DELIVERY SYSTEMS FOR CONTROLLED DRUG RELEASE Russian patent published in 2021 - IPC C07D405/12 C07D519/04 C07H15/252 C07H19/10 C07H19/24 C07K5/06 C07K5/72 A61K47/54 A61P35/00 

FIELD: biochemistry.

SUBSTANCE: invention relates to the compound of Formula (I)

or a pharmaceutically acceptable salt thereof, diastereomer or stereoisomer wherein the Agent is selected from the group consisting of a cytostatic agent, a cytotoxic agent and a derivative of any of the above, the Spacer is absent or is selected from the group consisting of and , n is 0, X is unsubstituted 6-membered aryl, Y is absent or is selected from the group consisting of unsubstituted C₁-C6 alkylene, -NH-C(O)-, -C(O)-NH-, C(O)-O- and -O-C(O)-, R₁ is absent or is unsubstituted C₁-C₁₈ alkylene or R₁ has the following formula:

R₂ is selected from the group consisting of -H and unsubstituted C₁-C₁₂ alkyl, each of Z₁, Z₂, Z₃ and Z₄ independently represents -H, halogen or -NO₂, PBG represents an unsubstituted maleimide group, while when the Spacer is absent, the Agent is bound to nitrogen adjacent to the Spacer through a double bond, and wherein at least one of Z₁, Z₂, Z₃ and Z₄ is not Н. Also proposed is a pharmaceutical composition, a method for treating a malignant neoplasm and the use of a compound or composition in the manufacture of a medicament.

EFFECT: proposed compounds can be used for efficient and controlled drug delivery and release.

46 cl, 8 dwg, 1 tbl, 13 ex