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Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of use thereof
Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of use thereof
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机译:大环生长素释放肽受体拮抗剂和反向激动剂及其使用方法
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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/or variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as antagonists or inverse 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, cardiovascular disorders, obesity and obesity-associated disorders, gastrointestinal disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
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