CLASS- AND ISOFORM-SPECIFIC HDAC INHIBITORS AND USES THEREOF
申请人:President and Fellows of Harvard College
公开号:US20150307444A1
公开(公告)日:2015-10-29
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.
The Preparation of 1,6-Didesoxy-D-altritol, 1,6-Didesoxygalactitol and 1,6-Didesoxy-L-mannitol<sup>1</sup>
作者:Emmanuel Zissis、Nelson K. Richtmyer
DOI:10.1021/ja01137a039
日期:1952.9
Process for Producing Carbon-Reduced Aldose Compounds
申请人:Okitsa Mitsuhito
公开号:US20090030191A1
公开(公告)日:2009-01-29
The present invention provides a process capable of industrially producing 5-deoxy-L-arabinose, important as a raw material for the production of sapropterin useful as a therapeutic agent for atypical hyperphenylalaninemia, satisfactorily efficiently even with a simple production apparatus. Provided is the process for producing 5-deoxy-L-arabinose characterized by including: reacting L-rhamnose with a C
11-16
straight chain alkyl mercaptan compound in the presence of an acid catalyst to prepare L-rhamnose dialkylmercaptal; subjecting then the obtained compound to an oxidation reaction to prepare a sulfonyl derivative; and subjecting then the sulfonyl derivative to a carbon-reduction reaction to prepare 5-deoxy-L-arabinose. The present production process can also be applied to a process for producing compounds obtained by removing one carbon atom from other aldol compounds, and thus the present invention provides a general process for producing compounds obtained by reducing the number of carbon atoms from aldose compounds.
US9540317B2
申请人:——
公开号:US9540317B2
公开(公告)日:2017-01-10
Baggett et al., Journal of the Chemical Society, 1965, p. 3401,3403