CONJUGATE CONTAINING FOLIC ACID AND INDOLE-3-CARBINOL FOR MEDICAL USE Russian patent published in 2019 - IPC A61P35/00 A61P29/00 A61P9/00 C07D207/46 C07D209/12 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound of general formula B_x-(S)_y-L-(S')_z-D_n (I), in which B is a substance selected from vitamins, peptides, tumor-specific peptides, tumor cells-specific aptamers, tumor cells-specific carbohydrates, monoclonal or polyclonal antibodies, antibody fragments, proteins expressed on metastatic tumor cells; x is 0, 1 or 2; S is lysine or is a bifunctional carrier; y equals 0, or 1, or 2; L is a carrier – polyethylene glycol; S' is a bifunctional carrier selected from L-2-amino-adipic acid (AD) and β-glutamine acid (β – Glu); z is 0, or 1, or 2; D is indole-3-carbinol (I3C), wherein said compound is selected from: B-Lys-PEG-I3C, B-Lys-PEG-AD-(I3C)₂, B-Lys-PEG-βGLU-(I3C)₂, F-PEG-I3C, F-PEG-AD-(I3C)₂, F-PEG-βGLU-(I3C)₂, F-Lys-PEG-I3C, F-Lys-PEG-AD-(I3C)₂, F-Lys-PEG-βGLU-(I3C)₂, F₂-AD-PEG-I3C, F₂-AD-PEG-βGLU-(I3C)₂, F₂-AD-PEG-AD-(I3C)₂, wherein F is folic acid; Lys is lysine; PEG is polyethylene glycol or monomethoxy-polyethylene glycol (mPEG), homobifunctional or heterobifunctional; AD is L-2-amino-adipic acid, β-GLU is β-glutamic acid and I3C is indole-3-carbinol (BC). Invention also relates to versions of a method of producing a compound, to the use of said compound, to pharmaceutical or nutraceutical preparations, to a method of treating or preventing a tumor, to a method of treating or preventing an inflammatory disease.

EFFECT: proposed compound has anti-tumor activity, more selective, less toxic and is characterized by improved pharmacological properties.

21 cl, 2 tbl, 8 ex