6-SUBSTITUTED ISOQUINOLINES AND ISOQUINOLINONES EFFECTIVE AS Rho-KINASE INHIBITORS

FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to 6-substituted isoquinoline and isoquinolinone derivatives of formulaor to its stereoisomer and/or tautomer forms and/or a pharmaceutically acceptable salt, wherein Rrepresents H, OH or NH; Rrepresents H; Rrepresents H, a halogen atom, CN...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: KLEEMANN KHAJNTS-VERNER, PLETTENBURG OLIVER, VESTON DZHON, LORENTS KATRIN, LEN MATTIAS
Format: Patent
Sprache:eng ; rus
Schlagworte:
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to 6-substituted isoquinoline and isoquinolinone derivatives of formulaor to its stereoisomer and/or tautomer forms and/or a pharmaceutically acceptable salt, wherein Rrepresents H, OH or NH; Rrepresents H; Rrepresents H, a halogen atom, CN or (C-C)alkylene-(C-C)aryl; Rrepresents H, a halogen atom, (C-C)alkyl; Rrepresents H, a halogen atom, (C-C)alkyl, O-(C-C)alkyl; Rrepresents H; Rand Rare absent; Rrepresents (C-C)alkyl, (C-C)heteroalkyl, (C-C)cycloalkyl, (C)hetrocycloalkyl, (C-C)alkylene-(C-C)cycloalkyl, (C-C)alkylene-(C-C)aryl, (C-C)alkylene-(C)heterocycloalkyl; Rrepresents H; Rrepresents (C-C)alkyl, (C-C)cycloalkyl, (C)heteroaryl or (C-C)aryl; Rand Rindependently represent H, (C-C)alkyl, (C-C)alkylene-R'; n is equal to 0; m is equal to 2 or 3; s is equal to 1 or 2; r is equal to 1; L represents O or NH; R' represents (C-C)cycloalkyl, (C-C)aryl; wherein in the rests, R, R-Ralkyl or alkylene are unsubstituted or optionally substituted by one or more OCH; wherein in the rests, R, R-Ralkyl or alkylene are unsubstituted or optionally substituted by one or more halogen atoms; wherein (C-C)heteroaryl group means (C-C)alkyl groups, wherein at least one carbon atom is substituted by O;. (C)heterocycloalkyl group means a monocyclic carbon ring system containing 6 ring atoms wherein one carbon atom can be substituted by 1 oxygen atom or 1 sulphur atom which can be optionally oxidated; (C)heteroaryl means a monoring system wherein one or more carbon atoms can be substituted by 1 nitrogen atom or 1 sulphur atom or a combination of various heteroatoms. Also, the invention refers to using the compound of formula (I) and to a therapeutic agent based on the compound of formula (I).EFFECT: there are prepared new compounds effective for treating and/or preventing diseases associated with Rho-kinase and/or mediated by Rho-kinase by phosphorylation of myosin light chain phosphatase, and the compositions containing these compounds.32 cl, 111 ex Изобретение относится к 6-замещенным изохинолиновым и изохинолиноновым производным формулы (I) или к его стереоизомерным и/или таутомерным формам и/или к их фармацевтически приемлемой соли, где Rпредставляет собой Н, ОН или NH; Rпредставляет собой Н; Rпредставляет собой Н, атом галогена, CN или (C-C)алкилен-(С-С)арил; Rпредставляет собой H, атом галогена, (C-C)алкил; Rпредставляет собой Н, атом галогена, (C-C)алкил, О-(C-C)алкил; Rпредставляет собой Н; Rи Rотсутствует; Rпредс