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. 03, 2018

Filed:

Aug. 07, 2015
Applicants:

University of Cape Town, Cape Town, ZA;

University of Louisville Research Foundation Inc., Louisville, KY (US);

Inventors:

Virna Drucille Leaner, Goodwood, ZA;

Pauline Janet Van Der Watt, Observatory, ZA;

John Olaf Trent, Louisville, KY (US);

Assignees:
Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 487/04 (2006.01); A61K 31/4985 (2006.01); A61K 31/553 (2006.01); A61K 31/40 (2006.01); A61K 31/5377 (2006.01);
U.S. Cl.
CPC ...
A61K 31/4985 (2013.01); A61K 31/40 (2013.01); A61K 31/5377 (2013.01); A61K 31/553 (2013.01);
Abstract

Compounds, including quinoxaline derivatives of formula I, for use in the treatment of cancer are described. In general, the compounds inhibit the import of proteins and transcription factors such as Kpnα, AP-1, P65, NFAT into the nucleus of a cell by inhibiting the nuclear import protein, Kpnβ1. Cancer cells have elevated levels of Kpnβ1 and the inhibition of their nuclear import activity induces cell apoptosis. The administration of an effective amount of any one of the compounds results in cell apoptosis in cancer cells, while non-cancer cells are substantially unaffected by the inhibition of Kpnβ1's nuclear import activity.


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