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1. 发明专利

IL199566A Insulinotropic complex using an immunoglobulin fragment 未知
公开(公告)号：IL199566A
公开(公告)日：2016-09-29
申请号：IL19956609
申请日：2009-06-25
申请人： DAE HAE SONG , CHANG KI LIM , TAE HUN SONG , YOUNG HOON KIM , SE CHANG KWON , GWAN SUN LEE , SUNG YOUB JUNG , IN YOUNG CHOI , HANMI SCIENCE CO LTD , HANMI SCIENCE CO LTD
发明人： 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分类号： A61K20060101 , A61P20060101 , C07K20060101
摘要： 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.

2. 发明专利

IL205667A Pharmaceutical composition for treating obesity-related disease comprising exendin-4 peptide conjugate 未知
公开(公告)号：IL205667A
公开(公告)日：2016-11-30
申请号：IL20566710
申请日：2010-05-10
申请人： DAE HAE SONG , MIN YOUNG KIM , YOUNG JIN PARK , EUN HEE KANG , SUNG YOUB JUNG , SE CHANG KWON , GWAN SUN LEE , HANMI SCIENCE CO LTD , HANMI SCIENCE CO LTD
发明人： DAE HAE SONG , MIN YOUNG KIM , YOUNG JIN PARK , EUN HEE KANG , SUNG YOUB JUNG , SE CHANG KWON , GWAN SUN LEE
IPC分类号： A61K20060101 , A61P20060101
摘要： 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.

3. 发明专利

IL203288A Insulinotropic peptide derivative wherein its n-terminal amino acid is modified 未知
公开(公告)号：IL203288A
公开(公告)日：2016-02-29
申请号：IL20328810
申请日：2010-01-13
申请人： DAE HAE SONG , CHANG KI LIM , SE CHANG KWON , YOUNG HOON KIM , GWAN SUN LEE , SUNG MIN BAE , SUNG YOUB JUNG , HANMI SCIENCE CO LTD , HANMI SCIENCE CO LTD
发明人： DAE HAE SONG , CHANG KI LIM , SE CHANG KWON , YOUNG HOON KIM , GWAN SUN LEE , SUNG MIN BAE , SUNG YOUB JUNG
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.

4. 发明申请

WO2022043923A1 SYNTHESIS OF POZIOTINIB DERIVATIVE 审中-公开
公开(公告)号：WO2022043923A1
公开(公告)日：2022-03-03
申请号：PCT/IB2021/057844
申请日：2021-08-26
申请人： HANMI SCIENCE CO., LTD.
发明人： BANG, Keuk Chan , MOON, Young Ho , CHANG, Young Kil
IPC分类号： C07D401/14 , C07D401/12 , C07D239/94 , C07D239/88 , C07D211/06 , A61K31/517
摘要： A method for the synthesis of a compound of Formula (II) is provided. Also disclosed is the salt form of the compound. The method includes the introduction of a piperidinyl moiety in a polar aprotic solvent system, followed by the removal of the protecting group and the acrylation step.

5. 发明申请

WO2013051900A3 BLOOD COAGULATION FACTOR Ⅶ AND ⅦA DERIVATIVES, CONJUGATES AND COMPLEXES COMPRISING THE SAME, AND USE THEREOF 审中-公开
标题翻译：血凝蛋白因子Ⅶ和ⅦA衍生物，缀合物和包含它们的复合物及其用途
公开(公告)号：WO2013051900A3
公开(公告)日：2013-06-13
申请号：PCT/KR2012008102
申请日：2012-10-05
申请人： HANMI SCIENCE CO LTD
发明人： KIM DAE JIN , LEE BYUNG SUN , HONG SUNG HWAN , HUH YONG HO , JUNG SUNG YOUB , KWON SE CHANG
IPC分类号： A61K38/36 , A61K38/16 , A61K48/00 , A61P7/04
CPC分类号： A61K38/4846 , A61K47/6815 , A61K48/00 , C07K2319/30 , C07K2319/31 , C07K2319/50 , C12N9/6437
摘要： The present invention relates to a blood coagulation factor Ⅶ derivative, a blood coagulation factor Ⅶa derivative, FacⅦ and FacⅦa conjugates each prepared by linking a polymer capable of extending the blood half-life to the derivative, FacⅦ and Ⅶa complexes each prepared by linking a carrier to the conjugate, genes encoding the FacⅦ and FacⅦa derivatives, expression vectors comprising the genes, transformants introduced with the expression vectors, a method for preparing the FacⅦ and FacⅦa derivatives using the transformants, a method for preparing the FacⅦa conjugate and complex, a FacⅦa complex prepared by the method, a pharmaceutical composition for the prevention or treatment of hemophilia comprising the derivative, conjugate, or complex as an active ingredient, and a pharmaceutical composition for blood coagulation comprising the derivative, conjugate, or complex as an active ingredient. Further, the present invention relates to a method for preventing or treating hemophilia or for promoting blood coagulation, comprising administering to a subject a therapeutically effective amount of the composition. The FacⅦ or FacⅦa derivative of the present invention is able to bind with a carrier capable of improving the blood half-life while maintaining the activity of FacⅦ or FacⅦa, and they can be widely used in the development of effective prophylactic or therapeutic agent for hemophilia.
摘要翻译：本发明涉及一种凝血因子Ⅶ衍生物，凝血因子Ⅶa衍生物，FacⅦ和FacⅦa缀合物，每种缀合物通过将能够延长血液半衰期的聚合物连接到衍生物上而制备，FacⅦ和Ⅶa复合物各自通过将编码FacⅦa和FacⅦa衍生物的基因，包含该基因的表达载体，用该表达载体导入的转化子，使用转化体制备FacⅦ和FacⅦa衍生物的方法，制备FacⅦa缀合物和复合物的方法，由该方法制备的FacⅦa复合物，包含该衍生物，缀合物或复合物作为活性成分的用于预防或治疗血友病的药物组合物，以及包含该衍生物，缀合物或复合物作为活性成分的用于凝血的药物组合物。此外，本发明涉及用于预防或治疗血友病或促进凝血的方法，其包括向受试者施用治疗有效量的组合物。本发明的FacⅦ或FacⅦa衍生物能够在保持FacⅦ或FacⅦa活性的同时与能够改善血液半衰期的载体结合，并且它们可以广泛用于开发有效的血友病预防或治疗剂。

