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1. 发明授权

US08552195B2 Method for making donepezil 有权
标题翻译：制备多奈哌齐的方法
公开(公告)号：US08552195B2
公开(公告)日：2013-10-08
申请号：US13198775
申请日：2011-08-05
申请人： Kuen-Wang Sheu , Shu-Fen Huang
发明人： Kuen-Wang Sheu , Shu-Fen Huang
IPC分类号： C07D211/32
CPC分类号： C07D211/32
摘要： The method in accordance with the present invention has: mixing E2M, an organic solvent, a weak base, sodium dithionite, and a phase transfer catalyst to obtain an E2M mixture solution; heating the E2M mixture solution and adding water to obtain a heated E2M aqueous solution having an organic layer; and extracting the organic layer from the heated E2M aqueous solution, and condensing and drying the organic layer to obtain donepezil. Employing sodium dithionite as a reducing agent improves safety over hydrogen gas used in conventional methods and lowers the cost in contrast to the conventional noble metal catalysts that are extremely expensive. Furthermore, the method of the present invention requires only 60 minutes of reaction time to synthesize donepezil with a promising yield more than 85%, which greatly raises the efficiency and economic value of the manufacture of donepezil.
摘要翻译：根据本发明的方法具有：混合E2M，有机溶剂，弱碱，连二亚硫酸钠和相转移催化剂，得到E2M混合溶液; 加热E2M混合溶液并加水，得到具有有机层的加热的E2M水溶液; 从加热的E2M水溶液中萃取有机层，冷凝干燥有机层得到多奈哌齐。使用连二亚硫酸钠作为还原剂提高了与常规方法中使用的氢气相比的安全性，并且降低了与常规贵金属催化剂相当昂贵的成本。此外，本发明的方法仅需60分钟的反应时间合成多奈哌齐，产率高达85％以上，大大提高了多奈哌齐的制造效率和经济价值。

2. 发明申请

US20090186087A1 ENTERIC SUSTAINED-RELEASE COATED CORE AND PHARMACEUTICAL DOSAGE FORM AND METHOD FOR MANUFACTURING THE SAME 审中-公开
标题翻译： ENTERIC可持续发行涂层核心和药物剂型及其制造方法
公开(公告)号：US20090186087A1
公开(公告)日：2009-07-23
申请号：US12357129
申请日：2009-01-21
申请人： Min-Chuan HSU , Yu-Kao CHENG , Li-Chin LIN
发明人： Min-Chuan HSU , Yu-Kao CHENG , Li-Chin LIN
IPC分类号： A61K9/32
CPC分类号： A61K9/5047 , A61K9/2846 , A61K9/2866 , A61K9/5026
摘要： An enteric sustained-release coated core includes a drug-containing core and a coating film. The coating film includes 20%˜80% by weight of a hydrophobic polymer and 10%˜70% by weight of an enterosoluble material. The dissolution rate of the medical component in the drug-containing core is approximately less than 10% in hydrochloric acid solution of pH 1˜3 after 2 hours. The dissolution of the medical component in the drug-containing core sustains more than 5 hours in phosphate buffer solution of pH 5˜8.
摘要翻译：肠溶缓释包衣芯包括含药芯和涂膜。涂膜包含20重量％〜80重量％的疏水性聚合物和10重量％〜70重量％的肠溶性物质。药物组分在药物含核心中的溶解速率在2小时后在pH 1〜3的盐酸溶液中大约小于10％。医药成分在含药核心中的溶解在pH5〜8的磷酸盐缓冲溶液中维持5小时以上。

3. 发明申请

US20130078304A1 CONTROLLED RELEASE FORMULATION FOR TREATING SLEEP DISORDERS 审中-公开
标题翻译：用于治疗睡眠障碍的控制释放配方
公开(公告)号：US20130078304A1
公开(公告)日：2013-03-28
申请号：US13247302
申请日：2011-09-28
申请人： HSIEN-JEN HSIEH , KUO-HUA YANG , CHIH-SHENG YANG , YU-CHENG WEI , CHUNG-HSUAN LU
发明人： HSIEN-JEN HSIEH , KUO-HUA YANG , CHIH-SHENG YANG , YU-CHENG WEI , CHUNG-HSUAN LU
IPC分类号： A61K31/519 , A61P25/00 , A61K9/24 , A61K9/52 , A61K9/30 , A61K9/32
CPC分类号： A61K31/519 , A61K9/1676 , A61K9/209 , A61K31/437 , A61K2300/00
摘要： The invention relates to a controlled-release formulation for preventing and/or treating sleep disorders comprising Zaleplon or a pharmaceutically acceptable salt thereof in immediate release form and Zolpidem or a pharmaceutically acceptable salt thereof in sustained release form, wherein Zaleplon or a pharmaceutically acceptable salt thereof and Zolpidem or a pharmaceutically acceptable salt thereof are released in two phases where the first phase is a immediate release phase of Zaleplon or a pharmaceutically acceptable salt thereof and the second phase is a sustained release phase of Zolpidem or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及一种用于预防和/或治疗睡眠障碍的控释制剂，其包括立即释放形式的扎利波隆或其药学上可接受的盐和唑吡旦或其药学上可接受的盐，其为缓释形式，其中扎利波隆或其药学上可接受的盐和唑吡旦或其药学上可接受的盐在两相中释放，其中第一相是扎来普隆或其药学上可接受的盐的即时释放阶段，第二相是唑吡旦或其药学上可接受的盐的持续释放期。

