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1. 发明申请

WO2009078627A2 METHOD FOR PREPARING (R)-(-)-1-[(4-CHLOROPHENYL)PHENYLMETHYL]PIPERAZINE 审中-公开
标题翻译：制备（R） - （ - ） - 1 - [（4-氯苯基）苯基甲基]哌嗪的方法
公开(公告)号：WO2009078627A2
公开(公告)日：2009-06-25
申请号：PCT/KR2008007376
申请日：2008-12-12
申请人： HANMI PHARM IND CO LTD , HA TAE HEE , KIM WON JEOUNG , BAEK JONG OUK , JANG SUK MAN , LEE JAE CHUL , LEE YOON JU , SUH KWEE HYUN , LEE GWAN SUN
发明人： HA TAE HEE , KIM WON JEOUNG , BAEK JONG OUK , JANG SUK MAN , LEE JAE CHUL , LEE YOON JU , SUH KWEE HYUN , LEE GWAN SUN
IPC分类号： C07D295/073
CPC分类号： C07D295/073
摘要： The present invention relates to a novel method for preparing (R)-(-)-1-[(4-chlorophenyl)phenylmethyl]piperazine of formula (I), which is useful as an intermediate for preparing an antihistamine, levocetirizine.
摘要翻译：本发明涉及制备式（I）的（R） - （ - ） - 1 - [（4-氯苯基）苯甲基]哌嗪的新方法，其可用作制备抗组胺药左西替利嗪的中间体。

2. 发明申请

WO2013015535A3 NOVEL PYRIMIDINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION INCLUDING SAME AS AN ACTIVE INGREDIENT 审中-公开
标题翻译：新的嘧啶衍生物和包含其作为活性成分的药物组合物
公开(公告)号：WO2013015535A3
公开(公告)日：2013-04-11
申请号：PCT/KR2012005193
申请日：2012-06-29
申请人： KOREA HEALTH INDUSTRY DEV INST KHIDI , HANMI PHARMACEUTICAL CO LTD , PARK CHUL HYUN , KIM WON JEOUNG , JUNG YOUNG HEE , KIM NAM DU , CHANG YOUNG KIL , KIM MAENG SUP
发明人： PARK CHUL HYUN , KIM WON JEOUNG , JUNG YOUNG HEE , KIM NAM DU , CHANG YOUNG KIL , KIM MAENG SUP
IPC分类号： C07D495/04 , A61K31/519 , A61P3/10 , C07D487/04
CPC分类号： C07D495/04 , C07D487/04
摘要： The present invention relates to a compound selected from the group consisting of a compound represented by chemical formula 1 for inhibiting the activity of diacylglycerol 0-acyltransferase type 1, and pharmaceutically acceptable salts thereof, and to a pharmaceutical composition including same as an active ingredient. The compound of the present invention may be used as an effective therapeutic agent for treating, without side effects, diseases such as obesity, type II diabetes, dyslipidemia, metabolic syndrome, etc. induced by the activity of DGAT1. In chemical formula 1, A, B, X and R5-7 are the same as those defined in the present specification.
摘要翻译：本发明涉及选自用于抑制二酰甘油O-酰基转移酶1型活性的由化学式1表示的化合物及其药学上可接受的盐以及包含其作为活性成分的药物组合物。本发明的化合物可以作为有效的治疗剂用于治疗无副作用的由DGAT1的活性诱导的诸如肥胖症，II型糖尿病，血脂异常，代谢综合征等的疾病。在化学式1中，A，B，X和R5-7与本说明书中定义的那些相同。

3. 发明申请

WO2005047282A1 ANTIRESORPTIVE MUTUAL SALT OF RALOXIFENE AND BISPHOSPHONIC ACID 审中-公开
标题翻译：抗坏血酸和二磷酸的反相盐
公开(公告)号：WO2005047282A1
公开(公告)日：2005-05-26
申请号：PCT/KR2004/002954
申请日：2004-11-15
申请人： HANMI PHARM. CO., LTD. , HA, Tae Hee , KIM, Won Jeoung , YUN, Sangmin , KIM, Cheol Kyung , KIM, Han Kyong , SUH, Kwee-Hyun , LEE, Gwan Sun
发明人： HA, Tae Hee , KIM, Won Jeoung , YUN, Sangmin , KIM, Cheol Kyung , KIM, Han Kyong , SUH, Kwee-Hyun , LEE, Gwan Sun
IPC分类号： C07D409/12
CPC分类号： C07D333/56 , C07F9/3856 , C07F9/386 , C07F9/3865 , C07F9/3873 , C07F9/5721 , C07F9/582 , C07F9/65061
摘要： The mutual salt of raloxifene and bisphosphonic acid exhibits unexpectedly synergistic effects of two components to enhance bone mineral density (BMD), control blood-calcium density, and lower the serum cholesterol level.
摘要翻译：雷洛昔芬和双膦酸的相互盐显示两种成分的意外协同效应，以增强骨矿物质密度（BMD），控制血钙密度，降低血清胆固醇水平。

