62895-87-8Relevant academic research and scientific papers
Macrocyclic Modulators of the Ghrelin Receptor
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Paragraph 0423; 0425; 0426, (2018/05/03)
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.
Discovery of a new class of macrocyclic antagonists to the human motilin receptor
Marsault, Eric,Hoveyda, Hamid R.,Peterson, Mark L.,Saint-Louis, Carl,Landry, Annick,Vézina, Martin,Quellet, Luc,Wang, Zhigang,Ramaseshan, Mahesh,Beaubien, Sylvie,Benakli, Kamel,Beauchemin, Sophie,Déziel, Robert,Peeters, Théo,Fraser, Graeme L.
, p. 7190 - 7197 (2007/10/03)
A novel class of macrocyclic peptidomimetics was identified and optimized as potent antagonists to the human motilin receptor (hMOT-R). Well-defined structure-activity relationships allowed for rapid optimization of potency that eventually led to high aff
Olefins turned alkylating agents: Diastereoselective intramolecular Zr-catalyzed olefin alkylations
Cesati III, Richard R.,De Armas, Judith,Hoveyda, Amir H.
, p. 395 - 398 (2007/10/03)
(Equation Presented) 62% yield; 12 : 1 syn : anti The first examples of intramolecular Zr-catalyzed electrophilic alkylation of aryl olefins are disclosed. Substituted carbo-and heterocycles are prepared efficiently and diastereoselectively.
