Invention Grant
US07772227B2 Tricyclic 1-[(indol-3-yl)carbonyl]piperazine derivatives as cannabinoid CB1 receptor agonists 有权
三环1 - [(吲哚-3-基)羰基]哌嗪衍生物作为大麻素CB1受体激动剂

  • Patent Title: Tricyclic 1-[(indol-3-yl)carbonyl]piperazine derivatives as cannabinoid CB1 receptor agonists
  • Patent Title (中): 三环1 - [(吲哚-3-基)羰基]哌嗪衍生物作为大麻素CB1受体激动剂
  • Application No.: US10583013
    Application Date: 2004-12-13
  • Publication No.: US07772227B2
    Publication Date: 2010-08-10
  • Inventor: Julia Adam-Worrall
  • Applicant: Julia Adam-Worrall
  • Applicant Address: NL Oss
  • Assignee: N.V. Organon
  • Current Assignee: N.V. Organon
  • Current Assignee Address: NL Oss
  • Agent Susan Hess
  • International Application: PCT/EP2004/053421 WO 20041213
  • International Announcement: WO2005/058327 WO 20050630
  • Main IPC: A61K31/5365
  • IPC: A61K31/5365 A61K31/496 A61K31/4985
Tricyclic 1-[(indol-3-yl)carbonyl]piperazine derivatives as cannabinoid CB1 receptor agonists
Abstract:
The invention relates to tricyclic 1-[(indol-3-yl)carbonyl]piperazine derivative having the general Formula (I) wherein X is CH2, O or S; R represents 1-3 substituents independently selected from H, (C1-4)alkyl, (C1-4)alkyloxy and halogen; R1 is (C5-8)cycloalkyl; R2 is H or (C1-4)alkyl; R3, R3′, R4′ R4′, R5, R5′ and R6′ are independently hydrogen or (C1-4)-alkyl, optionally substituted with (C1-4)alkyloxy, OH or halogen; R6 is hydrogen or (C1-4)alkyl, optionally substituted with (C1-4)alkyloxy, OH or halogen; or R6 forms together with R7 a 4-7 membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O and S; R7 forms together with R6 a 4-7 membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O and S; or R7 is H, (C1-4)alkyl or (C3-5)cycloalkyl, the alkyl groups being optionally substituted with OH, halogen or (C1-4)alkyloxy; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said tricyclic 1-[(indol-3-yl)carbonyl]piperazine derivatives, and to the use of these derivatives in the treatment of pain, such as peri-operative pain, chronic pain neuropathic pain, cancer pain, and pain and spasticity associated with multiple sclerosis.
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