DUOCARMYCIN DERIVATIVE AND USE THEREOF

DUOCARMYCIN DERIVATIVE AND USE THEREOF

It is an object of the present invention to provide a conjugate of a duocarmycin derivative and a biotin-modified dimer, which is useful for pretargeting methods. According to the present invention, a compound represented by the following formula (1) or formula (2) is provided:wherein R1 and R2 each...

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Bibliographische Detailangaben
Hauptverfasser: KODAMA, Tatsuhiko, TATSUMI, Toshifumi, SUGIYAMA, Akira, TOKUYAMA, Hidetoshi, KANAI, Motomu, TSUKAGOSHI, Masanobu, SAKATA, Juri, YAMATSUGU, Kenzo
Format: Patent
Sprache:eng ; fre ; ger
Schlagworte:
CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:It is an object of the present invention to provide a conjugate of a duocarmycin derivative and a biotin-modified dimer, which is useful for pretargeting methods. According to the present invention, a compound represented by the following formula (1) or formula (2) is provided:wherein R1 and R2 each independently represent a hydrogen atom, a lower alkyl group, or a lower alkoxycarbonyl group; one of R3, R4, and R5 represents -O-L7-(Xaa)m-L6-N3, and the remaining two each independently represent a hydrogen atom, a lower alkyl group, or a lower alkoxycarbonyl group; X represents a reactive group; L6 and L7 each independently represent a divalent linking group; Xaa represents an amino acid residue; m represents an integer of 2 to 10; and Me represents a methyl group.