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1. 发明申请

US20070286903A1 Composition and method for taste masking 审中-公开
标题翻译：味道掩蔽的组合和方法
公开(公告)号：US20070286903A1
公开(公告)日：2007-12-13
申请号：US11451622
申请日：2006-06-13
申请人： Brian T. Becicka , Erik T. Michalson
发明人： Brian T. Becicka , Erik T. Michalson
IPC分类号： A61K9/24
CPC分类号： A61K9/1664 , A61K9/1617 , A61K9/1652
摘要： The present invention relates to a taste-masked composition of an active pharmaceutical ingredient (API) for oral delivery and a related method for the preparation of the taste-masked composition comprising a granulated mixture of the active pharmaceutical ingredient, an insoluble matrix component, a film-forming agent, and a water soluble binder
摘要翻译：本发明涉及用于口服递送的活性药物成分（API）的掩味组合物和用于制备掩味组合物的相关方法，其包含活性药物成分，不溶性基质组分，成膜剂和水溶性粘合剂

2. 发明授权

US06265579B1 Process for preparing piperazine-substituted aliphatic carboxylates 失效
标题翻译：制备哌嗪取代的脂肪族羧酸盐的方法
公开(公告)号：US06265579B1
公开(公告)日：2001-07-24
申请号：US09429660
申请日：1999-10-29
申请人： David John Fairfax , Pedro E. Hemandez , Erik T. Michalson
发明人： David John Fairfax , Pedro E. Hemandez , Erik T. Michalson
IPC分类号： C07D29515
CPC分类号： C07D295/088
摘要： A process is disclosed for the preparation of a piperazine-substituted aliphatic carboxylate having the formula where m and n are individually an integer of from 1 to 6, R and R′ are the same or different and are hydrogen, C1 to C6 alkyl or aryl or heteroaryl that is unsubstituted or is substituted with at least one substituent that is halo, C1 to C6 alkyl or C1 to C6 alkoxy and R″ is C3 to C12 branched alkyl or an organic or inorganic cation. The process comprises treating a solution comprising a compound of the formula wherein m, R and R′ are as defined above and an aliphatic ester of the formula X—(CH2)nCO(O)R″ where X is a leaving group and n and R″ are as defined above, with a base in the presence of an effective amount of a phase transfer catalyst, for a time and at a temperature sufficient to form a piperazine-substituted aliphatic carboxylate. Hydrolysis of the carboxylate with acid produces a piperazine-substituted aliphatic carboxylic acid or the acid salt thereof.
摘要翻译：公开了制备具有式m和n分别为1至6的整数的哌嗪取代的脂族羧酸酯的方法，R和R'相同或不同，为氢，C 1至C 6烷基或芳基或未被取代或被至少一个为卤素，C 1至C 6烷基或C 1至C 6烷氧基的取代基取代的杂芳基，R“为C 3至C 12支链烷基或有机或无机阳离子。该方法包括处理包含糠醛的化合物的溶液，R和R'如上所定义，并且所述式的脂族酯是离去基团，n和R“如上所定义，在存在有效量的相转移催化剂的时间和足以形成哌嗪取代的脂族羧酸酯的温度。羧酸酯与酸的水解产生哌嗪取代的脂族羧酸或其酸式盐。

