Novel Conjugates of CC-1065 Analogs and Bifunctional Linkers

Novel Conjugates of CC-1065 Analogs and Bifunctional Linkers

This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: Joosten Johannes Albertus Frederikus, BEUSKER Patrick Henry, Coumans Rudy Gerardus Elisabeth, Elgersma Ronald Christiaan, De Groot Franciscus Marinus Hendrikus, Menge Wiro Michael Petrus Bernardus, Spijker Henri Johannes
Format: Patent
Sprache:eng
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Beschreibung
Zusammenfassung:This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.