ACETAMIDE DERIVATIVES (VARIANTS), METHOD OF PREPARATION THEREOF (VARIANTS), PHARMACEUTICAL COMPOSITION AND AGENT Russian patent published in 2000 - IPC

Abstract RU 2160256 C2

FIELD: pharmaceutical industry, medicine. SUBSTANCE: described are new acetamide derivatives of formula I: wherein X is -O- or -NR4; R1 is hydrogen atom, lower alkyl group, lower alkenyl group or cycloalkyl lower alkyl group; R2 is lower alkyl group; C3-C7-cycloalkyl group; phenyl group; phenyl group substituted by halogen atom or lower alkoxy group; or phenyl lower alkyl group; or optionally R1 and R2 together with nitrogen atom to which they are attached from group of formula (a): wherein A is single bond, -CH2- or NH-; Ra and Rb are identical or different and each is hydrogen atom or lower alkyl group; or when A is single bond, and Ra and Rb are in position 2 and in position 3, carbon atoms in position2 and in position 3, and Ra and Ri are optionally combined to form phenyl ring; R3 is hydrogen atom, lower alkyl group or hydroxylower alkyl group; R4 is hydrogen atom or lower alkyl group or R3 and R4 are optionally combined with carbon atom and nitrogen atom to which they are attached to form pyrrolidine, piperidine or 2,3-dihydro-1H-indole ring; R5 is hydrogen atom, lower alkyl group, hydroxylower alkyl group, halogen atom, amino group, lower alkanoylamino group, nitro group; or lower alkoxycarbonyl group; R6 is hydrogen atom, lower alkyl group, trifluoromethyl group or phenyl group, or R5 and R6 are optionally combined to from (CH2)n (n is 3,4,5, or 6); R7 is hydrogen atoms, halogen atom, lower alkyl group, lower alkoxy group, trifluoromethyl group, amino group or nitro group; R8 is hydrogen atom or halogen atom; or pharmaceutically acceptable acid addition salt thereof. Said compound have selected effect on BZω3 which is peripheral type receptor and show high pharmacological activity. They are therefore useful for prophylaxis or treatment of central nervous system diseases such as diseases associated with symptoms of anxiety and also depression, epilepsy or the like. Also described are methods of preparing compounds of formula I and pharmaceutical composition and agent based thereof. EFFECT: improved properties of the title compounds. 18 cl, 21 tbl

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RU 2 160 256 C2

Authors

Teruja Murata

Kehtsukhiko Khino

Kiesi Furukava

Makoto Oka

Mari Itokh

Dates

2000-12-10Published

1996-04-10Filed