首页> 外国专利> NOVEL TRIAZOLE DERIVATIVES WITH IMPROVED RECEPTOR ACTIVITY AND BIOAVAILABILITY PROPERTIES AS GHRELIN ANTAGONISTS OF GROWTH HORMONE SECRETAGOGUE RECEPTORS

NOVEL TRIAZOLE DERIVATIVES WITH IMPROVED RECEPTOR ACTIVITY AND BIOAVAILABILITY PROPERTIES AS GHRELIN ANTAGONISTS OF GROWTH HORMONE SECRETAGOGUE RECEPTORS

机译:具有改善的受体活性和生物利用度特性的新型三唑衍生物,作为生长激素激素分泌受体的ghrelin拮抗剂

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)".
机译:本发明提供了具有改善的受体活性和生物利用度性能的新型三唑衍生物,其作为根据式(I)的生长激素促分泌素受体的生长素释放肽类似物配体,可用于治疗或预防哺乳动物,优选人类的生理和/或病理生理状况,由GHS受体介导。本发明进一步提供了可用于调节这些受体的GHS受体拮抗剂和激动剂,并且可用于治疗上述病症,特别是酒精障碍。吸毒;生长迟缓恶病质;短期,中期和/或长期的能源平衡监管;食物摄入的短期,中期和/或长期调节(刺激和/或抑制);摄取奖励食物;脂肪形成肥胖和/或肥胖;体重增加和/或减少;糖尿病,I型糖尿病,II型糖尿病;肿瘤细胞增殖;炎;炎症作用;胃术后肠梗阻;术后肠梗阻和/或胃切除术(ghrelin替代疗法)”。

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