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1. 发明授权

US06962911B2 Pyrrolopyrimidinone derivatives, process of preparation and use 有权
公开(公告)号：US06962911B2
公开(公告)日：2005-11-08
申请号：US10204327
申请日：2001-02-15
申请人： Dae-Kee Kim , Ju Young Lee , Do Hyun Ryu , Nam Kyu Lee , Suk Ho Lee , Nam-Ho Kim , Jae-Sun Kim , Je Ho Ryu , Jin-Young Choi , Guang-Jin Im , Won-Son Choi , Tae Kon Kim , Hoon Cha
发明人： Dae-Kee Kim , Ju Young Lee , Do Hyun Ryu , Nam Kyu Lee , Suk Ho Lee , Nam-Ho Kim , Jae-Sun Kim , Je Ho Ryu , Jin-Young Choi , Guang-Jin Im , Won-Son Choi , Tae Kon Kim , Hoon Cha
IPC分类号： A61K31/51 , A61K31/519 , A61K31/551 , A61P1/04 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/12 , A61P15/00 , A61P15/10 , A61P15/14 , A61P27/02 , A61P29/00 , A61P37/08 , A61P43/00 , C07D207/00 , C07D207/34 , C07D239/00 , C07D487/04 , A61P27/06
CPC分类号： C07D487/04 , C07D207/34
摘要： The invention relates to a series of pyrrolopyrimidinone derivatives of the formula (1): wherein R1 is H; C1-C3 alkyl optionally substituted with one or more fluoro atoms; or C3-C6 cycloalkyl; R2 is H; a halogen atom; C1-C6 alkyl optionally substituted with OH, C1-C3 alkoxy, C3-C6 cycloalkyl, or with one or more fluoro atoms; C3-C6 cycloalkyl; C2-C6 alkenyl; or C2-C6 alkynyl; R3 is H; C1-C6 alkyl optionally substituted with OH, C1-C3 alkoxy, C3-C6 cycloalkyl, or with one or more fluoro atoms; C3-C6 cycloalkyl; C2-C6 alkenyl; or C2-C6 alkynyl; R4 is C1-C6 alkyl optionally substituted with C3-C6 cycloalkyl or with one or more fluoro atoms; C2-C6 alkenyl; C2-C6 alkynyl; or C3-C6 cycloalkyl; and R5 is SO2NR6R7; NHSO2NR6R7; NHCOCONR6R7; NHSO2R8; NHCOR8; or phenyl or heterocyclyl either of which is optionally substituted with one or more fluoro atoms or C1-C3 alkyl.

2. 发明授权

US07495022B2 α,β-unsaturated hydroxamic acid derivatives and their use as histone deacetylase inhibitors 有权
标题翻译： α，β-不饱和异羟肟酸衍生物及其作为组蛋白脱乙酰酶抑制剂的用途
公开(公告)号：US07495022B2
公开(公告)日：2009-02-24
申请号：US10510630
申请日：2003-04-10
申请人： Dae-Kee Kim , Ju Young Lee , Nam Kyu Lee , Jae-Sun Kim , Junwon Lee , Suk Ho Lee , Jin Young Choi , Je Ho Ryu , Nam Ho Kim , Guang-Jin Im , Tae Kon Kim , Jung-Woo Seo , Young-Jue Bang
发明人： Dae-Kee Kim , Ju Young Lee , Nam Kyu Lee , Jae-Sun Kim , Junwon Lee , Suk Ho Lee , Jin Young Choi , Je Ho Ryu , Nam Ho Kim , Guang-Jin Im , Tae Kon Kim , Jung-Woo Seo , Young-Jue Bang
IPC分类号： A61K31/19 , C07D207/32
CPC分类号： C07D213/82 , C07C259/06 , C07C317/44 , C07D213/38 , C07D213/71 , C07D213/81 , C07D215/48 , C07D215/54 , C07D295/155
摘要： Disclosed are agents that inhibit histone deacetylase. More specifically, the present invention relates to novel hydroxamic acid derivatives or pharmaceutically acceptable salts thereof for anticancer agents or other therapeutic agents based on their histone deacetylase inhibitory activity.
摘要翻译：公开了抑制组蛋白脱乙酰酶的药剂。更具体地，本发明涉及用于抗癌剂或其它治疗剂的新型异羟肟酸衍生物或其药学上可接受的盐，基于其组蛋白脱乙酰酶抑制活性。

