公开(公告)号：US07456282B2

公开(公告)日：2008-11-25

申请号：US10554676

申请日：2004-06-12

申请人： Byoung-Suk Lee ,  Sang-Hoon Shin ,  Jong-Sik Park

发明人： Byoung-Suk Lee ,  Sang-Hoon Shin ,  Jong-Sik Park

IPC分类号： C07D473/32

CPC分类号： C07D473/32

摘要： The present invention relates to a new compound of 2-amino-9-(2-substituted ethyl)purine and an effective method for preparing 9-[4-acetoxy-3-(acetoxymethyl)but-1-yl]-2-aminopurin (famciclovir) using the same. The 2-amino-9-(2-substituted ethyl)purine according to the invention is represented by the following formula (II′): (Formula II′) wherein R is a hydroxy, halogen, mesyloxy or tosyloxy group. The inventive method for the preparation of famciclovir comprises the steps of halogenating 2-amino-9-(2-substituted ethyl)purine to give 2-amino-9-(2-halogenoethyl)purine, and reacting the halogenated compound with diethylmalonate. The inventive preparation method allows famciclovir, a purine derivative drug with effective antiviral activity, to be prepared in a high selectivity of 100% in a pure form by using the inventive new compound of 2-amino-9-(2-substituted ethyl)purine. In addition, the inventive method allows the utilization of relatively mild reaction conditions, and thus, has high industrial process efficiency.

摘要翻译： 本发明涉及2-氨基-9-（2-取代乙基）嘌呤的新化合物和制备9- [4-乙酰氧基-3-（乙酰氧基甲基）丁-1-基] -2-氨基嘌呤的有效方法 （泛昔洛韦）使用相同。 根据本发明的2-氨基-9-（2-取代的乙基）嘌呤由下式（II'）表示：（式II'）其中R是羟基，卤素，甲磺酰氧基或甲苯磺酰氧基。 用于制备泛昔洛韦的本发明方法包括以下步骤：将2-氨基-9-（2-取代的乙基）嘌呤卤化，得到2-氨基-9-（2-卤代乙基）嘌呤，并使卤代化合物与丙二酸二乙酯反应。 本发明的制备方法允许泛昔洛韦（一种具有有效抗病毒活性的嘌呤衍生物）通过使用本发明新的2-氨基-9-（2-取代的乙基）嘌呤化合物以高纯度的100％选择性制备 。 此外，本发明的方法允许利用相对温和的反应条件，因此具有高工业过程效率。

公开(公告)号：US20060258862A1

公开(公告)日：2006-11-16

申请号：US10554676

申请日：2004-06-12

申请人： Byoung-Suk Lee ,  Sang-Hoon Shin ,  Jong-Sik Park

发明人： Byoung-Suk Lee ,  Sang-Hoon Shin ,  Jong-Sik Park

IPC分类号： C07D473/12

CPC分类号： C07D473/32

摘要： The present invention relates to a new compound of 2-amino-9-(2-substituted ethyl)purine and an effective method for preparing 9-[4-acetoxy-3-(acetoxymethyl)but-1-yl]-2-aminopurin (famciclovir) using the same. The 2-amino-9-(2-substituted ethyl)purine according to the invention is represented by the following formula (II′): (Formula II′) wherein R is a hydroxy, halogen, mesyloxy or tosyloxy group. The inventive method for the preparation of famciclovir comprises the steps of halogenating 2-amino-9-(2-substituted ethyl)purine to give 2-amino-9-(2-halogenoethyl)purine, and reacting the halogenated compound with diethylmalonate. The inventive preparation method allows famciclovir, a purine derivative drug with effective antiviral activity, to be prepared in a high selectivity of 100% in a pure form by using the inventive new compound of 2-amino-9-(2-substituted ethyl)purine. In addition, the inventive method allows the utilization of relatively mild reaction conditions, and thus, has high industrial process efficiency.

