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1. 发明申请

WO2012015211A3 OPTHALMIC FORMULATION CONTAINING CYCLOSPORINE A 审中-公开
标题翻译：含环孢菌素A的眼用制剂A
公开(公告)号：WO2012015211A3
公开(公告)日：2012-05-24
申请号：PCT/KR2011005485
申请日：2011-07-26
申请人： CHONG KUN DANG PHARM CORP , YOON MIN-JI , PARK HYEON-WOO , SHIN TAEK-HWAN , PARK SHIN-JUNG , PARK JUN-HONG
发明人： YOON MIN-JI , PARK HYEON-WOO , SHIN TAEK-HWAN , PARK SHIN-JUNG , PARK JUN-HONG
IPC分类号： A61K38/12 , A61P27/02 , A61P27/04
CPC分类号： A61K38/13 , A61K9/0014 , A61K9/0048 , A61K9/10 , A61K47/14 , A61K47/26
摘要： The present invention relates to a novel opthalmic formulation containing poor water-soluble cyclosporine as a main ingredient, which has improved product appearance, stability and reduced foreign matter irritation as compared to conventional eye drop formulations. The eye drop formulation of the present invention comprises cyclosporine, which is useful as an ophthalmic medication, macrogol 15 hydroxystearate as a surfactant, and oil. Macrogol 15 hydroxystearate is used as a surfactant so as to significantly improve turbidity as compared to conventional eye drop formulations that use polyoxyethylated castor oil or polysorbate 80, thus preventing blurred vision when dropped into the eye of the user. The cyclosporine particles are reduced in size and dispersed into uniform particulate solution so that an eye drop formulation is prepared which is free of irritation caused by foreign matter.
摘要翻译：本发明涉及含有水溶性差的环孢菌素作为主要成分的新型眼用制剂，与常规滴眼剂制剂相比，该制剂具有改善的产品外观，稳定性和降低的异物刺激性。本发明的滴眼剂制剂包含可用作眼科用药的环孢菌素，作为表面活性剂的聚乙二醇15羟基硬脂酸酯和油。与使用聚氧乙烯蓖麻油或聚山梨酯80的常规滴眼剂制剂相比，聚乙二醇15羟基硬脂酸酯用作表面活性剂以显着改善浊度，从而防止当掉入使用者眼睛时的视觉模糊。环孢菌素颗粒被减小尺寸并分散成均匀的颗粒溶液，从而制备出无异物引起的刺激性的滴眼剂。

2. 发明申请

WO2009119980A2 BENZOPHENONE THIAZOLE DERIVATIVES USEFUL FOR INHIBITING FORMATION OF MICROTUBULE AND METHOD FOR PRODUCING THE SAME 审中-公开
标题翻译：用于抑制微生物形成的苯并噻唑衍生物及其生产方法
公开(公告)号：WO2009119980A2
公开(公告)日：2009-10-01
申请号：PCT/KR2009001095
申请日：2009-03-05
申请人： CHONG KUN DANG PHARM CORP , CHOI NAM-SONG , KIM YOUNG-HOON , LEE JAE-KWANG , KANG HEE-RYONG , CHOI HO-JIN , MOON SEUNG-KEE , KIM SOO-JIN , PARK GYU-TAE , HAN BYEONG-HOON , KIM DAL-HYUN , CHOI JAE-HOON , LEE SUNG-SOOK , AHN SOON-KIL , LEE KYUNG-JOO , BAE SU-YEAL
发明人： CHOI NAM-SONG , KIM YOUNG-HOON , LEE JAE-KWANG , KANG HEE-RYONG , CHOI HO-JIN , MOON SEUNG-KEE , KIM SOO-JIN , PARK GYU-TAE , HAN BYEONG-HOON , KIM DAL-HYUN , CHOI JAE-HOON , LEE SUNG-SOOK , AHN SOON-KIL , LEE KYUNG-JOO , BAE SU-YEAL
IPC分类号： C07D417/10
CPC分类号： C07D417/10 , C07D417/14
摘要： The present invention relates to novel benzophenone thiazole derivatives of chemical formula 1, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof or solvates thereof, pharmaceutical compositions containing the same, use thereof as therapeutic agents and a method for producing the same. The benzophenone thiazole derivatives of the present invention have inhibitory activities against the formation of microtubules, and exterminate active proliferating cells of malignant tumors and thus can be used in treating the general growth state of a malignant tumor. R, R1 and R2 in chemical formula 1 are the same as those defined in the description of the invention.
摘要翻译：本发明涉及化学式1的新型二苯甲酮噻唑衍生物，其异构体，其药学上可接受的盐，其水合物或溶剂合物，含有它们的药物组合物，作为治疗剂的用途及其制备方法。本发明的二苯甲酮噻唑衍生物具有抗微管形成的抑制活性，能够消除恶性肿瘤的活性增殖细胞，可用于治疗恶性肿瘤的一般生长状态。化学式1中的R，R 1和R 2与本发明的说明书中定义的相同。

