FIELD: pharmaceutical chemistry. SUBSTANCE: invention relates to new phosphinic acid esters having general formula I: (I), wherein X is halogen, C1-C4-alkyl, or di-C1-C4-alkylamino group; h=0-3; Y halogen or di- C1-C4-alkylamino group; n'= 1-4; R1 and R2 are hydrogen atoms or, together, =NOH group; R3 and R4, independently, hydrogen, optionally substituted C1-C4-alkoxy group, 2,2,2-trichloro-1-hydroxyethyl, acetyl, or, together, =CHR″′ or =CH-CH=CHR″′ where R″′ is C1-C4-alkyl or phenyl optionally substituted by OH, COOH or nitro groups, and to their physiologically acceptable salts. Compounds I are prepared by interaction of hydrazine with phosphorylacetic acid ester. Compounds I exhibit high neotropical and antidepressive activity. Invention also relates to pharmaceutical composition exhibiting neotropical and antidepressive activity and containing, as active principle, compound I in effective amount. Therapeutically active dose of compound I is used for correction of metabolic processes in brain. EFFECT: expanded possibilities in correction of brain activity. 19 cl, 4 dwg, 13 tbl, 14 ex
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Authors
Dates
1999-11-27—Published
1994-01-11—Filed