[EN] PIPERAZINE DERIVATIVES AS TRPML MODULATORS<br/>[FR] DÉRIVÉS DE PIPÉRAZINE EN TANT QUE MODULATEURS DE TRPML
申请人:LIANG CONGXIN
公开号:WO2018005713A1
公开(公告)日:2018-01-04
The new piperazine derivatives are modulators of TRPML and are useful in treating disorders related to TRPML activities such as lysosome storage diseases, muscular dystrophy, age-related common neurodegenerative diseases, oxidative stress or reactive oxygen species (ROS) related diseases, and ageing.
Angrish, Chetna; Kumar, Anil; Chauhan, Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 2005, vol. 44, # 7, p. 1515 - 1518
作者:Angrish, Chetna、Kumar, Anil、Chauhan
DOI:——
日期:——
Potent 2′-aminoanilide inhibitors of cFMS as potential anti-inflammatory agents
作者:Raymond J. Patch、Benjamin M. Brandt、Davoud Asgari、Nand Baindur、Naresh K. Chadha、Taxiarchis Georgiadis、Wing S. Cheung、Ioanna P. Petrounia、Robert R. Donatelli、Margery A. Chaikin、Mark R. Player
DOI:10.1016/j.bmcl.2007.09.057
日期:2007.11
A series of 2 '-aminoanilides have been identified which exhibit potent and selective inhibitory activity against the cFMS tyrosine kinase. Initial SAR studies within this series are described which examine aroyl and amino group substitutions, as well as the introduction of hydrophilic substituents on the benzene core. Compound 47 inhibits the isolated enzyme (IC50 = 0.027 mu M) and blocks CSF-1-induced proliferation of bone marrow-derived macrophages (IC50 = 0.11 mu M) and as such, serves as a lead candidate for further optimization studies. (C) 2007 Elsevier Ltd. All rights reserved.