FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to 6-substituted isoquinoline and isoquinolinone derivatives of formula or to its stereoisomer and/or tautomer forms and/or a pharmaceutically acceptable salt, wherein R1 represents H, OH or NH2; R3 represents H; R4 represents H, a halogen atom, CN or (C1-C6)alkylene-(C6-C10)aryl; R5 represents H, a halogen atom, (C1-C6)alkyl; R7 represents H, a halogen atom, (C1-C6)alkyl, O-(C1-C6)alkyl; R8 represents H; R9 and R6 are absent; R10 represents (C1-C6)alkyl, (C1-C8)heteroalkyl, (C3-C8)cycloalkyl, (C6)hetrocycloalkyl, (C1-C6)alkylene-(C3-C8)cycloalkyl, (C1-C6)alkylene-(C6-C10)aryl, (C1-C6)alkylene-(C6)heterocycloalkyl; R11 represents H; R12 represents (C1-C6)alkyl, (C3-C8)cycloalkyl, (C5)heteroaryl or (C6-C10)aryl; R13 and R14 independently represent H, (C1-C6)alkyl, (C1-C6)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 (C3-C8)cycloalkyl, (C6-C10)aryl; wherein in the rests, R10, R12-R14 alkyl or alkylene are unsubstituted or optionally substituted by one or more OCH3; wherein in the rests, R10, R12-R14 alkyl or alkylene are unsubstituted or optionally substituted by one or more halogen atoms; wherein (C1-C8)heteroaryl group means (C1-C8)alkyl groups, wherein at least one carbon atom is substituted by O;. (C6)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; (C5)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
Title | Year | Author | Number |
---|---|---|---|
SUBSTITUTED ISOQUINOLINES AND ISOQUINOLINONES AS Rho-KINASE INHIBITORS | 2009 |
|
RU2538588C2 |
CYCLOHEXYLAMINIZOQUINOLONE AS Rho-KINASE INHIBITORS | 2006 |
|
RU2440988C2 |
CYCLOALKYLAMINE-SUBSTITUTED ISOQUINOLONE DERIVATIVES | 2007 |
|
RU2457203C2 |
SUBSTITUTED ISOQUINOLINE AND ISOQUINOLINONE DERIVATIVES AS Rho-KINASE INHIBITORS | 2007 |
|
RU2455302C2 |
BI- AND POLYCYCLIC SUBSTITUTED ISOQUINOLINE AND ISOQUINOLINONE DERIVATIVES, USEFUL AS RHO-KINASE INHIBITORS | 2009 |
|
RU2532481C2 |
CYCLOALKYLAMINE-SUBSTITUTED ISOQUINOLINE AND ISOQUINOLINONE DERIVATIVES | 2007 |
|
RU2468011C2 |
PIPERADINYL-SUBSTITUTED ISOQUINOLONE DERIVATIVES AS Rho-KINASE INHIBITORS | 2006 |
|
RU2414467C2 |
ISOQUINOLINE DERIVATIVES AS Rho-KINASE INHIBITORS | 2006 |
|
RU2443688C2 |
SUBSTITUTED AMINOPYRIMIDINE COMPOUNDS AND METHODS OF USE | 2014 |
|
RU2683793C2 |
TRICYCLIC COMPOUNDS, PHARMACEUTICAL COMPOSITION CONTAINING THEM AND USING THEM FOR TREATING IMMUNOLOGICAL AND ONCOLOGICAL COMPOUNDS | 2009 |
|
RU2545023C9 |
Authors
Dates
2014-09-10—Published
2009-06-19—Filed