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...

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Bibliographische Detailangaben
Hauptverfasser:	COUMANS, RUDY GERARDUS ELISABETH, SPIJKER, HENRI JOHANNES, BEUSKER, PATRICK HENRY, ELGERSMA, RONALD CHRISTIAAN, JOOSTEN, JOHANNES ALBERTUS FREDERIKUS, GROOT DE, FRANCISCUS MARINUS HENDRIKUS, MENGE, WIRO MICHAEL PETRUS BERNARDUS
Format:	Patent
Sprache:	eng ; pol
Schlagworte:	CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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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.