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1. 发明申请

WO2004110343A3 2-AMINO-9-(2-SUBSTITUTED ETHYL)PURINES AND PREPARING METHODS FOR 9-[4-ACETOXY-3-(ACETOXYMETHYL)BUT-1-YL]- 2- AMINOPURINE USING THE SAME 审中-公开
标题翻译： 2-氨基-9-（2-取代的乙醇）和9- [4-乙酰氧基-3-（乙酰氧基甲基）丁-1-炔基] -2-氨基嘌呤的制备方法
公开(公告)号：WO2004110343A3
公开(公告)日：2005-09-01
申请号：PCT/KR2004001405
申请日：2004-06-12
申请人： KYUNGDONG PHARM CO LTD , LEE BYOUNG-SUK , SHIN SANG-HOON , PARK JONG-SIK
发明人： LEE BYOUNG-SUK , SHIN SANG-HOON , PARK JONG-SIK
IPC分类号： A61K20060101 , 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。

2. 发明申请

WO2005013960A1 PREPARING METHOD FOR CONTROLLED RELEASED TYPE TABLET TAMSULOSIN HCL AND THE TABLET THEREOF 审中-公开
标题翻译：受控释放型片剂TAMSULOSIN HCL及其片剂的制备方法
公开(公告)号：WO2005013960A1
公开(公告)日：2005-02-17
申请号：PCT/KR2004/001421
申请日：2004-06-15
申请人： KYUNGDONG PHARM. CO., LTD. , LEE, BYOUNG-SUK , LEE, AH-RAM , PARK, JONG-SIK , KIM, EUN-JU , GIL, HYUNG-JOON
发明人： LEE, BYOUNG-SUK , LEE, AH-RAM , PARK, JONG-SIK , KIM, EUN-JU , GIL, HYUNG-JOON
IPC分类号： A61K31/18
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 HCI 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/二苯甲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。

3. 发明申请

WO2004007497A1 PROCESS FOR PREPARING 9-[4-ACETOXY-3-(ACETOXYMETHYL)BUT-1-YL]-2-AMINOPURINE 审中-公开
标题翻译：制备9- [4-乙酰氧基-3-（乙酰氧基甲基）丁-1-基] -2-氨基嘌呤的方法
公开(公告)号：WO2004007497A1
公开(公告)日：2004-01-22
申请号：PCT/KR2003/001396
申请日：2003-07-15
申请人： KYUNGDONG PHARM. CO., LTD. , LEE, Byoung-Suk , SHIN, Sang-Hoon
发明人： LEE, Byoung-Suk , SHIN, Sang-Hoon
IPC分类号： C07D473/32
CPC分类号： C07D473/00
摘要： Disclosed is a process for preparing 9-[4-acetoxy-3-(acetoxymethyl)but-1-yl]-2-aminopurine (called Famciclovir), a drug of purine derivatives having antiviral activity. This process comprises reacting 2-aminopurine with 2-acetoxymethyl-4-bromobut-1-yl-acetate in the presence of thallium (I) ethoxide to give the desired compound. According to this process, the desired compound can be prepared in very high selectivity and purity under mild reaction conditions.
摘要翻译：公开了一种制备具有抗病毒活性的嘌呤衍生物的9- [4-乙酰氧基-3-（乙酰氧基甲基）丁-1-基] -2-氨基嘌呤（称为泛昔洛韦）的方法。该方法包括在乙酸铊（I）存在下使2-氨基嘌呤与2-乙酰氧基甲基-4-溴丁-1-基 - 乙酸酯反应，得到所需化合物。根据该方法，可以在温和的反应条件下以非常高的选择性和纯度制备所需化合物。

4. 发明申请

WO2004110343A2 2-AMINO-9-(2-SUBSTITUTED ETHYL)PURINES AND PREPARING METHODS FOR 9-[4-ACETOXY-3-(ACETOXYMETHYL)BUT-1-YL]- 2- AMINOPURINE USING THE SAME 审中-公开
标题翻译： 2-氨基-9-（2-取代的乙醇）和9- [4-乙酰氧基-3-（乙酰氧基甲基）丁-1-炔基] -2-氨基嘌呤的制备方法
公开(公告)号：WO2004110343A2
公开(公告)日：2004-12-23
申请号：PCT/KR2004/001405
申请日：2004-06-12
申请人： KYUNGDONG PHARM. CO., LTD. , LEE, Byoung-Suk , SHIN, Sang-Hoon , PARK, Jong-Sik
发明人： LEE, Byoung-Suk , SHIN, Sang-Hoon , PARK, Jong-Sik
IPC分类号： A61K
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。

5. 发明申请

WO2002066436A1 PROCESS FOR PREPARING 2-(4-CHLOROBENZOLAMINO) -3-[2(1H) -QUINOLINON-4-YL]PROPRIONIC ACID 审中-公开
标题翻译：制备2-（4-氯苯甲酰氨基）-3- [2（1H） - 喹啉-4-基]丙酸的方法
公开(公告)号：WO2002066436A1
公开(公告)日：2002-08-29
申请号：PCT/KR2002/000262
申请日：2002-02-20
申请人： KYUNG DONG PHARM., CO., LTD , LEE, Byoung-suk , CHUN, Myung-hee
发明人： LEE, Byoung-suk , CHUN, Myung-hee
IPC分类号： C07D215/14
CPC分类号： C07D215/227 , C07C233/83
摘要： The invention relates to a novel method for preparing 2_(4_chlorobenzoylamino)_3_[2(1H)_quinolinon_4_yl] propionic acid, also known as Rebamipide represented by the formula I and useful for treatement of peptic ulcer from alkyl 2_(4_chlorobenzoylamino)_2_alkoxycarbonyl_3_[2(1H)_quinolinon_4_ yl] propionate represented by the formula II in the presence of a base solution for hydrolisis and decarboxylation to remove a carboxyl group:
摘要翻译：本发明涉及一种制备2-（4-氯苯甲酰氨基）-3- [2（1H） - 喹啉-4-基]丙酸的新方法，也称为由式I表示的瑞巴米特，可用于从烷基2（4-氯苯甲酰氨基）-2-烷氧基羰基-3 [[ 1H）_喹啉-4-基]丙酸乙酯在碱溶液存在下进行水解和脱羧以除去羧基：

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