BURT, John,GODWIN, Antony,FRIGERIO, Mark,BADESCU, George
申请号：
ES13786530
公开号：
ES2623209T3
申请日:
2013.10.11
申请国别(地区):
ES
年份:
2017
代理人:
摘要：
A conjugate comprising auristatin of formula: (((Dq-LK1) mP) p-LK2-LK3) n-Ab (I) in which D represents an auristatin q represents an integer of 1 to 10 Lk1 represents a linker m represents an integer of 1 to 10 P represents a bond or a valent group -P1-NH- z where z is 2 to 11 and P1 is a group containing at least one ethylene unit -CH2-CH2- or ethylene glycol unit -O-CH2-CH2 - p represents an integer of 1 to 10 Lk2 represents a bond or a linker valent and where y is from 2 to 11 and consisting of 1 to 9 residues aspartate and / or glutamate LK3 represents a linker of general formula: -CO-Ph-XY- (II) wherein Ph is a phenyl group optionally substituted X represents a CO group or a CH.OH group and Y represents a group of formula: ** ** Formula or Formula ** ** wherein each of A and B represents a C1-4 alkylene or alkenylene group Ab represents a protein or peptide capable of binding to a binding partner on a target, said protein or peptide attached to LK3 through two sulfur atoms derived from a disulfide bond in the protein or peptide binding being n represents an integer of 1 as where s is the number of disulfide bonds present in the protein or peptide binding before conjugation in LK3 being chosen meanings m, n, p, q, y and z such that the conjugate contains from 1 to 10 groups D.Un conjugado que contiene auristatina de la fórmula general: (((Dq-Lk1)m-P)p-Lk2-Lk3)n-Ab (I) en la que D representa un resto de auristatina q representa un número entero de 1 a 10 Lk1 representa un enlazador m representa un número entero de 1 a 10 P representa un enlace o un grupo valente z -P1-NH- donde z es de 2 a 11 y P1 es un grupo que contiene al menos una unidad de etileno -CH2-CH2- o una unidad de etilenglicol -O-CH2-CH2- p representa un número entero de 1 a 10 Lk2 representa un enlace o un enlazador valente y donde y es de 2 a 11 y que consiste en 1 a 9 residuos de aspartato y/o glutamato Lk3 representa un enlazador de la fórmula general: -CO-Ph-X-Y-(II) en la que Ph es un grupo fe
