PEPTIDOMIMETIC COMPOUNDS AND THEIR CONJUGATES OF ANTIBODIES WITH DRUGS Russian patent published in 2019 - IPC A61K47/68 C07K16/30 

FIELD: medicine.

SUBSTANCE: invention relates to a conjugate of an antibody with a drug for treating a malignant tumor, represented by formula (I), Ab—(L—D)_p, where Ab is an antibody, where the antibody binds to NaPi2b, CD33 or CD22; L is a peptidomimetic linker represented by the following formula —Str— (PM) —Sp—, where Str is an extension covalently attached to Ab; Sp is a bond or a spacer element covalently attached to a drug moiety; PM is a non-peptide chemical moiety selected from the group consisting of: and , Y is selected from C₁-C₆alkenyl, each R¹ independently represents (C₁-C₁₀alkyl)NHC(O)NH₂; R³ and R², each independently represent H or C₁-C₁₀ alkyl; R⁴ and R⁵ together can form C₃-C₇cycloalkyl ring; p is integer from 1 to 8; D is a drug moiety of formula (IA) or (IB): (IA) (IB), where R¹¹ represents a methoxy group, and R²² is C₁-C₅ alkoxy group. Invention also relates to two versions of non-peptide compounds which are suitable for preparing a conjugate, as well as a method of treating myeloid leukemia and a pharmaceutical composition for treating it. Disclosed group of inventions provides non-peptide linkers for ADC, which can be splitted with lysosomal enzymes.

EFFECT: disclosed are peptidomimetic compounds and their conjugates of antibodies with drugs.

43 cl, 2 dwg, 7 ex