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1.发明授权1-α-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivatives and process for the preparation thereof 失效1-α-卤代-2,2-二氟-2-脱氧-D-呋喃核糖衍生物及其制备方法公开(公告)号：US07858761B2
公开(公告)日：2010-12-28
申请号：US11572790
申请日：2005-06-21
Applicant: Jaeheon Lee , Gha-Seung Park , Moonsub Lee , Han Kyong Kim , Hyo-Jeong Bang , Young-Kil Chang , Gwan Sun Lee
Inventor： Jaeheon Lee , Gha-Seung Park , Moonsub Lee , Han Kyong Kim , Hyo-Jeong Bang , Young-Kil Chang , Gwan Sun Lee
CPC classification number: C07H3/08
Abstract: 1-α-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivative of formula (I) having the 3-hydroxy group protected with a biphenylcarbonyl group is a solid which can be easily purified by a simple procedure such as recrystallization, and therefore, it can be advantageously used as an intermediate in the preparation of gemcitabine in a large scale. Further, the 1-α-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivative of formula (I) can be prepared with high stereoselectivity using the compound of formula (V) as an intermediate.
Abstract translation: 具有用联苯基羰基保护的3-羟基的式（I）的1-α-卤代-2,2-二氟-2-脱氧-D-呋喃核糖衍生物是可以通过简单的方法容易地纯化的固体，例如 重结晶，因此可以有利地用作大量制备吉西他滨的中间体。 此外，式（I）的1-α-卤代-2,2-二氟-2-脱氧-D-呋喃核糖衍生物可以使用式（V）化合物作为中间体以高立体选择性制备。
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公开(公告)号：US20080194828A1
公开(公告)日：2008-08-14
申请号：US11996657
申请日：2006-07-11
Applicant: Tae Hee Ha , Won Jeong Kim , Hee Sook Oh , Chang Hee Park , Jae Chul Lee , Han Kyong Kim , Kwee-Hyun Suh
Inventor： Tae Hee Ha , Won Jeong Kim , Hee Sook Oh , Chang Hee Park , Jae Chul Lee , Han Kyong Kim , Kwee-Hyun Suh
IPC: C07D401/12 , A61P1/04
CPC classification number: C07D401/12
Abstract: Optically pure esomeprazole and its salt can be simply prepared by dissolving (S)-(−)-binol, a weak base and the racemic form of omeprazole in a mixture of a water-compatible organic solvent and water at a high temperature, cooling the mixed solution to crystallize the inclusion complex of esomeprazole and (S)-(−)-binol, and removing the (S)-(−)-binol moiety from the crystallized inclusion complex.
Abstract translation: 光学纯的埃索美拉唑及其盐可以简单地通过将（S） - （ - ） - 二醇，弱碱和外消旋形式的奥美拉唑在高温下溶解在与水相容的有机溶剂和水的混合物中，冷却 混合溶液以结晶埃索美拉唑和（S） - （ - ） - 二醇的包合络合物，并从结晶的包合物中除去（S） - （ - ） - 二醇部分。
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3.发明申请METHOD FOR PREPARING (3S,4S)-4-((R)-2-(BENZYLOXY)TRIDECYL)-3-HEXYL-2-OXETANONE AND NOVEL INTERMEDIATE USED THEREFOR 失效制备（3S，4S）-4 - （（R）-2-（苄氧基）吡啶-3-基）-3-甲基-2-氧代西他酮的方法及其所用的新型中间体公开(公告)号：US20110178330A1
公开(公告)日：2011-07-21
申请号：US13120561
申请日：2009-10-30
Applicant: Sang Min Yun , Dong Jin Hong , Weon Ki Yang , Jae Ho Yoo , Ji Sook Kim , Moon Sub Lee , Han Kyong Kim , Eun Jung Lim , Young Ho Moon , Young-Kil Chang , Gwan Sun Lee
Inventor： Sang Min Yun , Dong Jin Hong , Weon Ki Yang , Jae Ho Yoo , Ji Sook Kim , Moon Sub Lee , Han Kyong Kim , Eun Jung Lim , Young Ho Moon , Young-Kil Chang , Gwan Sun Lee
IPC: C07C53/00
CPC classification number: C07D305/12 , C07C51/09 , C07C51/353 , C07C59/29 , C07C59/72
Abstract: The present invention relates to a high-yield method for preparing highly pure (3S,4S)-4-((R)-2-(benzyloxy)tridecyl)-3-hexyl-2-oxetanone using a metal salt of (2S,3S,5R)-2-hexyl-3,5-dihydroxyhexadecanoic acid as an intermediate.
