Relevant articles and documents
Novel isoflavone derivative, preparation method therefor and medicinal use of novel isoflavone derivative
-
Paragraph 0022; 0050-0052, (2018/07/30)
The invention relates to the field of pharmaceutical chemistry, relates to an isoflavone derivative, a preparation method therefor and medicinal use of the novel isoflavone derivative and particularlyrelates to isoflavone derivatives represented by a general formula (I) shown in the description, preparation methods therefor, pharmaceutical compositions containing these compounds and medicinal useof the isoflavone derivatives and the pharmaceutical compositions, particularly use of drugs for preventing or treating hyperlipidemia, type II diabetes, atherosclerosis and non-alcoholic fatty hepatitis.
Structure-guided design and synthesis of isoflavone analogs of GW4064 with potent lipid accumulation inhibitory activities
Qiu, Rongmao,Luo, Guoshun,Cai, Xuerong,Liu, Linyi,Chen, Mingqi,Chen, Deying,You, Qidong,Xiang, Hua
supporting information, p. 3726 - 3730 (2018/10/20)
Our group has previously reported a series of isoflavone derivatives with antidyslipidemic activity. With this background, a series of isoflavone analogs of GW4064 were designed, synthesized and evaluated the lipid-lowering activity of analogs. As a result, most of compounds significantly reduced the lipid accumulation in 3T3-L1 adipocytes and four of them (10a, 11, 15c and 15d) showed stronger inhibitory than GW4064. The most potent compound 15d exhibited promising agonistic activity for FXR in a cell-based luciferase reporter assay. Meanwhile, 15d up-regulated FXR, SHP and BSEP gene expression and down-regulated the mRNA expression of lipogenesis gene SREBP-1c. Besides, an improved safety profile of 15d was also observed in a HepG2 cytotoxicity assay compared with GW4064. The obtained biological results were further confirmed by a molecular docking study showing that 15d fitted well in the binding pocket of FXR and interacted with some key residues simultaneously.
NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS AS FXR MODULATORS
-
Paragraph 0135, (2018/05/24)
The present technology is directed to compounds, compositions, and methods related to modulation of FXR. In particular, the present compounds and compositions may be used to treat FXR-mediated disorders and conditions, including, e.g., liver disease, hype
NOVEL FXR (NR1H4 ) BINDING AND ACTIVITY MODULATING COMPOUNDS
-
Page/Page column 34; 36, (2011/04/13)
The present invention relates to compounds which bind to the NR1 H4 receptor (FXR) and act as agonists of the NR1 H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.
Novel FXR (NR1H4) binding and activity modulating compounds
-
Page/Page column 13, (2011/04/14)
The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.
FARNESOID X RECEPTOR AGONISTS
-
Page/Page column 135, (2009/03/07)
The present invention relates to famesoid X receptors (FXR, NR1H4) FXR is a member of the nuclear receptor class of ligand-activate transcription factors More particularly, the present invention relates to compounds useful as agonists for FXR, pharmaceutical formulations comprising such compounds, and therapeutic use of the same Novel isoxazole compounds are disclosed as part of pharmaceutical compositions for the treatment of a condition mediated by decreased FXR activity, such as obesity, diabetes, cholestatic liver disease, liver fibrosis, and metabolic syndrome
Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064
Akwabi-Ameyaw, Adwoa,Bass, Jonathan Y.,Caldwell, Richard D.,Caravella, Justin A.,Chen, Lihong,Creech, Katrina L.,Deaton, David N.,Jones, Stacey A.,Kaldor, Istvan,Liu, Yaping,Madauss, Kevin P.,Marr, Harry B.,McFadyen, Robert B.,Miller, Aaron B.,III, Frank Navas,Parks, Derek J.,Spearing, Paul K.,Todd, Dan,Williams, Shawn P.,Wisely, G. Bruce
supporting information; experimental part, p. 4339 - 4343 (2009/04/06)
Starting from the known FXR agonist GW 4064 1a, a series of stilbene replacements were prepared. The 6-substituted 1-naphthoic acid 1b was an equipotent FXR agonist with improved developability parameters relative to 1a. Analog 1b also reduced the severit
FARNESOID X RECEPTOR AGONISTS
-
Page/Page column 66, (2009/01/23)
The present invention relates to famesoid X receptors (FXR, NR1 H4) FXR is a member of the nuclear receptor class of ligand-activated transcription factors More particularly, the present invention relates to compounds useful as agonists for FXR, pharmaceu
FARNESOID X RECEPTOR AGONISTS
-
Page/Page column 39, (2010/11/27)
The present invention provides novel substituted isoxazole compounds, pharmaceutical compositions, therapeutic uses and processes for preparing the same.
