LINKER-DRUG AND ANTIBODY-DRUG CONJUGATE (ADC) EMPLOYING THE SAME

A linker-drug represented by formula (I). In formula (I), C is a conjugating linker, L is a linker unit, D is a drug unit, and n is an integer ranging from 1 to 4. The structure of the conjugating linker is represented by formula (II). In formula (II), X is a leaving group, both of R 1 and R 2 are s...

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Bibliographische Detailangaben
Hauptverfasser:	CHANG, May-Hua, LU, Maggie, HWANG, Jenn-Tsang, HUNG, Chi-Y, FAN, Chia-Yu, KO, Yi-Ju, LIU, Chun-Min, CHANG, Li-Wen, CHENG, Ping-Fu
Format:	Patent
Sprache:	eng ; fre ; ger
Schlagworte:	HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:	A linker-drug represented by formula (I). In formula (I), C is a conjugating linker, L is a linker unit, D is a drug unit, and n is an integer ranging from 1 to 4. The structure of the conjugating linker is represented by formula (II). In formula (II), X is a leaving group, both of R 1 and R 2 are single bond or -NH- and Z is aryl, substituted aryl, heteroaryl, substituted heteroaryl, linear alkyl, cycloalkyl, heterocycloalkyl, or a combination thereof. The wave line of formula (II) indicates the covalent attachment site to L. The antibody is conjugated to the linker unit through a cysteine residue of the antibody. An antibody-drug conjugate (ADC) is also provided. C-(L-D) m (I)