Abstract translation: 本发明涉及使用（2S，4S）-4 - （（R）-2-（苄氧基）十三烷基）-3-己基-2-氧杂环丁酮的金属盐制备高纯度 3S，5R）-2-己基-3,5-二羟基十六烷酸作为中间体。
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公开(公告)号：US07888511B2
公开(公告)日：2011-02-15
申请号：US11996657
申请日：2006-07-11
Applicant: Tae Hee Ha , Won Jeong Kim , Hee Sook Oh , Chang Hee Park , Jae Chul Lee , Han Kyong Kim , Kwee-Hyun Suh
Inventor： Tae Hee Ha , Won Jeong Kim , Hee Sook Oh , Chang Hee Park , Jae Chul Lee , Han Kyong Kim , Kwee-Hyun Suh
IPC: C07D401/12
CPC classification number: C07D401/12
Abstract: Optically pure esomeprazole and its salt can be simply prepared by dissolving (S)-(−)-binol, a weak base and the racemic form of omeprazole in a mixture of a water-compatible organic solvent and water at a high temperature, cooling the mixed solution to crystallize the inclusion complex of esomeprazole and (S)-(−)-binol, and removing the (S)-(−)-binol moiety from the crystallized inclusion complex.
Abstract translation: 光学纯的埃索美拉唑及其盐可以简单地通过将（S） - （ - ） - 二醇，弱碱和外消旋形式的奥美拉唑在高温下溶解在与水相容的有机溶剂和水的混合物中，冷却 混合溶液以结晶埃索美拉唑和（S） - （ - ） - 二醇的包合络合物，并从结晶的包合物中除去（S） - （ - ） - 二醇部分。
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公开(公告)号：US20100190983A1
公开(公告)日：2010-07-29
申请号：US12669002
申请日：2008-08-04
Applicant: Young Ho Moon , Moon Sub Lee , Jae Ho Yoo , Ji Sook Kim , Han Kyong Kim , Chang Ju Choi , Young Kil Chang , Gwan Sun Lee
Inventor： Young Ho Moon , Moon Sub Lee , Jae Ho Yoo , Ji Sook Kim , Han Kyong Kim , Chang Ju Choi , Young Kil Chang , Gwan Sun Lee
IPC: C07D239/38 , C07D403/06
CPC classification number: C07D403/06
Abstract: Optically pure voriconazole can be prepared in a high yield by a) subjecting 1-(2,4-difluorophenyl)-2(1H-1,2,4-triazol-1-yl)ethanone to Reformatsky-type coupling reaction with a substituted thiopyrimidine derivative to obtain a desired (2R,3S)/(2S,3R)-enantiomeric pair; b) removing the thiol derivative from the enantiomer to obtain racemic voriconazole; and c) isolating the racemic voriconazole by way of optical resolution using an optically active acid.
Abstract translation: 可以通过以下方法制备光学纯的伏立康唑：a）使1-（2,4-二氟苯基）-2（1H-1,2,4-三唑-1-基）乙酮与取代基进行重新加成型偶联反应 硫代嘧啶衍生物，得到所需的（2R，3S）/（2S，3R） - 对映异构体对; b）从对映异构体中除去硫醇衍生物，得到外消旋的伏立康唑; 和c）使用光学活性酸通过光学拆分分离外消旋的伏立康唑。
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Patent Agency Ranking
6.发明申请METHOD OF PREPARING S-(-)-AMLODIPINE OR A SALT THEREOF AND AN INTERMEDIATE USED THEREIN 审中-公开制备S - （ - ） - 阿米膦酸或其盐及其使用的中间体的方法公开(公告)号：US20100099884A1
公开(公告)日：2010-04-22
申请号：US12523957
申请日：2008-01-29
Applicant: Sun Young JANG , Sungbum Kim , Sangmin Yun , Hyo Jeong Bang , Han Kyong Kim , Kwee Hyun Suh
Inventor： Sun Young JANG , Sungbum Kim , Sangmin Yun , Hyo Jeong Bang , Han Kyong Kim , Kwee Hyun Suh
IPC: C07D213/803
CPC classification number: C07D211/90
Abstract: The present invention provides a novel method for preparing S-(−)-amlodipine having a high optical purity or a salt thereof and an intermediate used therein.
Abstract translation: 本发明提供了一种制备具有高光学纯度的S - （ - ） - 氨氯地平或其盐和其中使用的中间体的新方法。
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7.发明申请Crystalline Azithromycin L-Malate Monohydrate and Pharmaceutical Composition Containing Same 审中-公开结晶阿奇霉素L-苹果酸一水合物和含有其的药物组合物公开(公告)号：US20090318375A1
公开(公告)日：2009-12-24
申请号：US11915929
申请日：2003-06-06
Applicant: Bo Sung Kwon , Eun Sook Kim , Hee Cheol Kim , Sangmin Yun , Myoung-sil Ko , Tae Hun Song , Han Kyong Kim , Kwee Hyun Suh , Gwansun Lee
Inventor： Bo Sung Kwon , Eun Sook Kim , Hee Cheol Kim , Sangmin Yun , Myoung-sil Ko , Tae Hun Song , Han Kyong Kim , Kwee Hyun Suh , Gwansun Lee
IPC: A61K31/7048 , C07H17/08 , A61P31/00
CPC classification number: C07H17/08
Abstract: This invention provides a crystalline azithromycin L-malate monohydrate for treating various microbial infections, which has high thermostability, solubility and non-hygroscopicity, a method for preparing same, and a pharmaceutical composition containing same.
