Therapeutic anti-tumor compound

A compound and hydrate technology, which can be used in antitumor drugs, phosphorus organic compounds, organic chemistry, etc., can solve the problems of limited use of Combretastatin and its derivatives, poor water solubility, etc.

Inactive Publication Date: 2010-06-16
HC SYNTHETIC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the water solubility of combretastatin and its derivatives is extremely poor, which largely limits the clinical use of combretastatin and its derivatives, and the design and preparation of water-soluble prodrugs is a research hotspot

Method used

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Embodiment 2

Embodiment 3

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Abstract

The invention provides a compound or a pharmaceutical salt thereof of formula (I) R1-O-(CH2)nO-L, wherein R1 represents a combretastatin type compound containing non-hydroxyl part, n is 1 to 10, and L represents CO-alkyl carboxylic acid, amino acid residues, phosphoryl or phosphoryl derivatives. The compound of the invention is used for in treatment of anti-tumor medicaments and has high water solubility.

Description

Technical field: The invention relates to antitumor compounds for use in therapy, methods of their use, formulations containing them and methods of their production. technical background: Combretastatin is isolated from the South African tropical plant Combretum Caffrum. It can quickly combine with tubulin, has a good selective anti-mitotic effect, destroys tumor blood vessels, causes the death of tumor vascular endothelial cells, and leads to the death of secondary tumor cells, and has extremely high anti-tumor activity , has great clinical application value. However, the water solubility of combretastatin and its derivatives is extremely poor, which largely limits the clinical use of combretastatin and its derivatives, and the design and preparation of water-soluble prodrugs is a research hotspot. Invention content: The purpose of the present invention is to provide a new derivative of combretastatin compound for treating tumors. Its structure is: R 1 -O-(CH 2 ) ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/09C07C229/08C07C69/40C07D317/22A61K31/661A61K31/6615A61K31/223A61K31/225A61K31/357A61P35/00
Inventor 杨成
Owner HC SYNTHETIC PHARMA CO LTD
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