公开(公告)号：US20120003712A1

公开(公告)日：2012-01-05

申请号：US13255199

申请日：2010-03-18

Applicant: Dae Hae Song ,  Jae Hee Shin ,  Jae Min Lee ,  Young Kyung Park ,  Se Chang Kwon ,  Gwan Sun Lee

Inventor： Dae Hae Song ,  Jae Hee Shin ,  Jae Min Lee ,  Young Kyung Park ,  Se Chang Kwon ,  Gwan Sun Lee

IPC: C12N9/00 ,  C07K14/505 ,  C07K14/52 ,  C07K14/53 ,  C07K14/575 ,  C07K14/585 ,  C07K14/59 ,  C07K14/595 ,  C07K14/605 ,  C07K14/61 ,  C07K14/62 ,  C07K14/655 ,  C07K7/16 ,  C07K7/04 ,  C07K9/00 ,  C07K14/475

CPC classification number: C07K1/1077 ,  A61K47/60 ,  C07K14/575 ,  C07K14/605 ,  C07K14/62

Abstract: The present invention provides a method for preparing a site-specific physiologically active polypeptide conjugate in a high yield by treating a physiologically active polypeptide with a non-peptidyl polymer in the presence of an alcohol at a specific pH, which can be desirably employed in the development of long acting formulations of various peptide drugs having high in-vivo activity and markedly prolonged in-blood half-life.

Abstract translation: 本发明提供了一种通过在特定pH下在醇的存在下用非肽基聚合物处理生理活性多肽而以高产率制备位点特异性生理活性多肽缀合物的方法，其可以理想地用于 开发具有高体内活性和明显延长的血液半衰期的各种肽药物的长效制剂。

公开(公告)号：US20110251387A1

公开(公告)日：2011-10-13

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] b] -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：US07968316B2

公开(公告)日：2011-06-28

申请号：US12063379

申请日：2006-08-16

Applicant: Sung youb Jung ,  Jin Sun Kim ,  Jin hwan Shin ,  Se-Chang Kwon ,  Gwan-Sun Lee ,  Dae hae Song

Inventor： Sung youb Jung ,  Jin Sun Kim ,  Jin hwan Shin ,  Se-Chang Kwon ,  Gwan-Sun Lee ,  Dae hae Song

IPC: C12P21/04 ,  C12N15/64 ,  C12N15/00 ,  C07H21/04

CPC classification number: C07K16/00 ,  A61K47/6811 ,  A61K47/6835 ,  C07K2317/41 ,  C07K2317/52

Abstract: Disclosed is a method for the mass production of a monomeric or dimeric immunoglobulin Fc region, free of initial methionine residues, using a recombinant expression vector comprising a nucleotide sequence coding for a recombinant immunoglobulin Fc region comprising an immunoglobulin Fc region linked at the N-terminus thereof to an immunoglobulin Fc region via a peptide bond.

Abstract translation: 公开了使用包含编码重组免疫球蛋白Fc区的核苷酸序列的重组表达载体大规模生产不含初始甲硫氨酸残基的方法，所述重组表达载体包含在N末端连接的免疫球蛋白Fc区 通过肽键与免疫球蛋白Fc区连接。

公开(公告)号：US20100330108A1

公开(公告)日：2010-12-30

申请号：US12744660

申请日：2008-11-28

Applicant: Dae Hae Song ,  Min Young Kim ,  Young Jin Park ,  Eun Hee Kang ,  Sung Youb Jung ,  Se Chang Kwon ,  Gwan Sun Lee

Inventor： Dae Hae Song ,  Min Young Kim ,  Young Jin Park ,  Eun Hee Kang ,  Sung Youb Jung ,  Se Chang Kwon ,  Gwan Sun Lee

IPC: A61K39/00 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  C07K16/00

CPC classification number: C07K19/00 ,  A61K47/6811 ,  A61K47/6813 ,  A61K47/6835 ,  C07K2319/30

Abstract: The present invention relates to a composition for treating obesity-related diseases comprising an insulinotropic peptide conjugate, more particularly, to a composition for treating obesity-related diseases comprising a conjugate prepared by covalently linking the insulinotropic peptide with a carrier substance via a non-peptidyl linker, and a method for treating obesity-related diseases by using the same. In particular, the composition for treating obesity-related diseases according to the present invention remarkably improves the efficacy of suppressing food intake and its duration to reduce body weight and body fat, thereby being useful for the treatment of obesity-related diseases.

Abstract translation: 本发明涉及一种用于治疗肥胖相关疾病的组合物，其包括促胰岛素肽缀合物，更具体地，涉及用于治疗肥胖相关疾病的组合物，其包含通过非肽基共价连接促胰岛素肽与载体物质而制备的缀合物 接头，以及通过使用它们来治疗肥胖相关疾病的方法。 特别地，本发明的治疗肥胖相关疾病的组合物显着地提高了抑制食物摄取的效果及其减轻体重和体脂的持续时间，从而可用于治疗肥胖相关疾病。

公开(公告)号：US07858761B2

公开(公告)日：2010-12-28

申请号：US11572790

申请日：2005-06-21

Applicant: Jaeheon Lee ,  Gha-Seung Park ,  Moonsub Lee ,  Han Kyong Kim ,  Hyo-Jeong Bang ,  Young-Kil Chang ,  Gwan Sun Lee

Inventor： Jaeheon Lee ,  Gha-Seung Park ,  Moonsub Lee ,  Han Kyong Kim ,  Hyo-Jeong Bang ,  Young-Kil Chang ,  Gwan Sun Lee

IPC: C07H23/00 ,  C07H11/04 ,  C07H5/02

CPC classification number: C07H3/08

Abstract: 1-α-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivative of formula (I) having the 3-hydroxy group protected with a biphenylcarbonyl group is a solid which can be easily purified by a simple procedure such as recrystallization, and therefore, it can be advantageously used as an intermediate in the preparation of gemcitabine in a large scale. Further, the 1-α-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivative of formula (I) can be prepared with high stereoselectivity using the compound of formula (V) as an intermediate.

