公开(公告)号：US06444796B1

公开(公告)日：2002-09-03

申请号：US09693795

申请日：2000-10-20

Applicant: Kwee-Hyun Suh ,  Mi-Ra Seong ,  Nam-Du Kim ,  Gwan-Sun Lee

Inventor： Kwee-Hyun Suh ,  Mi-Ra Seong ,  Nam-Du Kim ,  Gwan-Sun Lee

IPC: C07H100

CPC classification number: C07H17/08

Abstract: Pure Form II crystals of clarithromycin can be prepared by a simple, high-yield process comprising the steps of treating crude clarithromycin or different crystal forms of clarithromycin with formic acid in an organic solvent to obtain crystalline clarithromycin formate and neutralizing the clarithromycin formate with a base in a mixture of water and a water-miscible organic solvent.

Abstract translation: 克拉霉素的纯II型晶体可以通过简单的高产率方法制备，包括以下步骤：在有机溶剂中用甲酸处理克拉霉素或不同结晶形式的克拉霉素，得到结晶克拉霉素甲酸盐，并用碱中和克拉霉素甲酸盐 在水和水混溶性有机溶剂的混合物中。

公开(公告)号：US06388091B1

公开(公告)日：2002-05-14

申请号：US09990041

申请日：2001-11-20

Applicant: Kwang-Ok Lee ,  Hee-Seock Kim ,  Young-Jin Ham ,  Maeng-Sup Kim ,  Han-Kyeng Kim ,  Cheol-Kyeung Kim ,  Kum-Sin Jung ,  Hoe-Chul Lee ,  Ki-Eun Kim ,  Gwan-Sun Lee

Inventor： Kwang-Ok Lee ,  Hee-Seock Kim ,  Young-Jin Ham ,  Maeng-Sup Kim ,  Han-Kyeng Kim ,  Cheol-Kyeung Kim ,  Kum-Sin Jung ,  Hoe-Chul Lee ,  Ki-Eun Kim ,  Gwan-Sun Lee

IPC: C07D23358

CPC classification number: C07D231/12 ,  C07D209/88 ,  C07D233/56 ,  C07D249/08 ,  C07D403/06

Abstract: Pure -1,2,3,9-tetrahydro-9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-carbazol-4-one or a pharmaceutically acceptable salt thereof is prepared in a high yield by a simple process which reacts 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one with a 2-methylimidazole derivative in an organic solvent or in a mixture of an organic solvent and water in the presence of a halosilane compound.

Abstract translation: 制备纯的-1,2,3,9-四氢-9-甲基-3 - [（2-甲基-1H-咪唑-1-基）甲基] -4H-咔唑-4-酮或其药学上可接受的盐 通过使1,2,3,9-四氢-9-甲基-4H-咔唑-4-酮与有机溶剂或有机溶剂和有机溶剂的混合物中的2-甲基咪唑衍生物的单一方法以高产率 水在卤代硅烷化合物存在下。

公开(公告)号：US08624026B2

公开(公告)日：2014-01-07

申请号：US13502260

申请日：2010-10-19

Applicant: Nam Du Kim ,  Ji Yeon Chang ,  Dong Jun Kim ,  Hyun Seung Lee ,  Jae Hyuk Jung ,  Young Kil Chang ,  Gwan Sun Lee

Inventor： Nam Du Kim ,  Ji Yeon Chang ,  Dong Jun Kim ,  Hyun Seung Lee ,  Jae Hyuk Jung ,  Young Kil Chang ,  Gwan Sun Lee

IPC: C07D487/00

CPC classification number: A61K31/4985 ,  C07D487/04

Abstract: Disclosed are a novel, simple and low-cost method for preparing sitagliptin of formula (I), as DPP-IV (dipeptidyl peptidase IV) inhibitor, which is useful in treating type 2 diabetes mellitus and key intermediates used in said preparation of sitagliptin:

Abstract translation: 公开了用于制备式（I）的西他列汀的新型，简单和低成本的方法，DPP-IV（二肽基肽酶IV）抑制剂，其可用于治疗所述西他列汀制备中使用的2型糖尿病和关键中间体：

