502136-76-7Relevant academic research and scientific papers
2,4-Diaminopyrimidine derivatives as potent growth hormone secretagogue receptor antagonists
Serby, Michael D.,Zhao, Hongyu,Szczepankiewicz, Bruce G.,Kosogof, Christi,Xin, Zhili,Liu, Bo,Liu, Mei,Nelson, Lissa T. J.,Kaszubska, Wiweka,Falls, H. Douglas,Schaefer, Verlyn,Bush, Eugene N.,Shapiro, Robin,Droz, Brian A.,Knourek-Segel, Victoria E.,Fey, Thomas A.,Brune, Michael E.,Beno, David W. A.,Turner, Theresa M.,Collins, Christine A.,Jacobson, Peer B.,Sham, Hing L.,Liu, Gang
, p. 2568 - 2578 (2007/10/03)
Ghrelin, a gut-derived orexigenic hormone, is an endogenous ligand of the growth hormone secretagogue receptor (GHS-R). Centrally administered ghrelin has been shown to cause hunger and increase food intake in rodents. Inhibition of ghrelin actions with ghrelin antibody, peptidyl GHS-R antagonists, and antisense oligonucleosides resulted in weight loss and food intake decrease in rodents. Here we report the effects of GHS-R antagonists, some of which were potent, selective, and orally bioavailable. A structure-activity relationship study led to the discovery of 8a, which was effective in decreasing food intake and body weight in several acute rat studies.
Diaminopyrimidine derivatives as growth hormone secrectgogue receptor (GHS-R) antagonists
-
Page/Page column 26, (2010/02/13)
The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, the preparation of the compounds, compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by the action of ghrelin receptor, including Prader-Willi syndrome, eating disorder, weight gain, weight-loss maintainance following diet and exercise, obesity, and disorders associated with obesity such as noninsulin dependent diabetes mellitus.
Pyrimidine derivatives as ghrelin receptor modulators
-
Page/Page column 26, (2010/02/11)
The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, the preparation of the compounds, compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by ghrelin including anorexia, cancer cachexia, eating disorders, age-related decline in body composition, weight gain, obesity, and diabetes mellitus.
An expeditious synthesis of 6-alkyl-5-(4′ -amino-phenyl)-pyrimidine-2,4-diamines
Holsworth, Daniel D.,Stier, Michael,Edmunds, Jeremy J.,He, Wei,Place, Samuel,Maiti, Samarendra
, p. 3467 - 3475 (2007/10/03)
A rapid synthesis of a series of 6-alkyl substituted-5-(4′ -amino-phenyl)-pyrimidine-2,4-diamines is described. These analogs were produced in good yields on moderate scale (ca. 8 g) without chromatography. Furthermore, the methodology described herein al
