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1. 发明申请

US20110034550A1 Inclusion Compounds of Fumagillol Derivative or its Salt, and Pharmaceutical Compositions Comprising the Same 审中-公开
标题翻译：烟草衍生物或其盐的包含化合物和包含其的药物组合物
公开(公告)号：US20110034550A1
公开(公告)日：2011-02-10
申请号：US12756372
申请日：2010-04-08
申请人： Jae Hyun Kim , Su Kyung Lee , Won Kyu Choi , Jong Lae Lim , Soon Kil Ahn , Hee Jong Shin , Chung Il Hong
发明人： Jae Hyun Kim , Su Kyung Lee , Won Kyu Choi , Jong Lae Lim , Soon Kil Ahn , Hee Jong Shin , Chung Il Hong
IPC分类号： A61K31/336
CPC分类号： A61K47/6951 , A61K9/0019 , A61K31/336 , A61K47/02 , B82Y5/00 , C07D303/16 , C07D303/20 , C07D303/28 , C07D407/14 , C08B37/0015 , C08L5/16
摘要： The present invention relates to an inclusion compound of fumagillol derivative or its salt with hydroxypropyl-β-cyclodextrin or sulfobutylether-7-β-cyclodextrin, and pharmaceutical compositions comprising the same. The inclusion compound according to the present invention has superior water solubility and stability while exhibiting low toxicity, rendering it valuable as an anticancer agent or inhibitor of tumor metastasis.
摘要翻译：本发明涉及烟曲霉醇衍生物或其盐与羟丙基 - 环糊精或磺丁基醚-7 - 和 - 环糊精的包合物，以及包含其的药物组合物。根据本发明的包合物具有优异的水溶性和稳定性，同时显示出低毒性，使其作为肿瘤转移的抗癌剂或抑制剂是有价值的。

2. 发明申请

US20140155348A1 Inclusion Compounds of Fumagillol Derivative or its Salt, and Pharmaceutical Compositions Comprising the Same 审中-公开
标题翻译：烟草衍生物或其盐的包含化合物和包含其的药物组合物
公开(公告)号：US20140155348A1
公开(公告)日：2014-06-05
申请号：US13924768
申请日：2013-06-24
申请人： Jae Hyun Kim , Su Kyung Lee , Won Kyu Choi , Jong Lae Lim , Soon Kil Ahn , Hee Jong Shin , Chung Il Hong
发明人： Jae Hyun Kim , Su Kyung Lee , Won Kyu Choi , Jong Lae Lim , Soon Kil Ahn , Hee Jong Shin , Chung Il Hong
IPC分类号： A61K47/48 , A61K31/336
CPC分类号： A61K47/6951 , A61K9/0019 , A61K31/336 , A61K47/02 , B82Y5/00 , C07D303/16 , C07D303/20 , C07D303/28 , C07D407/14 , C08B37/0015 , C08L5/16
摘要： The present invention relates to an inclusion compound of fumagillol derivative or its salt with hydroxypropyl-β-cyclodextrin or sulfobutylether-7-β-cyclodextrin, and pharmaceutical compositions comprising the same. The inclusion compound according to the present invention has superior water solubility and stability while exhibiting low toxicity, rendering it valuable as an anticancer agent or inhibitor of tumor metastasis.
摘要翻译：本发明涉及烟曲霉醇衍生物或其盐与羟丙基 - 环糊精或磺丁基醚-7 - 和 - 环糊精的包合物，以及包含其的药物组合物。根据本发明的包合物具有优异的水溶性和稳定性，同时显示出低毒性，使其作为肿瘤转移的抗癌剂或抑制剂是有价值的。

