[EN] SUBSTITUTED 8 - AMINO - IMIDAZO [1, 2-A] PYRAZINES AS ANTIBACTERIAL AGENTS<br/>[FR] 8-AMINO-IMIDAZO[1,2-A]PYRAZINES SUBSTITUÉES EN TANT QU'AGENTS ANTIBACTÉRIENS
申请人:UCL BUSINESS PLC
公开号:WO2012168733A1
公开(公告)日:2012-12-13
The present invention relates to substituted imidazofi,2-a]pyrazines of Formula (I) and their use as antibacterial agents.
本发明涉及式(I)的取代咪唑并[2-a]吡嗪类化合物,以及它们作为抗菌剂的用途。
2- and 3-substituted imidazo[1,2-a]pyrazines as inhibitors of bacterial type IV secretion
作者:James R. Sayer、Karin Walldén、Thomas Pesnot、Frederick Campbell、Paul J. Gane、Michela Simone、Hans Koss、Floris Buelens、Timothy P. Boyle、David L. Selwood、Gabriel Waksman、Alethea B. Tabor
DOI:10.1016/j.bmc.2014.09.036
日期:2014.11
A novel series of 8-amino imidazo[1,2-a]pyrazine derivatives has been developed as inhibitors of the VirB11 ATPase HP0525, a key component of the bacterial type IV secretion system. A flexible synthetic route to both 2- and 3-aryl substituted regioisomers has been developed. The resultingseries of imidazo[1,2-a]pyrazines has been used to probe the structure–activity relationships of these inhibitors
一系列新型 8-氨基咪唑并[1,2- a ]吡嗪衍生物已被开发为 VirB11 ATPase HP0525(细菌 IV 型分泌系统的关键组成部分)的抑制剂。已开发出 2- 和 3- 芳基取代的区域异构体的灵活合成路线。由此产生的一系列咪唑并[1,2- a ]吡嗪已被用来探讨这些抑制剂的结构-活性关系,它们显示出作为抗菌剂的潜力。
[EN] WDR5-MYC INHIBITORS<br/>[FR] INHIBITEURS DE WDR5-MYC
申请人:UNIV VANDERBILT
公开号:WO2021021951A1
公开(公告)日:2021-02-04
Substituted N-phenyl sulfonamide compounds inhibit WDR5-MYC interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.
Disclosed are compounds of formula (I): wherein the variables R1, R2, R3 and Z are described herein, which are useful as inhibitors of the kinase activity of the IκB kinase (IKK) complex. The compounds are therefore useful in the treatment of IKK mediated diseases including autoimmune diseases inflammatory diseases and cancer. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.
Compounds of formula
and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.