332099-56-6Relevant articles and documents
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: Potent human histamine H4 antagonists
Venable, Jennifer D.,Cai, Hui,Chai, Wenying,Dvorak, Curt A.,Grice, Cheryl A.,Jablonowski, Jill A.,Shah, Chandra R.,Kwok, Annette K.,Ly, Kiev S.,Pio, Barbara,Wei, Jianmei,Desai, Pragnya J.,Jiang, Wen,Nguyen, Steven,Ling, Ping,Wilson, Sandy J.,Dunford, Paul J.,Thurmond, Robin L.,Lovenberg, Timothy W.,Karlsson, Lars,Carruthers, Nicholas I.,Edwards, James P.
, p. 8289 - 8298 (2007/10/03)
Three series of H4 receptor ligands,- derived from indoly-2-yl-(4-methyl-piperazin-1-yl)-methanones, have been synthesized and their structure-activity relationships evaluated for activity at the H 4 receptor in competitive binding and functional assays. In all cases, substitution of small lipophilic groups in the 4 and 5-positions led to increased activity in a [3H]histamine radiolabeled ligand competitive binding assay. In vitro metabolism and initial pharmacokinetic studies were performed on selected compounds leading to the identification of indole 8 and benzimidazole 40 as potent H4 antagonists with the potential for further development. In addition, both 8 and 40 demonstrated efficacy in in vitro mast cell and eosinophil chemotaxis assays.
Use of glycogen phosphorylase inhibitors
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, (2008/06/13)
The invention provides methods of treating prophylactically an individual in whom Type 2 diabetes mellitus has not yet presented, but in whom there is an increased risk of developing such condition, which methods comprise administering to an individual in need thereof an effective amount of a glycogen phosphorylase inhibitor; effective amounts of a glycogen phosphorylase inhibitor and a non-glycogen phosphorylase inhibiting anti-diabetic agent; or effective amounts of a glycogen phosphorylase inhibitor and an anti-obesity agent. The invention further provides methods of treating prophylactically an individual in whom Type 2 diabetes mellitus has not yet presented, but in whom there is an increased risk of developing such condition, which methods comprise administering to an individual in need thereof a pharmaceutical composition comprising effective amounts of a glycogen phosphorylase inhibitor and a non-glycogen phosphorylase inhibiting anti-diabetic agent; or effective amounts of a glycogen phosphorylase inhibitor and an anti-obesity agent.
Bicyclic pyrrolyl amides as glycogen phosphorylase inhibitors
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, (2008/06/13)
This invention relates to compounds of Formula I or stereoisomers, pharmaceutically acceptable salts or prodrugs thereof or a pharmaceutically acceptable salts of the prodrugs. This invention also relates to pharmaceutical compositions comprising a compou