cas 138022-01-2, tert-Butyl 4-((dimethylamino)methyl)piperidine-1-carboxylate

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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.
Peschke, Bernd,Ankersen, Michael,Bauer, Michael,Hansen, Thomas Kruse,Hansen, Birgit Sehested,Nielsen, Karin Kramer,Raun, Kirsten,Richter, Lutz,Westergaard, Lisbet
p. 487 - 501
(2007/10/03)