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1. 发明申请

WO2012165915A2 COMPOSITION FOR TREATING DIABETES COMPRISING LONG-ACTING INSULIN CONJUGATE AND LONG-ACTING INSULINOTROPIC PEPTIDE CONJUGATE 审中-公开
标题翻译：用于治疗包含长效胰岛素结合剂和长效胰岛素诱导性糖尿病的糖尿病的组合物
公开(公告)号：WO2012165915A2
公开(公告)日：2012-12-06
申请号：PCT/KR2012004367
申请日：2012-06-01
申请人： HANMI SCIENCE CO LTD , WOO YOUNG EUN , JANG MYUNG HYUN , PARK YOUNG JIN , PARK YOUNG KYUNG , LIM CHANG KI , KWON SE CHANG
发明人： WOO YOUNG EUN , JANG MYUNG HYUN , PARK YOUNG JIN , PARK YOUNG KYUNG , LIM CHANG KI , KWON SE CHANG
IPC分类号： A61K47/48 , A61K38/28 , A61K47/30 , A61P3/10
CPC分类号： A61K47/48415 , A61K38/26 , A61K38/28 , A61K47/68 , A61K47/6811 , A61K47/6883
摘要： The present invention relates to a composition for the prevention or treatment of diabetes comprising a long-acting insulin conjugate and a long-acting insulinotropic peptide conjugate, and a therapeutic method for the treatment of diabetes, and more particularly, concurrent administration of the long-acting insulin conjugate and the long-acting insulinotropic peptide conjugate inhibits weight gain caused by insulin treatment, and vomiting and nausea caused by insulinotropic peptide treatment, and reduces the required dose of insulin, thereby remarkably improving drug compliance. Moreover, each of the long-acting insulin conjugate and the long-acting insulinotropic peptide conjugate of the present invention is prepared by linking insulin or insulinotropic peptide with an immunoglobulin Fc region via a non-peptidyl linker, thereby showing improved in-vivo duration of efficacy and stability.
摘要翻译：本发明涉及一种用于预防或治疗糖尿病的组合物，其包含长效胰岛素缀合物和长效促胰岛素肽缀合物，以及用于治疗糖尿病的治疗方法，更具体地说，作用胰岛素结合物和长效促胰岛素肽结合物抑制胰岛素治疗引起的体重增加，以及由促胰岛素肽治疗引起的呕吐和恶心，并减少所需的胰岛素剂量，从而显着提高药物依从性。此外，本发明的长效胰岛素缀合物和长效促胰岛素肽缀合物中的每一种都是通过非肽基连接体将胰岛素或促胰岛素肽与免疫球蛋白Fc区连接而制备的，从而显示出改善的体内持续时间功效和稳定性。

2. 发明申请

WO2012169798A3 NOVEL OXYNTOMODULIN DERIVATIVES AND PHARMACEUTICAL COMPOSITION FOR TREATING OBESITY COMPRISING THE SAME 审中-公开
标题翻译：用于治疗包含其的肥胖症的新型氧化色氨酸衍生物和药物组合物
公开(公告)号：WO2012169798A3
公开(公告)日：2013-02-14
申请号：PCT/KR2012004494
申请日：2012-06-07
申请人： HANMI SCIENCE CO LTD , JUNG SUNG YOUB , JANG MYUNG HYUN , SHEN LING AI , PARK YOUNG KYUNG , PARK YOUNG JIN , KWON SE CHANG
发明人： JUNG SUNG YOUB , JANG MYUNG HYUN , SHEN LING AI , PARK YOUNG KYUNG , PARK YOUNG JIN , KWON SE CHANG
IPC分类号： C07K14/605 , A61K38/26 , A61P3/04
CPC分类号： C07K14/605 , A61K38/00 , A61K38/177 , A61K38/22 , A61K38/26 , A61K45/06 , C07K14/575 , C07K14/705
摘要： The present invention relates to a novel peptide showing more excellent activities on a glucagon like peptide-1 receptor and a glucagon receptor than native oxyntomodulin, and a composition for the prevention or treatment of obesity comprising the peptide as an active ingredient. Unlike native oxyntomodulin, the novel peptide of the present invention reduces food intake, suppresses gastric emptying, and facilitates lipolysis with reduced side-effects, and also shows excellent receptor-activating effects. Thus, it can be widely used in the treatment of obesity with safety and efficacy.
摘要翻译：本发明涉及一种与天然胃泌酸调节素相比，胰高血糖素样肽-1受体和胰高血糖素受体的活性更优异的新型肽，以及用于预防或治疗包含该肽作为活性成分的肥胖症的组合物。与本发明的胃泌酸调节蛋白不同，本发明的新型肽减少食物摄入，抑制胃排空，促进脂肪分解，副作用降低，并且还显示出优异的受体激活作用。因此，可广泛用于治疗肥胖症的安全性和有效性。