3. 发明申请

US20050124679A1 Alpha, beta-unsaturated hydroxamic acid derivatives and their use as histone deacetylase inhibitors 有权
标题翻译： α，β-不饱和异羟肟酸衍生物及其作为组蛋白脱乙酰酶抑制剂的用途
公开(公告)号：US20050124679A1
公开(公告)日：2005-06-09
申请号：US10510630
申请日：2003-04-10
申请人： Dae-Kee Kim , Ju Young Lee , Nam Kyu Lee , Jae-Sun Kim , Junwon Lee , Suk Ho Lee , Jin Young Choi , Nam Ho Kim , Guang-Jin Im , Tae Kon Kim , Tae Kon Kim , Jung-Woo Seo , Young-Jue Bang
发明人： Dae-Kee Kim , Ju Young Lee , Nam Kyu Lee , Jae-Sun Kim , Junwon Lee , Suk Ho Lee , Jin Young Choi , Nam Ho Kim , Guang-Jin Im , Tae Kon Kim , Tae Kon Kim , Jung-Woo Seo , Young-Jue Bang
IPC分类号： C07D401/04 , C07C259/06 , C07C317/44 , C07D213/38 , C07D213/71 , C07D213/81 , C07D213/82 , C07D215/48 , C07D215/54 , C07D295/155 , A61K31/40 , A61K31/19 , C07C259/04 , C07D207/30
CPC分类号： C07D213/82 , C07C259/06 , C07C317/44 , C07D213/38 , C07D213/71 , C07D213/81 , C07D215/48 , C07D215/54 , C07D295/155
摘要： Disclosed are agents that inhibit histone deacetylase. More specifically, the present invention relates to novel hydroxamic acid derivatives or pharmaceutically acceptable salts thereof for anticancer agents or other therapeutic agents based on their histone deacetylase inhibitory activity.
摘要翻译：公开了抑制组蛋白脱乙酰酶的药剂。更具体地，本发明涉及用于抗癌剂或其它治疗剂的新型异羟肟酸衍生物或其药学上可接受的盐，基于其组蛋白脱乙酰酶抑制活性。

4. 发明授权

US07442714B2 Amlodipine gentisate and a method of its preparation 失效
标题翻译：氨氯地平龙胆和其制备方法
公开(公告)号：US07442714B2
公开(公告)日：2008-10-28
申请号：US10583438
申请日：2004-12-15
申请人： Jae-Sun Kim , Jin Young Choi , Je Ho Ryu , Nam Kyu Lee , Jeong-soo Jang , Woo Jae Jang , Key An Um , Do Seung Kum
发明人： Jae-Sun Kim , Jin Young Choi , Je Ho Ryu , Nam Kyu Lee , Jeong-soo Jang , Woo Jae Jang , Key An Um , Do Seung Kum
IPC分类号： A61K31/44 , C07D213/80
CPC分类号： C07D211/90
摘要： The present invention relates to an acid salt of amlodipine gentisate and a method of its preparation. More particularly, the present invention relates to a crystalline acid salt of amlodipine gentisate of the following formula 1 prepared by reacting amlodipine and gentisic acid, which is useful for the treatment of cardiovascular diseases and has the advantages of low toxicity, excellent stability, improved pharmaceutical efficacies and long-lasting concentration in blood.
摘要翻译：本发明涉及一种氨氯地平龙胆酸的酸性盐及其制备方法。更具体地说，本发明涉及通过使氨氯地平和龙胆酸反应制备的下式1的氨氯地平结晶酸盐，其可用于治疗心血管疾病，并且具有毒性低，稳定性优异的药物血液中的功效和持久的浓度。

5. 发明授权

US07772400B2 Optical resolution method of amlodipine 失效
标题翻译：氨氯地平的光学拆分方法
公开(公告)号：US07772400B2
公开(公告)日：2010-08-10
申请号：US11792281
申请日：2005-12-02
申请人： Jae-Sun Kim , Jin Young Choi , Nam Ho Kim , Nam Kyu Lee
发明人： Jae-Sun Kim , Jin Young Choi , Nam Ho Kim , Nam Kyu Lee
IPC分类号： C07D213/803
CPC分类号： C07D211/90
摘要： The present invention relates to a method for optical resolution of amlodipines by using isopropanol solvent and optically active O,O′-dibenzoyl tartaric acid as chiral reagent. More particularly, the present invention relates to a method comprising (a) obtaining (R)- or (S)-amlodipine dibenzoyl tartrate salt or solvate thereof by reacting (R,S)-amlodipines with optically active O,O′-dibenzoyl tartaric acid in isopropanol solvent, and (b) treating the (R)- or (S)-amlodipine salt with a base, thus obtaining optically active amlodipine.
摘要翻译：本发明涉及通过使用异丙醇溶剂和光学活性的O，O-二苯甲酰基酒石酸作为手性试剂来旋光拆分氨氯地平的方法。更具体地说，本发明涉及一种方法，其包括（a）通过使（R，S） - 氨氯地平与光学活性的O，O-二苯甲酰基酒石酸盐反应获得（R） - 或（S） - 氨氯地平二苯甲酰酒石酸盐或其溶剂合物异丙醇溶剂中的酸，和（b）用碱处理（R） - 或（S） - 氨氯地平盐，从而得到光学活性的氨氯地平。

