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Substituted thiophene compound as well as preparation method and application thereof

A technology of compound and thiophene, which is applied in the fields of its preparation, medicine for diseases, substituted thiophene compounds, estrogen receptor-related receptor α inverse agonists, can solve problems affecting development, low activity in vivo, and poor structure-activity relationship. Clear and other issues

Active Publication Date: 2020-12-29
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these developed ERRα inverse agonists have problems such as low in vivo activity, unsatisfactory tissue specificity or subtype selectivity, and unclear structure-activity relationship, which also affects their subsequent development and related research.

Method used

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  • Substituted thiophene compound as well as preparation method and application thereof
  • Substituted thiophene compound as well as preparation method and application thereof
  • Substituted thiophene compound as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0114] The present invention will be further described below in conjunction with the examples, but these examples are absolutely not intended to limit the present invention.

[0115] About reagents and consumables: no special instructions, all reagents are commercially available, and the silica gel used for purification is 200-300 mesh column chromatography silica gel produced by Qingdao Ocean Chemical Factory

[0116] About Analytical Instruments:

[0117] Hydrogen spectra were recorded by Bruker Avance III 600, Bruker Avance III 500, Brucher AM-400 and GEMINI-300 nuclear magnetic resonance instruments, and chemical shifts were expressed in δ (ppm);

[0118] Mass spectra were recorded by a Finnigan MAT-95 mass spectrometer or an Agilent model 1200-6110 single quadrupole liquid chromatography-mass spectrometer.

[0119] Synthesis and Characterization of Compounds P-1 to P-28

[0120]

[0121] Step a: Compound 1a (25 g, 0.195 mol) was mixed with 100 mL of acetic acid, and ...

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PUM

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Abstract

The invention relates to a thiophene compound and pharmaceutically acceptable salts thereof represented by a general formula I, a preparation method thereof, a pharmaceutical composition containing the thiophene compound or pharmaceutically acceptable salts thereof, and applications of the thiophene compound and the pharmaceutically acceptable salts. The thiophene compound and the pharmaceuticallyacceptable salts thereof are used as a novel estrogen-related receptor alpha (ERR[alpha]) inverse agonist. The compound can be used to treat diseases associated with ERR and ERR[alpha], such as cancer, osteoporosis, diabetes, aging resistance, weight loss, and the like. After further optimization and screening, the compound is expected to be developed into a novel medicine for preventing and treating tumors or other ERR[alpha] related diseases.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a substituted thiophene compound, a preparation method and use thereof. More specifically, the present invention relates to a substituted thiophene compound, its preparation method, and its use as an estrogen receptor-related receptor (ERR) inverse agonist, especially an estrogen receptor-related receptor alpha (ERRα) ) inverse agonists, and their use in the preparation of medicaments for preventing, ameliorating, treating, and diseases mediated by ERRα activity. Background technique [0002] Nuclear receptors are a class of transcriptional regulators that are widespread in organisms and play an important role in cell growth, proliferation, differentiation, metabolism, immune response and apoptosis, and are indispensable in the treatment of human diseases. status. The estrogen receptor-related receptor (ERR), as a member of the nuclear receptor superfamily, mainly...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D333/16C07D333/20C07D333/18C07D333/24C07F9/6553C07D409/04C07D417/10C07D409/10C07D409/12A61K31/381A61K31/67A61K31/4436A61K31/4025A61K31/4178A61K31/4155A61K31/4196A61K31/427A61K31/5377A61K31/496A61P35/00A61P19/10A61P3/10A61P3/04A61P39/00
CPCC07D333/16C07D333/20C07D333/18C07D333/24C07F9/655345C07D409/04C07D417/10C07D409/10C07D409/12A61K31/381A61K31/67A61K31/4436A61K31/4025A61K31/4178A61K31/4155A61K31/4196A61K31/427A61K31/5377A61K31/496A61P35/00A61P19/10A61P3/10A61P3/04A61P39/00
Inventor 杨春皓李群益代天资漆学宇谭村陈海飞张留弟
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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