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A MEDICINE CONTAINING A SELF-DIVISIBLE LINKER
专利权人:
АСЦЕНДИС ФАРМА АС (DK)
发明人:
КЛЕЕМАНН, Феликс (DE),ХЕРЗЕЛЬ, Ульрих (DE),КАДЕН, Сильвия (DE),РАУ, Харальд (DE),ВЕГГЕ, Томас (DE)
申请号:
RU2018143571
公开号:
RU2018143571A
申请日:
2018.12.10
申请国别(地区):
RU
年份:
2020
代理人:
摘要:
The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising a drug linker conjugate D-L, wherein -D is an amine containing biologically active moiety; and -L is a non-biologically active linker moiety -L 1 represented by formula (I), wherein the dashed line indicates the attachment to the amine of the biologically active moiety and wherein R 1 , R 1a , R 2 , R 2a , R 3 , R 3a , X, X 1 , X 2 , X 3 have the meaning as indicated in the description and the claims and wherein L 1 is substituted with one to four groups L 2 -Z and optionally further substituted, provided that the hydrogen marked with the asterisk in formula (I) is not replaced by a substituent; wherein L 2 is a single chemical bond or a spacer; and Z is a carrier group and wherein D-H is a polypeptide selected from the group of polypeptides consisting of exendins, glucagon, glucagon-like peptides and insulins. The invention also relates pharmaceutical composition comprising said prodrugs and their use as medicaments.
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