SELECTIVE HDAC6 INHIBITORS Russian patent published in 2022 - IPC C07D249/12 C07D417/06 C07D417/04 C07D271/10 C07D405/04 C07D401/04 C07D471/04 C07D403/04 C07D405/14 C07D495/04 C07D409/04 C07D405/06 A61K31/4196 A61K31/4245 A61P35/00 

Abstract RU 2764718 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a compound by the formula (I) and (II), pharmaceutically acceptable salts and stereoisomers thereof, wherein A=N, O, S in the formula (I), A=N in the formula (II); B=C, N; C=N, O in the formula (I) when C=N in the formula (II); X=CH2, S, NH; n=0, 1; when n=1, a carbon atom can be substituted with R12 and R13, independently selected from the group including H, –Me, –phenyl, or together R12 and R13 can form a cyclopropane, cyclobutane, cyclopentane, or cyclohexane; when n=1, R6 is not absent; R4=R5=H, F; R1 is absent or selected from the group including –H, –NH2, –C1–C4 alkyl, phenyl, phenyl substituted with one or several halogens, methylfuran, methylphenyl, thiophene, and 2–(morpholine–4–yl)ethyl; R2 is absent or is selected from phenyl; R3 is absent or selected from o–methoxyphenyl, p–trifluoromethylphenyl, benzyl, or pyridyl; R6, R7 and R8 are defined in the claim of the invention, R9=R10 = –Me, –Et; R11 is selected from the group containing –H, –Cl and –CH3, provided that when pentachlorocyclohexane core constitutes 1,3,4-oxadiazol, R6 is not naphthyl in compounds by the formula (I). The invention also relates to a pharmaceutical composition for treating HDAC6-mediated diseases based on the described compounds.

(I)

(II)

EFFECT: production of new compounds and a pharmaceutical composition based thereon, exhibiting high selective inhibitory activity against the histone deacetylase 6 enzyme (HDAC6), applicable in medicine for treating multiple myeloma, breast cancer, and colon cancer.

8 cl, 5 dwg, 15 tbl, 27 ex

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RU 2 764 718 C2

Authors

Vergani, Barbara

Caprini, Gianluca

Fossati, Gianluca

Lattanzio, Maria

Marchini, Mattia

Pavich, Gianfranco

Pezzuto, Marcello

Ripamonti, Chiara

Sandrone, Giovanni

Steinkuhler, Christian

Stevenazzi, Andrea

Dates

2022-01-19Published

2018-04-12Filed