Silylation-Based Kinetic Resolution of α-Hydroxy Lactones and Lactams
摘要:
A silylation-based kinetic resolution has been developed for alpha-hydroxy lactones and lactams employing the chiral isothiourea catalyst (-)-benzotetramisole and triphenylsilyl chloride as the silyl source. The system is more selective for lactones than lactams, and selectivity factors up to 100 can be achieved utilizing commercially available reagents.
[EN] N/O-LINKED DEGRONS AND DEGRONIMERS FOR PROTEIN DEGRADATION<br/>[FR] DÉGRONS ET DÉGRONIMÈRES À LIAISON N/O POUR LA DÉGRADATION DE PROTÉINES
申请人:C4 THERAPEUTICS INC
公开号:WO2018237026A1
公开(公告)日:2018-12-27
This invention provides Degronimers that have E3 Ubiquitin Ligase targeting moieties (Degrons) that can be linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation. The invention also provides Degrons that can be used to treat disorders mediated by cereblon or an Ikaros family protein, and methods of use and compositions thereof as well as methods for their preparation.
HETEROCYCLIC DERIVATIVES AS MODULATORS OF ION CHANNELS
申请人:Zimmermann Nicole
公开号:US20100004300A1
公开(公告)日:2010-01-07
The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
Novel substituted piperidines of the general formulae (I) and (II) with the substituent definitions as explained in detail in the description are described. The compounds are suitable in particular as renin inhibitors and are highly potent.
Novel substituted piperidines of the general formulae (I) and (II)
with the substituent definitions as explained in detail in the description are described. The compounds are suitable in particular as renin inhibitors and are highly potent.
Novel substituted piperidines of the general formulae (I)
with the substituent definitions as explained in detail in the description are described. The compounds are suitable in particular as renin inhibitors and are highly potent.