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.

Date of Patent:
Apr. 30, 2002

Filed:

Jun. 22, 1998
Applicant:
Inventors:

Kyriacos C. Nicolaou, La Jolla, CA (US);

N. Paul King, San Diego, CA (US);

M. Ray Finlay, San Diego, CA (US);

Yun He, San Diego, CA (US);

Frank Roschangar, Durham, NC (US);

Dionisios Vourloumis, San Diego, CA (US);

Hans Vallberg, Huddinge, SE;

Francisco Sarabia, Torre de Benagalbon, ES;

Sacha Ninkovic, San Diego, CA (US);

David Hepworth, San Diego, CA (US);

Tianhu Li, San Diego, CA (US);

Assignee:

The Scripps Research Institute, La Jolla, CA (US);

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D / ; C07D / ; C07D / ;
U.S. Cl.
CPC ...
C07D / ; C07D / ; C07D / ;
Abstract

Novel analogs of epothilone A, epothilone B, and epothilone C are synthesized by Stille coupling thazole-stannanes to macrolactone intermediates. The synthetic epothilone analogs selectively prevent mitosis in cancer cells through the induction and stabilization of microtubulin assembly. Selected synthetic epothilone analogs are demonstrated to have greater bioactivity than their corresponding native compound.


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