Discovery of novel 2-(alkylmorpholin-4-yl)-6-(3-fluoropyridin-4-yl)-pyrimidin-4(3H)-ones as orally-active GSK-3β inhibitors for Alzheimer’s disease
摘要:
We herein describe the results of further evolution of GSK-3 beta inhibitors for Alzheimer's disease from our promising compounds with in vivo tau phosphorylation inhibitory activity by oral administration. Introduction of a low alkyl group instead of the phenyl group at the 3-position of the morpholine moiety aiming to improve pharmacokinetic profiles resulted in potent low molecular weight GSK-3 beta inhibitors with good in vitro pharmacokinetic profiles, which also showed in vivo tau phosphorylation inhibitory activity by oral administration. Effect of the stereochemistry of the alkyl moiety is also discussed using docking models. (C) 2015 Elsevier Ltd. All rights reserved.
[EN] CATALYTIC PREPARATION OF SEVERELY STERICALLY HINDERED AMINO-ETHER ALCOHOLS USING A METAL LOADED CATALYST<br/>[FR] PREPARATION CATALYTIQUE D'ALCOOLS AMINO-ETHER A ENCOMBREMENT STERIQUE SEVERE UTILISANT UN CATALYSEUR A CHARGE METALLIQUE
申请人:EXXONMOBIL RES & ENG CO
公开号:WO2005082834A1
公开(公告)日:2005-09-09
The present invention relates to a process for the production of severely sterically hindered amino-ether alcohols using a catalyst based on the combination of one or more catalytically active metals supported in a dispersed form on one or more ordered mesoporous materials as support.
[EN] SMALL MOLECULE FATTY ACID SYNTHASE INHIBITORS<br/>[FR] INHIBITEURS DE SYNTHASE D'ACIDES GRAS À PETITES MOLÉCULES
申请人:SANFORD BURNHAM MED RES INST
公开号:WO2015134790A1
公开(公告)日:2015-09-11
Provided herein are small molecule Fatty Acid Synthase Inhibitors, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.
METHOD FOR SEPARATING AROMATIC COMPOUNDS CONTAINED IN NAPHTHA
申请人:LOTTE CHEMICAL CORPORATION
公开号:US20160075952A1
公开(公告)日:2016-03-17
The present invention relates to a method for separating aromatic compounds contained in naphtha which includes an extraction step of contacting specific ionic liquids and naphtha and a step of separating the aromatic compounds from naphtha contacted with the ionic liquids.
BIS tertiary amino alkyl derivatives as solvents for acid gas removal from gas streams
申请人:AIR PRODUCTS AND CHEMICALS, INC.
公开号:EP0124835A2
公开(公告)日:1984-11-14
A process is set forth for the selective removal of acid gases such as H2S, COS and CO2from a gas stream by contacting the stream with a bis tertiary amino alkyl solvent compound such as bis-(2-morpholino ethyl) ether. When used in an aqueous solution, the compounds catalytically hydrolyze COS to H2S and CO2.
本发明提出了一种选择性去除气流中 H2S、COS 和 CO2 等酸性气体的工艺,方法是将气流与双叔氨基烷基溶剂化合物(如双(2-吗啉基乙基)醚)接触。在水溶液中使用时,这些化合物可催化 COS 水解为 H2S 和 CO2。
WATER-ABSORBENT RESIN DISPERSION AND POLYURETHANE COMPOSITION
申请人:SANYO CHEMICAL INDUSTRIES, LTD.
公开号:EP0789062A1
公开(公告)日:1997-08-13
A water-absorbent resin dispersion comprising a water-absorbent resin (B) or a hydrous gel thereof dispersed in a liquid or heat-meltable organic active-hydrogen compound (A), wherein said resin (B) is formed by the polymerization of a water-soluble monomer or its precursor and a cross-linker and/or a polysaccharide in the compound (A); and a process for producing a polyurethane resin by the reaction of the dispersion with an organic polyisocyanate compound. As the polyurethane resin is excellent in the capacity and rate of absorption, it is useful as absorbent articles such as paper diaper and sanitary goods, humidity modifiers, cutoff material, and so forth.