3. 发明申请

WO2012165916A3 NON-PEPTIDYL POLYMER-INSULIN MULTIMER AND METHOD FOR PRODUCING THE SAME 审中-公开
标题翻译：非肽聚合物 - 胰岛素多元及其生产方法
公开(公告)号：WO2012165916A3
公开(公告)日：2013-03-28
申请号：PCT/KR2012004368
申请日：2012-06-01
申请人： HANMI SCIENCE CO LTD , LIM SUNG IN , JANG MYUNG HYUN , KIM DAE JIN , JUNG SUNG YOUB , KWON SE CHANG
发明人： LIM SUNG IN , JANG MYUNG HYUN , KIM DAE JIN , JUNG SUNG YOUB , KWON SE CHANG
IPC分类号： A61K47/48 , A61K38/28 , A61K47/30 , A61P3/10
CPC分类号： C07K14/62 , A61K38/28 , A61K47/52 , A61K47/60 , A61K47/6921
摘要： The present invention relates to a non-peptidyl polymer-insulin multimer comprising two or more of a non-peptidyl polymer-insulin conjugate prepared by linking a non-peptidyl polymer and insulin via a covalent bond, in which the conjugates are complexed with cobalt ion to form a multimer, a method and kit for the preparation of the multimer, a pharmaceutical composition for the prevention or treatment of diabetes comprising the multimer as an active ingredient, and a method for preventing or treating diabetes by administering the composition to a subject.
摘要翻译：本发明涉及一种非肽基聚合物 - 胰岛素多聚体，其包含通过共价键连接非肽基聚合物和胰岛素而制备的两种或多种非肽基聚合物 - 胰岛素结合物，其中缀合物与钴离子络合以形成多聚体的制备方法和试剂盒，用于预防或治疗糖尿病的药物组合物，其包含多聚体作为活性成分，以及通过向受试者施用该组合物来预防或治疗糖尿病的方法。

4. 发明申请

WO2012173422A1 A CONJUGATE COMPRISING OXYNTOMODULIN AND AN IMMUNOGLOBULIN FRAGMENT, AND USE THEREOF 审中-公开
标题翻译：包含氧化色氨酸和免疫球蛋白片段的结合物及其用途
公开(公告)号：WO2012173422A1
公开(公告)日：2012-12-20
申请号：PCT/KR2012004722
申请日：2012-06-15
申请人： HANMI SCIENCE CO LTD , JUNG SUNG YOUB , KIM DAE JIN , PARK SUNG HEE , WOO YOUNG EUN , CHOI IN YOUNG , KWON SE CHANG
发明人： JUNG SUNG YOUB , KIM DAE JIN , PARK SUNG HEE , WOO YOUNG EUN , CHOI IN YOUNG , KWON SE CHANG
IPC分类号： C07K14/575 , A61K38/26 , A61K47/48 , A61P3/04 , C07K17/00
CPC分类号： A61K47/6889 , A61K38/00 , A61K38/26 , A61K45/06 , A61K47/48215 , A61K47/48369 , A61K47/48415 , A61K47/60 , A61K47/68 , A61K47/6801 , A61K47/6811 , C07K14/575 , C07K2319/30
摘要： The present invention relates to a conjugate comprising oxyntomodulin, an immunoglobulin Fc region, and non-peptidyl polymer wherein the conjugate being obtainable by covalently linking oxyntomodulin to immunoglobulin Fc region via non-peptidyl polymer, and a pharmaceutical composition for the prevention or treatment of obesity comprising the conjugates. The conjugate comprising oxyntomodulin and the immunoglobulin Fc of the present invention reduces food intake, suppresses gastric emptying, and facilitates lipolysis without side-effects, unlike native oxyntomodulin, and also shows excellent receptor-activating effects and long-term sustainability, compared to native oxyntomodulin. Thus, it can be widely used in the treatment of obesity with safety and efficacy.
摘要翻译：本发明涉及包含胃泌酸调节蛋白，免疫球蛋白Fc区和非肽基聚合物的缀合物，其中通过非肽基聚合物共价连接胃泌酸调节蛋白与免疫球蛋白Fc区域可获得的缀合物和用于预防或治疗肥胖症的药物组合物包括缀合物。与天然胃泌酸调节蛋白不同，包含胃泌酸调节素和本发明的免疫球蛋白Fc的缀合物与天然胃泌酸调节素相比，降低食物摄入，抑制胃排空，并且促进无副作用的脂解作用，并且与天然胃泌酸调节素相比也显示出优异的受体激活作用和长期可持续性。因此，可广泛用于治疗肥胖症的安全性和有效性。

