NOVEL CONJUGATES OF ANALOGUES OF CC-1065 AND BIFUNCTIONAL LINKERS Russian patent published in 2020 - IPC C07D471/04 A61K31/437 A61P35/00 

FIELD: organic chemistry.

SUBSTANCE: invention relates to a heterocyclic compound of formula (IIII-AZ), where R^5a is methyl, AZ is

,

V¹ is selected from valyl-citrulline, valyl-lysine, phenylalanyl-lysine, alanyl-phenylalanyl-lysine and D-alanyl-phenylalanyl-lysine,

CL is

L is selected from , q varies from 1 to 4, and Ab is selected from CD19 antibody, CD22 antibody, CD30 antibodies, CD33 antibodies, CD56 antibodies, CD70 antibodies, CD74 antibodies, CD138 antibodies, CLL-1 antibodies, 5T4 antibodies, CD303 antibodies, Tag 72 antibodies, carbohydrate similar to Lewis A antibodies, EphB3 antibodies, HMW-MAA antibodies, CD38 antibodies, Cripto antibodies, EphA2 antibodies, GPNMB antibodies, integrin antibodies, MN antibodies, Her2 antibodies and PSMA antibodies or epitope-binding fragment or derivative of any of them. Invention also relates to use of the compound of formula (III-AZ) as a drug for treating or preventing tumor in a mammal.

EFFECT: obtaining novel conjugates useful for treating a tumor.

4 cl, 7 dwg, 16 ex