Abstract translation: 本发明提供了一种用于治疗各种微生物感染的结晶阿奇霉素L-苹果酸盐一水合物，其具有高的热稳定性，溶解性和非吸湿性，其制备方法和含有它们的药物组合物。
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8.发明申请PHARMACEUTICAL COMPOSITION CONTAINING CLOPIDOGREL CAMPHORSULFONATE OR POLYMORPHIC FORMS THEREOF 审中-公开含有角叉菜酮或其多形态的药物组合物公开(公告)号：US20090209576A1
公开(公告)日：2009-08-20
申请号：US12293357
申请日：2007-03-15
Applicant: Won Jeoung Kim , Han Kyong Kim , Kwee Hyun Suh , Gwan Sun Lee
Inventor： Won Jeoung Kim , Han Kyong Kim , Kwee Hyun Suh , Gwan Sun Lee
IPC: A61K31/4365 , C07D495/04 , A61P7/00
CPC classification number: A61K31/47
Abstract: A pharmaceutical composition of the present invention which comprises clopidogrel camphorsulfonate of formula (I) or its polymorphic forms as an active ingredient is useful for treating or preventing a platelet aggregation-associated disease.
Abstract translation: 包含式（I）的氯吡格雷樟脑磺酸盐或其多晶型物质作为活性成分的本发明的药物组合物可用于治疗或预防血小板聚集相关疾病。
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公开(公告)号：US20070249818A1
公开(公告)日：2007-10-25
申请号：US11573869
申请日：2003-12-29
Applicant: Jaeheon Lee , Gha Seung Park , Moonsub Lee , Hyo-Jeong Bang , Jae Lee , Cheol Kim , Chang-Ju Choi , Han Kyong Kim , Hoe Chul Lee , Young-Kil Chang , Gwan Lee
Inventor： Jaeheon Lee , Gha Seung Park , Moonsub Lee , Hyo-Jeong Bang , Jae Lee , Cheol Kim , Chang-Ju Choi , Han Kyong Kim , Hoe Chul Lee , Young-Kil Chang , Gwan Lee
IPC: C07H19/00
Abstract: This invention relates to an improved method for stereoselectively preparing 2¢¥-deoxy-2¢¥,2¢¥-difluorocytidine of formula (I), which comprises the steps of reacting a 1-halo ribofuranose compound of formula (III) with a nucleobase of formula (IV) in a solvent to obtain a nucleoside of formula (II) with removing the silyl halide of formula (V) produced during the reaction; and deprotecting the nucleoside of formula (II) to obtain 2¢¥-deoxy-2¢¥,2¢¥-difluorocytidine of formula (I).
Abstract translation: 本发明涉及一种用于立体选择性制备式（I）的2'-二脱氧-2¢¥，2¢-二氟胞苷的改进方法，其包括以下步骤：使式（III）的1-卤代呋喃核糖化合物与 （IV）的核碱基在溶剂中得到式（II）的核苷，同时除去反应中产生的式（Ⅴ）的甲硅烷基卤化物; 并使式（II）的核苷脱保护，得到式（I）的2¢¥脱氧-2¢¥，2¢¥ - 二氟胞苷。
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10.发明授权Pharmaceutical composition comprising crystalline sibutramine methanesulfonate hemihydrate 失效包含结晶西布曲明甲磺酸盐半水合物的药物组合物公开(公告)号：US06900245B2
公开(公告)日：2005-05-31
申请号：US10678325
申请日：2003-10-03
Applicant: Jae-Heon Lee , Gha-Seung Park , Jae-Cheol Lee , Han-Kyong Kim , Young-Kil Chang , Gwan-Sun Lee
Inventor： Jae-Heon Lee , Gha-Seung Park , Jae-Cheol Lee , Han-Kyong Kim , Young-Kil Chang , Gwan-Sun Lee
IPC: A61K31/13 , A61K31/205
CPC classification number: A61K31/205 , C30B7/00
Abstract: The present invention relates to a pharmaceutical composition for treating or preventing obesity, comprising novel crystalline sibutramine methanesulfonate hemihydrate of formula (I). The crystalline sibutramine methanesulfonate hemihydrate according to the present invention has a much higher solubility in water, and enhanced stability under a high humidity/temperature condition, as compared with sibutramine hydrochloride monohydrate
Abstract translation: 本发明涉及用于治疗或预防肥胖症的药物组合物，其包含式（I）的新型结晶西布曲明甲磺酸盐半水合物。 与西布曲明盐酸盐一水合物相比，本发明的结晶西布曲明甲磺酸盐半水合物在水中的溶解度高，并且在高湿度/温度条件下提高了稳定性
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