80127-39-5Relevant articles and documents
Characterization of 3,3-dimethyl substituted N-aryl piperidines as potent microsomal prostaglandin E synthase-1 inhibitors
Kuklish, Steven L.,Antonysamy, Stephen,Bhattachar, Shobha N.,Chandrasekhar, Srinivasan,Fisher, Matthew J.,Fretland, Adrian J.,Gooding, Karen,Harvey, Anita,Hughes, Norman E.,Luz, John G.,Manninen, Peter R.,McGee, James E.,Navarro, Antonio,Norman, Bryan H.,Partridge, Katherine M.,Quimby, Steven J.,Schiffler, Matthew A.,Sloan, Ashley V.,Warshawsky, Alan M.,York, Jeremy S.,Yu, Xiao-Peng
, p. 4824 - 4828 (2016)
Here we report on novel, potent 3,3-dimethyl substituted N-aryl piperidine inhibitors of microsomal prostaglandin E synthases-1(mPGES-1). Example 14 potently inhibited PGE2synthesis in an ex vivo human whole blood (HWB) assay with an IC50
Method of inhibiting protein tyrosine phosphatase 1B and/or T-cell protein tyrosine phosphatase 4 and/or other PTPases with an Asp residue at position 48
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Page/Page column 54-55, (2010/11/23)
The present invention provides a method of inhibiting a member of a family of Protein Tyrosine Phosphatases (PTPases, PTPs) such as PTP1B, TC-PTP, CD45, SHP-1, SHP-2, PTPα, PTPε, PTPμ, PTPδ, PTPσ, PTPζ, PTPβ, PTPD1, PTPD2, PTPH1, PTP-MEG1, PTP-LAR, and HePTP by exposing said Ptpase member by administration to a host or otherwise to at least one compound with certain structural, physical and spatial characteristics that allow for the interaction of said compound with specific residues of the active site of PTP1B and/or TC-PTP. These compounds are indicated in the management or treatment of a broad range of diseases such as autoimmune diseases, acute and chronic inflammation, osteoporosis, various forms of cancer and malignant diseases, and type I diabetes and type II diabetes, as well as in the isolation of PTPases and in elucidation or further elucidation of their biological function.
Hetero diels-alder type reactions between danishefsky's dienes in the presence of lewis base catalysts. An efficient method for the synthesis of substituted 2,3-dihydropyran-4-ones
Kitazawa, Takayuki,Mukaiyama, Teruaki
, p. 417 - 427 (2008/02/09)
Alkoxy anion such as methoxide anion works effectively as Lewis base catalyst to activate silicon-carbon bond of 1-methoxy-3-trimethylsilyloxy-1,3-butadiens (Danishefsky's dienes) in the reaction between aldehydes and ketones. By using Lewis base as catal