Synthesis of <i>trans</i>-2-Substituted Cyclopropylamines from α-Chloroaldehydes
作者:Michael S. West、L. Reginald Mills、Tyler R. McDonald、Jessica B. Lee、Deeba Ensan、Sophie A. L. Rousseaux
DOI:10.1021/acs.orglett.9b03172
日期:2019.10.18
report the synthesis of trans-2-substituted cyclopropylamines in high diastereoselectivity from readily available α-chloroaldehydes. The reaction proceeds via trapping of an electrophilic zinc homoenolate with an amine followed by ring closure to generate the cyclopropylamine. We have also observed that cyclopropylamine cis/trans-isomerization occurs in the presence of zinchalidesalts and that this
[EN] HETEROCYCLIC COMPOUNDS, METHODS OF MAKING THEM AND THEIR USE IN THERAPY<br/>[FR] COMPOSES HETEROCYCLIQUES, PROCEDES DE PRODUCTION DE CEUX-CI ET UTILISATION DE CEUX-CI DANS UN TRAITEMENT
申请人:AFFINIUM PHARM INC
公开号:WO2004052890A1
公开(公告)日:2004-06-24
In part, the present invention is directed to antibacterial compounds of formula (I) wherein A is a bicyclic heteroaryl ring or a tricyclic ring and R2 is an heterocyclic residue; L is a bond, or L is alkyl, alkenyl or cycloalkyl.
[EN] TGFBETAR1 INHIBITOR-ASGR ANTIBODY CONJUGATES AND USES THEREOF<br/>[FR] CONJUGUÉS INHIBITEUR DE TGFBETAR1-ANTICORPS ANTI-ASGR ET UTILISATIONS ASSOCIÉES
申请人:SILVERBACK THERAPEUTICS INC
公开号:WO2021072203A1
公开(公告)日:2021-04-15
Various conjugates and compositions thereof are disclosed for use in the treatment of a liver disease, such as liver cancer and liver fibrosis. The compositions comprise conjugates, wherein the conjugates are comprised of an antibody or antibody construct specific for ASGR1 or ASGR2 attached to a TGFβR1 inhibitor via a linker. Additionally provided are the methods of preparation of the conjugates and compositions thereof.
[EN] ALK5 INHIBITORS, CONJUGATES, AND USES THEREOF<br/>[FR] INHIBITEURS D'ALK5, CONJUGUÉS ET LEURS UTILISATIONS
申请人:SILVERBACK THERAPEUTICS INC
公开号:WO2021011834A1
公开(公告)日:2021-01-21
ALK5 inhibitor compounds, conjugates, and pharmaceutical compositions for use in the treatment of disease, such as cancer, are disclosed herein. The disclosed compounds are useful, among other things, in the treating of cancer and fibrosis and modulating ALK5. Additionally, compounds incorporated into a conjugate with an antibody construct are described herein.
Compositions comprising multiple bioactive agents, and methods of using the same
申请人:Berman M. Judd
公开号:US20060142265A1
公开(公告)日:2006-06-29
In part, the present invention is directed to compositions comprising a FabI inhibitor and at least one other bioactive agent. In another part, the present invention is directed to antibacterial compositions comprising a compound of formulas I-III and at least one other antibacterial agent.