| 摘要 |
The invention relates to (indol-3-yl)-heterocycle derivatives having general Formula (I) wherein A represents a 5-membered aromatic heterocyclic ring, wherein XXand Xare independently selected from N, O, S and CR; R is H or (С)alkyl; or R, when present in Xor X, may form together with Ra 5-8 membered ring; Ris a 5-8 membered saturated carbocyclic ring, optionally containing a heteroatom selected from О and S; Ris H, CHor CH-CHor Ris joined together with Rto form a 6-membered ring, optionally containing a heteroatom selected from О and S, and which heteroatom is bonded to the 7-position of the indole ring; Rand Rare independently H, (С)аlкуl or (C)cycloalkyl, the alkyl groups being optionally substituted with OH, (С)alkyloxy, (С)alkylthio, (С)alkylsulfonyl, CN or halogen; or Rtogether with Rand the N to which they are bonded form a 4-8 membered ring optionally containing a further heteroatom selected from О and S, and which is optionally substituted with OH, (С)alkyl, (С)alkyloxy, (С)alkyloxy-(С)alkyl, or halogen; or Rtogether with Rforms a 4-8 membered ring optionally containing a further heteroatom selected from О and S, and which is optionally substituted with OH, (С)alkyl, (С)alkyloxy, (С)alkyloxy-(С)alkyl, or halogen; or Rtogether with R, when present in Xor X, forms a 5-8 membered ring; Ris H or (С)alkyl; or Rtogether with Rforms a 4-8 membered ring optionally containing a further heteroatom selected from О and S, and which is optionally substituted with OH, (С)alkyl, (С)alkyloxy, (С)alkyloxy-(С)alkyl, or halogen; R' is H or (С)alkyl; Rrepresents 1-3 substituents independently selected from H, (С)alkyl, (С)alkyloxy, CN and halogen; Ris H, (С)аlкуl, (С)alkyloxy, CN or halogen; or Ris joined together with Rto form a 6-membered ring, optionally containing a further heteroatom selected from О and S, and which heteroatom is bonded to the 7-position of the indole ring; or a pharmaceutically acceptable salt thereof, as agonists of the cannabinoid CB1 receptor, which can be used in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer pain and pain and spasticity associated with multiple sclerosis. |