5. 发明申请

WO2012057525A3 LIQUID FORMULATIONS OF LONG ACTING INTERFERON ALPHA CONJUGATE 审中-公开
标题翻译：长效α干扰素的液体制剂
公开(公告)号：WO2012057525A3
公开(公告)日：2012-06-28
申请号：PCT/KR2011008038
申请日：2011-10-26
申请人： HANMI SCIENCE CO LTD , IM DAE SEONG , LEE JAE MIN , LEE JONG SOO , BAE SUNG MIN , KWON SE CHANG
发明人： IM DAE SEONG , LEE JAE MIN , LEE JONG SOO , BAE SUNG MIN , KWON SE CHANG
IPC分类号： A61K9/08 , A61K38/21 , A61K47/36 , A61P31/12
CPC分类号： A61K47/48415 , A61K9/0019 , A61K38/212 , A61K47/26 , A61K47/68 , A61K47/6813 , C07K14/56 , C07K16/46 , C07K2319/30
摘要： Disclosed is a liquid formulation in which a long-acting INFa conjugate that has improved in vivo duration and stability can be stored stably for a long period of time. It comprises a stabilizer comprising a buffer, a sugar alcohol, a non-ionic surfactant and an isotonic agent. Being free of human serum albumin and other potential factors harmful to the body, the liquid formulation is free of concerns about viral infections and guarantees excellent storage stability to long-acting INFa conjugates.
摘要翻译：公开了一种液体制剂，其中具有改善的体内持续时间和稳定性的长效INFα缀合物可长期稳定储存。它包含含有缓冲剂，糖醇，非离子表面活性剂和等渗剂的稳定剂。由于没有人体血清白蛋白和其他对身体有害的潜在因素，该液体制剂不受病毒感染的担忧，并且保证长效INFα缀合物具有优异的储存稳定性。

