LANG, Lixin;THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES;NIU, Gang;KIESEWETTER, Dale O.;CHEN, Xiaoyuan;TIAN, Rui
发明人:
CHEN, Xiaoyuan,NIU, Gang,LANG, Lixin,TIAN, Rui,KIESEWETTER, Dale O.
申请号：
USUS2020/015818
公开号：
WO2020/160222A3
申请日:
2020.01.30
申请国别(地区):
US
年份:
2020
代理人:
摘要：
A compound of Formula (I) or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt, is disclosed. Compositions comprising the compound and methods of use are also disclosed. Those dimeric Evans Blue derivatives, denoted as N(tEB)2, reversibly bind two molecules of albumin via the two albumin binding regions of each NtEB in the dimer, resulting in significantly increased binding affinity to albumin and extended circulation half-life in vivo. Further, when the N(tEB)2 is conjugated to a peptide therapeutic, the in situ formation of the complex of N(tEB)2 with two albumin molecules resulted in increased resistance of the peptide therapeutic from proteolysis.L'invention concerne un composé de formule I ou un ester, un amide, un solvate ou un sel pharmaceutiquement acceptable de celui-ci, ou un sel d'un tel ester ou amide ou un solvate d'un tel ester, amide ou sel, formule (I). L'invention concerne également des compositions comprenant le composé et des procédés d'utilisation.
