1194731-76-4

Upstream product

• 128071-98-7 4-bromo-2-fluoropyridine 
• 1679-18-1 4-Chlorophenylboronic acid 
• 1194732-41-6 C₁₁H₁₃BrN₂ 
• 1187744-24-6 4-(4-chlorophenyl)-2-fluoropyridine 
• 1173155-38-8 4-(4-chloro-phenyl)-1H-pyridin-2-one 
• 1194732-26-7 5-bromo-1-[1-(2-fluoro-ethyl)-azetidin-3-yl]-2,3-dihydro-1H-indole 
• 1194732-27-8 3-{5-[4-(4-chloro-phenyl)-2-oxo-2H-pyridin-1-yl]-2,3-dihydro-indol-1-yl}-azetidine-1-carboxylic acid 
• 1194732-22-3 3-(5-bromo-2,3-dihydro-indol-1-yl)-azetidine-1-carboxylic acid tert-butyl ester 
• 22190-33-6 5-bromoindoline 
• 762-49-2 2-fluoroethyl bromide 

Relevant academic research and scientific papers

Strategies to lower the Pgp efflux liability in a series of potent indole azetidine MCHR1 antagonists

A series of potent indolyl azetidine rMCHR1 antagonists were found to show poor CNS penetration due to Pgp efflux. We envisioned a strategy which included: lowering basicity; changing the conformational flexibility motif; and removal of a hydrogen bond donor, in an attempt to optimize this property while maintaining target receptor efficacy. This work resulted in mitigation of Pgp efflux, and led us to identify 1-dihydroindolyl azetidine derivatives with CNS penetration and excellent rMCHR1 binding affinity.

AZETIDINE DERIVATIVES

The present invention relates to azetidine derivatives which bind to the MCH l receptor. In separate aspects, the subject invention is directed to uses of said compounds in the preparation of a pharmaceutical composition for the treatment of metabolic and