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:
Nov. 18, 2014

Filed:

Nov. 06, 2012
Applicants:

Whitehead Institute for Biomedical Research, Cambridge, MA (US);

Dana-farber Cancer Institute, Inc., Boston, MA (US);

Inventors:

Nathanael Gray, Boston, MA (US);

Jae Won Chang, Boston, MA (US);

Jianming Zhang, Cambridge, MA (US);

Carson C. Thoreen, Jamaica Plain, MA (US);

Seong Woo Anthony Kang, Cambridge, MA (US);

David M. Sabatini, Cambridge, MA (US);

Qingsong Liu, Brookline, MA (US);

Attorneys:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
A61K 31/4375 (2006.01); C07D 471/06 (2006.01); C07D 471/04 (2006.01); C07D 498/04 (2006.01); C07D 471/14 (2006.01); C07D 519/00 (2006.01);
U.S. Cl.
CPC ...
C07D 471/04 (2013.01); C07D 498/04 (2013.01); C07D 471/14 (2013.01); C07D 519/00 (2013.01);
Abstract

The present invention relates to small molecule modulators of mTORC1 and mTORC2, syntheses thereof, and intermediates thereto. Such small molecule modulators are useful in the treatment of proliferative diseases (e.g., benign neoplasms, cancers, inflammatory diseases, autoimmune diseases, diabetic retinopathy) and metabolic diseases. Novel small molecules are provided that inhibit one or more of mTORC1, mTORC2, and PI3K-related proteins. Novel methods of providing soluble mTORC1 and mTORC2 complexes are discussed, as well as methods of using the soluble complexes in a high-throughput manner to screen for inhibitory compounds.


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