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1. 发明申请

US20130116213A1 NOVEL FUSED PYRIMIDINE DERIVATIVES FOR INHIBITION OF TYROSINE KINASE ACTIVITY 有权
公开(公告)号：US20130116213A1
公开(公告)日：2013-05-09
申请号：US13805183
申请日：2011-06-20
申请人： Mi Young Cha , Seok Jong Kang , Mi Ra Kim , Ju Yeon Lee , Ji Young Jeon , Myoung Gi Jo , Eun Joo Kwak , Kwang Ok Lee , Tae Hee Ha , Kwee Hyun Suh , Maeng Sup Kim
发明人： Mi Young Cha , Seok Jong Kang , Mi Ra Kim , Ju Yeon Lee , Ji Young Jeon , Myoung Gi Jo , Eun Joo Kwak , Kwang Ok Lee , Tae Hee Ha , Kwee Hyun Suh , Maeng Sup Kim
IPC分类号： A61K31/675 , A61K31/519 , A61K31/5377 , C07D491/048 , C07F9/6561 , A61K31/553 , A61K31/55 , C07D495/04 , A61K31/541
CPC分类号： C07D495/04 , A61K31/519 , A61K31/5377 , A61K31/538 , A61K31/541 , A61K31/55 , A61K31/553 , A61K31/675 , A61K45/06 , C07D491/04 , C07D491/048 , C07D493/04 , C07D519/00 , C07F9/3834 , C07F9/6561
摘要： The present invention relates to a novel fused pyrimidine derivative having an inhibitory activity for tyrosine kinases, and a pharmaceutical composition for preventing or treating cancers, tumors, inflammatory diseases, autoimmune diseases, or immunologically mediated diseases comprising same as an active ingredient.

2. 发明授权

US08106076B2 Crystalline S-omeprazole strontium hydrate, method for preparing same, and pharmaceutical composition containing same 有权
标题翻译：结晶S-奥美拉唑锶水合物，其制备方法和含有它们的药物组合物
公开(公告)号：US08106076B2
公开(公告)日：2012-01-31
申请号：US12425499
申请日：2009-04-17
申请人： Tae Hee Ha , Hee Sook Oh , Won Jeoung Kim , Chang Hee Park , Eun Young Kim , Young Hoon Kim , Kwee Hyun Suh , Gwan Sun Lee
发明人： Tae Hee Ha , Hee Sook Oh , Won Jeoung Kim , Chang Hee Park , Eun Young Kim , Young Hoon Kim , Kwee Hyun Suh , Gwan Sun Lee
IPC分类号： A61K31/4439 , C07D401/12
CPC分类号： C07D401/12
摘要： This invention provides a crystalline S-omeprazole strontium hydrate for the prevention or treatment of gastric acid-related diseases, which has high optical purity, theremostability, solubility and nonhygroscopicity, a method for preparing same, and a pharmaceutical composition containing same.
摘要翻译：本发明提供了一种用于预防或治疗胃酸相关疾病的结晶性S-奥美拉唑水合锶，其具有高光学纯度，耐受性，溶解性和不吸湿性，其制备方法和含有该组合物的药物组合物。

3. 发明申请

US20090036683A1 METHOD FOR PREPARING CLOPIDOGREL 1,5-NAPHTHALENEDISULFONATE OR HYDRATE THEREOF 失效
标题翻译：制备氯硝酸盐的方法1,5-萘硫代磺酸盐或其水合物
公开(公告)号：US20090036683A1
公开(公告)日：2009-02-05
申请号：US12293959
申请日：2007-03-16
申请人： Kwee Hyun Suh , Sang Min Yun , Eun Sook Kim , Gwan Sun Lee
发明人： Kwee Hyun Suh , Sang Min Yun , Eun Sook Kim , Gwan Sun Lee
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The present invention relates to a method for preparing clopidogrel 1,5-naphthalenedisulfonate or a hydrate thereof, which comprises reacting a clopidogrel-acid addition salt with disodium 1,5-naphthalenedisulfonate or its hydrate in water, or a mixture of water and an organic solvent. High quality clopidogrel 1,5-naphthalenedisulfonate can be prepared by the inventive method by way of using non-corrosive disodium 1,5-naphthalenedisulfonate.
摘要翻译：本发明涉及一种氯吡格雷1,5-萘二磺酸盐或其水合物的制备方法，该方法包括使氯吡格雷酸加成盐与1,5-萘二磺酸二钠或其水合物在水中或水与有机物的混合物溶剂。通过本发明方法可以通过使用1,5-萘二磺酸非腐蚀性二钠制备高质量的氯萘吡格雷1,5-萘二磺酸盐。

