NOVEL ISOQUINOLINE DERIVATIVES, PROCESS OF THEIR PREPARATION AND PHARMACEUTICALS COMPRISING THEM

• Main Authors: KISS ILLONA DR, BENCZE ZSOLT, HERMECZ ISTVAN DR, VERTESI CSABA DR, DEBRECZENI LORAND DR, GAAL JOZSEF DR, KAPUI ZOLTAN, PAP MARIA H, SZEREDY JUDIT DR, TAKACS KALMAN DR, ORI JANOS, KORMOCZY PETER SZEKELY DR, SZABO MARIA
• Format: Patent
• Language: Czech; English
• Published: 17.04.1996
• Edition: 6
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Řešení spočívá v nových isochinolinových derivátech obecného vzorce I, v němž R znamená atom vodíku nebo alkoxyskupinu o 1 až 6 atomech uhlíku, R.sup.1 .n.znamená atom vodíku nebo alkyl o 1 až 6 atomech uhlíku, R.sup.2 .n.znamená alkyl o 1 až 6 atomech uhlíku, R.sup.3 .n.znamená atom vodíku, alkyl o 1 až 6 atomech uhlíku, popřípadě substituovaný jednou nebo dvěma alkoxyskupinami řetězcem o 1 až 4 atomech uhlíku nebo znamená cykloalkyl o 4 až 7 atomech uhlíku, R.sup.4 .n.znamená atom vodíku nebo alkyl o 1 až 6 atomech uhlíku, popřípadě substituovaný jednou nebo dvěma hydroxylovými skupinami a/nebo jednou nebo dvěma alkoxyskupinami řetězcem o 1 až 4 atomech uhlíku nebo znamená cykloalkyl o 4 až 7 atomech uhlíku nebo R.sup.3 .n.a R.sup.4 .n.tvoří spolu s atomem dusíku, na nějž jsou vázány čtyřčlenný až osmičlenný cyklický zbytek obecného vzorce a, popřípadě substituovaný jednou nebo dvěma alkoxyskupinami o 1 až 4 atomech uhlíku a/nebo jednou nebo dvěma alkylovými skupiŕ The invention relates to novel compounds of the general formula (I), wherein R means hydrogen or a straight or branched chain C1-6alkoxy group; R stands for hydrogen or a straight or branched chain C1-6alkyl group; R represents hydrogen or a straight or branched chain C1-6alkyl group: R means hydrogen: a straight or branched chain C1-6alkyl group optionally substituted by one or two hydroxyl and/or one or two straight or branched chain C1-4alkoxy group(s): or a C4-7cycloalkyl group; R stands for hydrogen or a straight or branched chain C1-6alkyl group optionally substituted by one or two hydroxyl and/or one or two straight or branched chain C1-4alkoxy group(s): or a C4-7cycloalkyl group; or R and R together with the nitrogen atom, to which they are attached form a 4 to 8-membered cyclic group of formula optionally substituted by one or two straight or branched chain C1-4alkoxy and/or one or two straight or branched chain C1-4alkyl group(s), where optionally an oxygen or sulfur atom or an N-R group may be substituted for a ring carbon atom, where R means hydrogen or a straight or branched chain C1-6 aliphatic alkyl group, the 4- to 8-membered cycle optionally being condensed with a benzene ring; R stands for hydrogen or a C1-10acyl group and the salts and hydrates thereof as well as pharmaceutical compositions containing these compounds. The compounds of the invention antagonize the effects of constrictive mediators, e.g. histamine, acetylcholine or serotonin; they show an antiallergic action and possess an antiinflammatory effect. Thus, these compounds can therapeutically be used as bronchodilators as well as antiallergic or antiinflammatory drugs, particularly in the treatment of bronchial asthma.