The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Patent No.:

US 7838706 B1

PDF
Full Text
Expired
Date of Patent:
Nov. 23, 2010

Filed:

May. 16, 2007
Applicants:

Weiping Shen, Shanghai, CN;

Jianping Wang, Zhejiang, CN;

Jianguo Wang, Zhejiang, CN;

Inventors:

Weiping Shen, Shanghai, CN;

Jianping Wang, Zhejiang, CN;

Jianguo Wang, Zhejiang, CN;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07C 237/00 (2006.01); C07C 235/00 (2006.01); C07C 233/00 (2006.01); C07C 231/00 (2006.01); A61K 31/165 (2006.01); A61K 31/16 (2006.01); A61K 31/66 (2006.01);
U.S. Cl.
CPC ...
Abstract

The invention disclosed a total synthesis process of novel ethoxy combretastatins and their prodrugs. Combretastatins are chemically modified by ethoxy substituted on the 4'-position of their B aryl ring and are converted to be their soluble prodrugs of phosphate or their inner salt of phosphorylcholine by modifying the hydroxyl on the 3′-position of their B aryl ring. Similarly, 3′-amino combretastatin is 4′-ethoxy chemically modified and further side chain of amino acid can be introduced to the amino to form soluble prodrug of amino acidamide. The structure of the said compound is showed as formula (I). Ethoxy combretastatins possess potent tubulin polymerization inhibitory activity and can be used for the treatment of inhibiting tumor or neovascular.


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