摘要翻译： 本发明涉及2-氨基-9-（2-取代乙基）嘌呤的新化合物和制备9- [4-乙酰氧基-3-（乙酰氧基甲基）丁-1-基] -2-氨基嘌呤的有效方法 （泛昔洛韦）使用相同。 根据本发明的2-氨基-9-（2-取代的乙基）嘌呤由下式（II'）表示：（式II'）其中R是羟基，卤素，甲磺酰氧基或甲苯磺酰氧基。 用于制备泛昔洛韦的本发明方法包括以下步骤：将2-氨基-9-（2-取代的乙基）嘌呤卤化得到2-氨基-9-（2-卤代乙基）嘌呤，并使该卤代化合物与丙二酸二乙酯反应。 本发明的制备方法允许泛昔洛韦（一种具有有效抗病毒活性的嘌呤衍生物）通过使用本发明新的2-氨基-9-（2-取代的乙基）嘌呤化合物以高纯度的100％选择性制备 。 此外，本发明的方法允许利用相对温和的反应条件，因此具有高工业过程效率。

公开(公告)号：US20060204570A1

公开(公告)日：2006-09-14

申请号：US10565987

申请日：2004-06-15

申请人： Byoung-Suk Lee ,  Ah-Ram Lee ,  Jong-Sik Park ,  Eun-Ju Kim ,  Hyung-Joon Gil

发明人： Byoung-Suk Lee ,  Ah-Ram Lee ,  Jong-Sik Park ,  Eun-Ju Kim ,  Hyung-Joon Gil

IPC分类号： B27N3/00 ,  A61K9/22

CPC分类号： A61K9/2018 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/2095 ,  A61K31/137 ,  A61K31/18 ,  Y10S514/96 ,  Y10S514/961 ,  Y10S514/964

摘要： The present invention relates to a simple and effective method for preparing a tamsulosin HCl sustained-release tablet and a tamsulosin HCl sustained-release tablet produced thereby. The method comprises the steps of: dissolving tamsulosin HCl as an active ingredient in an organic solvent; dissolving the tamsulosin HCl solution in hydroxypropylmethylcellulose phthalate to prepare a binder solution; and kneading the binder solution with a hydroxypropylmethylcellulose phthalate/glyceryl dibehenate mixture as an excipient and allows tamsulosin HCl to be released at uniformly controlled amounts in a subtained-release manner in vivo by controlling drug release rate according to different pH environments in vivo, so that it shows improved bioavailability and minimized side effects.

摘要翻译： 本发明涉及一种简单而有效的制备坦索罗辛缓释片剂和由此制备的坦索罗辛缓释片剂的方法。 该方法包括：将坦索罗辛HCl作为活性成分溶解于有机溶剂中; 将盐酸坦洛新溶液溶解在羟丙基甲基纤维素邻苯二甲酸酯中以制备粘合剂溶液; 并将粘合剂溶液与羟丙基甲基纤维素邻苯二甲酸酯/二乙酸甘油酯混合物作为赋形剂捏合，并且通过根据体内不同的pH环境控制药物释放速率，以体内释放的方式以均匀的控制量释放坦索罗辛HCl，使得 它显示出改进的生物利用度和最小化的副作用。

公开(公告)号：US07314638B2

公开(公告)日：2008-01-01

申请号：US10565987

申请日：2004-06-15

申请人： Byoung-Suk Lee ,  Ah-Ram Lee ,  Jong-Sik Park ,  Eun-Ju Kim ,  Hyung-Joon Gil

发明人： Byoung-Suk Lee ,  Ah-Ram Lee ,  Jong-Sik Park ,  Eun-Ju Kim ,  Hyung-Joon Gil

IPC分类号： A61K31/18 ,  A61K9/22 ,  A61K9/24 ,  A61K47/14 ,  A61P13/00 ,  A61P13/08

CPC分类号： A61K9/2018 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/2095 ,  A61K31/137 ,  A61K31/18 ,  Y10S514/96 ,  Y10S514/961 ,  Y10S514/964

