Prodrugs of cytotoxic active agents having enzymatically cleavable groups

US11685714B2 · kind B2 · utility

Assignee

• Bayer Pharma Aktiengesellschaft · DE

Inventors

• Hans-Georg Lerchen · Leverkusen, DE
• Anne-Sophie REBSTOCK · Écully, FR
• Leo MARX · Wuppertal, DE
• Sarah Anna Liesa Johannes · Düsseldorf, DE
• Beatrix Stelte-Ludwig · Wülfrath, DE
• Lisa DIETZ · Wuppertal, DE
• Carsten TERJUNG · Bochum, DE
• Christoph MAHLERT · Wuppertal, DE
• Simone Greven · Dormagen, DE
• Anette SOMMER · Berlin, DE
• Sandra BERNDT · Hohen Neuendorf, DE

Key dates

• Filing date: Mar 21, 2017
• Grant date: Jun 27, 2023
• Expiry date: Jun 15, 2039

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D401/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

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.