710322-57-9Relevant academic research and scientific papers
Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists
Swanson, Devin M.,Shah, Chandra R.,Lord, Brian,Morton, Kirsten,Dvorak, Lisa K.,Mazur, Curt,Apodaca, Richard,Xiao, Wei,Boggs, Jamin D.,Feinstein, Mark,Wilson, Sandy J.,Barbier, Ann J.,Bonaventure, Pascal,Lovenberg, Timothy W.,Carruthers, Nicholas I.
experimental part, p. 4413 - 4425 (2009/12/24)
A series of small molecules consisting of a heterocyclic core flanked by two basic functionalities were synthesized and screened for in vitro affinity at the human histamine H3 receptor (hH3R). Nine of the twenty-eight compounds tested were found to possess a hH3R Ki of less than 5 nM and consisted of a diverse range of central hetero-aromatic linkers (pyridine, pyrazine, oxazole, isoxazole, thiazole, furan, thiophene, and pyrrole). One member of this series, (4-isopropyl-piperazin-1-yl)-(6-piperidin-1-ylmethyl-pyridin-3-yl)-methanone (37), was found to be a high affinity, selective antagonist that crosses the blood-brain barrier and occupies H3 receptors after oral administration in the rat.
Non-Imidazole heterocyclic compounds
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Page/Page column 19-20, (2008/06/13)
Certain non-imidazole heterocyclic compounds are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.
5-SUBSTITUTED-PYRAZINE OR PYRIDINE GLUCOKINASE ACTIVATORS
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Page 140, (2010/02/07)
The present invention provides a compound according to formula (I) where the substituent designations are provided in the specification. Pharmaceutical compositions comprising a compound according to formula (I) are also provided, said compounds being glucokinase activators which are useful in the treatment of type II diabetes.
