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21. 发明申请

US20150025227A1 IGG FC FRAGMENT FOR A DRUG CARRIER AND METHOD FOR THE PREPARATION THEREOF 审中-公开
标题翻译：用于药物载体的IGG FC片段及其制备方法
公开(公告)号：US20150025227A1
公开(公告)日：2015-01-22
申请号：US14327064
申请日：2014-07-09
申请人： HANMI SCIENCE CO., LTD.
发明人： Sung Youb JUNG , Jin Sun Kim , Geun Hee Yang , Se Wang Kwon , Gwan Sun Lee
IPC分类号： A61K47/48 , C07K16/46
CPC分类号： 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
摘要： Disclosed is an IgG Fc fragment useful as a drug carrier. A recombinant vector expressing the IgG Fc fragment, a transformant transformed with the recombinant vector, and a method of preparing an IgG Fc fragment are disclosed. When conjugated to a certain drug, the IgG Fc fragment improves the in vivo duration of action of the drug and minimizes the in vivo activity reduction of the drug.
摘要翻译：公开了可用作药物载体的IgG Fc片段。公开了表达IgG Fc片段的重组载体，用重组载体转化的转化体和制备IgG Fc片段的方法。当缀合到某种药物时，IgG Fc片段改善了药物作用的体内持续时间并使药物的体内活性降低最小化。

22. 发明申请

US20140377290A1 SITE-SPECIFIC GLP-2 CONJUGATE USING AN IMMUNOGLOBULIN FRAGMENT 有权
标题翻译：使用免疫球蛋白片段的特异性GLP-2结合蛋白
公开(公告)号：US20140377290A1
公开(公告)日：2014-12-25
申请号：US14369436
申请日：2012-12-28
申请人： HANMI SCIENCE CO., LTD.
发明人： Seung Su Kim , Se Young Lim , Sung Youb Jung , Se Chang Kwon
IPC分类号： A61K47/48
CPC分类号： A61K47/48415 , A61K38/26 , A61K47/48215 , A61K47/48369 , A61K47/60 , A61K47/68 , A61K47/6811
摘要： The present invention relates to a glucagon-like peptide-2 (GLP-2) conjugate comprising native GLP-2 or its derivative and an immunoglobulin Fc fragment being covalently linked via a non-peptidyl polymer, wherein the native GLP-2 or its derivative has a thiol group introduced at its C-terminal end, and one end of the non-peptidyl polymer is linked to an amino acid residue of the GLP-2 other than the N-terminal amino group thereof; a method for preparing the GLP-2 conjugate; a pharmaceutical composition comprising the same; and a method for treating or preventing intestinal disease, intestinal injury, or gastrosia by using the same. Since the GLP-2 conjugate of the present invention has a remarkably increased binding affinity to a GLP-2 receptor, it shows a prolonged in vivo half-life and an improved in vivo durability and stability.
摘要翻译：本发明涉及包含天然GLP-2或其衍生物的胰高血糖素样肽-2（GLP-2）结合物和通过非肽基聚合物共价连接的免疫球蛋白Fc片段，其中天然GLP-2或其衍生物在其C末端具有硫醇基，非肽基聚合物的一端与除了其N-末端氨基以外的GLP-2的氨基酸残基连接; 制备GLP-2缀合物的方法; 包含其的药物组合物; 以及通过使用该方法治疗或预防肠道疾病，肠损伤或胃癌的方法。由于本发明的GLP-2结合物对GLP-2受体的结合亲和力显着增加，因此其体内半衰期延长，体内耐久性和稳定性提高。

