Bayer Pharma Aktiengesellschaft

Bayer Aktiengesellschaft

Leo Marx

Hans-Georg Lerchen

Anne-Sophie Rebstock

Beatrix Stelte-Ludwig

Simone Greven

Christoph Mahlert

Anette Sommer

Carsten Terjung

Sandra Berndt

Yolanda Cancho Grande

Lisa Dietz

Sarah Anna Liesa Johannes

Hannah Joerissen

The present invention relates to novel binder-prodrug conjugates (APDCs) where binders are conjugated with inactive precursor compounds of kinesin spindle protein inhibitors, and to antibody-drug conjugates ADCs and to processes for producing these APDCs and ADCs.

Antibody drug conjugates with 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 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.

Prodrugs of cytotoxic active agents having enzymatically cleavable groups

The invention relates to novel prodrugs or conjugates of the general formula (Ia) in which cytotoxic drugs, for example kinesin spindle protein inhibitors, are masked with legumain-cleavable groups and hence release the drug, 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.

Antibody drug conjugates (ADCS) and antibody prodrug conjugates (APDCS) with enzymatically cleavable groups

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Wuppertal, Germany

Leo Marx