4. 发明申请

US20140052081A1 DONEPEZIL TRANSDERMAL PATCH 审中-公开
标题翻译：多奈米德超声波贴片
公开(公告)号：US20140052081A1
公开(公告)日：2014-02-20
申请号：US13979579
申请日：2012-01-12
申请人： Kuo-Hua Yang , Chih-Sheng Yang , Hsuen-Yau Lin
发明人： Kuo-Hua Yang , Chih-Sheng Yang , Hsuen-Yau Lin
IPC分类号： A61K9/70 , A61K31/445
CPC分类号： A61K9/7061 , A61K31/445
摘要： The present invention relates to a donepezil transdermal patch comprising a backing layer and a pressure sensitive adhesive matrix layer, wherein the pressure sensitive adhesive matrix layer comprises donepezil free base and an acrylic pressure sensitive adhesive agent selected from the group consisting of a copolymer of 2-ethylhexyl acrylate and vinyl acetate and a copolymer of 2-ethylhexyl acrylate, vinyl acetate, and hydroxyl-containing monomers, and wherein 2-ethylhexyl acrylate is present in an amount of about 65% to about 75%, vinyl acetate is present in an amount of about 25% to about 35%, and the hydroxyl-containing monomers are in an amount of about 0% to about 10%, based on the total weight of the copolymer.
摘要翻译：本发明涉及包含背衬层和压敏粘合剂基质层的多奈哌齐透皮贴剂，其中压敏粘合剂基质层包含多奈哌齐游离碱和丙烯酸压敏粘合剂，其选自2- 丙烯酸乙基己酯和乙酸乙烯酯和丙烯酸2-乙基己酯，乙酸乙烯酯和含羟基单体的共聚物，其中丙烯酸2-乙基己酯以约65％至约75％的量存在，乙酸乙烯酯的存在量为约25％至约35％，并且含羟基单体的量为约0％至约10％，基于共聚物的总重量。

5. 发明申请

US20120027853A1 PROCESS FOR PREPARATION OF ANTI-TUBERCULAR COMBINATION AND PHARMACEUTICAL COMPOSITION PREPARED THEREFROM 有权
标题翻译：制备抗结核药物的方法和制备的药物组合物
公开(公告)号：US20120027853A1
公开(公告)日：2012-02-02
申请号：US12846476
申请日：2010-07-29
申请人： Li-Heng Pao , Nion-Heng Shiao , Kuo-Hua Yang , Jui-Ming Chou
发明人： Li-Heng Pao , Nion-Heng Shiao , Kuo-Hua Yang , Jui-Ming Chou
IPC分类号： A61K9/28 , A61P31/06 , B05D7/00 , A61K31/497
CPC分类号： A61K31/497 , A61K9/2077 , A61K9/209 , A61K9/2866 , A61K31/166 , A61K2300/00
摘要： This invention relates to a process for preparing a pharmaceutical composition comprising four antitubercular drugs: rifampin or a pharmaceutically acceptable salt thereof, isoniazid or a pharmaceutically acceptable salt thereof, pyrazinamide or a pharmaceutically acceptable salt thereof and ethambutol or a pharmaceutically acceptable salt thereof, wherein rifampin and isoniazid are in separate layers. The invention also provides a pharmaceutical composition prepared therefrom having advantageous stability and bioavailability.
摘要翻译：本发明涉及一种制备药物组合物的方法，其包含四种抗结核药物：利福平或其药学上可接受的盐，异烟肼或其药学上可接受的盐，吡嗪酰胺或其药学上可接受的盐和乙胺丁醇或其药学上可接受的盐，其中利福平异烟肼分开。本发明还提供由其制备的药物组合物，其具有有利的稳定性和生物利用度。