3. 发明授权

US06673951B1 Process for catalytically hydrogenating phytosterols 有权
标题翻译：催化氢化植物甾醇的方法
公开(公告)号：US06673951B1
公开(公告)日：2004-01-06
申请号：US10229413
申请日：2002-08-29
申请人： Erik T. Michalson , James D. Devore
发明人： Erik T. Michalson , James D. Devore
IPC分类号： C07J900
CPC分类号： C07J9/00
摘要： The present invention provides a process for catalytically hydrogenating unsaturated phytosterol compounds. The catalyst used for such hydrogenation is an alumina-supported transition metal selected from the group consisting of nickel, palladium, platinum, ruthenium, rhodium and mixtures thereof. The process involves the following steps. Admixing a solvent, the alumina-supported transition metal catalyst and a material that contains at least one unsaturated phytosterol compound and hydrogenating said admixture for a time and at a temperature and pressure sufficient to cause the hydrogenation of the material that contains at least one of said unsaturated phytosterol compounds; separating said alumina-supported transition metal catalyst from said mixture; admixing with a new solvent a material that contains at least one unsaturated phytosterol compound and hydrogenating said admixture for a time and at a temperature and pressure sufficient to cause the hydrogenation of the material that contains at least one unsaturated phytosterol compound; and separating the alumina-supported transition metal catalyst from the hydrogenated mixture. Such separated catalyst may be used again for subsequent hydrogenations of materials that contain phytosterol compounds. The hydrogenation process disclosed herein can also be applied to the hydrogenation of fatty acids derived from unsaturated phytosterols, e.g., tall oil, vegetable oil and their distillation products.
摘要翻译：本发明提供了一种催化氢化不饱和植物甾醇化合物的方法。用于这种氢化的催化剂是选自镍，钯，铂，钌，铑及其混合物的氧化铝负载的过渡金属。该方法包括以下步骤：将溶剂，氧化铝负载的过渡金属催化剂和含有至少一种不饱和植物甾醇化合物的材料混合并将所述混合物氢化一段时间并在足以引起材料氢化的温度和压力下其含有至少一种所述不饱和植物甾醇化合物; 从所述混合物中分离所述氧化铝负载的过渡金属催化剂; 与新溶剂混合含有至少一种不饱和植物甾醇化合物的材料，并将所述混合物氢化一段时间，并在足以引起含有至少一种不饱和植物甾醇化合物的材料的氢化的温度和压力下进行; 以及从氢化混合物中分离氧化铝负载的过渡金属催化剂。这种分离的催化剂可以再次用于随后的含有植物甾醇化合物的材料的氢化。本文公开的氢化方法也可以应用于来自不饱和植物甾醇如妥尔油，植物油及其蒸馏产物的脂肪酸的氢化。

4. 发明授权

US06239277B1 Process for preparing piperazine-substituted aliphatic carboxylates 失效
标题翻译：制备哌嗪取代的脂肪族羧酸盐的方法
公开(公告)号：US06239277B1
公开(公告)日：2001-05-29
申请号：US09421514
申请日：1999-10-20
申请人： Pedro E. Hernandez , David John Fairfax , Erik T. Michalson
发明人： Pedro E. Hernandez , David John Fairfax , Erik T. Michalson
IPC分类号： C07D29510
CPC分类号： C07D295/088
摘要： A process is disclosed for the preparation of a piperazine-substituted aliphatic carboxylate having the formula where m and n are individually an integer of from 1 to 6, R and R′ are the same or different and are hydrogen, C1 to C6 alkyl or aryl or heteroaryl that is unsubstituted or is substituted with at least one substituent that is halo, C1 to C6 alkyl or C1 to C6 alkoxy and R″ is C3 to C12 branched alkyl or an organic or inorganic cation. The process comprises treating a solution comprising a compound of the formula wherein m, R and R′ are as defined above and an aliphatic ester of the formula X—(CH2)n—O—CH2—CO(O)R″ where X is a leaving group and n and R″ are as defined above, with an effective amount of a base for a time and at a temperature sufficient to form a piperazine-substituted aliphatic carboxylate. Hydrolysis of the carboxylate with acid produces a piperazine-substituted aliphatic carboxylic acid or the acid salt thereof.
摘要翻译：公开了制备具有式m和n分别为1至6的整数的哌嗪取代的脂族羧酸酯的方法，R和R'相同或不同，为氢，C 1至C 6烷基或芳基或未被取代或被至少一个为卤素，C 1至C 6烷基或C 1至C 6烷氧基的取代基取代的杂芳基，R“为C 3至C 12支链烷基或有机或无机阳离子。该方法包括处理包含糠醛的化合物的溶液，R和R'如上所定义，并且所述式的脂族酯是离去基团，n和R“如上定义，并且有效量碱处理一段时间并在足以形成哌嗪取代的脂族羧酸酯的温度下进行。羧酸酯与酸的水解产生哌嗪取代的脂族羧酸或其酸式盐。

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