1147552-75-7

Upstream product

• 143557-91-9 (1R,3S,5S)-tert-butyl 3-hydroxy-8-azabicyclo[3.2.1]octane-8-carboxylate 
• 1147557-61-6 C₁₂H₁₆ClN₃O 
• 1147557-54-7 C₁₇H₂₄ClN₃O₃ 
• 937734-25-3 tert-butyl (1R,3s,5S)-3-[(4-nitrobenzoyl)oxy]-8-azabicyclo[3.2.1]octane-8-carboxylate 
• 4316-97-6 4,6-dichloro-5-methylpyrimidine 
• 194222-05-4 (1R,3R,5S)-tert-butyl 3-hydroxy-8-azabicyclo[3.2.1]octane-8-carboxylate 
• 185099-67-6 N-Boc-nortropinone 

Relevant academic research and scientific papers

Discovery of a nortropanol derivative as a potent and orally active GPR119 agonist for type 2 diabetes

The lead optimization studies of a series of GPR119 agonists incorporating a nortropanol scaffold are described. Extensive structure-activity relationship (SAR) studies of the lead compound 20f led to the identification of compound 36j as a potent, single digit nanomolar GPR119 agonist with high agonist activity. Compound 36j was orally active in lowering blood glucose levels in a mouse oral glucose tolerance test and increased plasma insulin levels in a rat hyperglycemic model. It showed good to excellent pharmacokinetic properties in rats and monkeys and no untoward activities in counter-screen assays. Compound 36j demonstrated an attractive in vitro and in vivo profile for further development.

BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF

The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.