6. 发明申请

WO2012057527A3 METHOD FOR MASS PRODUCTION OF FACTOR VII/VIIA 审中-公开
标题翻译：大量生产VII / VIIA因子的方法
公开(公告)号：WO2012057527A3
公开(公告)日：2012-07-26
申请号：PCT/KR2011008040
申请日：2011-10-26
申请人： HANMI SCIENCE CO LTD , KIM CHANG HWAN , HONG SUNG KAP , LEE BYUNG SUN , HONG SUNG HWAN , KWON SE CHANG
发明人： KIM CHANG HWAN , HONG SUNG KAP , LEE BYUNG SUN , HONG SUNG HWAN , KWON SE CHANG
IPC分类号： C12N15/85 , C07K14/745 , C12N15/12
CPC分类号： C12N9/6437 , C07K14/745 , C12N15/85 , C12N2830/85
摘要： Disclosed is a method for the mass production of human coagulation factor VII. The method comprises a) constructing an expression vector carrying i) a dihydrofolate reductase promoter devoid of one or more CCGCC repeat sequences from the GC-rich region thereof and a dihydrofolate reductase (DHFR) gene operably linked thereto and ii) a cytomegalovirus (CMV) promoter and a human coagulation factor VII gene operably linked thereto; b) transfecting the expression vector of step a) into an animal cell line; c) culturing the transfected animal cell line of step b) in the presence of a dihydrofolate reductase inhibitor to select cells which express human coagulation factor VII with high efficiency; and d) adding sodium butyrate to the selected animal cells of step c), and a cell line for mass production of human coagulation factor VII. Employing a vector carrying a DHFR promoter devoid of GC-rich repeating sequences, the method can produce human coagulation factor VII at high efficiency on a large scale, which contributes to the treatment of hemophilia.
摘要翻译：公开了大量生产人凝血因子VII的方法。该方法包括：a）构建表达载体，其携带i）没有来自其富含GC的区域的一个或多个CCGCC重复序列的二氢叶酸还原酶启动子和与其可操作地连接的二氢叶酸还原酶（DHFR）基因，和ii）巨细胞病毒（CMV）启动子和与之有效连接的人凝血因子VII基因; b）将步骤a）的表达载体转染到动物细胞系中; c）在二氢叶酸还原酶抑制剂的存在下培养步骤b）的转染的动物细胞系以选择以高效率表达人凝血因子VII的细胞; 和d）向步骤c）的选定动物细胞中加入丁酸钠，以及大量生产人凝血因子VII的细胞系。携带携带没有富含GC的重复序列的DHFR启动子的载体，该方法可大规模高效地产生人凝血因子VII，这有助于血友病的治疗。

7. 发明申请

WO2009011544A3 INSULINOTROPIC PEPTIDE DERIVATIVE WHEREIN ITS N-TERMINAL AMINO ACID IS MODIFIED 审中-公开
标题翻译：胰岛素衍生物其N-末端氨基酸被修饰
公开(公告)号：WO2009011544A3
公开(公告)日：2009-03-19
申请号：PCT/KR2008004170
申请日：2008-07-16
申请人： HANMI PHARMACEUTICAL CO LTD , SONG DAE HAE , LIM CHANG KI , KIM YOUNG HOON , KWON SE CHANG , LEE GWAN SUN , BAE SUNG MIN , JUNG SUNG YOUB
发明人： SONG DAE HAE , LIM CHANG KI , KIM YOUNG HOON , KWON SE CHANG , LEE GWAN SUN , BAE SUNG MIN , JUNG SUNG YOUB
IPC分类号： C07K14/65
CPC分类号： C07K14/46 , A61K38/26 , C07K14/57563 , C07K14/605
摘要： 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.
摘要翻译：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。

8. 发明申请

WO2011090306A2 LIQUID FORMULATIONS FOR LONG-ACTING ERYTHROPOIETIN CONJUGATE 审中-公开
标题翻译：用于长期治疗肾上腺素受体的液体制剂
公开(公告)号：WO2011090306A2
公开(公告)日：2011-07-28
申请号：PCT/KR2011000370
申请日：2011-01-18
申请人： HANMI HOLDINGS CO LTD , BAE SUNG MIN , IM DAE SEONG , KIM MIN YOUNG , LIM CHANG KI , JUNG SUNG YOUB , KWON SE CHANG
发明人： BAE SUNG MIN , IM DAE SEONG , KIM MIN YOUNG , LIM CHANG KI , JUNG SUNG YOUB , KWON SE CHANG
IPC分类号： A61K9/08 , A61K9/22 , A61K38/16 , A61P7/06
CPC分类号： A61K47/02 , A61K9/0019 , A61K47/10 , A61K47/183 , A61K47/26 , A61K47/6811 , A61K47/6835
摘要： Disclosed is a liquid formulation which allows long-acting EPO conjugates, that have improved in vivo duration and stability, to be stable when stored for a long period of time. It comprises a stabilizer composition characterized by buffer and mannitol. Being free of human serum albumin and other potential factors harmful to the body, the liquid formulation is free of concerns about viral infections and guarantees excellent storage stability to long-acting EPO conjugates.
摘要翻译：公开了一种液体制剂，其允许具有改善的体内持续时间和稳定性的长效EPO缀合物在长时间储存时是稳定的。它包括以缓冲液和甘露醇为特征的稳定剂组合物。没有人血清白蛋白和其他对身体有害的潜在因素，液体制剂没有对病毒感染的担忧，并保证了对长效EPO共轭物的极好的储存稳定性。

