SYMMETRICAL TRIS-ARYL-AMIDE DERIVATIVES AND THEIR USE AS ANTI-HEPARANASE
申请人:Leadiant Biosciences SA
公开号:EP3381898A1
公开(公告)日:2018-10-03
The present invention relates to tris-aryl-amide derivatives having an anti-heparanase activity, in particular it relates to ureido/thioureido/ether tris-aryl-amide derivatives of formula
The invention also relates to the use of such compounds as a medicament, in particular for the treatment of diseases and disorders associated with heparanase activity, and to pharmaceutical compositions comprising the same.
[EN] SYMMETRICAL TRIS-ARYL-AMIDE DERIVATIVES AND THEIR USE AS ANTI-HEPARANASE<br/>[FR] DÉRIVÉS SYMÉTRIQUES DE TRIS-ARYL-AMIDE ET LEUR UTILISATION COMME ANTI-HÉPARANASE
申请人:LEADIANT BIOSCIENCES SA IN LIQUIDAZIONE
公开号:WO2018177861A1
公开(公告)日:2018-10-04
The present invention relates to tris-aryl-amide derivatives having an anti-heparanase activity, in particular it relates toureido/thioureido/ether tris-aryl-amide derivatives of formula (I). The invention also relates to the use of such compounds as a medicament, in particular for the treatment of diseases and disorders associated with heparanase activity, and to pharmaceutical compositions comprising the same.
Iron‐Catalyzed C
<sub>α</sub>
H Oxidation of Tertiary, Aliphatic Amines to Amides under Mild Conditions
作者:Christopher J. Legacy、Anqi Wang、Brian J. O'Day、Marion H. Emmert
DOI:10.1002/anie.201507738
日期:2015.12
precious metal catalyzed, oxidative protocols to generate such functionalities. However, simple tertiary alkyl amines cannot be used as starting materials in these protocols. The research described herein enables the oxidative synthesis of amides from simple, noncyclic tertiary alkyl amines under synthetically useful, mild conditions through a biologically inspired approach: Fe‐catalyzed CαH functionalization