摘要： The present invention relates to a simple and effective method for preparing a tamsulosin HCl sustained-release tablet and a tamsulosin HCl sustained-release tablet produced thereby. The method comprises the steps of: dissolving tamsulosin HCl as an active ingredient in an organic solvent; dissolving the tamsulosin HCl solution in hydroxypropylmethylcellulose phthalate to prepare a binder solution; and kneading the binder solution with a hydroxypropylmethylcellulose phthalate/glyceryl dibehenate mixture as an excipient and allows tamsulosin HCl to be released at uniformly controlled amounts in a subtained-release manner in vivo by controlling drug release rate according to different pH environments in vivo, so that it shows improved bioavailability and minimized side effects.

摘要翻译： 本发明涉及一种简单而有效的制备坦索罗辛缓释片剂和由此制备的坦索罗辛缓释片剂的方法。 该方法包括：将坦索罗辛HCl作为活性成分溶解于有机溶剂中; 将盐酸坦洛新溶液溶解在羟丙基甲基纤维素邻苯二甲酸酯中以制备粘合剂溶液; 并将粘合剂溶液与羟丙基甲基纤维素邻苯二甲酸酯/二乙酸甘油酯混合物作为赋形剂捏合，并且通过根据体内不同的pH环境控制药物释放速率，以体内释放的方式以均匀的控制量释放坦索罗辛HCl，使得 它显示出改进的生物利用度和最小化的副作用。

公开(公告)号：US07086871B2

公开(公告)日：2006-08-08

申请号：US10960969

申请日：2004-10-12

申请人： Jong-Sik Park

发明人： Jong-Sik Park

IPC分类号： H01R12/00

CPC分类号： H01R12/716 ,  H05K1/18 ,  H05K2201/10189 ,  H05K2201/10446

摘要： A bent wafer and a PCB assembly for a refrigerator provided with the same includes a bent wafer including a wafer body formed in a bent shape and a plurality of pin terminals coupled to the wafer body and a PCB having a quadrangular shape, on which wafer including the bent wafer are mounted, thereby compactly mounting the wafer on the PCB, relatively reducing a size of the PCB, and reducing the number of assembling processes for mounting the wafer on the PCB.

摘要翻译： 具有该弯曲晶片的弯曲晶片和用于冰箱的印刷电路板组件包括：弯曲晶片，其包括形成为弯曲形状的晶片本体和耦合到晶片体的多个引脚端子和具有四边形形状的PCB，晶片包括 安装弯曲的晶片，从而将晶片紧凑地安装在PCB上，相对减小PCB的尺寸，并减少将晶片安装在PCB上的组装过程的数量。

公开(公告)号：US20050085108A1

公开(公告)日：2005-04-21

申请号：US10960969

申请日：2004-10-12

申请人： Jong-Sik Park

发明人： Jong-Sik Park

IPC分类号： F25D29/00 ,  F25D11/00 ,  H01R12/00 ,  H01R24/00 ,  H05K1/18

CPC分类号： H01R12/716 ,  H05K1/18 ,  H05K2201/10189 ,  H05K2201/10446

摘要： A bent wafer and a PCB assembly for a refrigerator provided with the same includes a bent wafer including a wafer body formed in a bent shape and a plurality of pin terminals coupled to the wafer body and a PCB having a quadrangular shape, on which wafer including the bent wafer are mounted, thereby compactly mounting the wafer on the PCB, relatively reducing a size of the PCB, and reducing the number of assembling processes for mounting the wafer on the PCB.

摘要翻译： 具有该弯曲晶片的弯曲晶片和用于冰箱的印刷电路板组件包括：弯曲晶片，其包括形成为弯曲形状的晶片本体和耦合到晶片体的多个引脚端子和具有四边形形状的PCB，晶片包括 安装弯曲的晶片，从而将晶片紧凑地安装在PCB上，相对减小PCB的尺寸，并减少将晶片安装在PCB上的组装过程的数量。