abstract |
The present invention is a novel, constitutive modulator that has been demonstrated to be a selective modulator of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and / or variants thereof). Provided are macrocycles having a defined locus. Methods for synthesizing new compounds are also described herein. These compounds, as ghrelin receptor antagonists or inverse agonists, further include, but are not limited to, metabolic and / or endocrine disorders, cardiovascular diseases, obesity and obesity related diseases, gastrointestinal disorders, genetic diseases It is useful as an agent for the treatment and prevention of a range of medical conditions, including hyperproliferative disorders and inflammatory diseases. |