Prodrugs of cytotoxic active agents having enzymatically cleavable groups

The invention relates to novel prodrugs or conjugates of the general formula (Ia)in which La, n, R and D have the definitions given in the description and which have a structural motif reduced to an asparagine derivative as cleavage site for tumour-associated proteases such as legumain, in which cyt...

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Bibliographic Details
Main Authors Johannes, Sarah Anna Liesa, Mahlert, Christoph, Dietz, Lisa, Joerissen, Hannah, Marx, Leo, Sommer, Anette, Lerchen, Hans-Georg, Rebstock, Anne-Sophie, Stelte-Ludwig, Beatrix, Greven, Simone
Format Patent
LanguageEnglish
Published 13.08.2024
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:The invention relates to novel prodrugs or conjugates of the general formula (Ia)in which La, n, R and D have the definitions given in the description and which have a structural motif reduced to an asparagine derivative as cleavage site for tumour-associated proteases such as legumain, in which cytotoxic drugs, for example kinesin spindle protein inhibitors, are released by legumain cleavage, and to the use of these prodrugs or conjugates for treatment and/or prevention of diseases, and to the use of these prodrugs or conjugates for production of medicaments for treatment and/or prevention of diseases, especially of hyperproliferative and/or angiogenic disorders, for example cancers. Reduction of the legumain-cleavable substrate peptide sequence to an asparagine derivative as structural motif, as a result of slowed legumain cleavage, achieves an increase in stability in the lysosomes of healthy organs while simultaneously maintaining the high anti-tumour effect.
Bibliography:Application Number: US201716472634