Ascendis Pharma A/S
Prodrug Comprising a Drug Linker Conjugate

Abstract:

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.sup.1 represented by formula (I): ##STR00001## wherein the dashed line indicates the attachment to the amine of the biologically active moiety and wherein R.sup.1, R.sup.1a, R.sup.2, R.sup.2a, R.sup.3, R.sup.3a, X, X.sup.1, X.sup.2, X.sup.3 have the meaning as indicated in the description and the claims and wherein L.sup.1 is substituted with one to four groups L.sup.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.sup.2 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.