19-NOR NEUROACTIVE STEROIDS AND METHODS OF USING THEM Russian patent published in 2019 - IPC C07J43/00 A61K31/58 A61P25/00 

Abstract RU 2700264 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof. In formula (I) is a single or double bond, as valence allows; A has formula (A-1) or formula (A-2), where attachment point is in G1 or G2 in formula (A-1) and attachment point is in G2 or G3 in formula (A-2); G1 is N, NRN1 or CRG1, as valence allows; G2 is N or -C=N-, as valence allows; G3 is N or CRG3, as valence allows; G4 is N or CRG4, as valence allows; G5 is N or CRG5, as valence allows; G6 is N or CRG6, as valence allows; and G7 is N or CRG7, as valence allows; in each case RG1, RG2, RG3, RG4, RG5, RG6 and RG7 independently represents hydrogen, halogen, -CN, -ORGA or unsubstituted C1-6 alkyl; in each case RN1 is unsubstituted C1-6 alkyl; in each case RGA independently represents hydrogen, C1-6 alkyl substituted with fluorine or unsubstituted C1-6 alkyl; R1 is C1-6 alkyl substituted with fluorine, methoxy or ethoxy, or unsubstituted C1-6 alkyl; R2 is hydrogen; R3a is hydrogen and R3b is hydrogen; each R4a or R4b independently represents hydrogen; provided that if the bond p is a double bond, then the bond q is a single bond, provided that if the bond q is a double bond, then the bond p is a single bond and R4b is absent; and provided that both bonds q and p are single bonds, hydrogen in C5 is in alpha or beta configuration. Invention also refers to pharmaceutical salts of compounds, to a pharmaceutical composition, to individual compounds and their pharmaceutically acceptable salts.

, (A-1), (A-2).

EFFECT: obtaining novel compounds of formula (I), having the GABA modulator property.

21 cl, 13 dwg, 3 tbl, 95 ex

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RU 2 700 264 C2

Authors

Botella, Gabriel Martinez

Kharrison, Bojd L.

Robisho, Alber, Zhan

Salituro, Franchesko Dzh.

Berezis, Richard Tomas

Dates

2019-09-16Published

2014-04-17Filed