Antibody-drug conjugate having cyclic benzylidene acetal linker

To provide an antibody-drug conjugate having a linker which is able to accurately control a hydrolysis rate at the pH of the weakly acidic environment in the living body. An antibody-drug conjugate having a cyclic benzylidene acetal linker represented by formula (1) or formula (2), wherein Y is an a...

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Bibliographische Detailangaben
Hauptverfasser:	Tsubusaki, Takuma, Yamamoto, Yuji
Format:	Patent
Sprache:	eng
Schlagworte:	ACYCLIC OR CARBOCYCLIC COMPOUNDS CHEMISTRY COMPOSITIONS BASED THEREON HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVINGCARBON-TO-CARBON UNSATURATED BONDS MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY ORGANIC MACROMOLECULAR COMPOUNDS PEPTIDES PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES THEIR PREPARATION OR CHEMICAL WORKING-UP
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Beschreibung
Zusammenfassung:	To provide an antibody-drug conjugate having a linker which is able to accurately control a hydrolysis rate at the pH of the weakly acidic environment in the living body. An antibody-drug conjugate having a cyclic benzylidene acetal linker represented by formula (1) or formula (2), wherein Y is an antibody; D is a drug; R 1 and R 6 are each independently a hydrogen atom or a hydrocarbon group; R 2 , R 3 , R 4 and R 5 are each independently an electron-withdrawing or electron-donating substituent or a hydrogen atom; s is 1 or 2, t is 0 or 1, and s + t is 1 or 2; w is an integer of 1 to 20; and Z 1 and Z 2 are each independently a selected divalent spacer.