Macrocyclic modulators of the ghrelin receptor
    3.
    再颁专利
    Macrocyclic modulators of the ghrelin receptor 有权
    生长素释放肽受体的大环调节剂

    公开(公告)号:USRE42013E1

    公开(公告)日:2010-12-28

    申请号:US12636048

    申请日:2009-12-11

    IPC分类号: A61K38/12 C07K5/12 C07K1/00

    摘要: The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.

    摘要翻译: 本发明提供已被证明是生长素释放肽受体(生长激素促分泌素受体,GHS-R1a和亚型,同种型及其变体)的选择性调节剂的新型构象定义的大环化合物。 本文还描述了合成新化合物的方法。 这些化合物可用作生长素释放肽受体的激动剂,并且用作治疗和预防一系列医学病症的药物,包括但不限于代谢和/或内分泌疾病,胃肠道疾病,心血管疾病,肥胖症和肥胖相关疾病, 中枢神经系统疾病,遗传疾病,过度增殖性疾病和炎症性疾病。