公开(公告)号：US08569490B2

公开(公告)日：2013-10-29

申请号：US13140640

申请日：2009-12-24

Applicant: Jaeheon Lee ,  Gha-Seung Park ,  Jin Hee Kim ,  Ji Eun Lee ,  Chul Hyun Park ,  Tae Jin Choi ,  Eun-Ju Park ,  Cheol Kyung Kim ,  Eun Jung Lim ,  Young-Kil Chang ,  Gwan Sun Lee

Inventor： Jaeheon Lee ,  Gha-Seung Park ,  Jin Hee Kim ,  Ji Eun Lee ,  Chul Hyun Park ,  Tae Jin Choi ,  Eun-Ju Park ,  Cheol Kyung Kim ,  Eun Jung Lim ,  Young-Kil Chang ,  Gwan Sun Lee

IPC: C07D473/18 ,  C07F7/08 ,  C07C49/517

CPC classification number: C07D473/18

Abstract: The present invention relates to a novel, high-yield and low-cost method for preparing entecavir, [1-S-(1α,3α,4β)]-2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H-purin-6-one, an antiviral agent, and novel intermediates used therein.

Abstract translation: 本发明涉及一种制备恩替卡韦[1-S-（1α，3α，4α）] -2-氨基-1,9-二氢-9- [4-羟基 -3-（羟甲基）-2-亚甲基环戊基] -6H-嘌呤-6-酮，抗病毒剂及其中使用的新型中间体。

公开(公告)号：US08476230B2

公开(公告)日：2013-07-02

申请号：US12523050

申请日：2008-01-04

Applicant: Dae Hae Song ,  Chang Ki Lim ,  Tae Hun Song ,  Young Hoon Kim ,  Se Chang Kwon ,  Gwan Sun Lee ,  Sung Youb Jung ,  In Young Choi

Inventor： Dae Hae Song ,  Chang Ki Lim ,  Tae Hun Song ,  Young Hoon Kim ,  Se Chang Kwon ,  Gwan Sun Lee ,  Sung Youb Jung ,  In Young Choi

IPC: A61K38/00 ,  A61K39/395 ,  A61P5/50

CPC classification number: C07K14/57563 ,  A61K38/00 ,  A61K47/6835 ,  C07K14/605

Abstract: The present invention relates to an insulinotropic peptide conjugate having improved in-vivo duration of efficacy and stability, comprising an insulinotropic peptide, a non-peptide polymer and an immunoglobulin Fc region, which are covalently linked to each other, and a use of the same. The insulinotropic peptide conjugate of the present invention has the in-vivo activity which is maintained relatively high, and has remarkably increased blood half-life, and thus it can be desirably employed in the development of long acting formulations of various peptide drugs.

Abstract translation: 本发明涉及具有改善的功效和稳定性的体内持续时间的促胰岛素肽缀合物，其包含彼此共价连接的促胰岛素肽，非肽聚合物和免疫球蛋白Fc区，并且使用它们 。 本发明的促胰岛素肽缀合物具有保持较高的体内活性，并且血液半衰期显着增加，因此可以理想地用于开发各种肽药物的长效制剂。

公开(公告)号：US08349969B2

公开(公告)日：2013-01-08

申请号：US12993336

申请日：2009-05-19

Applicant: Pyeong-uk Park ,  Seong-Nyun Kim ,  Woo-Hyuk Choi ,  Hak-Sun Jang ,  Gwan-Sun Lee ,  Se-Chang Kwon

Inventor： Pyeong-uk Park ,  Seong-Nyun Kim ,  Woo-Hyuk Choi ,  Hak-Sun Jang ,  Gwan-Sun Lee ,  Se-Chang Kwon

IPC: C08F283/06 ,  C08G65/332 ,  C08G65/333 ,  C08G65/334

CPC classification number: C08G65/326 ,  C08G65/323 ,  C08G65/324 ,  C08G65/3312 ,  C08G65/33317 ,  C08G65/33337 ,  C08G65/33365 ,  C08G65/33368 ,  C08G65/3346 ,  C08G65/337 ,  C08G65/338

Abstract: A method for preparing high-purity polyethyleneglycol-alkylenealdehydes and derivatives thereof is provided.

