Prodrugs comprising an aminoalkyl glycine linker

US11633487B2 · kind B2 · utility

Assignee

• ASCENDIS PHARMA A/S · DK

Inventors

• Nicola Bisek · Heidelberg, DE
• Harald Rau · Würzburg, DE
• Felix Cleemann · Mainz, DE
• Thomas Knappe · Heidelberg, DE
• Romy Reimann · Heidelberg, DE

Key dates

• Filing date: Aug 4, 2015
• Grant date: Apr 25, 2023
• Expiry date: Aug 8, 2038

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K47/6889
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to novel prodrugs of primary or secondary amine- or hydroxyl-comprising biologically active moieties and pharmaceutically acceptable salts thereof, prodrug reagents, pharmaceutical compositions comprising these prodrugs and the use of these prodrugs. A disclosed prodrug may include a biologically active moiety reversibly and covalently linked to a specialized protective group; the linker may be reversible (i.e., hydrolytically cleavable in the absence of enzymes under physiological conditions) and, upon cleavage, may release a drug in its unmodified, pharmacologically active form.