3. 发明授权

US07718695B2 Inclusion compounds of fumagillol derivative or its salt, and pharmaceutical compositions comprising the same 有权
标题翻译：烟曲霉醇衍生物或其盐的包合物和包含其的药物组合物
公开(公告)号：US07718695B2
公开(公告)日：2010-05-18
申请号：US11828025
申请日：2007-07-25
申请人： Jae Hyun Kim , Su Kyung Lee , Won Kyu Choi , Jong Lae Lim , Soon Kil Ahn , Hee Jong Shin , Chung Il Hong
发明人： Jae Hyun Kim , Su Kyung Lee , Won Kyu Choi , Jong Lae Lim , Soon Kil Ahn , Hee Jong Shin , Chung Il Hong
IPC分类号： A61K31/336 , C07D303/12
CPC分类号： A61K47/48969 , A61K9/0019 , A61K31/336 , A61K47/02 , A61K47/6951 , B82Y5/00 , C07D303/16 , C07D303/20 , C07D303/28 , C07D407/14 , C08B37/0015 , C08L5/16
摘要： The present invention relates to an inclusion compound of fumagillol derivative or its salt with hydroxypropyl-β-cyclodextrin or sulfobutylether-7-β-cyclodextrin, and pharmaceutical compositions comprising the same. The inclusion compound according to the present invention has superior water solubility and stability while exhibiting low toxicity, rendering it valuable as an anticancer agent or inhibitor of tumor metastasis.
摘要翻译：本发明涉及烟曲霉醇衍生物或其盐与羟丙基 - 环糊精或磺丁基醚-7 - 和 - 环糊精的包合物，以及包含其的药物组合物。根据本发明的包合物具有优异的水溶性和稳定性，同时显示出低毒性，使其作为肿瘤转移的抗癌剂或抑制剂是有价值的。

4. 发明申请

US20130029936A1 Inclusion Compounds of Fumagillol Derivative or its Salt, and Pharmaceutical Compositions Comprising the Same 审中-公开
公开(公告)号：US20130029936A1
公开(公告)日：2013-01-31
申请号：US13414215
申请日：2012-03-07
申请人： Jae Hyun Kim , Su Kyung Lee , Won Kyu Choi , Jong Lae Lim , Soon Kil Ahn , Hee Jong Shin , Chung Il Hong
发明人： Jae Hyun Kim , Su Kyung Lee , Won Kyu Choi , Jong Lae Lim , Soon Kil Ahn , Hee Jong Shin , Chung Il Hong
IPC分类号： C08B37/16 , A61P35/00 , A61P35/04 , A61K31/724
CPC分类号： A61K47/6951 , A61K9/0019 , A61K31/336 , A61K47/02 , B82Y5/00 , C07D303/16 , C07D303/20 , C07D303/28 , C07D407/14 , C08B37/0015 , C08L5/16
摘要： The present invention relates to an inclusion compound of fumagillol derivative or its salt with hydroxypropyl-β-cyclodextrin or sulfobutylether-7-β-cyclodextrin, and pharmaceutical compositions comprising the same. The inclusion compound according to the present invention has superior water solubility and stability while exhibiting low toxicity, rendering it valuable as an anticancer agent or inhibitor of tumor metastasis.

5. 发明授权

US06306434B1 Pharmaceutical composition comprising cyclosporin solid-state microemulsion 失效
标题翻译：包含环孢菌素固态微乳液的药物组合物
公开(公告)号：US06306434B1
公开(公告)日：2001-10-23
申请号：US09555619
申请日：2000-06-01
申请人： Chung Il Hong , Jung Woo Kim , Nam Hee Choi , Hee Jong Shin , Su Geun Yang , Jae Hyun Kim , Jong Lae Lim , Chong Kook Kim
发明人： Chung Il Hong , Jung Woo Kim , Nam Hee Choi , Hee Jong Shin , Su Geun Yang , Jae Hyun Kim , Jong Lae Lim , Chong Kook Kim
IPC分类号： A61K966
CPC分类号： A61K38/13 , A61K9/1075 , A61K9/146 , A61K9/1652 , A61K9/4858 , A61K9/4866
摘要： A pharmaceutical composition comprising a cyclosporin solid-state microemulsion is disclosed. In a preferred embodiment, the composition comprises a cyclosporin microemulsion dispersed in an enteric carrier. The composition does not dissolve in external phases such as artificial gastric fluid, but dissolves rapidly in artificial intestinal fluid, whereby it releases the cyclosporin microemulsion, providing rapid delivery of cyclosporin. The composition effectively maintains a therapeutic blood concentration of cyclosporin with once a day dosing, providing for convenience of administration and avoiding adverse effects induced by increasing peak blood cyclosporin concentrations associated with conventional cyclosporin formulations.
摘要翻译：公开了包含环孢菌素固态微乳液的药物组合物。在优选的实施方案中，组合物包含分散在肠载体中的环孢菌素微乳液。该组合物不溶于人造胃液等外部相，但在人造肠液中快速溶解，由此释放环孢菌素微乳液，提供环孢菌素的快速输送。该组合物每天一次有效地维持环孢菌素的治疗血液浓度，提供给药的便利性，并避免通过增加与常规环孢菌素制剂相关的峰值血液环孢菌素浓度而诱发的不良反应。