6. 发明申请

WO2013051883A2 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 审中-公开
标题翻译：制备1-（4-（4-（3,4-二氯-2-氟代苯基氨基）-7-甲氧基喹唑啉-6-基氧）哌啶-1-基） - 丙-2-酮-1-酮盐酸盐和中间体的方法在那里使用
公开(公告)号：WO2013051883A2
公开(公告)日：2013-04-11
申请号：PCT/KR2012008077
申请日：2012-10-05
申请人： HANMI SCIENCE CO LTD
发明人： BANG KEUK CHAN , MOON YOUNG HO , CHANG YOUNG KIL
IPC分类号： C07D401/12 , A61K31/517
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-烯的改进方法 -1-酮盐酸盐，其选择性和有效地抑制由表皮生长因子受体（EGFR）过表达诱导的癌细胞生长并防止由酪氨酸激酶突变引起的耐药性发展，以及其中使用的中间体。

7. 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。

8. 发明申请

WO2012173422A9 A CONJUGATE COMPRISING OXYNTOMODULIN AND AN IMMUNOGLOBULIN FRAGMENT, AND USE THEREOF 审中-公开
公开(公告)号：WO2012173422A9
公开(公告)日：2012-12-20
申请号：PCT/KR2012/004722
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 , C07K17/00 , A61K38/26 , A61K47/48 , A61P3/04
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.

9. 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。

10. 发明申请

WO2013133659A1 AN IMPROVED PROCESS FOR PREPARATION OF PHYSIOLOGICALLY ACTIVE POLYPEPTIDE COMPLEX 审中-公开
标题翻译：用于制备生理活性多肽复合物的改进方法
公开(公告)号：WO2013133659A1
公开(公告)日：2013-09-12
申请号：PCT/KR2013/001885
申请日：2013-03-08
申请人： HANMI SCIENCE CO., LTD.
发明人： JANG, Myung Hyun , KIM, Min Young , LEE, Jong-Soo , KIM, Dae Jin , BAE, Sung Min , KWON, Se Chang
IPC分类号： C07K19/00 , C07K1/10 , A61K47/48
CPC分类号： C07K1/1077 , A61K38/28 , A61K47/60 , A61K47/68 , A61K47/6883 , C07K1/1075 , C07K2319/30
摘要： Disclosed is a method for the preparation of a complex in which a physiologically active polypeptide is covalently bonded to an immunoglobulin constant region via a non-peptidyl linker. The method is characterized by the employment of a reducing agent, by which conventional problems of low production yield and modification of the polypeptide can be overcome. The physiologically active polypeptide-non-peptidyl polymer-immunoglobulin constant region complex can be produced with high purity and yield as well as at low cost. Thus, the method is industrially useful. Moreover, by exhibiting a prolonged action profile, the physiologically active polypeptide-non-peptidyl polymer-immunoglobulin constant region complex can be effectively used for developing long-acting formulations of physiologically active polypeptides which have improved drug compliance.
摘要翻译：公开了一种制备复合物的方法，其中生理活性多肽通过非肽基连接体与免疫球蛋白恒定区共价结合。该方法的特征在于使用还原剂，可以克服生产产率低和多肽修饰的常规问题。生理活性多肽 - 非肽基聚合物 - 免疫球蛋白恒定区复合物可以以高纯度和产率以及低成本生产。因此，该方法在工业上是有用的。此外，通过显示延长的作用特征，生理活性多肽 - 非肽基聚合物 - 免疫球蛋白恒定区复合物可以有效地用于开发具有改善的药物依从性的生理活性多肽的长效制剂。

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