Abstract translation: 提供了制备高纯度聚乙二醇 - 亚烷基醛及其衍生物的方法。

公开(公告)号：US20110200623A1

公开(公告)日：2011-08-18

申请号：US13055406

申请日：2009-07-23

Applicant: Dae Hae Song ,  Jae Hee Shin ,  Mi Ji Lee ,  Sung Hee Hong ,  Se Chang Kwon ,  Gwan Sun Lee

Inventor： Dae Hae Song ,  Jae Hee Shin ,  Mi Ji Lee ,  Sung Hee Hong ,  Se Chang Kwon ,  Gwan Sun Lee

IPC: A61K39/395 ,  C07K17/00 ,  C12N9/96 ,  A61K39/00 ,  A61P31/00 ,  A61P5/00 ,  A61P5/50

CPC classification number: A61K47/48715 ,  A61K47/60 ,  A61K47/6811 ,  A61K47/6889 ,  C07K14/59 ,  C07K19/00 ,  C07K2319/31

Abstract: Disclosed is a protein complex, comprising a physiologically active polypeptide, a dimeric protein and a non-peptidyl polymer having three functional ends (3-arm), with the linkage of both the physiologically active polypeptide and the dimeric protein to the 3-arm non-peptidyl polymer via respective covalent bonds. The protein complex guarantees the long acting activity and biostability of a physiologically active polypeptide. Having the ability to maintain the bioactivity of physiologically active polypeptides or peptides highly and to significantly improve the serum half life of the polypeptides or peptides, the protein complex can be applied to the development of sustained release formulations of various physiologically active polypeptide drugs. Also, it utilizes raw materials including the physiologically active polypeptides without significant loss, thereby increasing the production yield. Further, it can be easily purified.

Abstract translation: 公开了一种蛋白质复合物，其包含生理活性多肽，二聚体蛋白质和具有三个功能性末端（3-臂）的非肽基聚合物，其具有生理活性多肽和二聚体蛋白质与3-臂非 - - 肽基聚合物。 蛋白质复合物保证生理活性多肽的长效和生物稳定性。 具有维持生理活性多肽或肽的生物活性以及显着改善多肽或肽的血清半衰期的能力，蛋白质复合物可用于开发各种生理活性多肽药物的持续释放制剂。 此外，它利用包括生理活性多肽的原料，而不会显着损失，从而提高产量。 此外，它可以容易地纯化。

公开(公告)号：US07799907B2

公开(公告)日：2010-09-21

申请号：US11573869

申请日：2005-12-29

Applicant: Jaeheon Lee ,  Gha Seung Park ,  Moonsub Lee ,  Hyo-Jeong Bang ,  Jae Chul Lee ,  Cheol Kyong Kim ,  Chang-Ju Choi ,  Han Kyong Kim ,  Hoe Chul Lee ,  Young-Kil Chang ,  Gwan Sun Lee

Inventor： Jaeheon Lee ,  Gha Seung Park ,  Moonsub Lee ,  Hyo-Jeong Bang ,  Jae Chul Lee ,  Cheol Kyong Kim ,  Chang-Ju Choi ,  Han Kyong Kim ,  Hoe Chul Lee ,  Young-Kil Chang ,  Gwan Sun Lee

IPC: C07H19/073

CPC classification number: C07H19/04 ,  Y02P20/55

Abstract: Provided is an improved method for stereoselectively preparing 2′-deoxy-2′,2′-difluorocytidine of formula (I), which includes reacting a 1-halo ribofuranose compound with a nucleobase of formula (IV) in a solvent to obtain a nucleo side of formula (II) with removal of a silyl halide ((alkyl)3SiX (X=halide)); and deprotecting the nucleoside of formula (II) to obtain 2′-deoxy-2′,2′-difluorocytidine of formula (I). 2′-Deoxy-2′,2′-difluorocytidine of formula (I) is effective for treating various cancers such as non-small cell lung (NSCLC), pancreatic, bladder, breast or ovarian cancers.

