1368227-63-7Relevant academic research and scientific papers
Discovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus
Lizarzaburu, Mike,Turcotte, Simon,Du, Xiaohui,Duquette, Jason,Fu, Angela,Houze, Jonathan,Li, Leping,Liu, Jinqian,Reagan, Jeff,Yu, Ming,Medina, Julio C.,Murakoshi, Michiko,Oda, Kozo,Okuyama, Ryo,Nara, Futoshi
, p. 5942 - 5947,6 (2020/07/30)
The discovery and initial optimization of a series of phenylalanine based agonists for GPR142 is described. The structure-activity-relationship around the major areas of the molecule was explored to give agonists 90 times more potent than the initial HTS hit in a human GPR142 inositol phosphate accumulation assay. Removal of CYP inhibition by exploration of the pyridine A-ring is also described.
PHENYLALANINE AMIDE DERIVATIVES USEFUL FOR TREATING INSULIN-RELATED DISEASES AND CONDITIONS
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Page/Page column 120-121, (2010/09/03)
Provided herein are compounds of formula I: wherein A, B, X, R1 , R2 and subscript n are as defined in the following disclosure. Compositions comprising the compounds are also provided, as well as methods for their use, for example, in treatment of type 2 diabetes and type 2 diabetes-related conditions
