COMPOSITION OF TETRAHYDROQUINOLINES AS BROMODOMAIN BET MODIFYING AGENTS Russian patent published in 2020 - IPC C07D215/20 C07D401/04 C07D401/12 C07D401/14 C07D471/04 A61K31/47 A61K31/4709 A61P35/00 

FIELD: organic chemistry.

SUBSTANCE: invention relates to a heterocyclic compound of formula (IV) or a pharmaceutically acceptable salt thereof, wherein R⁴ represents -O(CH₂)_nR^d; R⁸ denotes C₁-C₆ alkyl, C₃-cycloalkyl or -O-C₁-C₆ alkyl; each R^a and R^b independently represent hydrogen or C₁-C₆ alkyl; each R^c independently represents -(CH₂)_nR^a, -(CH₂)_nOR^a, -C(O)OR^a, -C(O)NR^aR^b, -S(O)₂R^a, -S(O)₂NR^aR^b, C₁-C₆ haloalkyl, C₃-C₄ cycloalkyl, 4-, 5-, 6- or 8-member heterocycloalkyl containing 1 to 2 heteroatoms selected from a group consisting of O, N and S, halogen, cyano or oxo, wherein heterocycloalkyl is unsubstituted or substituted with one or two R^e; R^d is C₁-C₆ alkyl, C₃-C₆ cycloalkyl, 4–6-membered heterocycloalkyl comprising 1, 2 hetero atoms selected from the group consisting of O, N and S, C₆-aryl or 5-, 6-, 9- or 10-membered heteroaryl comprising 1, 2, 4 heteroatom selected from a group consisting of O, N and S, wherein said alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl are optionally substituted with 1–3 substitutes independently selected from R^a, R^b and R^c; each R^e is independently halogen, -OH, C₁-C₆ alkyl, oxo, C₁-C₆ alkoxy or -S(O)₂(C₁-C₆ alkyl); and n is equal to 0, 1 or 2. Invention also relates to a pharmaceutical composition based on the compound of formula (IV).

EFFECT: novel tetrahydroquinoline derivatives which are useful in inhibiting one or more BET bromodomains are obtained.

30 cl, 10 tbl, 120 ex