9. 发明申请

WO2012011752A3 NOVEL LONG-ACTING GLUCAGON CONJUGATE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME FOR THE PREVENTION AND TREATMENT OF OBESITY 审中-公开
标题翻译：新型长效GLUCAGON CONJUGATE和药物组合物，包括预防和治疗肥胖症
公开(公告)号：WO2012011752A3
公开(公告)日：2012-05-31
申请号：PCT/KR2011005375
申请日：2011-07-21
申请人： HANMI HOLDINGS CO LTD , WOO YOUNG EUN , LEE JONG SOO , SHEN LING AI , KIM DAE JIN , JUNG SUNG YOUB , CHOI IN YOUNG , KWON SE CHANG
发明人： WOO YOUNG EUN , LEE JONG SOO , SHEN LING AI , KIM DAE JIN , JUNG SUNG YOUB , CHOI IN YOUNG , KWON SE CHANG
IPC分类号： A61K38/26 , A61K31/4164 , A61P3/00 , A61P3/04 , C07K14/605
CPC分类号： A61K47/48415 , A61K31/4164 , A61K38/26 , A61K45/06 , A61K47/68 , A61K47/6811 , A61K47/6883 , C07K14/605 , A61K2300/00
摘要： Disclosed is a novel long-acting glucagon conjugate in which glucagon or its derivative is covalently linked to a polymer carrier via a non-peptide linker, and a pharmaceutical composition comprising the same as an effective ingredient useful for the prevention and treatment of obesity. Since the long-acting glucagon conjugate of the present invention shows improved in vivo durability and stability, when used in combination with an anti-obesity drug, it is possible to induce synergistic effects on the loss of body weight and decrease in food intake without causing any side-effects such as fluctuation in blood glucose level. Accordingly, the long-acting peptide conjugate of the present invention is very effective for the prevention and treatment of obesity.
摘要翻译：公开了一种新颖的长效胰高血糖素缀合物，其中胰高血糖素或其衍生物通过非肽接头共价连接到聚合物载体，以及包含其作为有效成分的药物组合物，其用于预防和治疗肥胖症。由于本发明的长效胰高血糖素缀合物显示出改善的体内耐久性和稳定性，当与抗肥胖药物组合使用时，可以对体重的损失和食物摄取减少引起协同效应，而不引起任何副作用，如血糖水平波动。因此，本发明的长效肽结合物对于预防和治疗肥胖症是非常有效的。

10. 发明申请

WO2010107256A3 METHOD FOR PREPARING A SITE-SPECIFIC PHYSIOLOGICALLY ACTIVE POLYPEPTIDE CONJUGATE 审中-公开
标题翻译：制备基因特异性生理活性多肽共聚物的方法
公开(公告)号：WO2010107256A3
公开(公告)日：2011-03-17
申请号：PCT/KR2010001674
申请日：2010-03-18
申请人： HANMI HOLDINGS CO LTD , SONG DAE HAE , SHIN JAE HEE , LEE JAE MIN , PARK YOUNG KYUNG , KWON SE CHANG , LEE GWAN SUN
发明人： SONG DAE HAE , SHIN JAE HEE , LEE JAE MIN , PARK YOUNG KYUNG , KWON SE CHANG , LEE GWAN SUN
IPC分类号： C07K1/14 , C07K1/10 , C07K1/18
CPC分类号： C07K1/1077 , A61K47/60 , C07K14/575 , C07K14/605 , C07K14/62
摘要： 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.
摘要翻译：本发明提供了通过在特定pH下在醇的存在下用非肽基聚合物处理生理活性多肽来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。

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