发明授权
US08067456B2 Tetrahydrocarbazole derivatives having improved biological action and improved solubility as ligands of G-protein coupled receptors (GPCPs)
有权
具有改善的生物学作用和改善作为G蛋白偶联受体（GPCR）配体的溶解度的四氢咔唑衍生物
- 专利标题： Tetrahydrocarbazole derivatives having improved biological action and improved solubility as ligands of G-protein coupled receptors (GPCPs)
- 专利标题（中）： 具有改善的生物学作用和改善作为G蛋白偶联受体（GPCR）配体的溶解度的四氢咔唑衍生物
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申请号： US12070214申请日： 2008-02-14
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公开(公告)号： US08067456B2公开(公告)日： 2011-11-29
- 发明人: Klaus Paulini , Matthias Gerlach , Eckhard Gunther , Emmanuel Polymeropoulos , Silke Baasner , Peter Schmidt , Ronald Kühne , Arvid Söderhäll
- 申请人： Klaus Paulini , Matthias Gerlach , Eckhard Gunther , Emmanuel Polymeropoulos , Silke Baasner , Peter Schmidt , Ronald Kühne , Arvid Söderhäll
- 申请人地址： DE Frankfurt am Main
- 专利权人： AEterna Zentaris GmbH
- 当前专利权人： AEterna Zentaris GmbH
- 当前专利权人地址： DE Frankfurt am Main
- 代理机构： Goodwin Procter LLP
- 优先权： DE102004033902 20040714
- 主分类号： A61K31/403
- IPC分类号： A61K31/403 ; C07D209/82
摘要：
The present invention provides novel tetrahydrocarbazole derivatives which have improved properties and which can be employed as inhibitors of GPCRs. This results in the possibility of using the novel compounds to treat pathological conditions whose severity depends on the pathobiochemical effect of GPCRs. The compounds of the invention act in particular via an antagonistic inhibition of the LHRH receptor. The invention further provides medicaments which comprise one or more of the novel compounds as active ingredient. The medicaments are suitable in particular to be employed in an oral dosage form for a mammal, in particular a human.