发明名称 Tricyclic 1-[(indol-3-yl)carbonyl]piperazine derivatives as cannabinoid cb1 receptor agonists
摘要 The invention relates to tricyclic 1-[(in-dol-3-yl)carbonyl]piperazine derivative having the general Formula (I) wherein X is CH<SUB>2</SUB>, O or S; R represents 1-3 substituents independently selected from H, (C<SUB>1-4</SUB>)alkyl, (C<SUB>1-4</SUB>)alkyloxy and halogen; R<SUB>1 </SUB>is (C<SUB>5-8</SUB>)cycloalkyl; R<SUB>2 </SUB>is H or (C<SUB>1-4</SUB>)alkyl; R<SUB>3</SUB>, R<SUB>3</SUB>', R<SUB>4</SUB>', R<SUB>4</SUB>', R<SUB>5</SUB>, R<SUB>5</SUB>' and R<SUB>6</SUB>' are independently hydrogen or (C<SUB>1-4</SUB>)-alkyl, optionally substituted with (C<SUB>1-4</SUB>)alkyloxy, OH or halogen; R<SUB>6 </SUB>is hydrogen or (C<SUB>1-4</SUB>)alkyl, optionally substituted with (C<SUB>1-4</SUB>)alkyloxy, OH or halogen; or R<SUB>6 </SUB>forms together with R<SUB>7</SUB>a 4-7 membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O and S; R<SUB>7 </SUB>forms together with R<SUB>6 </SUB>a 4-7 membered saturated heterocydic ring, optionally containing a further heteroatom selected from O and S; or R<SUB>7 </SUB>is H, (C<SUB>1-4</SUB>)alkyl or (C<SUB>3-5</SUB>)cycloalkyl, the alkyl groups being optionally substituted with OH, halogen or (C<SUB>1-4</SUB>)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.
申请公布号 US2007088025(A1) 申请公布日期 2007.04.19
申请号 US20040583013 申请日期 2004.12.13
申请人 AKZO NOBEL N.V. 发明人 ADAM-WORRALL JULIA
分类号 A61K31/542;A61K31/496;A61K31/5383;C07D471/04;C07D471/06;C07D491/04;C07D498/04;C07D498/16;C07D519/00 主分类号 A61K31/542
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