| abstract |
FIELD: organic chemistry, chemical technology, biochemistry, medicine, pharmacy. n SUBSTANCE: invention relates to new derivatives of propene carboxylic acid amidooximes of the formula (I): n wherein R means phenyl that is substituted optionally with 1-3 substitutes wherein substitute means (C 1 -C 2 )-alkyl or (C 1 -C 2 )-alkoxy-group; R' means hydrogen atom (H); R 4 and R 5 mean independently of one another H, (C 1 -C 5 )-alkyl, phenyl that is substituted optionally with 1-3 substitutes wherein substitute means (C 1 -C 2 )-alkyl or (C 1 -C 2 )-alkoxy-group; or R 4 and R 5 in common with adjacent nitrogen atom form 5- or 6-membered saturated or unsaturated heterocyclic group that can comprise additional nitrogen atom or oxygen atom as a heteroatom and it can be condensed with benzene ring, and heterocyclic group and/or benzene ring can comprise one or two substitutes wherein substitute means (C 1 -C 2 )-alkyl or (C 1 -C 2 )-alkoxy-group; R 1 and R 2 mean H; R 3 means H, OH; or R 1 in common with R 2 forms carbonyl group wherein carbon atom is joined with oxygen atom adjacent with R 1 and with nitrogen atom adjacent with R 2 ; R 3 means H, OH; or R 2 means H; and R 1 in common with R 3 form a valence bond between oxygen atom adjacent with R 1 and carbon atom adjacent with R 3 ; and its geometric isomers and/or optical isomers, and/or its pharmaceutically acceptable acid-additive salts. Compounds of the formula (I) inhibit activity of poly(adenisone diphosphate ribose) polymerase and can be used in pharmaceutical composition in treatment of states based on inhibition of this enzyme activity, and in treatment of states associated with oxygen insufficiency of heart and brain. Also, invention describes methods for preparing compounds of the formula (I). n EFFECT: improved preparing method, valuable medicinal properties of compounds and compositions. n 9 cl, 1 tbl, 41 ex |