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Muscle atrophy inhibitor containing quercetin glycoside

A technology of uses, compounds, applied in the field of medicine, which can solve the problem of not providing data, etc.

Inactive Publication Date: 2016-12-21
INSTITUT CURIE +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

No data provided regarding potential activity as an antineoplastic agent

Method used

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  • Muscle atrophy inhibitor containing quercetin glycoside
  • Muscle atrophy inhibitor containing quercetin glycoside
  • Muscle atrophy inhibitor containing quercetin glycoside

Examples

Experimental program
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Embodiment Construction

[0047] The present inventor has determined the new purposes of the cephalosporin derivative of formula (I):

[0048]

[0049] It is of therapeutic importance for the treatment of cancer as an inhibitor of the CXCR4 receptor.

[0050] The inventors have surprisingly found that cephalosporin compounds substituted by an alkenyl chain at the 3-position of the cephalosporin core have significant CXCR4 inhibitory activity.

[0051] Specifically, compared with the compounds disclosed in patent application WO 02 / 099430, using wherein R 3 Compounds of formula (I) according to the invention which represent a methyl or hydrogen atom surprisingly show a better CXCR4 inhibition profile.

[0052] Accordingly, the present invention relates to a compound of formula (I) for use in the treatment of cancer, in particular having CXCR4 receptor antagonist activity:

[0053]

[0054] in:

[0055] ■R 1 express:

[0056] - a hydrogen atom, or

[0057] --CO-R 4 unit or –CO 2 -R 4 unit, ...

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Abstract

The purpose of the present invention is to provide a novel muscle atrophy inhibitor containing an ingredient that can be taken safely over an extended period of time. It was discovered that a glycoside of quercetin, which is a type of polyphenol contained in plants and the like, has an inhibitory effect on the expression of myostatin which is involved in muscle atrophy. The present invention provides a novel muscle atrophy inhibitor containing quercetin glycoside, the muscle atrophy inhibitor having exceptional bioavailability and high safety.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the use of CXCR4 receptor antagonists in cancer treatment. Background technique [0002] Classical antitumor chemotherapy exploits the proliferative behavior of cancer cells to induce cell death through DNA damage. In contrast, more recent therapeutic approaches have involved the interaction of cancer cells with their microenvironment through chemokine receptors and their ligands (Domanska et al., European Journal of Cancer, 2013, 49, 219-230). An important and representative chemokine-receptor pair is the chemokine ligand CXCL12 and its receptor CXCR4. CXCR4 / CXCL12 is involved in the proliferation of primary tumors, the migration of tumor cells and the establishment of tumor metastasis. Therefore, CXCL12 / CXCR4 appears to be an attractive therapeutic approach, and their interaction can be disrupted by CXCR4 antagonists. Several CXCR4 inhibitors have been approved for cancer treatment a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/545A61P35/00
CPCA61K45/06A61K31/545A61P11/00A61P15/00A61P17/00A61P35/00A61P43/00A61K2300/00A61K47/32
Inventor 阿尔诺·锡南·卡拉波加维奥莱塔·伊莎贝尔·佩雷斯-努埃诺米歇尔·苏谢迪迪埃·德科丹
Owner INSTITUT CURIE
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