6. 发明申请

US20100081669A1 PRESSURE SENSITIVE ADHESIVE MATRIX DEVICE OR SYSTEM FOR THE TREATMENT OR PREVENTION OF ONYCHOMYCOSIS OR TINEA PEDIS 有权
标题翻译：用于治疗或预防结核病或TINEA PEDIS的压敏敏感胶粘剂装置或系统
公开(公告)号：US20100081669A1
公开(公告)日：2010-04-01
申请号：US12570656
申请日：2009-09-30
申请人： Kuo-Hua Yang , Yung-Jin Lee , Li-Chin Lin
发明人： Kuo-Hua Yang , Yung-Jin Lee , Li-Chin Lin
IPC分类号： A61K31/496 , A61K9/70 , A61P31/10
CPC分类号： A61K31/496 , A61K9/7023 , A61K9/7061 , A61K47/14
摘要： Disclosed is a pressure-sensitive adhesive matrix patch device for treatment or prevention of fungal toenails or fingernails or foot infections comprising an antifungal agent or two or more antifungals in combination and adhesively secured to a dorsal site of an infected palm or foot, rather than an area of infection and surrounding skin. A method for the transdermal treatment or prevention of fungal toenails or fingernails or foot infections with an antifungal agent is also disclosed, the method comprising adhesively securing to a dorsal site of an infected palm or foot a pressure-sensitive adhesive matrix patch device for a time sufficient to deliver an effective amount of the antifungal agent to an area of infection.
摘要翻译：公开了一种用于治疗或预防真菌趾甲或指甲或足部感染的压敏粘合剂基质贴片装置，其包含抗真菌剂或两种或更多种抗真菌剂的组合，并且粘附地固定到感染的手掌或足部的背部，而不是感染区域和周围皮肤。还公开了用抗真菌剂透皮治疗或预防真菌脚趾甲或指甲或足部感染的方法，所述方法包括将感染的手掌或足部的背部部位粘合固定一段时间的压敏粘合剂基质贴片装置足以将有效量的抗真菌剂递送至感染区域。

7. 发明申请

US20150064129A1 WOUND HEALING COMPOSITION 审中-公开
标题翻译：创伤治疗组合物
公开(公告)号：US20150064129A1
公开(公告)日：2015-03-05
申请号：US14018120
申请日：2013-09-04
申请人： Taiwan Biotech Co., Ltd.
发明人： LiChin Lin , YuKao Cheng , YuHua Chen , ShuFang Chiang
IPC分类号： A61K31/79 , A61K31/728
CPC分类号： A61K31/79 , A61K9/06 , A61K31/728 , A61L26/0023 , A61K2300/00
摘要： The invention discloses a composition comprising hyaluronic acid with a high molecular weight and povidone-iodine in low amount that has advantageous efficacy in enhancing wound healing and maintains high stability. Also disclosed is a method of using the composition of the invention in healing wounds.
摘要翻译：本发明公开了一种组合物，其含有低分子量的透明质酸和聚维酮碘，其在增强伤口愈合方面具有有利的效果并保持高稳定性。还公开了使用本发明的组合物治疗伤口的方法。

8. 发明授权

US09308203B2 Pressure sensitive adhesive matrix device or system for the treatment or prevention of onychomycosis or tinea pedis 有权
标题翻译：用于治疗或预防甲真菌病或足癣的压敏粘合剂基质装置或系统
公开(公告)号：US09308203B2
公开(公告)日：2016-04-12
申请号：US12570656
申请日：2009-09-30
申请人： Kuo-Hua Yang , Yung-Jin Lee , Li-Chin Lin
发明人： Kuo-Hua Yang , Yung-Jin Lee , Li-Chin Lin
IPC分类号： A61K9/70 , A61K47/14 , A61K31/496
CPC分类号： A61K31/496 , A61K9/7023 , A61K9/7061 , A61K47/14
摘要： Disclosed is a pressure-sensitive adhesive matrix patch device for treatment or prevention of fungal toenails or fingernails or foot infections comprising an antifungal agent or two or more antifungals in combination and adhesively secured to a dorsal site of an infected palm or foot, rather than an area of infection and surrounding skin. A method for the transdermal treatment or prevention of fungal toenails or fingernails or foot infections with an antifungal agent is also disclosed, the method comprising adhesively securing to a dorsal site of an infected palm or foot a pressure-sensitive adhesive matrix patch device for a time sufficient to deliver an effective amount of the antifungal agent to an area of infection.
摘要翻译：公开了一种用于治疗或预防真菌趾甲或指甲或足部感染的压敏粘合剂基质贴片装置，其包含抗真菌剂或两种或更多种抗真菌剂的组合，并且粘附地固定到感染的手掌或足部的背部，而不是感染区域和周围皮肤。还公开了用抗真菌剂透皮治疗或预防真菌脚趾甲或指甲或足部感染的方法，所述方法包括将感染的手掌或足部的背部部位粘合固定一段时间的压敏粘合剂基质贴片装置足以将有效量的抗真菌剂递送至感染区域。

