Novel triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors
申请人:Perrissoud Daniel
公开号:US20070037857A1
公开(公告)日:2007-02-15
The present invention provides novel triazole derivatives 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 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; 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).
本发明提供了一种新型的三唑衍生物,作为生长激素分泌素受体的胃泌素类似物配体,其符合以下公式(I),可用于治疗或预防哺乳动物,尤其是人类,通过GHS受体介导的生理和/或病理条件。本发明还提供了可用于调节这些受体并用于治疗上述疾病的GHS受体拮抗剂和激动剂,特别是生长迟缓、虚弱、短期、中期和/或长期能量平衡的调节;短期、中期和/或长期食物摄入的调节(刺激和/或抑制);脂肪生成、脂肪堆积和/或肥胖;体重增加和/或减少;糖尿病、糖尿病I型、糖尿病II型、肿瘤细胞增殖;炎症、炎症效应、胃术后肠梗阻、术后肠梗阻和/或胃切除(胃泌素替代疗法)。