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Novel estrogen-related receptor alpha inhibitor and medical application thereof

A technology of estrogen and inhibitors, which is applied in the field of new estrogen-related receptor α inhibitors, and achieves the effect of broad application prospects

Inactive Publication Date: 2017-03-08
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the reasons of efficacy and safety, there are no approved marketed anti-tumor drugs among the above-mentioned inhibitors

Method used

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  • Novel estrogen-related receptor alpha inhibitor and medical application thereof
  • Novel estrogen-related receptor alpha inhibitor and medical application thereof
  • Novel estrogen-related receptor alpha inhibitor and medical application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] The time-resolved fluorescence resonance energy transfer detection technology (Time-Resolved Fluoresence Resonance Energy Transfer Assay, TR-FRET Assay) was used to test the competitive binding activity of the compounds of the present invention to ERRα at the molecular level.

[0026] This example illustrates that the compounds involved in the present invention can effectively inhibit the binding of ERRα to co-activator PGC-1α, indicating that the compounds involved in the present invention competitively bind to ERRα (molecular level). TR-FRET is a technique familiar to those skilled in the art.

[0027]FRET (Fluoresence Resonance Energy Transfer) is fluorescence resonance energy transfer, which is based on the energy transfer of two fluorescent groups (donor and acceptor). In the case of two fluorescent groups in close proximity, the interaction between biomacromolecules can be measured with fluorescent labels and energy transfer between the two. When the two groups a...

Embodiment 2

[0043] The preparation of formula I compound

[0044] Step 1, preparation of compound 2

[0045]

[0046] 3β-Hydroxyoleanane-13(18)-ene-28-carboxylic acid (1) (20 g, 0.044 mol) was dissolved in THF (600 mL), and LiAlH was added in portions 4 (7 g, 0.183 mol). Stir at reflux for 1.5 hours. Add methanol and water to quench, extract with ethyl acetate, combine organic layers, wash with saturated brine, and dry over anhydrous sodium sulfate. After spin-drying, a white solid 2 (17 g, yield 88%) was obtained by silica gel column chromatography. IR (film, cm -1 )3374, 2928, 2868, 2359, 1633, 1455, 1384, 1359, 1044, 996, 971; 1 H NMR (300MHz, DMSO-d6) δ3.60 (brs, 2H), 3.23 (dd, J = 5.5, 10.9Hz, 1H), 2.75-2.69 (m, 1H), 2.32 (d, J = 14.1Hz, 1H), 1.93-0.72(m, 22H), 1.18(s, 3H), 0.99(s, 3H), 0.94(s, 3H), 0.86(s, 6H), 0.77(s, 3H), 0.74(s ,3H); 13 C NMR (75MHz, DMSO-d6) δ136.9, 130.9, 77.3, 61.1, 55.4, 50.5, 44.5, 40.9, 39.2, 39.0, 38.9, 37.3, 35.2, 34.9, 33.2, 32.5, 32.2, 29.0, ...

Embodiment 3

[0066] tablet

[0067] The formula I compound (50g) prepared in Example 2, hydroxypropylmethylcellulose E (150g), starch (200g), povidone K30 appropriate amount and magnesium stearate (1g) were mixed, granulated, pressed piece.

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PUM

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Abstract

The invention discloses a novel estrogen-related receptor alpha (ERR alpha) inhibitor, which is a compound of a formula I and pharmaceutically acceptable salt or solvate thereof. A pharmaceutical composition containing the compound can be used for preparing medicines for preventing and treating diseases including mammary cancer, cervical carcinoma, ovarian cancer, prostatic cancer, stomach cancer, colon cancer and the like.

Description

technical field [0001] The invention relates to a novel estrogen-related receptor alpha inhibitor and its medical use. Background technique [0002] Estrogen plays an important role in the growth, development and metabolism of organisms, and its abnormal level may also be the cause of some tumors. Estrogen regulates its physiological effects by binding to specific nuclear receptors in target cells - estrogen receptors (Estrogen receptor, ER) α and β. Studies have found that a class of orphan nuclear receptors that can produce biological functions without binding to ligands—Estrogen-related receptors (ERRs) are also involved in the complex signal transduction system of estrogen, and are associated with Diseases caused by estrogen are closely related. [0003] ERR and ER belong to the third class of nuclear receptors, mainly including three subtypes: ERRα (NR3B1), ERRβ (NR3B2), and ERRγ (NR3B3). Among them, ERRα was first screened by Giguere et al. using the cDNA of the DNA...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J63/00A61K31/56A61P35/00
CPCC07J63/008
Inventor 孙宏斌赵慧陈冬寅林超
Owner CHINA PHARM UNIV
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