REGULATORS-DERIVATIVES OF STEROIDS, METHODS OF THEIR OBTAINING AND THEIR USE Russian patent published in 2023 - IPC C07J3/00 C07J5/00 C07J7/00 C07J17/00 C07J43/00 A61K31/573 A61K31/58 A61P25/00 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula (IV), its stereoisomer or a pharmaceutically acceptable salt thereof, and its use for the preparation of a medicinal product that activates the GABA_A receptor, as well as for the treatment of a disease associated with the central nervous system (CNS) selected from the following group: sleep disorder, mood disorder, schizophrenia spectrum disorder, spasmodic disorder, memory disorder and/or cognitive disorder, dyskinesia, personality disorder, autism spectrum disorder, pain, traumatic brain injury, vascular disease, substance abuse disorder, and/or withdrawal syndrome and tinnitus. In the general formula (IV), Z is selected from the group consisting of -CH₂- and -CH₂NH-; ring A is selected from the group consisting of a 3–8 membered heterocyclyl containing one or two heteroatoms selected from N and S, phenyl and a 5–10 membered heteroaryl containing one to four heteroatoms selected from N, where each of 3–8 membered heterocyclyl, phenyl and 5–10 membered heteroaryl optionally further substituted with one or more substituents selected from the group consisting of C_1-3 alkyl, C_1-3 haloalkyl, halogen, oxo, nitro, cyano, methoxy, cyclopropyl, -(CH₂)_n1SR₂₅, -(CH₂)_n1C(O)R₂₅ and -(CH₂)_n1C(O)OR₂₅; each R^a is the same or different and each is selected from the group consisting of hydrogen atom, C_1-3 alkyl, C_1-3 haloalkyl, methoxy, halogen, nitro, cyano, cyclopropyl, -(CH₂)_n1C(O)R₂₃, -(CH₂)_n1C(O)OR₂₃, -(CH₂)_n1S(O)_m1R₂₃ and -(CH₂)_n1 S(O)(NR₂₃)R₂₄, where each of C_1-3 alkyl and cyclopropyl is optionally further substituted with one or more substituents selected from the group consisting of cyano and hydroxy; R_15a is selected from the group consisting of C_1-3 alkyl, C_1-3 haloalkyl, halogen, cyclopropyl, -(CH₂)_n1OR₂₃ and -(CH₂)_n1SR₂₃; R_16a represents a hydrogen atom; or R_15a and R_16a may form cyclopropyl, where cyclopropyl is optionally further substituted with one or more halogens; x is an integer equal to either 0, 1, or 3. The remaining values of the variables are indicated in the claims.

EFFECT: creation of new GABA_A regulators with good activity and excellent metabolism in vivo.

12 cl, 3 tbl, 179 ex