Amine derivatives of folic acid analogs

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 immunorea...

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Bibliographic Details
Main Authors COUGHLIN; DANIEL J, RODWELL; JOHN D
Format Patent
LanguageEnglish
Published 18.08.1992
Subjects
CHEMISTRY
HUMAN NECESSITIES
HYGIENE
INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES
MEASURING
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
PHYSICS
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
TESTING
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Summary: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.
Bibliography:Application Number: US19890426374