| 摘要 |
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 Ris H, OH or NH; Ris H; Ris H, halogen or (C-C)alkylene-R'; Ris H, halogen, (C-C)alkyl; Ris H, halogen, (C-C)alkyl, O-(C-C)alkyl; Ris H; Ris absent; or is one of (C-C)alkylene related to a cycloalkyl ring related to a cycloalkyl ring, wherein (C-C)alkylene forms a second bond to another carbon atom of the cycloalkyl ring to form a bicyclic ring system, Ris H, phenyl, or pyridine, wherein phenyl is unsubstituted or substituted; Ris H, (C-C)alkyl; or Rand Rtogether with the carbon atom to which they are attached form (C)cycloalkyl; Ris (C-C)alkyl, (C-C)cycloalkyl or phenyl; or Ris H, provided r=2 and another Ris other than H; or Rand Rtogether with the carbon atom to which they are attached form (C)cycloalkyl; Rand Rare independently H, (C-C)alkyl, (C-C)alkylene-R', C(O)O-(C-C)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 (C-C)cycloalkyl, (C-C)aryl; wherein in Rand Rresidues, alkyl is unsubstituted or optionally substituted by one OCH; wherein in Rand Rresidues, alkyl is unsubstituted or optionally substituted by one or more halogens; wherein in Rand Rresidues, (C-C)aryl is unsubstituted or optionally substituted by one or two groups optionally specified in halogen, CN, (C-C)alkyl, O-(C-C)alkyl, SO-(C-C)alkyl, CFand OCF. 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 |
