发明名称 N-substituted noribogaine prodrugs
摘要 This invention relates generally to prodrugs of noribogaine. This invention also relates to pharmaceutical compositions comprising the prodrugs of noribogaine as well as method of treating pain, addiction and/or stress using such compounds and/or pharmaceutical compositions.
申请公布号 US9586954(B2) 申请公布日期 2017.03.07
申请号 US201414257841 申请日期 2014.04.21
申请人 DEMERX, INC. 发明人 Mash Deborah C.
分类号 A61K31/55;C07D453/06;C07D471/22;A61K9/127;A61K9/00;A61K47/14;A61K9/02;A61K9/10;A61K9/20;A61K9/48 主分类号 A61K31/55
代理机构 Foley & Lardner LLP 代理人 Foley & Lardner LLP
主权项 1. A compound of Formula I: wherein L is selected from the group consisting of a covalent bond and a cleavable linker group; R1 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, substituted aryl, cycloalkyl, substituted cycloalkyl, heteroaryl, substituted heteroaryl, heterocyclic, and substituted heterocyclic provided that R1 is not a saccharide or an oligosaccharide; R10 is hydrogen or —OR provided that when R1 is hydrogen and R10 is hydrogen, L is a cleavable linker group; R11 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, (CH2)mOC(O)alkyl, (CH2)mOH, (CH2)mOalkyl, CH2—X-alkyl or (CH2)mO(CH2)pO(CH2)qO(CH2)rCH3, where each of m, p and q is 1, 2 or 3; and r is 0, 1 or 2, X is O or NH; provided that R11 is not ethyl; provided that when R11 is substituted ethyl, R10 excludes —OH; and provided that when R11 is substituted ethyl, R10 excludes —OCONR3R4; and R is selected from the group consisting of hydrogen, a hydrolysable group selected from the group consisting of —C(O)R2, —C(O)NR3R4 and —C(O)OR5, where R2 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl and substituted alkynyl, R3 and R4 are independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclic and substituted heterocyclic, R5 is selected from the group consisting of alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclic and substituted heterocyclic, provided that R is not a saccharide or an oligosaccharide; or a pharmaceutically acceptable salt thereof.
地址 Fort Lauderdale FL US