Novel antiasthmatic agents with dual activities of thromboxane A2 synthetase inhibition and bronchodilation. 1. 2-[2-(1-Imidazolyl)alkyl]-1(2H)-phthalazinones
摘要:
A number of 4-substituted 2-[omega-(1-imidazolyl)allryl]-1(2H)-phthalazinones were synthesized in order to develop agents possessing both thromboxane Az synthetase inhibitory and bronchodilatory activities. The pharmacological evaluation of these compounds disclosed that they have both activities to various extents. Both activities were slightly dependent on the length of the 2-substituents and largely affected by the nature of the 4-substituents. Compounds bearing phenyl and thienyl groups exhibited relatively high and well-rounded activities. Among these compounds, 12j and 15f were found to be the most effective agents having well-rounded activities in vitro and in vivo. Introduction of a carboxyl group reduced both activities contrary to our expectation. 4-(3-Pyridyl)phthalazinone 18b was of particular interest because of unexpectedly high in vivo activities in spite of an absence of significant in vitro activities.
Synthesis of synthons: The asymmetric hydrogenation and subsequent in situ lactonization with Ru-diphosphines results in the direct conversion of a series of 2-acylarylcarboxylates including 2-aroylarylcarboxylates into the corresponding optically active 3-substituted phthalides under mild reaction conditions.
Process for forming filled bearings from fluoropolymer dispersions stabilized with anionic polyelectrolyte dispersing agents
申请人:Cavanaugh Robert John
公开号:US20070281101A1
公开(公告)日:2007-12-06
The present invention provides a process for making a filled fluoropolymer bearing comprising providing an aqueous fluoropolymer dispersion comprising fluoropolymer particles and anionic polyelectrolyte dispersing agent in an amount sufficient for stabilization. The dispersion contains less than about 300 ppm fluorosurfactant based on the weight of the dispersion. The dispersion is coagulated to make a mush and a bearing filler is added to the dispersion prior to or after making the mush. The mush containing bearing filler is applied onto a bearing substrate to produce a coated substrate which is sintered and formed into a bearing.
Concentrated fluoropolymer dispersions stabilized with anionic polyelectrolyte dispersing agents
申请人:Cavanaugh Robert John
公开号:US20070282044A1
公开(公告)日:2007-12-06
An aqueous fluoropolymer dispersion comprising fluoropolymer particles having an average particle size of about 10 to about 400 nm. The dispersion has a solids content of at least about 35 to about 70 wt % and comprises about 0.03 wt % to about 10 wt % anionic polyelectrolyte dispersing agent based on the weight of fluoropolymer solids. The dispersion has a Gel Time of at least about 100 seconds.