Patent number: 11225469
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.
Type:
Grant
Filed:
January 15, 2016
Date of Patent:
January 18, 2022
Assignees:
Whitehead Institute for Biomedical Research, Dana-Farber Cancer Institute, Inc., The United States of America, as represented by the Secretary, Department of Health and Human Services
Inventors:
David M. Sabatini, Michael Pacold, Matthew B. Boxer, Jason M. Rohde, Kyle R. Brimacombe, Min Shen, Ganesha Bantukallu, Li Liu
Publication number: 20180105508
Abstract: The present invention provides compounds pounds 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.
Type:
Application
Filed:
January 15, 2016
Publication date:
April 19, 2018
Applicants:
Whitehead Institute for Biomedical Research, Dana-Farber Cancer Institute, Inc.
Inventors:
David M. Sabatini, Michael Pacold, Matthew B. Boxer, Jason M. Rohde, Kyle R. Brimacombe, Min Shen