发明名称 Compounds and Methods for Producing a Conjugate
摘要 The present disclosure provides conjugate structures and compound structures used to produce these conjugates. The disclosure also encompasses methods of production of such conjugates, as well as methods of using the same.
申请公布号 US2016038602(A1) 申请公布日期 2016.02.11
申请号 US201514704802 申请日期 2015.05.05
申请人 Redwood Bioscience, Inc. 发明人 Kudirka Romas Alvydas;Albers Aaron Edward;Rabuka David
分类号 A61K47/48;C12N9/96;C07K16/22;G01N33/533;C07D405/04;C12N9/12;C07K16/40;A61K38/10;C07D231/20 主分类号 A61K47/48
代理机构 代理人
主权项 1. A conjugate comprising: at least one modified amino acid residue of the formula: wherein X is N, NH, O, S, CH or CH2; Y1 and Y2 are each independently selected from N, O and S; n is 1 or 2; R2 is selected from hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocyclyl, and substituted heterocyclyl; R3 is selected from alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, amino, substituted amino, carboxyl, carboxyl ester, acyl amino, alkylamide, substituted alkylamide, aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocyclyl, and substituted heterocyclyl; R4 is optional and if present is selected from hydrogen, hydroxyl, halogen, cyano, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkylalkoxy, substituted alkylalkoxy, acyl, carboxyl, and carboxyl ester; R5 is optional and if present is hydrogen or hydroxyl; and R6 is selected from hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, amino, substituted amino, carboxyl, carboxyl ester, acyl amino, alkylamide, substituted alkylamide, aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocyclyl, and substituted heterocyclyl, wherein one of W1 and W2 is a polypeptide and the other is a drug or a detectable label, wherein the dotted lines represent optional bonds, wherein when the dotted line between the R4-carbon and the R5-carbon is a double bond, n is 1 and R4 and R5 are not present, and wherein, when n is 2, the dotted line between the R4-carbon and the R5-carbon is not a double bond and R5 is not present.
地址 Emeryville CA US