PRODRUG CONTAINING A SELF-CLEAVABLE LINKER Russian patent published in 2023 - IPC A61K47/60 A61K47/65 A61K38/17 A61K38/18 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a prodrug, or a pharmaceutically acceptable salt thereof, containing a drug-linker conjugate D-L, wherein D is a nitrogen-containing polypeptide; L is a biologically inactive linker fragment L¹ represented by the structural formula (I) where the dotted line demonstrates the attachment to the nitrogen of the polypeptide through the formation of an amide bond, where R¹, R^la, R², R^2a, R³, R^3a, X, X¹, X², X³ have the meanings given in the claims, and where L¹ is substituted by 1–4 L²-Z groups, provided that the hydrogen marked with * in formula (I) cannot be substituted by a substituent; where L² represents a single chemical bond or spacer; and Z represents a carrier group such as a linear or branched poly(ethylene glycol) with a molecular weight of 2,000 to 150,000 Da.

EFFECT: obtaining a prodrug containing a self-cleavable linker.

12 cl, 3 dwg, 52 ex