Non-fused thiophene derivatives and their uses

A fused, compound technology, used in the medical field, that can solve problems such as application limitations

Pending Publication Date: 2020-11-13
ENYO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although these drugs are effective in reducing influenza-related morbidity and mortality, the emergence of drug resistance poses severe limitations to their use, and there is an urgent need to develop new anti-influenza drugs that target resistant forms

Method used

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  • Non-fused thiophene derivatives and their uses
  • Non-fused thiophene derivatives and their uses
  • Non-fused thiophene derivatives and their uses

Examples

Experimental program
Comparison scheme
Effect test

Embodiment A

[0364] Example A - Chemistry

[0365] abbreviation

[0366] Aq water-based

[0367] br s broad singlet

[0368] CDCl 3 deuterated chloroform

[0369] d doublet

[0370] DAD Diode Array Detector

[0371] DCM dichloromethane (methylene dichloride)

[0372] dd doublet doublet doublet

[0373] ddd doublet doublet doublet doublet

[0374] DIPEA N,N-Diisopropylethylamine

[0375] DMF N,N-Dimethylformamide

[0376] DMSO Dimethyl Sulfoxide

[0377] doublet of dq quartet

[0378] doublet of dt triplet

[0379] EtOAc ethyl acetate

[0380] Et 2 O diethyl ether

[0381] EtOH ethanol

[0382] g grams

[0383] hours

[0384] HATU O-(7-Azabenzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate

[0385] HCl hydrochloric acid

[0386] HPLC High Pressure Liquid Chromatography

[0387] i-PrOH Isopropanol

[0388] LC / MS Liquid Chromatography / Mass Spectrometry

[0389] LiOH lithium hydroxide

[0390] m multiplet

[0391] M Molarity

[0392] MeCN acetonit...

Embodiment B

[0767] Example B - Biology

Embodiment B1

[0768] Example B1 - Antiviral effect

[0769] The antiviral effect of the compounds of the invention has been tested on the A549 cell line infected with H1N1 (Influenza A / New Caledonia / 20 / 99). IC50s are reported in Table 1 below. The results show that the compounds of the present invention exhibit antiviral effects.

[0770] Table 1:

[0771]

[0772]

[0773] Materials and methods

[0774] Human A549 cells (80,000 cells / well in 96-well plates) were treated with a range of concentrations of test compounds and immediately incubated in DMEM / 1% penicillin / streptomycin supplemented with 0.25 μg / ml TPCK trypsin (Sigma) Infection with H1N1A / New Caledonia / 20 / 99 virus (clinical isolate) was performed at an MOI of 0.1 and incubated at 37°C in 5% CO2. Forty-eight hours after infection, the supernatant (25 μl) was collected and transferred to a 96-well black flat-bottomed plate, mixed with 25 μl Ca++ / Mg++-containing PBS (Thermo Fisher) and 50 μl 2′-(4-methylumbelliferyl)- ...

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PUM

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Abstract

The present invention relates to a new class of non-fused thiophene derivatives and their uses for treating diseases such as infection, cancer, metabolic diseases, cardiovascular diseases, iron storage disorders and inflammatory disorders.

Description

technical field [0001] The present invention relates to the field of medicine, in particular non-fused thiophene derivatives and their use for the treatment of diseases such as infection, cancer, metabolic diseases, cardiovascular diseases, iron storage disorders and inflammatory disorders. Background technique [0002] Viruses are small infectious agents that replicate only in living cells of other organisms. They can infect all types of life forms, from animals and plants to microbes, including bacteria and archaea. Of these, more than 400 viruses are known to cause disease in humans, many of which cause severe lesions that eventually lead to death. Specifically, in 2012, HIV was classified as the sixth leading cause of death worldwide, with 1.5 million deaths per year (WHO, Fact sheet N° 310, 2014). Seasonal influenza viruses cause influenza, which affects approximately 20% of the world's population and causes 250,000 to 500,000 deaths per year (WHO, Fact sheet N° 211, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D233/38A61P31/04A61P3/00A61P35/00A61P31/12A61K31/381
CPCC07D233/38A61P31/04A61P3/00A61P35/00A61P31/12C07D333/38A61K31/381A61K31/351A61K31/397A61K31/5377A61P31/00C07D409/12C07D413/12C07D409/04A61P3/08C07D333/04
Inventor 艾瑞克·梅尔德伦贝诺伊特·德沙塞彼得·梅钦卡里纳·法比耶娜·马拉古保罗·科林·米歇尔·温希普让-劳伦特·帕帕里尼马克·钱伯斯杰米·大卫·奈特罗贝塔·拉纳罗
Owner ENYO PHARMA
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