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Title:
CYTOTOXIC ANTIBODY CONJUGATE
Document Type and Number:
Japanese Patent JPH02256700
Kind Code:
A
Abstract:

NEW MATERIAL: A cytotoxic antibody conjugate represented by formula I (wherein m is 1-10, Ab is an antibody recognizing an antigen related to undesired cells or its fragment, x is a group represented by formula II (R is H or phenyl and n is 0-5) and M is a group represented by formula III (wherein R3 is S or O; R4 is CO, SO2, CONH, etc., Z is a methotrexate medicine represented by formula IV (R6 is H or a salt and t is 1-6)].

USE: An anti-cancer agent.

PROCESS: For example, a compd. represented by formula [R7-CO-X=R8] [wherein R7 is a carboxylic acid active group, R8 is O, (OH3)2 or (OCH2CH3)2] is reacted with a monoclonal antibody specific to a tumor related antigen to obtain a derived antibody represented by formula V and this antibody is reacted with methotrexate-hydrazine represented by the formula H2NHN-M to obtain the cytotoxic medicine conjugate represented by the formula I.


Inventors:
DEIBITSUDO AASAA JIYONSON
BENNETSUTO KOORUMAN RAGUTSUZA
UIRIAMU REONAADO SUKOTSUTO
Application Number:
JP20554489A
Publication Date:
October 17, 1990
Filing Date:
August 07, 1989
Export Citation:
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Assignee:
LILLY CO ELI
International Classes:
A61K39/395; A61K47/48; A61P35/00; C07D475/08; C07K1/113; C07K14/00; C12P21/08; C07K14/705; C07K16/00; C07K19/00; C12R1/91; (IPC1-7): A61K39/395; C07D475/08; C07K3/08; C07K15/12; C07K15/28; C12P21/08
Attorney, Agent or Firm:
Aoyama Ryo (1 person outside)