220534-06-5Relevant academic research and scientific papers
3-SPIROCYCLIC PIPERIDINE DERIVATIVES AS GHRELIN RECEPTOR AGONISTS
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Page/Page column 77, (2012/12/13)
The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicam
Discovery of a new class of glucosylceramide synthase inhibitors
Koltun, Elena,Richards, Steven,Chan, Vicky,Nachtigall, Jason,Du, Hongwang,Noson, Kevin,Galan, Adam,Aay, Naing,Hanel, Art,Harrison, Amanda,Zhang, Jeff,Won, Kwang-Ai,Tam, Danny,Qian, Fawn,Wang, Tao,Finn, Patricia,Ogilvie, Kathleen,Rosen, Jon,Mohan, Raju,Larson, Christopher,Lamb, Peter,Nuss, John,Kearney, Patrick
scheme or table, p. 6773 - 6777 (2011/12/05)
A novel series of potent inhibitors of glucosylceramide synthase are described. The optimization of biochemical and cellular potency as well as ADME properties led to compound 23c. Broad tissue distribution was obtained following oral administration to mice. Thus 23c could be another useful tool compound for studying the effects of GCS inhibition in vitro and in vivo.
Structure activity studies of the serine-AIB dipeptide domain in 2,3-dihydroisothiazole based growth hormone secretagogues
Evers, Britta,Ruehter, Gerd,Berg, Martina,Dodge, Jeffrey A.,Hankotius, Dirk,Hary, Ulrike,Jungheim, Louis N.,Mest, Hans-Juergen,De La Nava, Eva-Maria Martin,Mohr, Michael,Muehl, Brian S.,Petersen, Soenke,Sommer, Birgit,Riedel-Herold, Grit,Tebbe, Mark J.,Thrasher, Kenneth J.,Voelkers, Silke
, p. 6748 - 6762 (2007/10/03)
A series of growth hormone secretagogues (GHSs) based on 2,3-dihydroisothiazole has been synthesized in the search for a potential treatment of growth hormone deficiency or frailty in the elderly. This paper describes the evaluation of the SAR of the benzyl-d-Ser-aminoisobutyric acid dipeptide fragment. Introduction of substituents in the peptide backbone and in the phenyl ring has been investigated, as well as replacements for the benzyl group and for the AIB residue. A number of modifications resulted in enhanced potency over the parent benzyl-d-Ser-AIB derivative.
GROWTH HORMONE SECRETAGOGUES
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Page/Page column 108-109, (2010/02/07)
This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.