9. 发明授权

US08868225B2 Server for integrated pharmaceutical analysis and report generation service, method of integrated pharmaceutical manufacturing and research and development numerical analysis, and computer readable recording medium 有权
标题翻译：集成药物分析和报告生成服务的服务器，药物制药综合制造与研发数值分析方法，计算机可读记录介质
公开(公告)号：US08868225B2
公开(公告)日：2014-10-21
申请号：US13102818
申请日：2011-05-06
申请人： Yung-Jin Lee , Ching-Feng Wang , Hung-Liang Chen , Ju-Min Chiu
发明人： Yung-Jin Lee , Ching-Feng Wang , Hung-Liang Chen , Ju-Min Chiu
IPC分类号： G06F19/00 , G06Q50/22 , G06Q10/10
CPC分类号： G06Q10/10 , G06F19/00 , G06Q50/22
摘要： A web-based tool (as a server) for integrated pharmaceutical analysis and report generation service is provided in the present invention. The server can be used for numerical analysis and report generation for pharmaceutical manufacturing, research and development, and has advantages such as simple operation, complicated but fast calculation and professional report generation, and high accuracy. The server includes at least one pharmaceutical manufacturing and research and development numerical analysis system configured to perform different pharmaceutical manufacturing and research and development numerical analyses and generate different reports. Each of the at least one pharmaceutical manufacturing and research and development numerical analysis system includes an input module configured to receive, via a user interface, at least one of a template file and a backup file previously output by the server as at least one input file, wherein the at least one input file includes a plurality of data fields to provide corresponding data; at least one calculation module, each configured to execute a built-in pharmaceutical manufacturing and research and development numerical analysis calculation program, thereby automatically performing a pharmaceutical manufacturing and research and development numerical analysis calculation on at least one of the data of the at least one input file and on-line filled data; and an output module configured to generate at least one of a backup file and a report file as at least one output file based on the result of the pharmaceutical manufacturing and research and development numerical analysis calculation performed by the at least one calculation module and provide the at least one file via the user interface.
摘要翻译：本发明提供了用于集成药物分析和报告生成服务的基于网络的工具（作为服务器）。服务器可用于药品制造，研发的数值分析和报告生成，具有操作简单，计算复杂，计算专业，报表生成精度高，精度高等优点。该服务器包括至少一个药物制造和研发数值分析系统，配置为执行不同的药物制造和研究与开发数值分析，并生成不同的报告。所述至少一个药物制造和研发数值分析系统中的每一个包括输入模块，该输入模块被配置为经由用户界面接收由服务器预先输出的模板文件和备份文件中的至少一个作为至少一个输入文件，其中所述至少一个输入文件包括多个数据字段以提供对应的数据; 至少一个计算模块，每个计算模块被配置为执行内置的药物制造和研发数值分析计算程序，从而自动对所述至少一个的数据中的至少一个数据进行药物制造和研究与开发数值分析计算输入文件和在线填充数据; 以及输出模块，被配置为基于由所述至少一个计算模块执行的药物制造和研究和开发数值分析计算的结果，将备份文件和报告文件中的至少一个作为至少一个输出文件，并且提供至少一个文件通过用户界面。

10. 发明授权

US08765997B2 Process for preparing 4-borono-L-phenylalanine 有权
标题翻译：制备4-二羟基-L-苯丙氨酸的方法
公开(公告)号：US08765997B2
公开(公告)日：2014-07-01
申请号：US13910233
申请日：2013-06-05
申请人： Taiwan Biotech Co., Ltd.
发明人： Chia-Cheng Shaw , Kuen-Wang Sheu , Shu-Fen Huang
IPC分类号： C07C229/00
CPC分类号： C07F5/025 , C07F5/02 , Y02P20/55
摘要： Provided is a process for preparing 4-borono-L-phenylalanine, which has steps of: reacting N-protected (S)-4-halophenylalanine of formula (I), a boronating agent and an organolithium to obtain a reaction mixture, wherein the reaction mixture comprises N-protected (S)-4-boronophenylalanine of formula (II) and the R group represents a protecting group; isolating the N-protected (S)-4-boronophenylalanine from the reaction mixture; deprotecting the R group of the N-protected (S)-4-boronophenylalanine to obtain L-BPA.
摘要翻译：提供了制备4-二羟基-L-苯丙氨酸的方法，其具有以下步骤：使式（I）的N-保护的（S）-4-卤代苯丙氨酸，硼化剂和有机锂反应，得到反应混合物，其中反应混合物包含式（II）的N-保护的（S）-4-硼苯丙氨酸，R基团表示保护基; 从反应混合物中分离N-保护的（S）-4-硼苯丙氨酸; 使N-保护的（S）-4-硼苯丙氨酸的R基脱保护而获得L-BPA。

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