254905-64-1Relevant articles and documents
THERAPEUTIC ISOXAZOLE COMPOUNDS
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Page/Page column 42, (2009/04/24)
The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.
The influence of conformational restriction in the C-terminus of growth hormone secretagogues on their potency
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)
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.
