Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of using the same .

Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of using the same

Номер патента: EP1891090A2
Опубликовано: 27-02-2008
Автор(ы): Graeme Fraser, Hamid Hoveyda
Принадлежит: Tranzyme Pharma Inc

Реферат: 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.

Рисунок 1. Взаимосвязь патентов (ближайшие 20).

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