The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Aug. 13, 2024
Filed:
Dec. 18, 2017
Bayer Aktiengesellschaft, Leverkusen, DE;
Bayer Pharma Aktiengesellschaft, Berlin, DE;
Hans-Georg Lerchen, Leverkusen, DE;
Anne-Sophie Rebstock, Champagne au Mont d'Or, FR;
Leo Marx, Wuppertal, DE;
Sarah Anna Liesa Johannes, Hilden, DE;
Beatrix Stelte-Ludwig, Wülfrath, DE;
Lisa Dietz, Wuppertal, DE;
Hannah Joerissen, Heiligenhaus, DE;
Christoph Mahlert, Wuppertal, DE;
Simone Greven, Dormagen, DE;
Anette Sommer, Berlin, DE;
BAYER AKTIENGESELLSCHAFT, Leverkusen, DE;
BAYER PHARMA AKTIENGESELLSCHAFT, Berlin, DE;
Abstract
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.