6. 发明授权

US6028067A Cyclosporin-containing microemulsion preconcentrate composition 失效
标题翻译：含环孢菌素的微乳液预浓缩组合物
公开(公告)号：US6028067A
公开(公告)日：2000-02-22
申请号：US67363
申请日：1998-04-27
申请人： Chung Il Hong , Jung Woo Kim , Nam Hee Choi , Hee Jong Shin , Su Geun Yang
发明人： Chung Il Hong , Jung Woo Kim , Nam Hee Choi , Hee Jong Shin , Su Geun Yang
IPC分类号： A61K9/107 , A61K9/48 , A61K38/13 , A61K31/545
CPC分类号： A61K9/4858 , A61K38/13 , A61K9/1075 , Y10S514/937 , Y10S514/951
摘要： The present invention relates to a microemulsion preconcentrate composition comprising (1) cyclosporin as an active component; (2) alkyl ester of polycarboxylic acid and/or carboxylic acid ester of polyols as a lipophilic solvent; (3) oil; and (4) surfactant. The composition according to the present invention is characterized in that it dissolves in an external phase such as water, artificial gastric fluid and artificial intestinal fluid by controlling the mixing ratio of the components thereby to get the microemulsion form of inner phase diameter of 100 nm or below. The composition according to the present invention can be formulated as the dosage form of a soft capsule, a hard capsule sealed with a gelatin banding at the conjugated portion, or an oral liquid preparation for oral administration. Especially, if the cyclosporin microemulsion preconcentrate comprising cyclosporin, oil, lipophilic solvent and surfactant is formulated in a soft capsule according to the present invention, the resultant capsule removes the disadvantages of the prior arts showing the reactivity of hydrophilic solvent with gelatin shell of soft capsule and the volatility of hydrophilic solvent wherein the hydrophilic solvent was essential component in the composition according to the existing patents.
摘要翻译：本发明涉及一种微乳液预浓缩组合物，其包含（1）环孢菌素作为活性成分; （2）多元羧酸的烷基酯和/或作为亲脂性溶剂的多元醇的羧酸酯; （3）油; 和（4）表面活性剂。根据本发明的组合物的特征在于通过控制组分的混合比例在水相，人造胃液和人造肠液等外界溶解，得到内相直径为100nm的微乳液形式，或下面。根据本发明的组合物可以配制成软胶囊的剂型，用共轭部分的明胶带密封的硬胶囊，或用于口服给药的口服液制剂。特别地，如果将包含环孢菌素，油，亲脂性溶剂和表面活性剂的环孢菌素微乳液预浓缩物配制在根据本发明的软胶囊中，则所得胶囊消除了现有技术的缺点，显示亲水性溶剂与软胶囊明胶壳的反应性和亲水性溶剂的挥发性，其中亲水性溶剂是根据现有专利的组合物中必需组分。

7. 发明授权

US06833461B2 Process for preparing simvastatin 失效
标题翻译：辛伐他汀的制备方法
公开(公告)号：US06833461B2
公开(公告)日：2004-12-21
申请号：US10468852
申请日：2003-08-25
申请人： Chung Il Hong , Jung Woo Kim , Hee Jong Shin , Tae Won Kang , Dong Ock Cho
发明人： Chung Il Hong , Jung Woo Kim , Hee Jong Shin , Tae Won Kang , Dong Ock Cho
IPC分类号： C07D30930
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。

