FIELD: pharmaceutical chemistry.
SUBSTANCE: group of inventions includes a compound of formula (I), its pharmaceutically acceptable salts, enantiomers, dihydrate (S)-N-methyl-N-(6-methyl-2-((4aS,5aR)-5a-methyl-1,4,4a,5,5a,6-hexahydrocyclopropa[f]indazol-3-yl)-1H-benzo[d]imidazol-5-yl)-2-morpholinopropanamide, pharmaceutical composition and the use based on them. In formula (I), each R1 is independently H or F; R2 is either H or (C1-C4)alkyl; each R3 is independently H, F or (C1-C4)alkyl; R5 and R6 independently represent H; halogen; OH; CN; (C1-C6)alkyl; hydroxy(C1-C6)alkyl; (C1-C4)alkoxy(C1-C6)alkyl; (C1-C6)alkyl substituted with one, two or three F; (C1-C6)alkoxy; or (C1-C6)alkoxy substituted with (C1-C4)alkoxy; R4 is selected from or
, each of which is optionally substituted with one or two substituents independently selected from oxo, (C1-C4)alkyl and hydroxy(C1-C4) alkyl.
EFFECT: benzimidazole derivatives exhibiting properties of ITK inhibitors.
26 cl, 7 dwg, 4 tbl, 56 ex
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Authors
Dates
2023-09-12—Published
2020-12-16—Filed