4. 发明申请

US20070197789A1 Method of preparing thieno[3,2-c]pyridine derivatives and intermediates used therein 失效
标题翻译：噻吩并[3,2-c]吡啶衍生物及其中使用的方法
公开(公告)号：US20070197789A1
公开(公告)日：2007-08-23
申请号：US10598790
申请日：2005-03-03
申请人： Sangmin Yun , Eun Kim , Hee Kim , Tae Ha , Kwee-Hyun Suh , Gwan Lee
发明人： Sangmin Yun , Eun Kim , Hee Kim , Tae Ha , Kwee-Hyun Suh , Gwan Lee
IPC分类号： C07D498/02 , C07D311/94 , C07D333/04
CPC分类号： C07D333/38 , C07D333/12 , C07D333/16 , C07D333/18 , C07D495/04
摘要： Ticlopidine and clopidogrel having high blood platelet aggregation inhibitory and anti-thrombotic activities are simply prepared by reacting a substituted thiophene derivative with a 2-chlorobenzylamine derivative.
摘要翻译：通过使取代的噻吩衍生物与2-氯苄胺衍生物反应，简单地制备具有高血小板聚集抑制和抗血栓形成活性的噻氯匹定和氯吡格雷。

5. 发明授权

US07652140B2 Method of preparing clopidogrel and intermediates used therein 失效
标题翻译：制备氯吡格雷的方法及其中使用的中间体
公开(公告)号：US07652140B2
公开(公告)日：2010-01-26
申请号：US11917794
申请日：2005-11-28
申请人： Eun Sook Kim , Hee Cheol Kim , Bo Sung Kwon , Sangmin Yun , Mi Young Ko , Cheol Kyung Kim , Kwee Hyun Suh
发明人： Eun Sook Kim , Hee Cheol Kim , Bo Sung Kwon , Sangmin Yun , Mi Young Ko , Cheol Kyung Kim , Kwee Hyun Suh
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： Optically pure clopidogrel can be prepared in a high yield by optically resolving a racemic form of the compound of formula (II) using an optically active amine to form the optically active form of the compound of formula (III) or its acid-addition salt; and methylating the compound of formula (III) or its acid-addition salt.
摘要翻译：光学纯氯吡格雷可以通过光学拆分式（II）化合物的外消旋形式，使用光学活性胺形成式（III）化合物或其酸加成盐的光学活性形式，以高产率制备; 并使式（III）化合物或其酸加成盐进行甲基化。

6. 发明授权

US07205395B2 Process of preparing azithromycin and crystalline 9-deoxo-9a-aza-9a-homoerythromycin A hydrate used therein 失效
标题翻译：制备阿奇霉素和结晶9-脱氧-9a-氮杂-9a-高红霉素A水合物的方法
公开(公告)号：US07205395B2
公开(公告)日：2007-04-17
申请号：US10509934
申请日：2002-04-03
申请人： Gi Jeong Kim , Mi Ra Seong , Sang Min Yun , Kwee Hyun Suh
发明人： Gi Jeong Kim , Mi Ra Seong , Sang Min Yun , Kwee Hyun Suh
IPC分类号： C07H17/08
CPC分类号： C07H17/08 , C07H17/00
摘要： Azithromycin is prepared in a high yield by a simple process using a crystalline 9-deoxo-9a-aza-9a-homoerythromycin A hydrate.
摘要翻译：通过使用结晶9-脱氧-9a-氮杂-9a-高红霉素A水合物的简单方法以高产率制备阿奇霉素。

7. 发明申请

US20050228012A1 Crystalline clopidogrel naphthalenesulfonate or hydrate thereof, method for preparing same and pharmaceutical composition containing same 失效
标题翻译：结晶氯吡格雷萘磺酸盐或其水合物，其制备方法和含有它们的药物组合物
公开(公告)号：US20050228012A1
公开(公告)日：2005-10-13
申请号：US10971028
申请日：2004-10-25
申请人： Sangmin Yun , Eun Kim , Hee Kim , Bo Kwon , Cheol Kim , Han Kim , Kwee-Hyun Suh , Gwan Lee
发明人： Sangmin Yun , Eun Kim , Hee Kim , Bo Kwon , Cheol Kim , Han Kim , Kwee-Hyun Suh , Gwan Lee
IPC分类号： A61K31/4365 , A61K31/4743 , C07D495/04 , C07D498/02
CPC分类号： C07D495/04
摘要： A crystalline clopidogrel naphthalenesulfonate or a hydrate thereof, a method for preparing same, and a pharmaceutical composition containing same are provided.
摘要翻译：提供结晶氯吡格雷萘磺酸盐或其水合物，其制备方法和含有它们的药物组合物。

