发明名称 Substituted 1-pyrrolidinyloxy, 1-piperidinyloxy and 1-azepanyloxy compounds for treating diseases associated with oxidative stress or endothelial dysfunction
摘要 Compounds are of the class of 1-pyrrolidinyloxy,1-piperidinyloxy, and 1-azepanyloxy derivatives of formula (I):; The compounds are useful in prevention, treatment or management of diseases, disorders or conditions associated with oxidative stress or endothelial dysfunction. The compounds include 2,2,5,5,-tetramethyl-3-(nitrooxymethyl)pyrrolidin-1-yl acetate.
申请公布号 US9604932(B2) 申请公布日期 2017.03.28
申请号 US201414769078 申请日期 2014.03.05
申请人 Radikal Therapeutics Inc. 发明人 Salzman Andrew Lurie;Jagtap Prakash;Southan Garry John
分类号 A61K31/40;C07D207/46;C07D223/04;C07D211/94 主分类号 A61K31/40
代理机构 Knobbe, Martens, Olson & Bear, LLP 代理人 Knobbe, Martens, Olson & Bear, LLP
主权项 1. A compound of the formula I:I or an enantiomer, diastereomer, racemate, or a pharmaceutically acceptable salt thereof, wherein each R1 is independently selected from the group consisting of H, —OH, —COR4, —COOR4, —OCOOR4, —OCON(R4)2, —(C1-C16)alkylene-COOR4, —CN, —NO2, —SH, —SR4, —(C1-C16)alkyl, —O—(C1-C16)alkyl, —N(R4)2, —CON(R4)2, —SO2R4, —SO2NHR4, —S(═O)R4, and a nitric oxide donor group of the formula —X1—X2—X3, wherein X1 is absent or selected from the group consisting of —O—, —S— and —NH—; X2 is absent or is (C1-C20)alkylene optionally substituted by one or more —ONO2 groups; and X3 is —NO or —ONO2, provided that at least one R1 group is a nitric oxide donor group; each R2 is independently selected from the group consisting of (C1-C16)alkyl, (C2-C16)alkenyl, and (C2-C16)alkynyl; R3 is selected from the group consisting of (C1-C10)alkyl, (C3-C10)cycloalkyl, (C6-C14)aryl, and 4-12-membered heterocyclyl, each of which may optionally be substituted with —OH, —COR5, —COOR5, —(C1-C8)alkylene-COOR5, —CN, —NO2, —(C1-C8)alkyl, —O—(C1-C8)alkyl, —N(R5)2, —CON(R5)2, —SO2R5, —SO2NHR5, or —S(═)R5; each R4 is independently selected from the group consisting of H, (C1-C8)alkyl, (C3-C10)cycloalkyl, (C6-C14)aryl, and 4-12-membered heterocyclyl, each of which other than H may optionally be substituted with —OH, —COR5, —COOR5, —OCOOR5, —OCON(R5)2, —(C1-C8)alkylene-COOR5, —CN, —NO2, —SH, —SR5, —(C1-C8)alkyl, —O—(C1-C8)alkyl, —N(R5)2, —CON(R5)2, —SO2R5, —SO2NHR5, or —S(═O)R5; each R5 is independently selected from the group consisting of H, (C1-C8)alkyl, (C3-C10)cycloalkyl, (C6-C14)aryl, and 4-12-membered heterocyclyl; and n is 1, 2 or 3.
地址 West Tisbury MA US