PYRROLO[2,3-C]PYRIDINES AS IMAGING AGENTS FOR NEUROFIBRILLARY TANGLES Russian patent published in 2023 - IPC C07D471/04 C07D519/00 A61K31/437 A61K31/4725 A61K51/04 A61P25/28 C07B59/00 

FIELD: medicine.

SUBSTANCE: invention relates to pyrrolopyridine compounds, namely to a compound of the formula (I), marked with an isotope, where the compound is a compound marked with ²H, ³H, ¹⁸F isotope. In the formula (I): X is CH or N; R is hydrogen or -C_1-6alkyl, the specified alkyl is optionally substituted with 1-3 R^a groups; R¹ is hydrogen, -C_1-6alkyl, -CN, -C_2-6alkenyl, -(CH₂)_nOR, or -(CH₂)_nhalogen; R² is -C_1-6alkyl, -OC_1-6alkyl, -C_2-6alkenylR³, -C_2-6alkynylR³, pyridine, pyrazole, piperidine, pyrimidine, imidazole, triazole, thiazole, pyrazine, quinoline, naphthyl, -NC(O)C_6-10phenyl, -C(O)NC_6-10aryl, the specified alkyl, alkenyl, alkynyl, pyridine, pyrazole, piperidine, pyrimidine, imidazole, triazole, thiazole, pyrazole, pyrazine, quinoline, naphthyl, phenyl, and aryl are optionally substituted with 1-3 R^a groups; or neighboring R¹, together with R², can form phenyl, pyrol, furan, pyridine, piperidine, a bicyclic ring is optionally substituted with 1-3 R^a groups; R³ is hydrogen, -C_1-6alkyl, phenyl, pyridyl, thiazole, which are optionally substituted with 1 R^a group; R^a is -C_1-6alkyl, phenyl, pyridine, -CN, NO₂, (CH₂)_nhalogen, -(CH₂)_nN(R)₂, (CH₂)_nOR, the specified alkyl, phenyl, and pyridine are optionally substituted with 1-3 R^b groups; R^b is hydrogen; n is equal to 0-4. A compound marked with isotopes, selected from a group of individual compounds, compositions containing a compound of the formula (I), marked with an isotope, and a method for measurement of tau protein depositions in a patient are also proposed.

EFFECT: proposed compounds can be used in binding and imaging of tau protein aggregates in patients with Alzheimer’s disease and other neurodegenerative diseases characterized by tau protein pathology, as well as for measurement of clinical efficiency of therapeutic agents for the treatment of Alzheimer’s disease and other neurodegenerative diseases characterized by tau protein pathology.

28 cl, 2 dwg, 2 tbl, 57 ex