3. 发明申请

WO0145484A3 AN IMPROVED PROCESS FOR PREPARING SIMVASTATIN 审中-公开
标题翻译：制备SIMVASTATIN的改进方法
公开(公告)号：WO0145484A3
公开(公告)日：2002-03-28
申请号：PCT/KR0100301
申请日：2001-02-27
申请人： CHONG KUN DANG PHARM CORP , HONG CHUNG IL , KIM JUNG WOO , SHIN HEE JONG , KANG TAE WON , CHO DONG OCK
发明人： HONG CHUNG IL , KIM JUNG WOO , SHIN HEE JONG , KANG TAE WON , CHO DONG OCK
IPC分类号： A44C5/00 , A61K31/366 , A61P3/06 , A61P43/00 , C07B53/00 , C07D309/30
CPC分类号： C07D309/30 , Y02P20/55
摘要： The present invention relates to an improved process for preparing simvastatin and more particularly, the improved process for preparing simvastatin expressed by formula 1 with high yield and high purity by performing the following sequential processes comprising: (i) hydrolysis of lovastatin as starting material with potassium t-butoxide in an organic solvent and small amount of water under a mild reaction condition, followed by lactonization of the obtained solid intermediate with preventing from formation of by-products; (ii) protection of an alcohol group with t-butyldimethylsilyl group which can be easily removed with concentrated hydrochloric acid without the formation of by-products; (iii) acylation of the obtained protected intermediate with acyloxytriphenyl phosphonium salt as an acylating agent under a mild reaction condition; and (iv) removal of the silyl protective group with a concentrated hydrochloric acid. The present invention is to provide the improved process of preparing simvastatin expressed by formula 1 environmentally sound, economically efficient, and industrially useful.
摘要翻译：本发明涉及一种制备辛伐他汀的改进方法，更具体地说，涉及通过进行以下顺序方法制备具有高产率和高纯度的式1所表达的辛伐他汀的改进方法，包括：（i）将洛伐他汀作为原料与钾叔丁醇在有机溶剂和少量水中，在温和的反应条件下，然后将所得固体中间体内酯化，防止副产物的形成; （ii）用叔丁基二甲基甲硅烷基保护醇基，其可以用浓盐酸容易地除去而不形成副产物; （iii）在温和的反应条件下用酰氧基三苯基鏻盐作为酰化剂酰化所得保护的中间体; 和（iv）用浓盐酸除去甲硅烷基保护基。本发明提供了由式1表达的辛伐他汀的改进方法，其在环境无害，经济有效和工业上有用。

