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:
Jan. 18, 2022

Filed:

Jan. 15, 2016
Applicants:

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

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

The United States of America, As Represented BY the Secretary, Department of Health and Human Services, Bethesda, MD (US);

Inventors:

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

Michael Pacold, Cambridge, MA (US);

Matthew B. Boxer, New Market, MD (US);

Jason M. Rohde, Poolesville, MD (US);

Kyle R. Brimacombe, Highland, NY (US);

Min Shen, Boyds, MD (US);

Ganesha Bantukallu, Falls Church, VA (US);

Li Liu, Germantown, MD (US);

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 401/12 (2006.01); C07D 213/75 (2006.01); C07D 213/40 (2006.01); A61K 45/06 (2006.01); C07D 233/88 (2006.01); C07D 213/78 (2006.01); C07D 235/30 (2006.01); C07D 249/14 (2006.01); C07D 231/40 (2006.01); A61P 43/00 (2006.01); A61P 35/00 (2006.01);
U.S. Cl.
CPC ...
C07D 401/12 (2013.01); A61K 45/06 (2013.01); A61P 35/00 (2018.01); A61P 43/00 (2018.01); C07D 213/40 (2013.01); C07D 213/75 (2013.01); C07D 213/78 (2013.01); C07D 231/40 (2013.01); C07D 233/88 (2013.01); C07D 235/30 (2013.01); C07D 249/14 (2013.01);
Abstract

The present invention provides compounds of Formula (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, pro-drugs, and compositions thereof. Also provided are methods and kits involving the compounds of Formula (I), (II) or (III) for treating diseases associated with the over-expression of phosphoglycerate dehydrogenase (PHGDH) in a subject, such as proliferative diseases (e.g., cancers (e.g., breast cancer, ER negative breast cancer, melanoma, cervical cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases). Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the activity of PHGDH or inhibit the serine biosynthetic pathway, or both.


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