8. 发明授权

US08513426B2 Crystalline S-omeprazole strontium hydrate, method for preparing same, and pharmaceutical composition containing same 有权
公开(公告)号：US08513426B2
公开(公告)日：2013-08-20
申请号：US12914032
申请日：2010-10-28
申请人： Tae Hee Ha , Hee Sook Oh , Won Jeoung Kim , Chang Hee Park , Eun Young Kim , Young Hoon Kim , Kwee Hyun Suh , Gwan Sun Lee
发明人： Tae Hee Ha , Hee Sook Oh , Won Jeoung Kim , Chang Hee Park , Eun Young Kim , Young Hoon Kim , Kwee Hyun Suh , Gwan Sun Lee
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： Disclosed are a crystalline S-omeprazole strontium hydrate for the prevention or treatment of gastric acid-related diseases, which has high optical purity, theremostability, solubility and nonhygroscopicity, a method for preparing same, and a pharmaceutical composition containing same.

9. 发明授权

US07763730B2 Method preparation clopidogrel and intermediates used therein 失效
标题翻译：方法制备氯吡格雷及其中使用的中间体
公开(公告)号：US07763730B2
公开(公告)日：2010-07-27
申请号：US12549850
申请日：2009-08-28
申请人： Eun Sook Kim , Hee Cheol Kim , Bo Sung Kwon , Sangmin Yun , Mi Young Ko , Cheol Kyung Kim , Kwee Hyun Suh
发明人： Eun Sook Kim , Hee Cheol Kim , Bo Sung Kwon , Sangmin Yun , Mi Young Ko , Cheol Kyung Kim , Kwee Hyun Suh
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： Optically pure clopidogrel can be prepared in a high yield by optically resolving a racemic form of the compound of formula (II) using an optically active amine to form the optically active form of the compound of formula (III) or its acid-addition salt; and methylating the compound of formula (III) or its acid-addition salt.
摘要翻译：光学纯氯吡格雷可以通过光学拆分式（II）化合物的外消旋形式，使用光学活性胺形成式（III）化合物或其酸加成盐的光学活性形式，以高产率制备; 并使式（III）化合物或其酸加成盐进行甲基化。

10. 发明申请

US20100168433A1 PROCESS FOR PREPARING BEPOTASTINE AND INTERMEDIATES USED THEREIN 审中-公开
标题翻译：用于制备BEPOTASTINE及其中间体的方法
公开(公告)号：US20100168433A1
公开(公告)日：2010-07-01
申请号：US12663983
申请日：2008-06-05
申请人： Tae Hee Ha , Chang Hee Park , Won Jeoung Kim , Soohwa Cho , Han Kyong Kim , Kwee Hyun Suh
发明人： Tae Hee Ha , Chang Hee Park , Won Jeoung Kim , Soohwa Cho , Han Kyong Kim , Kwee Hyun Suh
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： A process for stereospecific preparation of bepotastine of formula (I) and novel intermediates used therein having formulae (II) to (IV) are provided. The inventive process comprises subjecting (RS)-4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidine to a reaction with a 4-halobutanoic acid l-menthyl ester, halo being chloro, bromo or iodo, in an organic solvent in the presence of a base to produce (RS)-bepotastine l-menthyl ester of formula (II), conducting a reaction of the compound of formula (II) with N-benzyloxycarbonyl L-aspartic acid in an organic solvent to induce selective precipitation of bepotastine l-menthyl ester.N-benzyloxycarbonyl L-aspartate of formula (III), filtering the precipitates formed in step 2) to isolate the compound of formula (III), treating the compound of formula (III) with a base to liberate bepotastine l-menthyl ester of formula (IV), and hydrolyzing the compound of formula (IV) in the presence of a base. The inventive process can provide bepotastine having a high optical purity of not less than 99.5% in a high yield, and thus, is useful in the development of anti-histamines and anti-allergic agents.
摘要翻译：提供了式（I）的贝他辛汀的立体特异性制备方法和其中使用的具有式（II）至（IV）的新型中间体。本发明的方法包括使（RS）-4 - [（4-氯苯基）（2-吡啶基）甲氧基]哌啶与4-卤代丁酸1-薄荷酯，卤素为氯，溴或碘的有机反应溶剂在碱的存在下反应以制备式（II）的（RS） - 贝斯塔司汀l-薄荷酯，在有机溶剂中进行式（II）化合物与N-苄氧基羰基L-天冬氨酸的反应，以诱导选择性贝他辛汀1-薄荷酯的沉淀。式（III）的N-苄氧基羰基L-天冬氨酸盐，过滤步骤2）中形成的沉淀物以分离式（III）化合物，用碱将式（III）化合物释放式（IV）的布他辛酯l-薄荷酯，并在碱的存在下水解式（IV）的化合物。本发明方法可以以高产率提供具有不低于99.5％的高光学纯度的贝他斯汀，因此可用于抗组胺和抗过敏剂的开发。

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