President and Fellows of Harvard College;Dana-Farber Cancer Institute, Inc.
发明人:
Ralph Mazitschek,James E. Bradner
申请号：
US15399550
公开号：
US20170267630A1
申请日:
2017.01.05
申请国别(地区):
US
年份:
2017
代理人:
摘要：
HDAC inhibitors of the general formula (I) and (II) and pharmaceutically acceptable salts thereof, as described herein, are useful as inhibitors of histone deacetylases or other deacetylases, and thus are useful for the treatment of various diseases and disorders associated with acetylase/deacetylase activity as described herein (e.g., cancer). In certain embodiments, the compounds of the invention selectively target either a class or isoform of the HDAC family. Another aspect of the invention provides an assay for determining the inhibitory effect of a test compound on an HDAC protein comprising: incubating the HDAC protein with a substrate of general formula (IIIc) in the presence of a test compound； and determining the activity of the HDAC protein.
