C17-, C20- AND C21-SUBSTITUTED NEUROACTIVE STEROIDS AND METHODS OF THEIR USE Russian patent published in 2024 - IPC C07J1/00 C07J7/00 C07J9/00 C07J17/00 C07J41/00 C07J43/00 A61K31/565 A61K31/567 A61K31/57 A61K31/573 A61K31/575 A61K31/58 A61P23/00 A61P25/00 

Abstract RU 2828261 C2

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula (1-A) or a pharmaceutically acceptable salt thereof, where: a) a compound of formula (1-A) is a compound of formula (1-A-1), where each RY4 is independently C1-C20 alkyl, cyano or halo; and e is either 0 or 2; or b) a compound of formula (1-A) is a compound of formula (1-A-3) wherein each RY1 is hydrogen, C1-C6 alkyl, or C6 cycloalkyl; and each RY2 is independently C1-C6 alkyl, C6 cycloalkyl, C6 heterocyclyl having 1–4 heteroatoms, where each heteroatom is selected from N, O or S, C6 aryl or C6 heteroaryl having 1–4 heteroatoms, where each heteroatom is selected from N, O or S; and b= 0 or 1; or c) a compound of formula (1-A) is a compound of formula (1-A-5) wherein each RY3 is C6 aryl or C5-C6 heteroaryl having 1–4 heteroatoms, where each heteroatom is selected from N, O or S; or two RY3 groups are joined together to form a 6-membered ring; c is 1, 2 or 3; and d is either 0, 1, or 2; and where R3 represents C1-C6 alkyl; RX is independently either hydrogen or C1-C6 alkyl, RY is independently C6 aryl, C6 cycloalkyl, or C6 heterocyclyl containing 1–4 heteroatoms, where each heteroatom is selected from N, O, or S; or RX and RY are joined together to form a 6-membered heterocyclic ring; R19 is hydrogen or C1-C6 alkyl; R 5 is hydrogen; and represents a single bond. The invention also relates to a pharmaceutical composition with the ability to inhibit the function of the GABA receptor, based on these compounds.

EFFECT: obtaining new compounds and a pharmaceutical composition based on them which can be used in medicine in the treatment of cancer.

15 cl, 2 tbl, 108 ex

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RU 2 828 261 C2

Authors

Robichaud, Albert, J.

Martinez Botella, Gabriel

Harrison, Boyd, L.

Salituro, Francesco, G.

Griffin, Andrew

Blanco-Pillado, Maria, Jesus

Dates

2024-10-08Published

2017-07-11Filed