6. 发明申请

US20080249314A1 Optical Resolution Method of Amlodipine 失效
标题翻译：氨氯地平的光学分辨方法
公开(公告)号：US20080249314A1
公开(公告)日：2008-10-09
申请号：US11792281
申请日：2005-12-02
申请人： Jae-Sun Kim , Jin Young Choi , Nam Ho Kim , Nam Kyu Lee
发明人： Jae-Sun Kim , Jin Young Choi , Nam Ho Kim , Nam Kyu Lee
IPC分类号： C07D213/803
CPC分类号： C07D211/90
摘要： The present invention relates to a method for optical resolution of amlodipines by using isopropanol solvent and optically active O,O′-dibenzoyl tartaric acid as chiral reagent. More particularly, the present invention relates to a method comprising (a) obtaining (R)— or (S)-amlodipine dibenzoyl tartrate salt or solvate thereof by reacting (R,S)-amlodipines with optically active O,O′-dibenzoyl tartaric acid in isopropanol solvent, and (b) treating the (R)— or (S)-amlodipine salt with a base, thus obtaining optically active amlodipine.
摘要翻译：本发明涉及通过使用异丙醇溶剂和光学活性的O，O-二苯甲酰基酒石酸作为手性试剂来旋光拆分氨氯地平的方法。更具体地说，本发明涉及一种方法，其包括（a）通过使（R，S） - 氨氯地平与光学活性的O，O-二苯甲酰基酒石酸盐反应获得（R） - 或（S） - 氨氯地平二苯甲酰酒石酸盐或其溶剂合物异丙醇溶剂中的酸，和（b）用碱处理（R） - 或（S） - 氨氯地平盐，从而得到光学活性的氨氯地平。

7. 发明申请

US20080207614A1 QUINAZOLINE DERIVATIVES FOR THE TREATMENT AND PREVENTION OF DIABETES AND OBESITY 审中-公开
标题翻译：用于治疗和预防糖尿病和肥胖的喹诺酮衍生物
公开(公告)号：US20080207614A1
公开(公告)日：2008-08-28
申请号：US11772098
申请日：2007-06-29
申请人： Nam Kyu Lee , Jun Won Lee , Sukho Lee , Guang-Jin Im , Hye Young Han , Tae Kon Kim , Yong Hyuk Kim , Wie-Jong Kwak , Sang Woong Kim , Joohun Ha , Eon Kyum Kim , Jung Kyu Lee , Choong Yeul Yoo , Dae Yeon Lee
发明人： Nam Kyu Lee , Jun Won Lee , Sukho Lee , Guang-Jin Im , Hye Young Han , Tae Kon Kim , Yong Hyuk Kim , Wie-Jong Kwak , Sang Woong Kim , Joohun Ha , Eon Kyum Kim , Jung Kyu Lee , Choong Yeul Yoo , Dae Yeon Lee
IPC分类号： A61K31/517 , A61P3/10 , C07D239/72 , C07D413/02 , C07D401/02 , C07D239/86 , A61P3/04
CPC分类号： C07D239/91 , C07D239/93 , C07D239/94 , C07D239/95 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to novel quinazoline derivatives effective in lowering blood glucose level and body weight, and a medicine for treatment and/or prevention of diabetes and/or obesity, which comprises the compound as an active ingredient.
摘要翻译：本发明涉及有效降低血糖水平和体重的新型喹唑啉衍生物，以及用于治疗和/或预防糖尿病和/或肥胖症的药物，其包含该化合物作为活性成分。

