Methods of using macrocyclic modulators of the ghrelin receptor

Details Methods of using macrocyclic modulators of the ghrelin receptor Methods of using macrocyclic modulators of the ghrelin receptor

C - Chemistry, Metallurgy

07

K

C07K 5/12 (2006.01) A61K 38/12 (2006.01) A61P 1/14 (2006.01)

Patent

CA 2571237

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.

L'invention concerne des nouveaux composés macrocycliques définis de manière conformationnelle qui présentent une activité de modulateurs sélectifs du récepteur de la ghréline (récepteur des sécrétagogues de l'hormone de croissance, GHS-R1a et sous-types, isoformes et variants associés). L'invention concerne également des procédés de synthèse desdits nouveaux composés. Ces composés sont utiles en tant qu'antagonistes du récepteur de la ghréline et en tant que médicaments pour le traitement et la prévention de divers états médicaux de type, entre autres, troubles métaboliques et/ou endocriniens, troubles gastrointestinaux, troubles cardiovasculaires, obésité et troubles associés à l'obésité, troubles du système nerveux central, troubles génétiques, troubles hyperprolifératifs et troubles inflammatoires.

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