4. 发明申请

WO2008153289A2 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：WO2008153289A2
公开(公告)日：2008-12-18
申请号：PCT/KR2008003161
申请日：2008-06-05
申请人： HANMI PHARM IND CO LTD , HA TAE HEE , PARK CHANG HEE , KIM WON JEOUNG , CHO SOOHWA , KIM HAN KYONG , SUH KWEE HYUN
发明人： HA TAE HEE , PARK CHANG HEE , KIM WON JEOUNG , CHO SOOHWA , KIM HAN KYONG , SUH KWEE HYUN
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-苄氧羰基L-天冬氨酸的反应，以诱导选择性将式（III）的贝他辛汀1-薄荷酯β-苄氧羰基L-天冬氨酸的沉淀，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1-薄荷酯，并在碱的存在下水解式（Ⅳ）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。

5. 发明申请

WO2010077062A3 PREPARATION METHOD OF STATIN COMPOUND AND BENZOTHIAZOLYL SULFONE COMPOUND USED THEREIN 审中-公开
公开(公告)号：WO2010077062A3
公开(公告)日：2010-07-08
申请号：PCT/KR2009/007881
申请日：2009-12-29
申请人： HANMI PHARM. CO., LTD. , KIM, Hee Seock , KIM, Won Jeoung , KIM, Hee Cheol , SIM, Jae Yi , CHO, Seong Mi , BYUN, Eun Young , JEON, Ji Young , LEE, Yoon Ju , SUH, Kwee Hyun , LEE, Gwan Sun
发明人： KIM, Hee Seock , KIM, Won Jeoung , KIM, Hee Cheol , SIM, Jae Yi , CHO, Seong Mi , BYUN, Eun Young , JEON, Ji Young , LEE, Yoon Ju , SUH, Kwee Hyun , LEE, Gwan Sun
IPC分类号： C07D239/18 , C07D215/02
摘要： The inventive method comprising subjecting a novel benzothiazolyl sulfone compound to a reaction with an aldehyde to obtain a vinyl intermediate and removing the hydroxy and carboxy protective groups of the vinyl intermediate is simple and efficient in preparing a statin compound or a salt thereof which is useful for treating hyperlipemia.

6. 发明申请

WO2009078627A3 METHOD FOR PREPARING (R)-(-)-1-[(4-CHLOROPHENYL)PHENYLMETHYL]PIPERAZINE 审中-公开
公开(公告)号：WO2009078627A3
公开(公告)日：2009-06-25
申请号：PCT/KR2008/007376
申请日：2008-12-12
申请人： HANMI PHARM. CO., LTD. , HA, Tae Hee , KIM, Won Jeoung , BAEK, Jong Ouk , JANG, Suk Man , LEE, Jae Chul , LEE, Yoon Ju , SUH, Kwee Hyun , LEE, Gwan Sun
发明人： HA, Tae Hee , KIM, Won Jeoung , BAEK, Jong Ouk , JANG, Suk Man , LEE, Jae Chul , LEE, Yoon Ju , SUH, Kwee Hyun , LEE, Gwan Sun
IPC分类号： C07D295/073
摘要： The present invention relates to a novel method for preparing (R)-(-)-1-[(4-chlorophenyl)phenylmethyl]piperazine of formula (I), which is useful as an intermediate for preparing an antihistamine, levocetirizine.

7. 发明申请

WO2008153289A3 PROCESS FOR PREPARING BEPOTASTINE AND INTERMEDIATES USED THEREIN 审中-公开
公开(公告)号：WO2008153289A3
公开(公告)日：2008-12-18
申请号：PCT/KR2008/003161
申请日：2008-06-05
申请人： HANMI PHARM. CO., LTD. , HA, Tae Hee , PARK, Chang Hee , KIM, Won Jeoung , CHO, Soohwa , KIM, Han Kyong , SUH, Kwee Hyun
发明人： HA, Tae Hee , PARK, Chang Hee , KIM, Won Jeoung , CHO, Soohwa , KIM, Han Kyong , SUH, Kwee Hyun
IPC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.

