Bayer Aktiengesellschaft

Bayer Pharma Aktiengesellschaft

Hannah Joerissen

Lisa Dietz

Raimund Kast

Hartmut Beck

Jens Nagel

Chantal Fuerstner

Timo Stellfeld

Mark Meininghaus

Peter Hauff

Joerg Mueller

Karoline Droebner

Michaela Bairlein

Johanna Anlahr

Clemens-Jeremias Von Buehler

Hans-Georg Lerchen

Anne-Sophie Rebstock

Beatrix Stelte-Ludwig

Simone Greven

Sonja Anlauf

Christoph Mahlert

Sarah Anna Liesa Johannes

Carsten Terjung

Anette Sommer

Leo Marx

Uwe Muenster

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 present application relates to novel substituted N-arylethyl-2-aminoquinoline-4-carboxamide derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of fibrotic and inflammatory disorders.

Substituted N-arylethyl-2-aminoquinoline-4-carboxamides and use thereof

The present application relates to novel substituted N-arylethyl-2-arylquinoline-4-carboxamide derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of fibrotic and inflammatory disorders.

Substituted-arylethyl-2-arylquinoline-4-carboxamides and use thereof

Growing community of inventors

Heiligenhaus, Germany

Hannah Joerissen