4. 发明申请

WO2014104784A4 SUSTAINED-RELEASE LIPID PRE-CONCENTRATE OF CATIONIC PHARMACOLOGICALLY ACTIVE SUBSTANCE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME 审中-公开
标题翻译：阳离子药理活性物质的持续释放脂质预浓缩物及含有该物质的药物组合物
公开(公告)号：WO2014104784A4
公开(公告)日：2014-07-31
申请号：PCT/KR2013012259
申请日：2013-12-27
申请人： CHONG KUN DANG PHARM CORP
发明人： YU HA NA , BAIK HYE JUNG , YANG WON KYU , KO JIN YOUNG , JUNG SUNG BUM , AN SUNG WON , KI MIN HYO
IPC分类号： A61K9/20 , A61K9/06 , A61K9/08 , A61K47/30
CPC分类号： A61K9/1274 , A61K9/1075 , A61K31/00 , A61K31/4196 , A61K31/519 , A61K31/522 , A61K38/08 , A61K38/09 , A61K38/11 , A61K38/13 , A61K38/21 , A61K38/26 , A61K38/27 , A61K38/28 , A61K47/12 , A61K47/14 , A61K47/20 , A61K47/24 , A61K47/26 , A61K47/28 , A61K2300/00
摘要： Disclosed is a sustained-release lipid pre-concentrate, comprising: a) at least one liquid crystal former; b) at least one neutral phospholipid; c) at least one liquid crystal hardener; and d) at least one anionic anchoring agent, wherein the sustained-release pre-concentrate exists as a lipid liquid phase in the absence of aqueous fluid and forms into a liquid crystal upon exposure to aqueous fluid. The sustained-release lipid pre-concentrate is configured to enhance the sustained release of cationic pharmacologically active substance through ionic interaction between the anionic anchoring agent and the cationic pharmacologically active substance.
摘要翻译：公开了缓释脂质预浓缩物，其包含：a）至少一种液晶形成剂; b）至少一种中性磷脂; c）至少一种液晶硬化剂; 和d）至少一种阴离子锚定剂，其中所述缓释预浓缩物在不存在水性流体的情况下作为脂质液相存在并且在暴露于含水流体时形成液晶。持续释放脂质预浓缩物被配置为通过阴离子锚定剂和阳离子药理活性物质之间的离子相互作用来增强阳离子药理活性物质的持续释放。

5. 发明申请

WO2012141487A3 CYCLOALKENYL ARYL DERIVATIVES FOR CETP INHIBITOR 审中-公开
标题翻译：环糊精ARYL衍生物用于CETP抑制剂
公开(公告)号：WO2012141487A3
公开(公告)日：2013-01-10
申请号：PCT/KR2012002739
申请日：2012-04-12
申请人： CHONG KUN DANG PHARM CORP , LEE SEOHEE , OH JUNGTAEK , LEE JAEKWANG , LEE JAEWON , BAE SUYEAL , HA NINA , LEE SERA
发明人： LEE SEOHEE , OH JUNGTAEK , LEE JAEKWANG , LEE JAEWON , BAE SUYEAL , HA NINA , LEE SERA
IPC分类号： C07D263/16 , A61K31/421 , A61P3/06 , A61P9/00 , C07D263/22 , C07D413/06
CPC分类号： C07D263/24 , C07D263/16 , C07D263/22 , C07D401/06 , C07D413/06 , C07D413/08 , C07D413/10 , C07D417/12
摘要： The present invention relates to cycloalkenyl aryl derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof; a method for preparing the derivatives; and pharmaceutical compositions containing the same. The compounds of the present invention show the effect of CETP activity inhibition. It means that the compounds can increase HDL-cholesterol and decrease LDL-cholesterol.
摘要翻译：本发明涉及环烯基芳基衍生物，其异构体，其药学上可接受的盐，其水合物或溶剂合物; 制备衍生物的方法; 和含有它们的药物组合物。本发明的化合物显示CETP活性抑制的作用。这意味着这些化合物可以增加HDL-胆固醇并降低LDL-胆固醇。

6. 发明申请

WO2006033505A8 PAROXETINE CHOLATE OR CHOLIC ACID DERIVATIVE SALTS, AND COMPOSITION COMPRISING PAROXETINE AND CHOLIC ACID OR CHOLIC ACID DERIVATIVES 审中-公开
标题翻译：异黄酮或胆酸衍生物，以及包含PAROXETINE和胆酸或胆酸衍生物的组合物
公开(公告)号：WO2006033505A8
公开(公告)日：2006-09-14
申请号：PCT/KR2004003477
申请日：2004-12-28
申请人： CHONG KUN DANG PHARM CORP , LEE SANG JOON , SHIN HEE JONG , KI MIN HYO , LEE SU KYOUNG , KIM BOK YOUNG , LEE HONG WOO
发明人： LEE SANG JOON , SHIN HEE JONG , KI MIN HYO , LEE SU KYOUNG , KIM BOK YOUNG , LEE HONG WOO
IPC分类号： C07D405/12 , A61K31/445 , A61P25/24
CPC分类号： C07D405/12 , C07J43/00
摘要： Disclosed herein is a paroxetine cholate or cholic acid derivative salt and a composition comprising paroxetine and cholic acid or a derivative thereof. Further disclosed is a pharmaceutical composition comprising the paroxetine salt or the composition. The pharmaceutical composition can be formulated into an oral preparation for swallowing without water as an orally disintegrating tablet for paroxetine.
摘要翻译：本文公开了帕罗西汀胆酸盐或胆酸衍生物盐和包含帕罗西汀和胆酸或其衍生物的组合物。还公开了包含帕罗西汀盐或组合物的药物组合物。作为帕罗西汀的口腔崩解片剂，可以将药物组合物配制成无水的口服制剂。