8. 发明申请

WO2010098583A3 NOVEL METHOD FOR PREPARING STATIN COMPOUNDS OR SALTS THEREOF, AND INTERMEDIATE COMPOUNDS USED IN SAME 审中-公开
标题翻译：用于制备苯丙胺化合物或其盐的新方法及其使用的中间体化合物
公开(公告)号：WO2010098583A3
公开(公告)日：2011-01-06
申请号：PCT/KR2010001152
申请日：2010-02-24
申请人： HANMI HOLDINGS CO LTD , KIM HEE SEOCK , KIM HEECHEOL , SIM JAE YI , CHO SEONG MI , KIM WON JEOUNG , SUH KWEE HYUN , LEE GWAN SUN
发明人： KIM HEE SEOCK , KIM HEECHEOL , SIM JAE YI , CHO SEONG MI , KIM WON JEOUNG , SUH KWEE HYUN , LEE GWAN SUN
IPC分类号： C07D215/00 , C07D309/10
CPC分类号： C07D309/10 , C07D215/44
摘要： The present invention relates to a novel method for preparing statin compounds or salts thereof, which are useful in treating and preventing hyperlipidemia-related diseases, and to intermediate compounds used in same. The method of the present invention can prepare statin compounds from novel intermediate compounds in a simple and efficient manner.
摘要翻译：本发明涉及可用于治疗和预防高脂血症相关疾病的他汀类化合物或其盐的新方法及其中所用的中间体化合物。本发明的方法可以简单有效地从新型中间体化合物制备他汀类化合物。

9. 发明申请

WO2010077062A2 PREPARATION METHOD OF STATIN COMPOUND AND BENZOTHIAZOLYL SULFONE COMPOUND USED THEREIN 审中-公开
标题翻译：苯并芘化合物及其使用的苯并噻唑类磺化合物的制备方法
公开(公告)号：WO2010077062A2
公开(公告)日：2010-07-08
申请号：PCT/KR2009007881
申请日：2009-12-29
申请人： HANMI PHARM IND CO LTD , KIM HEE SEOCK , KIM WON JEOUNG , KIM HEE CHEOL , SIM JAE YI , CHO SEONG MI , BYUN EUN YOUNG , JEON JI YOUNG , LEE YOON JU , SUH KWEE HYUN , LEE GWAN SUN
发明人： KIM HEE SEOCK , KIM WON JEOUNG , KIM HEE CHEOL , SIM JAE YI , CHO SEONG MI , BYUN EUN YOUNG , JEON JI YOUNG , LEE YOON JU , SUH KWEE HYUN , LEE GWAN SUN
IPC分类号： C07D239/18 , C07D215/02
CPC分类号： C07D417/12 , C07D215/14 , C07D239/18 , C07D405/06 , Y02P20/55
摘要： The inventive method comprising subjecting a novel benzothiazolyl sulfone compound to a reaction with an aldehyde to obtain a vinyl intermediate and removing the hydroxy and carboxy protective groups of the vinyl intermediate is simple and efficient in preparing a statin compound or a salt thereof which is useful for treating hyperlipemia.
摘要翻译：本发明的方法包括使新的苯并噻唑基砜化合物与醛反应以获得乙烯基中间体并除去乙烯基中间体的羟基和羧基保护基团在制备他汀类化合物或其盐中是简单和有效的，其可用于治疗高脂血症。

10. 发明申请

WO2008123701A1 NOVEL CRYSTALLINE BEPOTASTINE METAL SALT HYDRATE, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME 审中-公开
标题翻译：新型水晶金属盐水合物，其制备方法和包含其的药物组合物
公开(公告)号：WO2008123701A1
公开(公告)日：2008-10-16
申请号：PCT/KR2008/001912
申请日：2008-04-04
申请人： HANMI PHARM. CO., LTD. , HA, Tae Hee , PARK, Chang Hee , KIM, Won Jeoung , OH, Hee Sook , CHO, Seung Hwan , KIM, Cheol Kyung , SUH, Kwee Hyun , LEE, Gwan Sun
发明人： HA, Tae Hee , PARK, Chang Hee , KIM, Won Jeoung , OH, Hee Sook , CHO, Seung Hwan , KIM, Cheol Kyung , SUH, Kwee Hyun , LEE, Gwan Sun
IPC分类号： C07D401/12 , A61K31/58 , A61K9/20 , A61K31/137
CPC分类号： C07D401/12 , A61K9/143
摘要： The present invention discloses a non-hygroscopic crystalline bepotastine metal salt hydrate, a method for preparing same, and a pharmaceutical composition comprising same for treating or preventing a histamine-mediated disease or an allergic disease.
摘要翻译：本发明公开了一种非吸湿结晶贝卡斯汀金属盐水合物及其制备方法，以及包含其的药物组合物，用于治疗或预防组胺介导的疾病或过敏性疾病。

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