LIGAND-DRUG CONJUGATE OF EXATECAN ANALOGUE, ITS PRODUCTION METHOD AND ITS USE Russian patent published in 2023 - IPC C07D491/22 C07K16/18 C07K16/32 A61K38/07 A61K47/54 A61K47/65 A61K47/68 A61P35/00 

FIELD: organic chemistry.

SUBSTANCE: invention relates to the field of organic chemistry, namely to a ligand-drug conjugate or its pharmaceutically acceptable salt of the formula (Pc-L-Y-Dr), where Y is -O-(CR^aR^b)_m-CR¹R²-C(O)-; R^a and R^b are a hydrogen atom; R¹ is C_3-6 cycloalkyl or C_3-6 cycloalkyl-C_1-6 alkyl; R² is a hydrogen atom; or R¹ and R², together with a carbon atom, to which they are attached, form C_3-6 cycloalkyl; m is 0 or 1; n is from 1 to 10, which can be an integer or a decimal number; Pc is an antibody; and L is a linker. The invention also relates to a compound of the formula (D₁) or to its pharmaceutically acceptable salt, a compound of the formula (L_a-Y-Dr) or to its pharmaceutically acceptable salt, a pharmaceutical composition for the treatment of cancer associated with expression of HER2 or B7H3, containing a ligand-drug conjugate of the formula (Pc-L-Y-Dr) or its pharmaceutically acceptable salt, or a compound of the formula (D₁), or its pharmaceutically acceptable salt, the use of a ligand-drug conjugate of the formula (Pc-L-Y-Dr) or its pharmaceutically acceptable salt, or a compound of the formula (D₁).

EFFECT: treatment of cancer associated with expression of HER2 or B7H3 with a conjugate of the formula (Pc-L-Y-Dr) or a compound of the formula (D₁).

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28 cl, 9 dwg, 4 tbl, 59 ex