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. 08, 2008

Filed:

Nov. 01, 2002
Applicants:

Shaomeng Wang, Saline, MI (US);

Dajun Yang, Rockville, MD (US);

Istvan J. Enyedy, Milton, MA (US);

Inventors:

Shaomeng Wang, Saline, MI (US);

Dajun Yang, Rockville, MD (US);

Istvan J. Enyedy, Milton, MA (US);

Assignee:
Attorney:
Primary Examiner:
Int. Cl.
CPC ...
A61K 31/44 (2006.01); A61K 31/335 (2006.01); A61K 31/135 (2006.01); A61K 31/505 (2006.01); A61K 31/65 (2006.01);
U.S. Cl.
CPC ...
Abstract

The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and/or Bcl-X. In particular, the present invention provides non-peptide cell permeable small molecules (e.g., tricyclo-dibenzo-diazocine-dioxides) that bind to a pocket in Bcl-2/Bcl-Xthat block the anti-apoptotic function of these proteins in cancer cells and tumor tissues exhibiting Bcl-2 protein overexpression. In preferred embodiments, the small molecules of the present invention are active at the BH3 binding pocket of Bcl-2 family proteins (e.g., Bcl-2, Bcl-X, and Mcl-1). The compositions and methods of the present invention are useful therapeutics for cancerous diseases either alone or in combination with chemotherapeutic or other drugs.


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