Prodrug comprising a drug linker conjugate

Details Prodrug comprising a drug linker conjugate Prodrug comprising a drug linker conjugate

A - Human Necessities

61

K

A61K 47/48 (2006.01)

Patent

CA 2712224

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 R1, R1a R2 , R2a , R3, R3a, X, X1, X2, X3 have the meaning as indicated in the description and the claims and wherein L1 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 L2 is a single chemical bond or a spacer; and Z is a carrier group.The invention also relates to A-L, wherein A is a leaving group, pharmaceutical composition comprising said prodrugs and their use as medicaments.

Linvention concerne un promédicament ou son sel pharmaceutiquement acceptable comprenant un conjugué médicament-lieur D-L, -D étant un fragment biologiquement actif contenant une amine; et L étant un fragment de lieur non biologiquement actif, -L1 représenté par la formule (I), la ligne en pointillé indiquant lattache à lamine du fragment biologiquement actif et R1, R1a, R2, R2a , R3, R3a, X, X1, X2, X3  ayant les mêmes significations que dans la description et les revendications et L1 étant substitué par un à quatre groupes L2 -Z et éventuellement davantage substitué à condition que lhydrogène marqué par lastérisque dans la formule (I) ne soit pas remplacé par un substituant; L2 étant une simple liaison chimique ou un espaceur; et Z étant un groupe porteur. Linvention concerne également A-L, A étant un groupe partant, une composition pharmaceutique comprenant lesdits promédicaments et leur utilisation comme médicaments.

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