HALOALLYLAMINE SULFONE DERIVATIVE AS LYSILOXIDASE INHIBITORS AND THEIR USE Russian patent published in 2023 - IPC C07C311/29 C07C317/28 C07C317/32 C07D209/08 C07D209/10 C07D213/71 C07D215/36 C07D277/64 C07C317/44 A61K31/145 A61K31/166 A61K31/18 A61K31/4402 A61K31/4409 A61K31/47 A61P11/00 A61P13/12 A61P17/02 A61P35/00 A61P9/00 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to novel compounds capable of inhibiting certain amine oxidase enzymes. The invention relates to a compound — the Z-isomer of formula I, its pharmaceutically acceptable salt or hydrate, which have inhibitory activity against lysyl oxidases LOX, LOXL1, LOXL2, LOXL3 and LOXL4. In this formula, A is C_6-10aryl or 5–10-membered heteroaryl, in which 1–2 ring atoms are heteroatoms independently selected from N and S; each R¹ is independently selected from the group consisting of X-R², halogen, deuterium, C_1-6alkyl, O-C_1-6alkyl, C_6-10aryl, -C(O)NR⁴R⁵ and -S(O)₂R⁶ where each C_1-6alkyl and C_6-10aryl is optionally substituted with one or more halogens; X is selected from the group consisting of O, OCH₂ and CONH; R² is selected from the group consisting of C_3-10cycloalkyl and C_6-10aryl, where each R² is optionally substituted with one or more R⁷; R⁴ and R⁵ are independently selected from the group consisting of hydrogen and C_1-6alkyl; R⁶ is C_1-6alkyl; R⁷ is -S(O)₂NR⁴R⁵; and n is either 0, 1, 2, 3, 4, 5, or 6. The invention also relates to a pharmaceutical composition for inhibiting the amine oxidase activity of any of LOX, LOXL1, LOXL2, LOXL3 and LOXL4, containing a compound of general formula I, its use for inhibiting the above amine oxidase activity, treating a condition associated with any of the LOX, LOXL1, LOXL2 proteins, LOXL3 and LOXL4, and for the manufacture of a medicinal product for the treatment of this condition.

EFFECT: using haloallylamine sulfone derivative as lysiloxidase inhibitors.

20 cl, 11 dwg, 8 tbl, 38 ex