[EN] INHIBITORS OF PROTEIN TYROSINE KINASE ACTIVITY<br/>[FR] INHIBITEURS D'ACTIVITÉ DE PROTÉINE TYROSINE KINASE
申请人:METHYLGENE INC
公开号:WO2009109035A1
公开(公告)日:2009-09-11
This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and opthalmological diseases, disorders and conditions.
[EN] 1-CYANO-PYRROLIDINE DERIVATIVES AS INHIBITORS OF USP30.<br/>[FR] DÉRIVÉS DE 1-CYANO-PYRROLIDINE EN TANT QU'INHIBITEURS DE L'USP 30
申请人:MISSION THERAPEUTICS LTD
公开号:WO2017093718A1
公开(公告)日:2017-06-08
The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylatingenzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C- terminal hydrolase 30 or Ubiquitin Specific Peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and cancer. Compounds of the invention include compounds having the formula (I) (I) or a pharmaceutically acceptable salt thereof, wherein R1, R 2, R 3, m, L and X are as defined herein.
configuration. Photoisomerization of the azo unit between cis and trans is achieved upon irradiation with 505 nm (trans→cis) and 435 nm (cis→trans). Concurrently with the isomerization and coordination/decoordination, the spin state of the Ni ion switches between singlet (low-spin) and triplet (high-spin). Previous studies have shown that the spin switching efficiency is strongly dependent on the solvent and
transition metals are necessary in the reaction of in situ generated arynes with nitrosoarenes to give substitutedcarbazoles. Depending on the fluoride source and the solvent, either N‐arylated carbazoles or NH‐carbazoles are obtained (see scheme; DME=dimethoxyethane, OTf=trifluoromethanesulfonate). In these cascades a CC and one or two CN bonds are formed. The reactions are easy to conduct and proceed
been synthesized and characterized by electrochemistry and UV/Vis spectroscopy. The electrochemical and photophysical studies indicate that the electronic communication in ferrocenylethynyl‐substituted derivatives is strongly influenced by the substituted position of the ferrocenylethynyl moiety. In situ electrochemical oxidation or chemical oxidation caused a characteristically weak ligand‐to‐metal charge‐transfer