TAU-PROTEIN TARGETING PROTACS AND ASSOCIATED METHODS OF USE
申请人:Arvinas, Inc.
公开号:US20180125821A1
公开(公告)日:2018-05-10
The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.
THIADIAZOLE ANALOGS THEREOF AND METHODS FOR TREATING SMN-DEFICIENCY-RELATED-CONDITIONS
申请人:AXFORD Jake
公开号:US20140206661A1
公开(公告)日:2014-07-24
The present invention provides a compound of Formula (X) or a pharmaceutically acceptable salt thereof;
a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
6-Heteroarylpyridoindolone Derivatives, Their Preparation and Therapeutic Use Thereof
申请人:MUNEAUX Yvette
公开号:US20080262020A1
公开(公告)日:2008-10-23
The disclosure relates to compounds of formula (I):
wherein R
1
, R
2
, R
3
, R
4
, are R
5
are as defined in the disclosure; their preparation method, compositions containing the same and therapeutic use thereof.
Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.