Novel oxybispyridylboronic acids: synthesis and study of their reactivity in Suzuki-type cross-coupling reactions
摘要:
This paper sets forth the synthesis of novel oxybispyridylboronic acids, which are prepared from the corresponding halo-oxybispyridines via halogen-metal exchange using n-butyllithium and treatment with triisopropylborate. A range of efficient cross-coupling reactions of these novel boronic acids with selected aryl halides is described. This strategy produces novel pyridylethers of interest in cholinergic medicinal chemistry. (c) 2006 Elsevier Ltd. All rights reserved.
The present invention relates to compounds that inhibit Protein Arginine N-Methyl Transferase 5 (PRMT5) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.
The present invention relates to aryl olefinic azacyclic compounds and aryl acetylenic azacyclic compounds, including pyridyl olefinic cycloalkylamines and pyridyl acetylenic cycloalkylamines. The present invention also relates to prodrug derivatives of the compounds of the present invention.
Substituted heteroarylamide analogs as mGluR5 negative allosteric modulators and methods of making and using the same
申请人:Conn P. Jeffrey
公开号:US08598345B2
公开(公告)日:2013-12-03
Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
[EN] MTA-COOPERATIVE PRMT5 INHIBITORS<br/>[FR] INHIBITEURS DE PRMT5 COOPÉRATIF À BASE DE MTA
申请人:MIRATI THERAPEUTICS INC
公开号:WO2022192745A1
公开(公告)日:2022-09-15
Disclosed are compounds of Formula IIA, IIA-1, IIB, IIB-1, IIC and IIC-1: and pharmaceutical compositions and methods of use thereof These compounds inhibit Protein Arginine M-Methyl Transferase 5 (PRMT5) activity and are useful in methods and pharmaceutical compositions for treating cancer.
The present invention relates to compounds that inhibit Protein Arginine N-Methyl Transferase 5 (PRMT5) activity. In particular, the present invention relates to compounds of Formula (I)
to pharmaceutical compositions comprising compounds of Formula (I) and to methods of use thereof, such as methods of treating cancer using the compounds of Formula (I) and pharmaceutical compositions comprising those compounds.