1026341-92-3

Upstream product

• 1026544-31-9 methyl-[2-phenyl-1-(2,2,6,6-tetramethyl-piperidin-4-ylcarbamoyl)-ethyl]-carbamic acid tert-butyl ester 
• 37553-65-4 N-tert-butoxycarbonyl-N-methyl-D-phenylalanine 
• 36768-62-4 4-AMINO-2,2,6,6-TETRAMETHYLPIPERIDINE 
• 1026082-58-5 Methyl-((R)-1-{methyl-[(R)-2-phenyl-1-(2,2,6,6-tetramethyl-piperidin-4-ylcarbamoyl)-ethyl]-carbamoyl}-2-naphthalen-2-yl-ethyl)-carbamic acid tert-butyl ester 

Downstream Products

• 1026965-14-9 {(E)-1,1,3-Trimethyl-4-[methyl-((R)-1-{methyl-[(R)-2-phenyl-1-(2,2,6,6-tetramethyl-piperidin-4-ylcarbamoyl)-ethyl]-carbamoyl}-2-naphthalen-2-yl-ethyl)-carbamoyl]-but-3-enyl}-carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

The influence of conformational restriction in the C-terminus of growth hormone secretagogues on their potency

In order to obtain more potent growth hormone secretagogues, a comparison of ipamorelin and NN703 suggested the addition of a polar group at the C-terminus of NN703. A study was conducted using constrained amines for this purpose. Here, substituted 4-piperidinylamino- and 4-dimethylaminopiperidino-substitutents were found to give the most active compounds. A replacement of the 4-dimethylaminopiperidino-substituent with 4-hydroxypiperidino resulted in a series of compounds, which showed in vitro activity with EC50 values in the low nanomolar range, and favourable kinetic properties, such as 40% oral bioavailability. The most promising compound was also tested in a swine in vivo model, resulting in a growth hormone level with a Cmax of over 40 ng mL-1.