БАРТ Джон (GB),ГОДВИН Энтони (GB),ФРИДЖЕРИО Марк (GB),БАДЕСКУ Джордж (GB)
申请号：
RU2015119561
公开号：
RU2015119561A
申请日:
2013.10.11
申请国别(地区):
RU
年份:
2016
代理人:
摘要：
1. auristatin containing conjugate of general formula: in which D - auristatin moiety q - an integer from 1 to 10 Lk- linker m - integer from 1 to 10 R represents a bond or a z-valent group -P-NH - wherein z has a value from 2 to 11 and Rpredstavlyaet a group containing at least one ethylene unit -CH-CH- or a single ethylene glycol unit -O-CH-CH- p - an integer from 1 to 10 a Lkpredstavlyaet bond or a y-valent linker, wherein y has a value from 2 to 11 and which consists of from 1 to 9 residues aspartate and / or glutamate Lkpredstavlyaet a linker of general f rmuly: wherein Ph represents an optionally substituted phenyl group X represents a group CO or SN.ON group, and Y represents a group of the formula: or c wherein each of A and B represents an alkylene or alkenylene group Ab represents a binding protein or peptide capable of binding with a binding partner on a target, said binding protein or peptide is associated with Lkposredstvom two sulfur atoms derived from a disulfide bond in the binding protein or peptide, and n - an integer from 1 to s, where s - number of disulfide bonds present in the binding protein or peptide to a nyugatsii with Lk values of m, n, p, q, y and z are selected such that the conjugate comprises from 1 to 10 groups D.2. The conjugate according to Claim. 1, wherein the auristatin is monometilauristatin monometilauristatin E or F, via the terminal atom linked azota.3. The conjugate according to Claim. 1 or 2, wherein the auristatin E monometilauristatinom is bonded through its terminal azota.4 atom. The conjugate according to Claim. 1, wherein the degradable Lkyavlyaetsya linkerom.5. . The conjugate of claim 4, wherein a Lkvklyuchaet one of the following groups: in which each of R, R , R and R represents a1. Содержащий ауристатин конъюгат общей формулы:в которой D - фрагмент ауристатинаq - целое число от 1 до 10Lk1 - линкерm - целое число от 1 до 10Р представляет собой связь или z-валентную группу -P1-NH-, где z имеет значение от 2 до 11