23. 发明授权

US08859767B2 Method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-prop-2-en-1-one hydrochloride and intermediates used therein 有权
标题翻译： 1-（4-（4-（3,4-二氯-2-氟苯基氨基）-7-甲氧基喹唑啉-6-基氧基）哌啶-1-基） - 丙-2-烯-1-酮盐酸盐和中间体在其中使用
公开(公告)号：US08859767B2
公开(公告)日：2014-10-14
申请号：US14349887
申请日：2012-10-05
申请人： Hanmi Science Co., Ltd.
发明人： Keuk Chan Bang , Young Ho Moon , Young Kil Chang
IPC分类号： C07D239/94 , C07D401/12
CPC分类号： C07D239/94 , A61K31/517 , C07D401/12
摘要： The present invention relates to an improved method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-prop-2-en-1-one hydrochloride, which selectively and effectively inhibits the growth of cancer cells induced by over-expression of an epidermal growth factor receptor (EGFR) and prevents the development of drug resistance caused by mutation of a tyrosine kinase, and intermediates used therein.
摘要翻译：本发明涉及一种制备1-（4-（4-（3,4-二氯-2-氟苯基氨基）-7-甲氧基喹唑啉-6-基氧基）哌啶-1-基） - 丙-2-烯 -1-盐酸盐，其选择性和有效地抑制由表皮生长因子受体（EGFR）的过表达诱导的癌细胞的生长，并且防止由酪氨酸激酶的突变引起的耐药性的发展及其中使用的中间体。

24. 发明授权

US11040110B2 Polypeptide complex comprising non-peptidyl polymer having three functional ends 有权
公开(公告)号：US11040110B2
公开(公告)日：2021-06-22
申请号：US16057454
申请日：2018-08-07
申请人： HANMI SCIENCE CO., LTD.
发明人： Dae Hae Song , Jae Hee Shin , Mi Ji Lee , Sung Hee Hong , Se Chang Kwon , Gwan Sun Lee
IPC分类号： A61K47/68 , A61K47/60 , C07K19/00 , A61P43/00 , A61P31/00 , A61P5/00 , A61P5/50 , C07K14/59
摘要： 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.

25. 发明授权

US10744187B2 Insulin conjugate using an immunoglobulin fragment 有权
公开(公告)号：US10744187B2
公开(公告)日：2020-08-18
申请号：US15965686
申请日：2018-04-27
申请人： HANMI SCIENCE CO., LTD.
发明人： Dae Hae Song , Jae Hee Shin , Young Jin Park , Dae Seong Im , Sung Min Bae , Se Chang Kwon
IPC分类号： A61K38/28 , A61K47/60 , A61K47/68
摘要： An insulin conjugate having improved in vivo duration and stability is provided. The conjugate is prepared by covalently linking insulin with an immunoglobulin Fc region via a non-peptidyl polymer, a long-acting formulation comprising the same, and a preparation method thereof. The insulin conjugate of the present invention maintains in vivo activity of the peptide at a relatively high level and remarkably increases the serum half-life thereof, thereby greatly improving drug compliance upon insulin treatment.

26. 发明申请

US20180360983A1 POLYPEPTIDE COMPLEX COMPRISING NON-PEPTIDYL POLYMER HAVING THREE FUNCTIONAL ENDS 审中-公开
公开(公告)号：US20180360983A1
公开(公告)日：2018-12-20
申请号：US16057454
申请日：2018-08-07
申请人： HANMI SCIENCE CO., LTD.
发明人： Dae Hae SONG , Jae Hee SHIN , Mi Ji LEE , Sung Hee HONG , Se Chang KWON , Gwan Sun LEE
IPC分类号： A61K47/68 , C07K14/59 , C07K19/00 , A61K47/60
摘要： 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.

27. 发明申请

US20170340753A1 Conjugate Comprising Oxyntomodulin And An Immunoglobulin Fragment, And Use Thereof 审中-公开
公开(公告)号：US20170340753A1
公开(公告)日：2017-11-30
申请号：US15636160
申请日：2017-06-28
申请人： HANMI SCIENCE CO., LTD
发明人： SUNG YOUB JUNG , DAE JIN KIM , SUNG HEE PARK , YOUNG EUN WOO , IN YOUNG CHOI , SE CHANG KWON
IPC分类号： A61K47/68 , C07K14/575 , A61K45/06 , A61K38/26 , A61K47/60 , A61K38/00
CPC分类号： A61K47/6889 , A61K38/00 , A61K38/26 , A61K45/06 , 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.

