PSMA-BINDING AGENTS AND USING THEM Russian patent published in 2013 - IPC C07D211/34 A61K31/33 A61K31/44 A61P9/10 A61P9/00 A61P35/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention describes a prostate-specific membrane antigen (PSMA) compounds having a structure wherein Z represents tetrazolium or CO₂Q; each Q is independently specified in hydrogen or a protective group; and wherein (A) m has a value of 0, 1, 2, 3, 4, 5 or 6; R represents a pyridine ring specified in a group including and wherein X represents fluorine, iodine, fluorine radioisotope, iodine radioisotope, chlorine, bromine, bromine radioisotope, astatine radioisotope, NO₂, NH₂, N⁺(R²)₃, Sn(R²)₃, Si(R²)₃, Hg(R²), B(OH)₂, -NHNH₂, -NHN=CHR³, -NHNH-CH₂R³; n has a value of 1, 2, 3, 4 or 5; Y represents O, S, N(R), C(O), NR'C(O), C(O)N(R'), OC(O), C(O)O, NR'C(O)NR, NR'C(S)NR', NR'S(O)₂, S(CH₂)_P, NR(CH₂)_p, O(CH₂)_p, OC(O)CHR⁸NHC(O), NHC(O)CHR⁸NHC(O) or a covalent bond; wherein p has a value of 1, 2 or 3, R' represents H or C₁-C₆ alkyl, and R⁸ represents hydrogen, alkyl, aryl or heteroaryl, each of which may be substituted; R² represents C₁-C₆ alkyl; and R³ represents alkyl, alkenyl, alkinyl, aryl or heteroaryl each of which is substituted by fluorine, iodine, fluorine radioisotope, iodine radioisotope, chlorine, bromine, bromine radioisotope or astatine radioisotope NO₂, NH₂, N⁺(R²)₃, Sn(R²)₃, Si(R²)₃, Hg(R²) or B(OH)₂; or (B) m has a value of 0, 1, 2, 3, 4, 5 or 6; Y represents O, S, N(R'), C(O), NR'C(O), C(O)N(R'), OC(O), C(O)O, NR'C(O)NR', NR'C(S)NR', NR'S(O)₂, S(CH₂)_P, NR'(CH₂)_P, O(CH₂)_p, OC(O)CHR⁸NHC(O), NHC(O)CHR⁸NHC(O) or a covalent bond; wherein p has a value of 1, 2 or 3, R' represents H or C₁-C₆ alkyl, and R⁸ represents hydrogen, alkyl, aryl or heteroaryl, each of which may be substituted; R represents wherein X' is specified in a group including NHNH₂, -NHN=CHR³ and -NHNH-CH₂R³; wherein R³ represents alkyl, alkenyl, alkinyl, aryl or heteroaryl each of which is substituted by fluorine, iodine, fluorine radioisotope, iodine radioisotope, bromine, bromine radioisotope and astatine radioisotope; NO₂, NH₂, N⁺(R²)₃, Sn(R²)₃, Si(R²)₃, Hg(R) or B(OH)_2; R² represents C₁-C₆ alkyl; n has a value of 1, 2, 3, 4 or 5; or (C) m has a value of 4, Y represents NR', and R represents wherein G represents O, NR' or a covalent bond; R' represents H or C₁-C₆ alkyl; p has a value of 1, 2, 3 or 4, and R⁷ is specified in a group including NH₂, N=CHR³, NH-CH₂R³, wherein R³ represents alkyl, alkenyl, alkinyl, aryl or heteroaryl, each of which is substituted by fluorine, iodine, fluorine radioisotope, iodine radioisotope, chlorine, bromine, bromine radioisotope or astatine radioisotope, NO₂, NH₂, N⁺(R²)₃, Sn(R²)₃, Si(R²)₃, Hg(R²), B(OH)₂; and R² represents C₁-C₆ alkyl; also described are a method for visualising cells, organs or tissues involving the cell effect or introduction of the above compound into the body, as well as a method of treating a tumour and a kit comprising the above compound.

EFFECT: there are prepared and described the new compounds that enables introducing radionuclides for SPECT-images and positron-emission tomography (PET) easily for the purpose of visualising, eg prostate cancer cells and angiogenesis.

24 cl, 5 tbl, 24 ex, 5 dwg