193085-21-1Relevant academic research and scientific papers
GPR119 AGONISTS
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Paragraph 00276-00277, (2021/04/17)
This disclosure is directed, at least in part, to GPR119 agonists useful for the treatment of conditions or disorders involving the gut-brain axis. In some embodiments, the GPR119 agonists are gut-restricted compounds. In some embodiments, the condition or disorder is a metabolic disorder, such as diabetes, obesity, nonalcoholic steatohepatitis (NASH), or a nutritional disorder such as short bowel syndrome.
Intramolecular Ring-Opening Decomposition of Aryl Azetidines
Bai, Guoyun,Brodney, Michael A.,Brown, Matthew F.,Butler, Christopher R.,Czabaniuk, Lara C.,Gilbert, Adam M.,Lachapelle, Erik A.,Li, Chao,McAllister, Laura A.,O'Connell, Thomas N.,Ogilvie, Kevin,Philippe, Laurence,Salomon-Ferrer, Romelia,Shapiro, Michael J.,Starr, Jeremy T.,Uccello, Daniel P.,Withka, Jane M.,Yan, Jiangli
supporting information, p. 1585 - 1588 (2021/10/21)
The ring strain present in azetidines can lead to undesired stability issues. Herein, we described a series of N-substituted azetidines which undergo an acid-mediated intramolecular ring-opening decomposition via nucleophilic attack of a pendant amide group. Studies were conducted to understand the decomposition mechanism enabling the design of stable analogues.
TARGETING COMPOUNDS
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Paragraph 0152, (2019/07/19)
The disclosure provides, at least in part, liver, intestine and/or kidney-targeting compounds and their use in treating liver, intestine and/or kidney disorders, such as non-alcoholic steatohepatitis, alcoholic steatohepatitis, hepatocellular carcinoma, liver cirrhosis, and hepatitis B; and/or chronic kidney disease, glomerular disease such as IGA nephropathy, lupus nephritis, or polycystic kidney disease. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
Synthesis and in vitro characterization of new growth hormone secretagogues derived from ipamorelin with dipeptidomimetic N-terminals
Peschke, Bernd,Ankersen, Michael,Sehested Hansen, Birgit,Kruse Hansen, Thomas,Langeland Johansen, Nils,Lau, Jesper,Madsen, Kjeld,Petersen, Hans,Thogersen, Henning,Watson, Brett
, p. 363 - 380 (2007/10/03)
The structural requirements for N-terminal features for the minimal structure of growth hormone secretagogues derived from ipamorelin are investigated. It is found, that incorporation of nonpolar peptidomimetic amino acids at the N-terminal can replace the Aib-His moiety and lead to compounds with high in vitro potency with respect to their growth hormone secretagogue properties. New unnatural amino acids with double bonds, ether- linkages, and 1,3-phenylene-moieties in the backbone proved to be valuable dipeptidomimetics. Using them, growth hormone secretagogues with high potencies were obtained.
Compounds with growth hormone releasing properties
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, (2008/06/13)
Compounds of peptide mimetic nature having the general formula I STR1 wherein a and b are independently 1 or 2, R1 and R2 are independently H or C1-6 alkyl, G and J are independently, inter alia, aromats, and D and E are independently several different groups are growth hormone secretagogous with improved bioavailability.