28. 发明申请

US20170022261A1 Novel Oxyntomodulin Derivatives and Pharmaceutical Composition For Treating Obesity Comprising the Same 审中-公开
标题翻译：新型羟醛调蛋白衍生物和药物组合物用于治疗包括其的肥胖症
公开(公告)号：US20170022261A1
公开(公告)日：2017-01-26
申请号：US15286708
申请日：2016-10-06
申请人： HANMI SCIENCE CO., LTD
发明人： Sung Youb Jung , Myung Hyun JANG , Ling Ai SHEN , Young Kyung PARK , Young Jin PARK , Se Chang KWON
IPC分类号： C07K14/605 , A61K38/26 , A61K45/06
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，可以广泛用于治疗肥胖症的安全性和有效性。

29. 发明授权

US09504757B2 Site-specific GLP-2 conjugate using an immunoglobulin fragment 有权
标题翻译：使用免疫球蛋白片段的位点特异性GLP-2缀合物
公开(公告)号：US09504757B2
公开(公告)日：2016-11-29
申请号：US14369436
申请日：2012-12-28
申请人： HANMI SCIENCE CO., LTD.
发明人： Seung Su Kim , Se Young Lim , Sung Youb Jung , Se Chang Kwon
IPC分类号： A61K38/26 , A61K47/48
CPC分类号： A61K47/48415 , A61K38/26 , A61K47/48215 , A61K47/48369 , A61K47/60 , A61K47/68 , A61K47/6811
摘要： Provided are a glucagon-like peptide-2 (GLP-2) conjugate containing native GLP-2 or its derivative and an immunoglobulin Fc fragment being covalently linked via a non-peptidyl polymer, wherein the native GLP-2 or its derivative has a thiol group introduced at its C-terminal end, and one end of the non-peptidyl polymer is linked to an amino acid residue of the GLP-2 other than the N-terminal amino group thereof; a method for preparing the GLP-2 conjugate; a pharmaceutical composition comprising the same; and a method for treating or preventing intestinal disease, intestinal injury, or gastrosis by using the same. Since the GLP-2 conjugate of the present invention has a remarkably increased binding affinity to a GLP-2 receptor, it shows a prolonged in vivo half-life and an improved in vivo durability and stability.
摘要翻译：提供含天然GLP-2或其衍生物的胰高血糖素样肽-2（GLP-2）结合物和通过非肽基聚合物共价连接的免疫球蛋白Fc片段，其中天然GLP-2或其衍生物具有硫醇在其C-末端引入基团，非肽基聚合物的一端与除了其N-末端氨基以外的GLP-2的氨基酸残基连接; 制备GLP-2缀合物的方法; 包含其的药物组合物; 以及通过使用该方法治疗或预防肠道疾病，肠损伤或胃肠疾病的方法。由于本发明的GLP-2结合物对GLP-2受体的结合亲和力显着增加，因此其体内半衰期延长，体内耐久性和稳定性提高。

30. 发明申请

US20150118255A1 LIQUID FORMULATION OF HIGHLY CONCENTRATED LONG-ACTING HUMAN GROWTH HORMONE CONJUGATE 有权
标题翻译：高浓度长效人类生长激素联合液的液体配方
公开(公告)号：US20150118255A1
公开(公告)日：2015-04-30
申请号：US14383820
申请日：2013-03-29
申请人： HANMI SCIENCE CO., LTD.
发明人： Hyung Kyu Lim , Hyun Uk Kim , Sung Hee Hong , Sung Min Bae , Se Chang Kwon
IPC分类号： A61K47/48 , A61K47/10 , A61K47/26 , A61K47/02 , A61K38/27 , A61K47/12
摘要： The present invention relates to a liquid formulation of highly concentrated long-acting human growth hormone conjugate, comprising a pharmaceutically effective amount of the long-acting human growth hormone conjugate in which human growth hormone (hGH) is linked to an immunoglobulin Fc region, and an albumin-free stabilizer, said stabilizer comprising a buffer, a non-ionic surfactant, a sugar alcohol, and sodium chloride as an isotonic agent, and a method for preparing the same.
摘要翻译：本发明涉及高浓度长效人生长激素结合物的液体制剂，其包含药学有效量的人类生长激素（hGH）与免疫球蛋白Fc区连接的长效人生长激素缀合物，以及不含白蛋白的稳定剂，所述稳定剂包含缓冲液，非离子表面活性剂，糖醇和作为等渗剂的氯化钠，及其制备方法。

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