8. 发明授权

US07601736B2 Pyridine derivatives, a process for their preparation and a pharmaceutical composition containing the same 有权
标题翻译：吡啶衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US07601736B2
公开(公告)日：2009-10-13
申请号：US10585029
申请日：2004-12-30
申请人： Hyung Ook Kim , Nam Kyu Lee , Joo Hyon Kim , Hae In Rhee , Yong-Baik Cho , Je Ho Ryu , Nam Ho Kim , Keun Ho Ryu , Jung Bum Yi , Jae Yoon Jung
发明人： Hyung Ook Kim , Nam Kyu Lee , Joo Hyon Kim , Hae In Rhee , Yong-Baik Cho , Je Ho Ryu , Nam Ho Kim , Keun Ho Ryu , Jung Bum Yi , Jae Yoon Jung
IPC分类号： A01N43/42 , A61K31/44 , C07D471/02 , C07D491/02 , C07D498/02
CPC分类号： C07D471/04 , C07D491/052
摘要： The invention relates to novel pyridine derivatives having an inhibitory effect on production of cytokines, which are involved in inflammatory responses, thus suggesting its usefulness as therapeutic agents for treating diseases related to inflammation, immune, chronic inflammation as well as an agent having an anti-inflammatory and analgesic effect. Further, this invention relates to a method of manufacturing the same and a pharmaceutical composition containing the same.
摘要翻译：本发明涉及具有抑制细胞因子产生抑制作用的新型吡啶衍生物，其涉及炎性反应，因此表明其用作治疗与炎症，免疫，慢性炎症有关的疾病的治疗剂以及具有抗炎作用的药物，炎症和镇痛作用。此外，本发明涉及其制造方法和含有该组合物的药物组合物。

9. 发明申请

US20080306277A1 Process for Preparation of Chiral Amlodipine Gentisate 审中-公开
标题翻译：手性氨氯地平龙胆酸的制备方法
公开(公告)号：US20080306277A1
公开(公告)日：2008-12-11
申请号：US12090264
申请日：2006-10-17
申请人： Jae-Sun Kim , Nam Ho Kim , Nam Kyu Lee
发明人： Jae-Sun Kim , Nam Ho Kim , Nam Kyu Lee
IPC分类号： C07D211/90
CPC分类号： C07D211/90
摘要： The present invention relates to a process for the preparation of optically pure amlodipine gentisate, more particularly to a continuous process for the preparation of optically pure amlodipine gentisate with good yield and high optical purity. The processes can be preformed by first reacting racemic (R,S)-amlodipine and optically pure O,O′-dibenzoyltartaric acid in the presence of a solvent including isopropanol to prepare (R)- or (S)-amlodipine dibenzoyltartarate diastereomer or a solvate thereof, treating the prepared amlodipine diastereomeric salt or a solvate thereof with a base and then finally adding gentisic acid.
摘要翻译：本发明涉及一种制备光学纯氨氯地平龙胆酸盐的方法，更具体地说，涉及一种以高产率和高光学纯度制备光学纯氨氯地平龙胆酸盐的连续方法。该方法可以通过在包含异丙醇的溶剂的存在下首先使外消旋（R，S） - 氨氯地平和光学纯的O，O-二苯甲酰基酒石酸反应来制备（R） - 或（S） - 氨氯地平二苯甲酰三酸盐非对映异构体或溶剂合物，用碱处理制备的氨氯地平非对映体盐或其溶剂合物，然后最后加入龙胆酸。

10. 发明申请

US20100099773A1 INCLUSION COMPLEX OF SIBUTRAMINE AND BETA-CYCLODEXTRIN 审中-公开
标题翻译：包含SIBUTRAMINE和BETA-CYCLODEXTRIN的复合物
公开(公告)号：US20100099773A1
公开(公告)日：2010-04-22
申请号：US12444080
申请日：2007-11-22
申请人： Jae-Sun Kim , Nam Ho Kim , Jin Young Lee , Nam Kyu Lee , Joon Gyo Oh , Yong Youn Hwang , Dong-Chul Shin , Yoon-Jung Lee , Key An Um , Sun Ho Kim , Jin-Heung Sung
发明人： Jae-Sun Kim , Nam Ho Kim , Jin Young Lee , Nam Kyu Lee , Joon Gyo Oh , Yong Youn Hwang , Dong-Chul Shin , Yoon-Jung Lee , Key An Um , Sun Ho Kim , Jin-Heung Sung
IPC分类号： A61K31/135 , A61P25/00
CPC分类号： A61K31/135 , A61K47/6951 , B82Y5/00 , C08B37/0015
摘要： The present invention relates to a sibutramine-containing inclusion complex having superior storage stability, and particularly to a pharmaceutically stable inclusion complex suitable for the drug formulation, which prepared by reacting a sibutramine (N,N-dimethyl-1-[1-(4-chlorophenyl)-cyclobutyl]-3-methylbutylamine) of Formula 1 and beta-cyclodextrin in a predetermined ratio, its preparation method and a pharmaceutical composition comprising the same.
摘要翻译：本发明涉及具有优异储存稳定性的西布曲明含量复合物，特别涉及适用于药物制剂的药学上稳定的包合络合物，其通过使西布曲明（N，N-二甲基-1- [1-（4 - 氯苯基） - 环丁基] -3-甲基丁胺）和β-环糊精，其制备方法和包含其的药物组合物。

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