发明授权
US08546435B2 Triazole derivatives with improved receptor activity and bioavailability properties as ghrelin antagonists of growth hormone secretagogue receptors
有权
具有改善的受体活性和生物利用度性质的三唑衍生物作为生长激素促分泌素受体的生长素释放肽拮抗剂
- 专利标题： Triazole derivatives with improved receptor activity and bioavailability properties as ghrelin antagonists of growth hormone secretagogue receptors
- 专利标题（中）： 具有改善的受体活性和生物利用度性质的三唑衍生物作为生长激素促分泌素受体的生长素释放肽拮抗剂
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申请号： US13235116申请日： 2011-09-16
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公开(公告)号： US08546435B2公开(公告)日： 2013-10-01
- 发明人: Babette Aicher , Gilbert Mueller , Klaus Paulini , Lars Blumenstein , Peter Schmidt , Matthias Gerlach , Michael Teifel , Jean Martinez , Jean-Alain Fehrentz , Anne-Laure Blayo
- 申请人： Babette Aicher , Gilbert Mueller , Klaus Paulini , Lars Blumenstein , Peter Schmidt , Matthias Gerlach , Michael Teifel , Jean Martinez , Jean-Alain Fehrentz , Anne-Laure Blayo
- 申请人地址： DE Frankfurt am Main FR Paris FR Montpellier FR Montpellier
- 专利权人： AEterna Zentaris GmbH,Centre National de la Recherche Scientifique,University of Montpellier I,University of Montpellier II
- 当前专利权人： AEterna Zentaris GmbH,Centre National de la Recherche Scientifique,University of Montpellier I,University of Montpellier II
- 当前专利权人地址： DE Frankfurt am Main FR Paris FR Montpellier FR Montpellier
- 代理机构： Oblon, Spivak, McClelland, Maier & Neustadt, L.L.P.
- 优先权： EP10177105 20100916
- 主分类号： A61K31/41
- IPC分类号： A61K31/41 ; C07D249/08
摘要：
The present invention provides novel triazole derivatives with improved receptor activity and bioavailability properties as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors. The present invention further provides GHS receptor antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular alcohol disorder, drug abuse, growth retardation, cachexia, short-, medium-, and/or long term regulation of energy balance, short-, medium-, and/or long term regulation (stimulation and/or inhibition) of food intake, intake of rewarding food, adipogenesis, adiposity and/or obesity, body weight gain and/or reduction, diabetes, diabetes type I, diabetes type II, tumor cell proliferation, inflammation, inflammatory effects, gastric postoperative ileus, postoperative ileus and/or gastrectomy (ghrelin replacement therapy).
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