CHARI, Ravi V. J.,ZHAO, Robert Yongxin,KOVTUN, Yelena,SINGH, Rajeeva,WIDDISON, Wayne Charles
申请号：
ES09739779
公开号：
ES2648122T3
申请日:
2009.04.30
申请国别(地区):
ES
年份:
2017
代理人:
摘要：
A crosslinker to make a cell-drug binding agent conjugate, wherein the crosslinker is represented by formula (I) ** Formula ** where: Y 'represents a functional group that enables reaction with a cell binding agent selected from between an antibody, a single chain antibody or an antibody fragment that binds to the target cell, where Y 'is selected from an N-hydroxysuccinimide ester, p-nitrophenyl ester, dinitrophenyl ester, pentafluorophenyl ester, disulfide pyridyl, nitropyridyl disulfide, maleimide, halogenoacetate or carboxylic acid chloride； Q represents a functional group that enables the connection of a cytotoxic drug through a disulfide, thioether, thioester, peptide, hydrazone, ester, ether, carbamate or amide linkage, where Q is selected from the group consisting of thiol, disulfide, amino, carboxy, aldehyde, maleimido, halogenoacetyl, hydrazine and hydroxy； one of R1, R2, R3, R4, R9 and R10 is a charged substituent selected from SO3 -, X-SO3 -, OPO3 2-, XOPO3 2-, N + R11R12R13 and X-N + R11R12R13, and the rest are H ； l, g and m are each 0； n is 1, where: R11, R12 and R13 are the same or different and are linear alkyl having 1 to 6 carbon atoms or branched or cyclic alkyl having 3 to 6 carbon atoms, and X represents phenyl or an alkyl linear having 1 to 6 carbon atoms or a branched or cyclic alkyl having 3 to 6 carbon atoms； and Z is absent.Un reticulante para elaborar un conjugado de agente de unión celular-fármaco, donde el reticulante se representa por la fórmula (I)**Fórmula** donde: Y' representa un grupo funcional que posibilita la reacción con un agente de unión celular seleccionado de entre un anticuerpo, un anticuerpo monocatenario o un fragmento de anticuerpo que se una a la célula diana, donde Y' se selecciona de entre un éster de N-hidroxisuccinimida, éster de p-nitrofenilo, éster de dinitrofenilo, éster de pentafluorofenilo, disulfuro de piridilo, disulfuro de nitropiridilo, maleimida, halogenoacetato o cloruro de ácido carboxílico； Q represen
