FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to substituted isoquinolines and isoquinolinones of formula 
(I) and to their stereoisomer and/or tautomer forms and/or pharmaceutically acceptable salts, wherein R1 is H, OH or NH2; R3 is H; R4 is H, halogen or (C1-C6)alkylene-R'; R5 is H, halogen, (C1-C6)alkyl; R7 is H, halogen, (C1-C6)alkyl, O-(C1-C6)alkyl; R8 is H; R6 is absent; or is one of (C1-C4)alkylene related to a cycloalkyl ring related to a cycloalkyl ring, wherein (C1-C4)alkylene forms a second bond to another carbon atom of the cycloalkyl ring to form a bicyclic ring system, R10 is H, phenyl, or pyridine, wherein phenyl is unsubstituted or substituted; R11 is H, (C1-C6)alkyl; or R11 and R12 together with the carbon atom to which they are attached form (C3)cycloalkyl; R12 is (C1-C6)alkyl, (C3-C8)cycloalkyl or phenyl; or R12 is H, provided r=2 and another R12 is other than H; or R11 and R12 together with the carbon atom to which they are attached form (C3)cycloalkyl; R13 and R14 are independently H, (C1-C6)alkyl, (C1-C6)alkylene-R', C(O)O-(C1-C6)alkyl, n is equal to 0; m is equal to 1 or 2; s is equal to 1 or 2; r is equal to 1 or 2; L is O, NH; R' is (C3-C8)cycloalkyl, (C6-C10)aryl; wherein in R11 and R12 residues, alkyl is unsubstituted or optionally substituted by one OCH3; wherein in R11 and R12 residues, alkyl is unsubstituted or optionally substituted by one or more halogens; wherein in R10 and R12 residues, (C6-C10)aryl is unsubstituted or optionally substituted by one or two groups optionally specified in halogen, CN, (C1-C6)alkyl, O-(C1-C6)alkyl, SO2-(C1-C6)alkyl, CF3 and OCF3. Also, the invention refers to using a compound of formula (I).
EFFECT: there are prepared new isoquinoline and isoquinolinone derivatives effective in treating and preventing the diseases related to Rho-kinase inhibition.
38 cl, 132 ex
| Title | Year | Author | Number |
|---|---|---|---|
| 6-SUBSTITUTED ISOQUINOLINES AND ISOQUINOLINONES EFFECTIVE AS Rho-KINASE INHIBITORS | 2009 |
|
RU2528229C2 |
| CYCLOALKYLAMINE-SUBSTITUTED ISOQUINOLINE AND ISOQUINOLINONE DERIVATIVES | 2007 |
|
RU2468011C2 |
| CYCLOALKYLAMINE-SUBSTITUTED ISOQUINOLONE DERIVATIVES | 2007 |
|
RU2457203C2 |
| CYCLOHEXYLAMINIZOQUINOLONE AS Rho-KINASE INHIBITORS | 2006 |
|
RU2440988C2 |
| 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 |
| 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 |
|
RU2675105C9 |
| SUBSTITUTED AMINOPYRIMIDINE COMPOUNDS AND METHODS OF USE | 2014 |
|
RU2683793C2 |
