发明名称 Multifunctional nitroxide derivatives and uses thereof
摘要 Multifunctional nitroxide derivatives comprising a potassium channel opener and a reactive oxygen species (ROS) degradation catalyst that can act as an anti-oxidant, as well as pharmaceutical compositions comprising them are provided. The multifunctional compounds and pharmaceutical compositions are useful for treatment of diseases, disorders or conditions associated with oxidative stress or endothelial dysfunction.
申请公布号 US9102659(B2) 申请公布日期 2015.08.11
申请号 US201113992396 申请日期 2011.12.08
申请人 RADIKAL THERAPEUTICS INC. 发明人 Jagtap Prakash;Salzman Andrew Lurie
分类号 A61K31/4439;C07D401/12;C07D207/46;C07D211/94;C07D223/12 主分类号 A61K31/4439
代理机构 Knobbe, Martens, Olson & Bear, LLP 代理人 Knobbe, Martens, Olson & Bear, LLP
主权项 1. A compound of formula I: or an enantiomer, diastereomer, racemate, or a pharmaceutically acceptable salt or solvate thereof, wherein A is a moiety of formula II linked through its terminal —NH group to any carbon atom of the pyridine, ring: R1 is absent or 1 to 54 substituents each independently selected from the group consisting of halogen, —CN, —OH, —NO2, —N(R6)2, —OCF3, —CF3, —OR6, —COR6, —COOR6, —CON(R6)2, —OCOOR6, —OCON(R6)2, —(C1-C8)alkylene-COOR6, —SR6, —SO2R6, —SO2N(R6)2, and —S(═O)R6, wherein said —(C1-C8)alkyl and —(C1-C8)alkylene-COOR6 may optionally be substituted with —OH, —OR3, —OCF3, —CF3, —COR3, —COOR3, —OCOOR3, —OCON(R3)2, —(C1-C8)alkylene-COOR3, —CN, —NH2, —NO2, —SH, —SR3, —(C1-C8)alkyl, —N(R3)2, —CON(R3)2, —SO2R3, or —S(═O)R3, or two adjacent R1 groups and the carbon atoms to which they are attached form a 5- or 6-membered carbocyclic or heterocyclic ring, (C6-C10)aryl, or 6- to 10-membered heteroaryl; R2 each independently is selected from the group consisting of H, halogen, —OCF3, —CF3, —OR7, —COR7, —COOR7, —OCOOR7, —OCON(R7)2, —(C1-C8)alkylene-COOR7, —CN, —NO2, —SH, —SR7, —N(R7)2, —CON(R7)2, —SO2R7, SO2N(R7)2, and —S(═O)R7; R3 each independently is selected from the group consisting of (C1-C8)alkyl, (C2-C8)alkenyl, and (C2-C8)alkynyl; R4 is selected from the group consisting of H, —COOR7, —(C1-C8)alkylene-COOR7, —CN, —(C1-C8)alkyl, and —CON(R7)2; R5 is selected from the group consisting of H, —OH, —CO—(C1-C8)alkyl, —COO—(C1-C8)alkyl, —CN, and —NH2; R6 each independently is selected from the group consisting of H, (C1-C8)alkyl, (C3-C10)cycloalkyl, 4-12-membered heterocyclyl, (C6-C14)aryl, and —(C1-C8)alkylene-NH2; and R7 each independently is selected from the group consisting of H, (C1-C8)alkyl, — (C1-C8)alkylene-NH2, (C3-C10)cycloalkyl, 4-12-membered heterocyclyl, and (C6-C14)aryl, each of which other than H may optionally be substituted with —OR6, —COR6, —COOR6, —OCOOR6, —OCON(R6)2, —(C1-C8)alkylene-COOR6, —CN, —NO2, —SR6, —N(R6)2, —CON(R6)2, —SO2R6, or —S(═O)R6.
地址 West Tisbury MA US