19-NOR C3, 3-DISUBSTITUTED C21-N-PYRAZOLYL STEROIDS AND METHODS OF USE THEREOF Russian patent published in 2018 - IPC C07J7/00 C07J43/00 A61K31/58 A61P25/00 

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; R¹ is C_1-6 alkyl optionally substituted with C_1-6 alkoxy or one to two halogen groups; R² is hydrogen, unsubstituted C_1-6 alkyl or -OR^A2, where R^A2 is an unsubstituted C_1-6 alkyl; R^3a is hydrogen and R^3b is hydrogen; each of R^4a and R^4b in each case independently represent hydrogen or halogen, provided that if between C₅ and C₆ is a simple bond, then hydrogen in position C₅ and substituent R^4a, each independently, is represented in an alpha or beta configuration, and R^4b is absent; each of R⁵, R⁶ and R⁷ in each case independently represent hydrogen, halogen, -NO₂, -CN, -C(=O)R^GA, -C(=O)OR^GA, -SR^GA, -S(=O)R^GA, -S(=O)₂R^GA, -S(=O)₂OR^GA or C_1-6 alkyl, optionally substituted with halogen; R^GA in each case independently represents unsubstituted C_1-6 alkyl; and where at least one of R⁵, R⁶ and R⁷ independently represents halogen, -NO₂, -CN, -C(=O)R^GA, -C(=O)OR^GA, -SR^GA, -S(O)R^GA, -S(=O)₂R^GA, -S(=O)₂OR^GA or C_1-6 alkyl, optionally substituted with halogen, where R^GA is an unsubstituted C_1-2 alkyl. Invention also relates to pharmaceutical compositions and to individual compounds.

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EFFECT: technical result: novel compounds of formula (I) having properties of a GABA modulator.

46 cl, 52 dwg, 5 tbl, 71 ex