发明名称 TRAPPING REAGENTS FOR REACTIVE METABOLITES SCREENING
摘要 The present invention provides compounds of Formula (I) and (II): (I) (II) wherein R1, R2, R4, R5, R6, X and n are as defined herein, and wherein R3 is hydrogen or a sulfur protecting group. Compounds of Formula (I) and (II), wherein R is hydrogen, may be useful in methods for detecting a reactive metabolite in a sample, e.g., wherein the metabolite is generated from the metabolism of a test compound, and wherein the metabolite and the compound of Formula (I) or (II) react to form a detectable adduct, e.g., detectable by mass spectrometry.
申请公布号 US2015168430(A1) 申请公布日期 2015.06.18
申请号 US201314402818 申请日期 2013.05.22
申请人 Biogen Idec MA Inc. 发明人 Penner Natalia
分类号 G01N33/94;C07K5/062 主分类号 G01N33/94
代理机构 代理人
主权项 1. A method for detecting a metabolite in a sample, the method comprising: contacting a sample comprising a metabolite and a compound of Formula (I) or (II): wherein the metabolite and the compound of Formula (I) or (II) react to form an adduct; and detecting the adduct;wherein: each instance of R1 and R2 is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, —C(═O)RA, —C(═O)ORA, —C(═O)N(RA)2, or an amino protecting group, or R1 and R2 are joined to form a substituted or unsubstituted heterocyclic ring; each instance of RA is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to an oxygen atom, or a nitrogen protecting group when attached to a nitrogen atom, or two RA groups are joined to form a substituted or unsubstituted heterocyclic ring; R3 is hydrogen; R5 and R6 are independently selected from —ORB, —N(RB)2, and a group of Formula (i):provided at least one of R5 and R6 is a group of Formula (i); each instance of RB is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, an oxygen protecting group when attached to an oxygen atom, or a nitrogen protecting group when attached to a nitrogen atom, or two RB groups are joined to form a substituted or unsubstituted heterocyclic ring; each instance of R4 is independently substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or an amino protecting group, or two R4 groups are joined to form a substituted or unsubstituted heterocyclic ring; n is 1, 2, 3, 4, 5, or 6; and X− is a counter anion.
地址 Cambridge MA US