NOVEL VINYLOGENIC ACID DERIVATIVES
FIELD: chemistry. ^ SUBSTANCE: invention relates to novel compounds of formula (I) ^ , where A denotes -CH2-, -O- or -NR'-, in which R' denotes hydrogen or C1-6alkyl, or R' and R4 form C2-5alkylene; R1 denotes hydrogen, amine group, C1-6alkyl, hydroxy group, -NR'R", (C0-6alk...
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Zusammenfassung: | FIELD: chemistry. ^ SUBSTANCE: invention relates to novel compounds of formula (I) ^ , where A denotes -CH2-, -O- or -NR'-, in which R' denotes hydrogen or C1-6alkyl, or R' and R4 form C2-5alkylene; R1 denotes hydrogen, amine group, C1-6alkyl, hydroxy group, -NR'R", (C0-6alkylene)-NR'R", where R' and R" are independently selected from a group comprising hydrogen, C1-6alkyl, heteroalkyl, formyl, C1-6alkylcarbonyl, arylcarbonyl optionally substituted with halogenalkyl, C1-6alkylsulphonyl, arylsulphonyl or -(C0-6alkylene)-OR', where R' denotes hydrogen, C1-6alkyl, formyl or C1-6alkylcarbonyl; R2 , R2 and R2 independently denote hydrogen, halogen, C1-6alkyl or C1-6alkoxy group; R3 denotes hydrogen, C1-6alkyl, aryl-C1-6alkyl, aryl optionally substituted with halogen, or heteroaryl, where the heteroaryl is a monocyclic or bicyclic ring containing 5-6 ring atoms and at least one aromatic ring containing one or three ring heteroatoms selected fron N, O and S, where the remaining ring atoms are carbon atoms, and the bonding site of the heteroaryl radical must be on the aromatic ring; R4 denotes hydrogen, C1-6alkyl, aryl, C3-7cycloalkyl-C1-6alkyl, aryl-C1-6alkyl; R5 denotes hydrogen or C1-6alkyl; or R4 and R5 together with the carbon atom to which they are bonded, form an optionally substituted C3-7cycloalkyl ring; R6 denotes hydrogen or C1-6alkyl; and pharmaceutically acceptable salts thereof, where the term "aryl" denotes phenyl or naphthyl. The invention also relates to a pharmaceutical composition based on compounds of formula I and having a inhibitory activity towards chymase. ^ EFFECT: novel compounds which can inhibit chymase are obtained and can be used as medicinal agents. ^ 22 cl, 79 ex, 1 tbl
Изобретение относится к новым соединениям формулы (I) ! где А обозначает -СН2-, -О- или -NR′-, в котором R′ обозначает водород или C1-6алкил или R′ и R4 образуют С2-5алкилен; R1 обозначает водород, аминогруппу, C1-6алкил, гидроксигруппу, -NR′R′′, (С0-6алкилен)-NR′R′′, где R′ и R′′ независимо выбраны из группы, включающей водород, С1-6алкил, гетероалкил, формил, C1-6алкилкарбонил, арилкарбонил, необязательно замещенный галогеналкилом, C1-6алкилсульфонил, арилсульфонил или -(С0-6алкилен)-OR′, где R′ обозначает водород, C1-6алкил, формил или C1-6алкилкарбонил; R2, R2′ и R2′′ независимо обозначают водород, галоген, C1-6алкил или С1-6алкоксигруппу; R3 обозначает водород, C1-6алкил, арил-С1-6алкил, арил, необязательно замещенный галогеном, или гетероарил, где "гетероарил" |
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