| 摘要 |
FIELD: chemistry.SUBSTANCE: invention relates to bi- and polycyclic substituted isoquinoline and isoquinolinones of formula (I), or to its stereoisomeric and/or tautomeric forms and/or to its pharmaceutically acceptable salts, where Rrepresents OH; R, R, Rand Rrepresents H; Rrepresents halogen or (C-C) alkyl; Rrepresents one (C-C)alkylene, bound to a cycloalkyl ring, in which (C-C)alkylene forms the second bond with the other carbon atom of the cycloalkyl ring with the formation of a bicyclic ring system, where in the bicyclic ring system one carbon atom is substituted with a group, independently selected from O, S or SO; and if m and s equal 2 or m equals 3 and s equals 1, Rrepresents a group CH-CH-(CH), which via one group CHis bound to the cycloalkyl ring, and two other CHgroups are bound to different carbon atoms of the cycloalkyl ring, and if m equals 3 and s equals 3, Rrepresents two methylene groups, bound to different carbon atoms of the cycloalkyl ring, where the methylene groups or group CH-CH-(CH)are bound to the carbon atoms of the cycloalkyl ring and form an adamantane system of formula (XX), where L can be bound to any secondary or tertiary carbon atom, or Rtogether with Rand an N atom form (C) heterocycloalkyl, bound with the cycloalkyl residue in the form of a spirocyclic ring system, where the bicyclic ring system, or the adamantane system, or a ring system, containing (C) heterocycloalkyl, represent non-substituted or optionally substituted with substituent R; Rrepresents (C-C)alkyl, (C-C)alkenyl, (C)aryl or cyclopropyl Rand Rindependently on each other represent H or (C-C)alkylene-(C)aryl; n equals 0 or 1; m equals 2 or 3; s equals 1, 2 or 3; L represents O; its stereoisomeric and/or tautomeric forms and/or its pharmaceutically acceptable salts. The invention also relates to the application of a formula (I)compound.EFFECT: novel bi- and polycyclic isoquinoline and isoquinolinone derivatives, useful as inhibitors of Rho-kinase, are obtained.22 cl, 22 ex |
