NEUROACTIVE STEROIDS, COMPOSITIONS AND USE THEREOF Russian patent published in 2019 - IPC C07J7/00 C07J43/00 A61K31/57 A61K31/58 A61P25/00 A61P25/08 A61P25/18 A61P25/20 A61P25/24 

Abstract RU 2699359 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I), in which A is selected from a group , , , and ; R1 is -CH3, -CH2F, -CHF2, -CH2CH3, -CH2OCH3 or -CH2OCH2CH3; R2 and R3 is selected independently from -H, halogen, -CH3, -OCH3 or -OCH2CH3; R4 is -CF3, cyano, -CH3, -C(O)ORa or -C(O)NRbRc; Ra is -H, or (C1-C2)alkyl; each Rb and Rc is independently H; and n is integer from 0 to 1; or when A is (A-3) or (A-5), R1 is-CH3, -CH2F, -CH2OCN3 or -CHF2, and n is equal to 0, then at least one of R2 and R3 is not H. Invention also relates to individual compounds, to a pharmaceutical composition, to a method of treating a CNS related disorder associated with GABA function, to a method of treating a seizure, to a method of treating epilepsy, to a method of treating epileptic status.

H(I).

EFFECT: technical result is obtaining novel compounds of formula (I), having properties of modulator GABAA, which can be useful in treating a CNS related disorder.

32 cl, 71 ex, 4 tbl, 22 dwg

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RU 2 699 359 C2

Authors

Botella, Gabriel Martinez

Harrison, Boyd L.

Robichaud, Albert Jean

Salituro, Francesco G.

Beresis, Richard Thomas

Dates

2019-09-05Published

2015-05-29Filed