Abstract translation: 提供了一种用于立体选择性制备式（I）的2'-脱氧-2'，2'-二氟胞苷的改进方法，其包括使1-卤代呋喃核糖化合物与式（IV）的核碱基在溶剂中反应以获得核 除去甲硅烷基卤化物（（烷基）3 SiX（X =卤化物））的式（II）侧。 并使式（II）的核苷脱保护，得到式（I）的2'-脱氧-2'，2'-二氟胞苷。 式（I）的2'-脱氧-2'，2'-二氟胞苷对于治疗各种癌症如非小细胞肺（NSCLC），胰腺，膀胱，乳腺或卵巢癌是有效的。

公开(公告)号：US20100179120A1

公开(公告)日：2010-07-15

申请号：US12663263

申请日：2008-06-05

Applicant: Kwang-Ok Lee ,  Mi Young Cha ,  Mi Ra Kim ,  Young Hee Jung ,  Chang Gon Lee ,  Se Young Kim ,  Keukchan Bang ,  Bum Woo Park ,  Bo Im Choi ,  Yun Jung Chae ,  Mi Young Ko ,  Han Kyong Kim ,  Young-Gil Ahn ,  Maeng Sup Kim ,  Gwan Sun Lee

Inventor： Kwang-Ok Lee ,  Mi Young Cha ,  Mi Ra Kim ,  Young Hee Jung ,  Chang Gon Lee ,  Se Young Kim ,  Keukchan Bang ,  Bum Woo Park ,  Bo Im Choi ,  Yun Jung Chae ,  Mi Young Ko ,  Han Kyong Kim ,  Young-Gil Ahn ,  Maeng Sup Kim ,  Gwan Sun Lee

IPC: A61K31/517 ,  C07D403/12 ,  A61K31/496 ,  A61K31/397 ,  A61P35/00

CPC classification number: C07D403/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14

Abstract: The present invention provides a novel amide derivative and a pharmaceutically acceptable salt thereof which selectively and effectively inhibits the growth of cancer cells induced by the overexpression of an epidermal growth factor receptor and also prevents the development of drug resistance caused by the mutation of EGFR tyrosine kinase, and a pharmaceutical composition comprising same as an active ingredient.

Abstract translation: 本发明提供了一种新颖的酰胺衍生物及其药学上可接受的盐，其选择性和有效地抑制由表皮生长因子受体过表达诱导的癌细胞的生长，并且还防止由EGFR酪氨酸激酶突变引起的耐药性的发展 ，以及含有活性成分的药物组合物。

公开(公告)号：US07737260B2

公开(公告)日：2010-06-15

申请号：US10535232

申请日：2004-11-13

Applicant: Young Min Kim ,  Dae Jin Kim ,  Sung Min Bae ,  Chang Ki Lim ,  Se Chang Kwon ,  Gwan Sun Lee

Inventor： Young Min Kim ,  Dae Jin Kim ,  Sung Min Bae ,  Chang Ki Lim ,  Se Chang Kwon ,  Gwan Sun Lee

IPC: C07K16/00

CPC classification number: A61K47/68 ,  A61K47/6811 ,  A61K47/6813 ,  A61K47/6835 ,  C07K14/505 ,  C07K14/535 ,  C07K14/56 ,  C07K14/61 ,  C07K16/46 ,  C07K19/00 ,  C07K2317/52 ,  C07K2317/732 ,  C07K2317/734 ,  C07K2319/30

Abstract: Disclosed are a protein conjugate with improved in vivo duration and stability and the use thereof. The protein conjugate includes a physiologically active polypeptide, a non-peptide polymer and an immunoglobulin Fc fragment. Since the three components are covalently linked, the protein conjugate has extended in vivo duration and enhanced stability for the physiologically active polypeptide. The protein conjugate maintains the in vivo activity at relatively high levels and remarkably increases the serum half-life for the physiologically active polypeptide, with less risk of inducing undesirable immune responses. Thus, the protein conjugate is useful for developing long-acting formulations of various polypeptide drugs.

Abstract translation: 公开了具有改善的体内持续时间和稳定性的蛋白质缀合物及其用途。 蛋白质缀合物包括生理活性多肽，非肽聚合物和免疫球蛋白Fc片段。 由于三种成分共价连接，因此蛋白质缀合物延长了生理活性多肽的体内持续时间和增强的稳定性。 蛋白质缀合物以较高的水平保持体内活性，并显着增加生理活性多肽的血清半衰期，具有诱导不良免疫反应的风险较小。 因此，蛋白质缀合物可用于开发各种多肽药物的长效制剂。