8. 发明授权

US6063762A Cyclosporin-containing microemulsion preconcentrate composition 失效
标题翻译：含环孢菌素的微乳液预浓缩组合物
公开(公告)号：US6063762A
公开(公告)日：2000-05-16
申请号：US146584
申请日：1998-09-03
申请人： Chung Il Hong , Jung Woo Kim , Nam Hee Choi , Hee Jong Shin , Su Geun Yang
发明人： Chung Il Hong , Jung Woo Kim , Nam Hee Choi , Hee Jong Shin , Su Geun Yang
IPC分类号： A61K38/00 , A61K9/107 , A61K9/48 , A61K38/13 , A61P37/06 , A61K9/10
CPC分类号： A61K38/13 , A61K9/1075 , A61K9/4858 , Y10S514/885 , Y10S514/937 , Y10S514/962 , Y10S514/97 , Y10S514/975
摘要： The present invention relates to a microemulsion preconcentrate composition comprising (1) cyclosporin as an active component; (2) alkyl ester of polycarboxylic acid and/or carboxylic acid ester of polyols as a lipophilic solvent; (3) oil; and (4) surfactant. The composition according to the present invention is characterized in that it dissolves in an external phase such as water, artificial gastric fluid and artificial intestinal fluid by controlling the mixing ratio of the components thereby to get the microemulsion form of inner phase diameter of 100 nm or below. The composition according to the present invention can be formulated as the dosage form of a soft capsule, a hard capsule sealed with a gelatin banding at the conjugated portion, or an oral liquid preparation for oral administration. Especially, in the case that the composition according to the present invention is formulated in a soft capsule, the resultant capsule does not show the disadvantages of the prior arts such as the reactivity of hydrophilic solvent with gelatin shell of soft capsule and the volatility of hydrophilic solvent. It is because the existing patents use a hydrophilic solvent as an essential component of their compositions but the present invention does not use any hydrophilic solvent.
摘要翻译：本发明涉及一种微乳液预浓缩组合物，其包含（1）环孢菌素作为活性成分; （2）多元羧酸的烷基酯和/或作为亲脂性溶剂的多元醇的羧酸酯; （3）油; 和（4）表面活性剂。根据本发明的组合物的特征在于通过控制组分的混合比例在水相，人造胃液和人造肠液等外界溶解，得到内相直径为100nm的微乳液形式，或下面。根据本发明的组合物可以配制成软胶囊的剂型，用共轭部分的明胶带密封的硬胶囊，或用于口服给药的口服液制剂。特别是，在将本发明的组合物配制成软胶囊的情况下，所得胶囊未显示现有技术的缺点，例如亲水性溶剂与软胶囊明胶壳的反应性和亲水性的挥发性溶剂。这是因为现有的专利使用亲水性溶剂作为其组成的必需组分，但是本发明不使用任何亲水性溶剂。

9. 发明申请

US20080125456A1 Injection of Tacrolimus 审中-公开
标题翻译：他克莫司注射
公开(公告)号：US20080125456A1
公开(公告)日：2008-05-29
申请号：US11718547
申请日：2005-11-11
申请人： Sang Joon Lee , Hee Jong Shin , Seok Kyu Lee , Ji Hun Yun
发明人： Sang Joon Lee , Hee Jong Shin , Seok Kyu Lee , Ji Hun Yun
IPC分类号： A61K31/436
CPC分类号： A61K47/10 , A61K9/0019 , A61K9/08 , A61K47/14
摘要： This invention relates to tacrolimus injection comprising tacrolimus as an active ingredient, macrogol 15 hydroxystearate as a surfactant and a non-aqueous solvent.
摘要翻译：本发明涉及他克莫司注射剂，其包含他克莫司作为活性成分，羟基硬脂酸羟肟酸锌15作为表面活性剂和非水溶剂。

10. 发明授权

US07229980B2 Paroxetine cholate or cholic acid derivative salts, and composition comprising paroxetine and cholic acid or derivative thereof 失效
标题翻译：帕罗西汀胆酸盐或胆酸衍生物盐，以及包含帕罗西汀和胆酸或其衍生物的组合物
公开(公告)号：US07229980B2
公开(公告)日：2007-06-12
申请号：US11048310
申请日：2005-01-31
申请人： Sang Joon Lee , Hee Jong Shin , Min Hyo Ki , Su Kyoung Lee , Bok Young Kim , Hong Woo Lee
发明人： Sang Joon Lee , Hee Jong Shin , Min Hyo Ki , Su Kyoung Lee , Bok Young Kim , Hong Woo Lee
IPC分类号： A61K31/56 , C07D215/04
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。

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