7. 发明申请

WO2005123138A9 PHARMACEUTICAL PELLET COMPOSITIONS FOR CONTROLLED RELEASE 审中-公开
标题翻译：用于控制释放的药物颗粒组合物
公开(公告)号：WO2005123138A9
公开(公告)日：2006-04-06
申请号：PCT/KR2005000666
申请日：2005-03-10
申请人： CHONG KUN DANG PHARM CORP , LEE SANG-JOON , SHIN HEE-JONG , KI MIN-HYO , YOON BOK-YOUNG
发明人： LEE SANG-JOON , SHIN HEE-JONG , KI MIN-HYO , YOON BOK-YOUNG
IPC分类号： A61K9/22 , A61K9/16 , A61K47/30
CPC分类号： A61K9/1635 , A61K9/1617 , A61K9/1652
摘要： The present invention provides a pharmaceutical composition in the form of pellet wherein controlled release of pharmacologically active substances can be effected. The present invention is characterized by a pharmaceutical composition for controlled release pellets, consisting es¬ sentially of: a) one or more pharmacologically active substances; b) one or more lipids having a low-melting point of less than 70°C and existing as a solid at room temperature; c) one or more hydrophilic substances; and d) one or more water-insoluble binding agents, prepared without melting the lipids.
摘要翻译：本发明提供了丸剂形式的药物组合物，其中可以实现药理活性物质的控制释放。本发明的特征在于用于控释丸剂的药物组合物，其包括：a）一种或多种药理活性物质; b）一种或多种低熔点小于70℃并在室温下作为固体存在的脂质; c）一种或多种亲水性物质; 和d）一种或多种不溶于脂质的水不溶性结合剂。

8. 发明申请

WO2012134231A2 BENZAMIDE DERIVATIVE AS CANNABINOID RECEPTOR (CB1) ANTAGONIST 审中-公开
标题翻译：苯甲酸衍生物作为CANNABINOID受体（CB1）拮抗剂
公开(公告)号：WO2012134231A2
公开(公告)日：2012-10-04
申请号：PCT/KR2012002405
申请日：2012-03-30
申请人： KOREA RES INST CHEM TECH , CHONG KUN DANG PHARM CORP , LEE HYUN-KYU , CHOI EUN BOK , YANG HEUI CHEOL , KIM KWANG-ROK , JANG TAEGSU , OH JUNG TAEK
发明人： LEE HYUN-KYU , CHOI EUN BOK , YANG HEUI CHEOL , KIM KWANG-ROK , JANG TAEGSU , OH JUNG TAEK
IPC分类号： C07C235/46 , A61K31/166 , A61P3/04 , C07D211/16
CPC分类号： C07C235/46 , C07C233/25 , C07C233/56 , C07C235/48 , C07C235/50 , C07C235/52 , C07C235/54 , C07C235/56 , C07C243/38 , C07C275/34 , C07C311/51 , C07C327/48 , C07C2601/14 , C07C2603/74 , C07D207/08 , C07D207/12 , C07D207/16 , C07D211/42 , C07D211/60 , C07D211/62 , C07D213/40 , C07D277/06 , C07D279/12 , C07D295/32
摘要： The present invention relates to a novel benzamide compound functioning as an inverse agonist or an antagonist of a cannabinoid receptor (CB1), or pharmaceutically acceptable salts thereof. The compound according to the invention is useful for the prevention or treatment of obesity and obesity- related metabolic diseases. In addition, the invention provides a method for preparing the benzamide compound, a pharmaceutical compound including the same, and a method for the prevention or treatment of obesity and obesity- related metabolic diseases.
摘要翻译：本发明涉及用作大麻素受体（CB1）的反向激动剂或拮抗剂的新型苯甲酰胺化合物或其药学上可接受的盐。根据本发明的化合物可用于预防或治疗肥胖症和肥胖相关的代谢疾病。此外，本发明提供了一种制备苯甲酰胺化合物的方法，包含该苯甲酰胺化合物的药物化合物，以及预防或治疗肥胖症和与肥胖有关的代谢性疾病的方法。

