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:
Jun. 18, 2019

Filed:

Apr. 23, 2014
Applicant:

H. Lee Moffitt Cancer Center and Research Institute, Inc., Tampa, FL (US);

Inventors:

Juan R. Del Valle, Tampa, FL (US);

Chih-Chi Andrew Hu, Tampa, FL (US);

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
A61K 9/00 (2006.01); C07D 311/16 (2006.01); A61K 45/06 (2006.01); A61K 31/519 (2006.01); A61K 31/52 (2006.01); C07D 311/18 (2006.01); C07D 491/052 (2006.01); A61K 31/37 (2006.01); A61K 31/395 (2006.01); A61K 31/436 (2006.01); A61K 31/55 (2006.01); A61K 33/24 (2019.01); A01K 67/027 (2006.01);
U.S. Cl.
CPC ...
C07D 311/16 (2013.01); A01K 67/0276 (2013.01); A61K 31/37 (2013.01); A61K 31/395 (2013.01); A61K 31/436 (2013.01); A61K 31/519 (2013.01); A61K 31/52 (2013.01); A61K 31/55 (2013.01); A61K 33/24 (2013.01); A61K 45/06 (2013.01); C07D 311/18 (2013.01); C07D 491/052 (2013.01); A01K 2217/075 (2013.01); A01K 2217/077 (2013.01); A01K 2227/105 (2013.01); A01K 2267/0331 (2013.01);
Abstract

Disclosed are XBP-1/IRE-1 inhibitors having formula disclosed herein. Methods of making and using these inhibitors for the treatment of cancer, in particular B cell cancers, are also disclosed. Also disclosed is a genetic XBP-1-knockout cancer mouse model. In still further aspects, the disclosed subject matter relates to methods for treating oncological and inflammatory disorders in a patient. For example, disclosed herein are methods whereby an effective amount of a compound or composition disclosed herein is administered to a patient having an oncological disorder, for example B-cell chronic lymphocytic leukemia (CLL), and who is in need of treatment thereof. XBP-1 deficiency causes leukemic cells to acquire phenotypes that are disadvantageous for their survival, such as compromised BCR signaling capability and increased surface expression of S1P1.


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