Abstract translation: 具有用联苯基羰基保护的3-羟基的式（I）的1-α-卤代-2,2-二氟-2-脱氧-D-呋喃核糖衍生物是可以通过简单的方法容易地纯化的固体，例如 重结晶，因此可以有利地用作大量制备吉西他滨的中间体。 此外，式（I）的1-α-卤代-2,2-二氟-2-脱氧-D-呋喃核糖衍生物可以使用式（V）化合物作为中间体以高立体选择性制备。

公开(公告)号：US20100255014A1

公开(公告)日：2010-10-07

申请号：US12757635

申请日：2010-04-09

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: A61K47/48 ,  C07K19/00

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。

公开(公告)号：US20100204451A1

公开(公告)日：2010-08-12

申请号：US12669372

申请日：2008-07-16

Applicant: Sung Youb Jung ,  Chang Ki Lim ,  Dae Hae Song ,  Sung Min Bae ,  Young Hoon Kim ,  Se Chang Kwon ,  Gwan Sun Lee

Inventor： Sung Youb Jung ,  Chang Ki Lim ,  Dae Hae Song ,  Sung Min Bae ,  Young Hoon Kim ,  Se Chang Kwon ,  Gwan Sun Lee

IPC: C07K14/00

CPC classification number: C07K14/46 ,  A61K38/26 ,  C07K14/57563 ,  C07K14/605

Abstract: The present invention relates to an N-terminal amino acid-modified insulinotropic peptide having a high activity, and to a pharmaceutical composition comprising the same. The insulinotropic peptide derivatives according to the present invention exhibit therapeutic effects, which are not observed in native and other insulinotropic peptide analogs. Therefore, the insulinotropic peptide derivatives and the pharmaceutical composition comprising the same according to the present invention can be effectively provided for the treatment of the diseases.

Abstract translation: 本发明涉及具有高活性的N-末端氨基酸修饰的促胰岛素肽以及包含其的药物组合物。 根据本发明的促胰岛素肽衍生物显示出在天然和其他促胰岛素肽类似物中未观察到的治疗效果。 因此，可以有效地提供促胰岛素肽衍生物和包含其的本发明的药物组合物用于治疗疾病。

公开(公告)号：US20100137367A1

公开(公告)日：2010-06-03

申请号：US12531003

申请日：2008-04-04

Applicant: Tae Hee Ha ,  Chang Hee Park ,  Won Jeoung Kim ,  Hee Sook Oh ,  Seung Hwan Cho ,  Cheol Kyung Kim ,  Kwee Hyun Suh ,  Gwan Sun Lee

Inventor： Tae Hee Ha ,  Chang Hee Park ,  Won Jeoung Kim ,  Hee Sook Oh ,  Seung Hwan Cho ,  Cheol Kyung Kim ,  Kwee Hyun Suh ,  Gwan Sun Lee

IPC: A61K31/4545 ,  C07D401/12 ,  A61P17/00

CPC classification number: C07D401/12 ,  A61K9/143

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20100105869A1

公开(公告)日：2010-04-29

申请号：US12603757

申请日：2009-10-22

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 ,  C07K14/555

CPC classification number: C07K16/00 ,  A61K47/60 ,  A61K47/643 ,  A61K47/6811 ,  A61K47/6883

Abstract: A protein conjugate having a prolonged in vivo half-life of a physiological activity, comprising i) a physiologically active polypeptide, ii) a non-peptidic polymer, and iii) an immunoglobulin, is useful for the development of a polypeptide drug due to the enhanced in vivo stability and prolonged half-life in blood, while reducing the possibility of inducing an immune response.

Abstract translation: 具有延长的生理活性的体内半衰期的蛋白质缀合物，其包含i）生理活性多肽，ii）非肽聚合物和iii）免疫球蛋白，可用于开发多肽药物，因为 增强血液中的体内稳定性和延长的半衰期，同时降低诱导免疫反应的可能性。

公开(公告)号：US20100099876A1

公开(公告)日：2010-04-22

申请号：US12518213

申请日：2007-12-11

Applicant: Gwan Sun Lee ,  Young-Kil Chang ,  Jaeheon Lee ,  Chul Hyun Park ,  Eun-Ju Park ,  Jaeho Yoo

Inventor： Gwan Sun Lee ,  Young-Kil Chang ,  Jaeheon Lee ,  Chul Hyun Park ,  Eun-Ju Park ,  Jaeho Yoo

IPC: C07D215/18 ,  C07F9/09

CPC classification number: C07D215/18

Abstract: The present invention relates to a method for preparing montelukast, an inhibitor against leukotrienes, and an intermediate used therein. According to the inventive method, high-purity montelukast or its sodium salt can be prepared in a high yield.

Abstract translation: 本发明涉及一种制备孟鲁司特，抑制白三烯的方法及其中使用的中间体。 根据本发明的方法，可以高产率制备高纯度孟鲁司特或其钠盐。