1194732-22-3

Upstream product

• 398489-26-4 tert-butyl 3-oxoazetidine-1-carboxylate 
• 22190-33-6 5-bromoindoline 

Downstream Products

• 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 
• 1194732-49-4 C₂₈H₃₁N₃O₄ 
• 1194731-95-7 4-benzyloxy-1-[1-(1-methyl-azetidin-3-yl)-2,3-dihydro-1H-indol-5-yl]-1H-pyridin-2-one 
• 1194731-96-8 1-(1-azetidin-3-yl-2,3-dihydro-1H-indol-5-yl)-4-benzyloxy-1H-pyridin-2-one 
• 1194732-29-0 C₂₂H₂₀ClN₃O 
• 1194731-76-4 4-(4-chloro-phenyl)-1-{1-[1-(2-fluoro-ethyl)-azetidin-3-yl]-2,3-dihydro-1H-indol-5-yl}-1H-pyridin-2- 
• 1194731-78-6 4-(4-chloro-phenyl)-1-[1-(1-methyl-azetidin-3-yl)-2,3-dihydro-1H-indol-5-yl]-1H-pyridin-2-one 
• 1194731-94-6 4-benzyloxy-1-{1-[1-(2-fluoro-ethyl)-azetidin-3-yl]-2,3-dihydro-1H-indol-5-yl}-1H-pyridin-2-one 

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