专利号:US-8853410-B2 优先权日:2009-04-30 标 题:Process for preparing substituted isoxazoline compounds and their precursors 发明人:RACK MICHAEL; KOERBER KARSTEN; KAISER FLORIAN 权利人:RACK MICHAEL; KOERBER KARSTEN; KAISER FLORIAN; BASF SE 摘要:The present invention relates to a new method of preparing halogenated styrene compounds of formula (VIII) n nwhich are precursors in the process of synthesis of substituted isoxazoline compounds of formula (I)n n nwherein R 1 to R 5 , R 8 and R 9 are described as in the description.n n The present invention relates further to the synthesis of compounds of formula (I) starting from acetophenones. The desired styrenes of formula are prepared from the appropriate substituted acetophenone. Asides bromo anilines react with formoxime. Obtained oximes undergo a cycloaddition with the styrenes and give isoxazolines. Compounds of formula (I) can then be prepared in a palladium catalyzed carbonylative amination reaction of the isoxazolines.
专利号:US-7312347-B2 优先权日:2005-09-22 标题 :Substituted optically active disphosphine compound 发明人:FUJIWARA TAKAHIRO; YOKOZAWA TOHRU 权利人:TAKASAGO PERFUMERY CO LTD 摘要:Provided is a method for producing an optically active compound, in more detail, for producing an optically active compound by asymmetric hydrogenation in a high yield and asymmetric yield. The present invention also provides a catalyst for asymmetric synthesis for the above production method, especially a catalyst for asymmetric hydrogenation, containing a transition metal complex. Further, the present invention provides a new diphosphine compound useful as a ligand of the above transition metal complex and a new transition metal complex containing the above diphosphine compound. n The present invention relates to a diphosphine compound represented by the following formula (1): n na transition metal complex using the compound, a catalyst for asymmetric synthesis comprising the above transition metal complex and a method for producing an optically active compound using the above catalyst for asymmetric synthesis.
专利号:US-11434192-B2 优先权日:2015-12-10 标 题:Process and intermediates 发明人:KLEINBECK-RINIKER FLORIAN KARL; MARTIN BENJAMIN; PENN GERHARD; VENTURONI FRANCESCO; SCHLAMA THIERRY; RUCH THOMAS; ALLMENDINGER THOMAS; WIETFELD BERNHARD; FILIPPONI PAOLO 权利人:NOVARTIS AG 摘要:The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril. It further relates to new intermediate compounds and their use for said new chemical synthesis route.
专利号:US-11389397-B2 优先权日:2020-05-21 标 题 :Method to reduce face mask and respirator discomfort 发明人:WEI EDWARD TAK 权利人:WEI EDWARD TAK 摘要:Wearing a face mask or a filtering facepiece respirator, especially in hot weather for more than one hour, causes discomfort. But, in a viral pandemic, a barrier to filter inhaled and exhaled air is necessary to protect against airborne pathogens. The sensations of heat abstraction, that is, coolness and cold, can be captured by the rational design of optimized molecules called TRPM8 receptor agonists. The topical application of these molecules alleviates the discomfort of wearing a face mask covering. Several entities were identified by synthesis and experiment as having the ideal properties for achieving this purpose. The preferred embodiments are certain 1-diisopropyl-phosphinoyl-alkanes described as DIPA-1-5, DIPA-1-6, DIPA-1-7, DIPA-1-8, and DIPA-1-9, collectively referred to herein as “DIPA compounds.â€? The applicant found that topical delivery of DIPA compounds to the facial skin, especially to the surface of the nares (nostrils), alleviates face mask discomfort. From these studies, it is hypothesized that it is the absence of cool air dynamics about the nostrils that causes face mask discomfort. The present discovery pertains to pharmaceutical compositions that relieve face mask discmfort.
专利号:US-11389462-B2 优先权日:2017-03-31 标 题 :Method to reduce face mask and respirator discomfort 发明人:WEI EDWARD TAK 权利人:WEI EDWARD TAK 摘要:Wearing a face mask or a filtering facepiece respirator, especially in hot weather for more than one hour, causes discomfort. But, in a viral pandemic, a barrier to filter inhaled and exhaled air is necessary to protect against airborne pathogens. The sensations of heat abstraction, that is, coolness and cold, can be captured by the rational design of optimized molecules. The topical application of these molecules alleviates the discomfort of wearing a face mask covering. Several entities were identified by synthesis and experiment as having the ideal properties for achieving this purpose. The preferred embodiments are certain 1-diisopropyl-phosphinoyl-alkanes described as DIPA-1-7, DIPA-1-8, and DIPA-1-9, collectively referred to herein as “DIPA compounds.â€? The applicant found that topical delivery of DIPA compounds to the facial skin, especially to the surface of the external nares (nostrils), alleviates face mask discomfort. From these studies, I hypothesize that the absence of cool air dynamics about the nostrils causes face mask discomfort, not just static heat accumulation or excess humidity. The present discovery pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions for relieving face mask discmfort.