SINGH, RAJEEVA,KOVTUN, YELENA,WILHELM, SHARON, D,CHARI, RAVI, V
申请号：
NZ58885109
公开号：
NZ588851A
申请日:
2009.04.30
申请国别(地区):
NZ
年份:
2013
代理人:
摘要：
Disclosed is a compound of formula (1) or (1): Z-Xl-(-CH2-CH2-O-)n-Yp-D (1) D-Yp-(-CH2-CH2-O-)n-Xl-Z (1) wherein: Z represents a reactive functionality that can form an amide or a thioether bond with a cell-binding agent wherein the reactive functionality is selected from the group consisting of a reactive carboxylic ester, a reactive sulfonic acid derivative, a reactive thioester group, a haloacetamide and a vinyl sulfone D represents a maytansinoid X represents an aliphatic, an aromatic or a heterocyclic unit attached to the cell-binding agent via a thioether bond, an amide bond, a carbamate bond, or an ether bond Y represents an aliphatic, an aromatic or a heterocyclic unit attached to the drug via a covalent bond selected from the group consisting of a thioether bond, an amide bond, a carbamate bond, an ether bond, an amine bond, a carbon-carbon bond and a hydrazine bond l is 0 or 1 p is 0 or 1 and n is an integer from 1 to 2000. Also disclosed is a cell-binding agent cytotoxic drug conjugate of formula (2) or (2): CB-[Xl-(-CH2-CH2-O-)n-Yp-D]m (2) [D-Yp-(-CH2-CH2-O-)n-Xl]m-CB (2) CB represents a cell-binding agent, wherein the cell-binding agent is an antibody and m is an integer from 2 to 15. Other substituents are as disclosed above. Further disclosed is a composition comprising the conjugate and the use of the conjugate for the manufacture of a medicament for treating a disease selected from tumour, autoimmune diseases, graft rejections, graft versus host disease, viral infections, and parasite infections.
