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. 15, 2008

Filed:

Aug. 23, 2002
Applicants:

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

Kenji Namoto, Solana Beach, CA (US);

Andreas Ritzen, Vanlose, DK;

Mitsuru Shoji, Tokyo, JP;

Trond Ulven, Copenhagen, DK;

Karl-heinz Altmann, Reinach, CH;

Inventors:

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

Kenji Namoto, Solana Beach, CA (US);

Andreas Ritzen, Vanlose, DK;

Mitsuru Shoji, Tokyo, JP;

Trond Ulven, Copenhagen, DK;

Karl-Heinz Altmann, Reinach, CH;

Assignee:

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

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
A61K 31/425 (2006.01); C07D 277/30 (2006.01); X07D 277/04 (2006.01);
U.S. Cl.
CPC ...
Abstract

The invention relates to cis- and trans-12, 13-cyclopropyl and 12,13-cyclobutyl epothilones of formula I to IV wherein Ar is a radical represented by the following structure: and the other radicals and symbols have the meanings as defined herein; to their chemical synthesis and biological evaluation; their use in the treatment of neoplastic diseases and to pharmaceutical preparations containing such compounds. The compounds described herein are potent tubulin polymerization promoters and cytotoxic agents.


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