different 6,7-dimethoxyquinazoline-2,4-diamines and evaluated their antimalarial activity via structure-activity relationship studies. Here, we summarize the results and report the discovery of 6,7-dimethoxy-N4-(1-phenylethyl)-2-(pyrrolidin-1-yl)quinazolin-4-amine (20, SSJ-717), which exhibits high antimalarial activity as a promising antimalarialdrug lead.
[EN] NOVEL SUBSTITUTED CYCLOBUTYLBENZENE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS<br/>[FR] NOUVEAUX COMPOSÉS CYCLOBUTYLBENZENE SUBSTITUÉS UTILISÉS EN TANT QU'INHIBITEURS DE L'INDOLÉAMINE 2,3-DIOXYGÉNASE (IDO)
申请人:MERCK SHARP & DOHME
公开号:WO2019074747A1
公开(公告)日:2019-04-18
Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (Formula (I)). Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.
The present invention relates to a compound according to Formula (I)
wherein
R
1
is selected from C
1
-C
6
alkyl, and said C
1
-C
6
alkyl is substituted with C
1
-C
6
alkoxy; and at least one of said C
1
-C
6
alkyl or said C
1
-C
6
alkoxy is branched; or a pharmaceutically acceptable salt thereof, solvate or solvate of a salt thereof, as well as, to compositions containing at least one compound according to Formula (I) and methods of treating at least one disease or condition therewith.
Substituted Fused Imidazole Derivatives, Pharmaceutical Compositions, and Methods of Use Thereof
申请人:Mjalli Adnan M. M.
公开号:US20110201604A1
公开(公告)日:2011-08-18
Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.