[EN] HETEROARYLS AMIDE DERIVATIVES AND THEIR USE AS GLUCOKINASE ACTIVATORS [FR] DÉRIVÉS D'AMIDES D'HÉTÉROARYLES ET LEUR UTILISATION COMME ACTIVATEURS DE LA GLUCOKINASE
[EN] PYRROLOBENZODIAZEPINE PRODRUGS AND ANTIBODY CONJUGATES THEREOF<br/>[FR] PROMÉDICAMENTS DE PYRROLOBENZODIAZÉPINE ET CONJUGUÉS D'ANTICORPS DE CEUX-CI
申请人:GENENTECH INC
公开号:WO2018031662A1
公开(公告)日:2018-02-15
The invention relates generally to pyrrolobenzodiazepine monomer and dimer prodrugs having a glutathione-activated disulfide prodrug moiety, a DT-diaphorase-activated quinone prodrug moiety or a reactive oxygen species-activated aryl boronic acid or aryl boronic ester prodrug moiety. The invention further relates to pyrrolobenzodiazepine prodrug dimer-antibody conjugates.
The present invention provides Formula (1A) compounds
that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R
1
, R
2
, R
3
, and R
4
are as described herein.