Amine derivatives of folic acid analogs

Details Amine derivatives of folic acid analogs Amine derivatives of folic acid analogs

1989-10-24

1992-08-18

Waddell, Frederick E.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

4 to 5 amino acid residues in defined sequence

544260, C07D47500

Patent

active

051401045

ABSTRACT:
Novel therapeutic antibody conjugates comprising amine derivatives of folic acid analogs covalently attached via a reactive amine group to an oxidized carbohydrate moiety of an antibody or antibody fragment are disclosed. The conjugates retain substantially the same immunorespecificity and immunoreactivity of the unconjugated antibody molecule. The immunospecificity and immunoreactivity of the antibody conjugates permits targeted delivery of the attached therapeutically effective amine derivative of folic acid analogs in vivo. The conjugates are therapeutically effective against a variety of neoplastic and non-neoplastic cellular disorders when administered in vivo. Methods for synthesizing the amine derivatives of folic acid analogs, methods for preparing the antibody conjugates, and methods for use of the conjugates in vivo are also disclosed.

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