An efficient asymmetric acyl-Mannichreaction of isoquinolines with α-(diazomethyl)phosphonate and diazoacetate has been developed using chiral spiro phosphoric acids as catalysts. This reaction allowed the construction of a series of chiral 1,2-dihydroisoquinolines bearing a tertiary stereocenter at the C1 position with up to 98% yield and 99% ee.
[EN] C3-CARBON LINKED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN DEGRADATION<br/>[FR] DÉGRONIMÈRES DE TYPE GLUTARIMIDE LIÉS AU CARBONE C3 POUR LA DÉGRADATION DE PROTÉINES CIBLES
申请人:C4 THERAPEUTICS INC
公开号:WO2017197046A1
公开(公告)日:2017-11-16
This invention provides Degronimers that have carbon-linked E3 Ubiquitin Ligase targeting moieties (Degrons), which 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 provides a compound of Formula (I)
or a pharmaceutically acceptable salt thereof; wherein
G is
R
1
, R
2
and R
3
are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
Macrocyclic peptides are disclosed having the general formula:
wherein R′, R
3
, R
3′
, R
4
, R
6
, X, Q, and W are described. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
THERAPEUTIC COMPOUNDS AND METHODS TO TREAT INFECTION
申请人:RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
公开号:US20190031624A1
公开(公告)日:2019-01-31
Disclosed herein are compounds of formula I:
or a salt thereof and compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods for treating or preventing a bacterial infection in an animal comprising administering to the animal a compound of formula I or a pharmaceutically acceptable salt thereof, alone or in combination with a bacterial efflux pump inhibitor.