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[2-[(5-nitro-1,3-thiazol-2-yl)carbamoyl]phenyl]ethanoate for use in lymphangioleiomyomatosis and other diseases

A carbamoyl, substituent technology, applied to [2-[(5-nitro-1 for lymphangioleiomyoma and other diseases, can solve problems such as insufficient biological process activity

Pending Publication Date: 2020-07-28
休伯特科斯特
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Instead, the pathogenic mechanism of many diseases is the inactivity of biological processes

Method used

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  • [2-[(5-nitro-1,3-thiazol-2-yl)carbamoyl]phenyl]ethanoate for use in lymphangioleiomyomatosis and other diseases
  • [2-[(5-nitro-1,3-thiazol-2-yl)carbamoyl]phenyl]ethanoate for use in lymphangioleiomyomatosis and other diseases
  • [2-[(5-nitro-1,3-thiazol-2-yl)carbamoyl]phenyl]ethanoate for use in lymphangioleiomyomatosis and other diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0141] Example 1 ( figure 1 ):

[0142] MEFs are mouse embryonic fibroblasts derived from TSC2 knockout (MEF110) and TSC2+ (MEF157) mice. Tsc2 mutations are known to cause tuberous sclerosis and lymphangioleiomyomatosis in humans.

[0143] at 37°C and 5% CO 2 Next, all cells were maintained in DMEM tissue culture medium supplemented with 10% fetal bovine serum to support cell proliferation.

[0144] In MEFs, ribosomal protein S6, a component of the 40S ribosome and phosphorylated at Ser236 by p70S6 kinase, can be analyzed by ELISA and Western blotting with phospho-specific antibodies for the detection of human and mouse forms of rpS6. This test is predictive of compounds having protective or therapeutic activity against respiratory and vascular diseases, fibrotic diseases or neurodegenerative diseases.

[0145] Cells were grown to 60-80% confluency in DMEM+10% serum. Two hours before the addition of the test compound of the invention, the medium was replaced with fresh s...

Embodiment 2

[0151] Example 2 ( figure 2 ):

[0152] 621-101 cells are human cells derived from angiomyolipoma. They had confirmed TSC2 mutations and were the only cells carrying disease-derived mutations used to model lymphangioleiomyoma.

[0153] Cells were grown to 60-80% confluency in DMEM+10% serum. Two hours before the addition of the test compound of the invention, the medium was replaced with fresh serum-free medium.

[0154] Compounds were added as 1:1000 dilutions of DMSO stocks. DMSO was added as a vehicle control and samples were incubated for an additional 60 minutes.

[0155] For ELISA, cells were harvested into 200 μl of cell lysis buffer containing protease and phosphatase inhibitors to preserve the phosphorylation status of rpS6. Lysates were stored at -80°C until use. ELISA was performed using 50 μl of lysate per sample, which was performed according to the manufacturer's instructions. For Western blotting, cells were harvested into 200 μl cell lysis buffer contai...

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PUM

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Abstract

The present invention relates to the use of the compound [2-[(5-nitro-1,3-thiazol-2- yl)carbamoyl]phenyl]ethanoate in a method of treatment or prophylaxis of vascular and respiratory disease, fibroticdisease and neurodegenerative disease, particularly interstitial pneumonia, tuberous sclerosis or lymphangioleiomyomatosis, collagen disease, interstitial lung disease, human kidney disease, nephritic syndrome, liver fibrosis or liver cirrhosis, Alzheimer's disease or Parkinson's disease.

Description

[0001] manual [0002] The present invention relates to [2-[(5-nitro-1,3-thiazole-2-substituent)carbamoyl]phenyl]acetate as a method for preventing and / or treating respiratory and vascular diseases, fibrotic diseases or the use of a therapeutic agent for a neurodegenerative disease. Background technique [0003] Therapeutic compounds effective in preventing and / or treating disease can be identified based on their activity in biological assays. Bioassays that mimic disease-causing mechanisms can be used to test the therapeutic activity of candidate compounds. [0004] The causative mechanism of many diseases is the overactivity of biological processes. Compounds that reduce the activity of biological processes are effective in preventing and / or treating diseases caused by overactive biological processes. Similarly, the pathogenic mechanism of many diseases is the overproduction of biomolecules. Compounds that can reduce the production of biomolecules or block the activity o...

Claims

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Application Information

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IPC IPC(8): A61K31/155A61K31/426A61P1/16A61P25/16A61P25/28
CPCA61K31/155A61K31/426A61P1/16A61P25/16A61P25/28A61K2300/00A61P11/00
Inventor 休伯特·科斯特
Owner 休伯特科斯特
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