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US 5,030,719 AGranted
Cytotoxic antibody conjugates and a process for preparation thereof
AssigneeTeijin Limited
InventorsNaoji Umemoto, Yoshinori Kato, Takeshi Hara
Life of this patent
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Abstract
Cytotoxic antibody conjugates in which a folic acid-antagonistic folic acid analogue is bound to an antibody or its fragment through an oligopeptide. The conjugates can be used as a chemotherapeutic agent against malignant tumors.
Claims7
Cytotoxic antibody conjugates wherein an antibody or its fragment which binds to antigenic cells is bound to a folic acid-antagonistic folic acid analgogue through an oligopeptide, wherein said cytotoxic antibody conjugate is represented by general formula (I)
- (R'--CO--NH--Y--CO--NHNHCOCH.sub. 2 --NH) Ab (I)
- where R' represents, together with CO, the residual group of a folic acid-antagonistic folic acid analogue, --NH--Y--CO--represents the residual group of an oligopeptide containing L-leucyl-L-alanyl-L-leucine, Ab represents an antibody or its fragment which bends to antigenic cells, and the N-atom adjacent to Ab is the nitrogen atom originating from the antibody or its fragment, and n is an integer of from 1 to 30.
A process for preparation of cytotoxic antibody conjugates of general formula (II)
- (RCONHNHCOCH.sub. 2 NH Ab (II)
- where R represents, together with CO, a monovalent organic group originating from a cytotoxic substance, Ab represents antibody or its fragment which binds to antagenic cells, the N-atom binding with Ab originates from an antibody or its fragment, and n is an integer of from 1 to 30,
- characterized by reaction of an antibody or its fragment which binds to antigenic cells with a halogenated acetyl hydrazide derivative of a cytotoxic substance having a general formula (III)
- RCONHNHCOCH.sub. 2 X (III)
- wherein the definition of R is the same as in formula (II), and X represents a halogen.
2 more elements
Dependencies are inferred from the claim text.