PYRROLO[2,3-C]PYRIDINES AS IMAGING AGENTS FOR NEUROFIBRILLAR TANGLES Russian patent published in 2019 - IPC C07D471/04 A61K31/437 A61K31/4709 A61K51/04 A61P25/28 

Abstract RU 2695373 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I):

or pharmaceutically acceptable salts thereof, where: X is CH or N; R is hydrogen or -C1-6alkyl, said alkyl is optionally substituted with 1–3 groups Ra; R1 is hydrogen, -C1-6alkyl, -CN, -C2-6alkenyl, -(CH2)nOR or -(CH2)nhalogen; R2 is -C1-6alkyl, -OC1-6 alkyl, -C2-6alkenylR3, -C2-6alkynylR3, pyridine, pyrazole, piperidine, pyrimidine, imidazole, triazole, thiazole, pyrazine, quinoline, naphthyl, -NC(O)C6-10phenyl, -C (O) NC6-10 aryl, said alkyl, alkenyl, alkynyl, pyridine, pyrazole, piperidine, pyrimidine, imidazole, triazole, thiazole, pyrazine, quinoline, naphthyl, phenyl and aryl are optionally substituted with 1–3 groups Ra; or adjacent R1 together with R2 can form phenyl, pyrrole, furan, pyridine, piperidine, formed bicyclic ring, optionally substituted with 1–3 Ra groups; R3 is hydrogen, -C1-6alkyl, - (CH2)nN (R)2, phenyl, pyridyl, thiazole, which are optionally substituted with 1 group Ra; Ra is -C1-6alkyl, phenyl, pyridine, -CN, NO2, (CH2)nhalogen, (CH2)nOR, - (CH2)nN(R)2; Rb is hydrogen and -C1-6alkyl,; and n equals 0–4.

EFFECT: compounds can be used for treating Alzheimer's disease and other neurodegenerative diseases characterized by tau protein pathology.

24 cl, 2 dwg, 2 tbl, 57 ex

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RU 2 695 373 C2

Authors

Walji, Abbas, M.

Hostetler, Eric

Greshock, Thomas

Li, Jing

Moore, Keith, P.

Bennacef, Idriss

Mulhearn, James

Selnick, Harold

Wang, Yaode

Yang, Kun

Fu, Jianmin

Dates

2019-07-23Published

2015-06-09Filed