9. 发明申请

WO2010140765A2 NOVEL METHOD FOR PREPARING ROSUVASTATIN, INTERMEDIATE COMPOUNDS USEFUL FOR PREPARING SAME, AND METHOD FOR PREPARING SAME 审中-公开
标题翻译：用于制备罗司他汀的新方法，用于制备其的中间体化合物及其制备方法
公开(公告)号：WO2010140765A2
公开(公告)日：2010-12-09
申请号：PCT/KR2010002169
申请日：2010-04-08
申请人： CHONG KUN DANG PHARM CORP , LEE HONGWOO , PARK DAEJONG , YOO CHOONGLEOL , NAM DONGHYUK , RYU HOHYUNG , KIM DONGJIN
发明人： LEE HONGWOO , PARK DAEJONG , YOO CHOONGLEOL , NAM DONGHYUK , RYU HOHYUNG , KIM DONGJIN
IPC分类号： C07D239/42 , A61K31/505 , A61P3/06
CPC分类号： C07D239/42 , C07C67/31 , C07C67/343 , C07C69/675 , C07C69/716 , C07D317/30 , C07D405/06 , C07D405/12 , C07D417/12
摘要： The present invention relates to novel intermediate compounds used in preparing Rosuvastatin or the pharmaceutically acceptable salts thereof, to a method for preparing same, and to a method for preparing Rosuvastatin or the pharmaceutically acceptable salts thereof from the intermediates. The preparation method of the present invention has the effect of providing Rosuvastatin hemi-calcium salts with an excellent yield rate.
摘要翻译：本发明涉及用于制备罗苏伐他汀或其药学上可接受的盐的新型中间体化合物，其制备方法，以及由中间体制备罗苏伐他汀或其药学上可接受的盐的方法。本发明的制备方法具有以优异的产率提供罗苏伐他汀半钙盐的效果。

10. 发明申请

WO2010074460A3 NOVEL PHARMACEUTICAL COMPOSITION FOR AMELIORATING SIDE EFFECTS OF A LIPASE INHIBITOR 审中-公开
标题翻译：用于抑制脂肪酶抑制剂的副作用的新型药物组合物
公开(公告)号：WO2010074460A3
公开(公告)日：2010-09-23
申请号：PCT/KR2009007614
申请日：2009-12-18
申请人： CHONG KUN DANG PHARM CORP , KIM SUN-KYUNG , LEE SU-KYOUNG , KI MIN-HYO
发明人： KIM SUN-KYUNG , LEE SU-KYOUNG , KI MIN-HYO
IPC分类号： A61K47/30 , A61K31/337
CPC分类号： A61K31/337 , A61K47/34
摘要： The present invention relates to a novel pharmaceutical composition for ameliorating the side effects of a lipase inhibitor. More particularly, the present invention relates to a pharmaceutical composition for ameliorating the side effects of a lipase inhibitor, comprising a pharmaceutically acceptable polyalkylene oxide-based amphiphilic polymer and water-soluble thickening agents. The composition of the present invention significantly ameliorates side effects such as oily spotting, steatorrhea, or the like caused by taking a lipase inhibitor.
摘要翻译：本发明涉及一种用于改善脂肪酶抑制剂的副作用的新型药物组合物。更具体地，本发明涉及用于改善脂肪酶抑制剂的副作用的药物组合物，其包含药学上可接受的聚环氧烷基两亲性聚合物和水溶性增稠剂。本发明的组合物显着地改善了由摄取脂肪酶抑制剂引起的副作用，如油性斑点，肉眼等。

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