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    CONJUGATES AND CONJUGATING REAGENTS
    1.
    发明公开
    CONJUGATES AND CONJUGATING REAGENTS 审中-公开
    共轭物和共轭试剂

    公开(公告)号：EP3220956A1

    公开(公告)日：2017-09-27

    申请号：EP15782051.5

    申请日：2015-10-08

    申请人： Polytherics Limited

    发明人： GODWIN, Antony ,  FRIGERIO, Mark

    IPC分类号： A61K47/50 ,  A61P35/00

    CPC分类号： A61K47/10 ,  A61K31/33 ,  A61K47/48369 ,  A61K47/48569 ,  A61K47/48715 ,  A61K47/60

    摘要： in which Pr represents said protein or peptide, each Nu represents a nucleophile present in or attached to the protein or peptide, each of A and B independently represents a C1-4alkylene or alkenylene chain, and W′ represents an electron withdrawing group or a group obtained by reduction of an electron withdrawing group; and in which said polyethylene glycol portion is or includes a pendant polyethylene glycol chain which has a terminal end group of formula —CH2CH2OR in which R represents a hydrogen atom, an alkyl group, or an optionally substituted aryl group. Also claimed are a method for making such a conjugate, and novel reagents useful in that method.

    摘要翻译： 本发明涉及蛋白质或肽与治疗剂，诊断剂或标记剂的缀合物，所述缀合物含有蛋白质或肽结合部分和聚乙二醇部分; 其中所述蛋白质或肽结合部分具有以下通式：其中Pr代表所述蛋白质或肽，每个Nu代表存在于或附着于蛋白质或肽中的亲核试剂，A和B各自独立地代表C1-4亚烷基或亚烯基 链，W表示吸电子基团或吸电子基团还原得到的基团; 并且其中所述聚乙二醇部分是或包括具有式-CH 2 CH 2 OR的末端基团的侧链聚乙二醇链，其中R表示氢原子，烷基或任选取代的芳基。 还要求保护这种缀合物的方法以及在该方法中有用的新型试剂。

    A SITE-SPECIFIC GLP-2 CONJUGATE USING AN IMMUNOGLOBULIN FRAGMENT
    2.
    发明公开
    A SITE-SPECIFIC GLP-2 CONJUGATE USING AN IMMUNOGLOBULIN FRAGMENT 审中-公开
    局部特定GLP-2免疫球蛋白片段共轭

    公开(公告)号：EP2797621A4

    公开(公告)日：2015-09-02

    申请号：EP12861579

    申请日：2012-12-28

    申请人： HANMI SCIENCE CO LTD

    发明人： KIM SEUNG SU ,  LIM SE YOUNG ,  JUNG SUNG YOUB ,  KWON SE CHANG

    IPC分类号： A61K38/26 ,  A61K47/30 ,  A61K47/48 ,  A61P1/00

    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.

    ENGINEERED POLYPEPTIDE CONJUGATES AND METHODS FOR MAKING THEREOF USING TRANSGLUTAMINASE
    4.
    发明公开
    ENGINEERED POLYPEPTIDE CONJUGATES AND METHODS FOR MAKING THEREOF USING TRANSGLUTAMINASE 审中-公开
    操纵多肽结合物和生产中使用谷氨酰胺转胺酶工艺FOR

    公开(公告)号：EP2635310A2

    公开(公告)日：2013-09-11

    申请号：EP11799826.0

    申请日：2011-11-03

    申请人： Rinat Neuroscience Corp. ,  Pfizer Inc.

    发明人： STROP, Pavel ,  DORYWALSKA, Magdalena Grazyna ,  RAJPAL, Arvind ,  SHELTON, David ,  LIU, Shu-Hui ,  PONS, Jaume ,  DUSHIN, Russell

    IPC分类号： A61K47/48

    CPC分类号： C07K17/02 ,  A61K47/48369 ,  A61K47/48384 ,  A61K47/48569 ,  A61K47/48715 ,  A61K47/68 ,  A61K47/6803 ,  A61K47/6851 ,  A61K47/6889 ,  C07K16/30 ,  C07K2317/31 ,  C07K2317/73

    摘要： The present invention provides engineered polypeptide conjugates (e.g., antibody-drug-conjugates, toxin-(biocompatible polymer) conjugates, antibody-(biocompatible polymer) conjugates, and bispecific antibodies) comprising acyl donor glutamine-containing tags and amine donor agents. In one aspect, the invention provides an engineered Fc-containing polypeptide conjugate comprising the formula (Fc-containing polypeptide)-T-A, wherein T is an acyl donor glutamine-containing tag engineered at a specific site or comprises an endogenous glutamine made reactive by the Fc-containing polypeptide engineering, wherein A is an amine donor agent, and wherein the amine donor agent is site-specifically conjugated to the acyl donor glutamine-containing tag or the endogenous glutamine. The invention also provides methods of making engineered polypeptide conjugates using transglutaminase.

    摘要翻译： 本发明提供了工程化的多肽缀合物（例如，抗体 - 药物偶联物，毒素（生物相容的聚合物）的缀合物，抗体（生物相容的聚合物）缀合物，以及双特异性抗体），其包括酰基供体含有谷氨酰胺标签和胺供体剂。 在一个方面，本发明提供了工程化的多肽缀合物，包含Formel-TA（包含Fc的多肽）的含Fc的，T是在特定位点或内源谷氨酰胺的包括工程改造的酰基供体含有谷氨酰胺标签的worin由作出反应 多肽工程含Fc，worin A是胺供体剂和worin所述胺供体试剂是位点特异性缀合到酰基供体含有谷氨酰胺标签或内源谷氨酰胺。 因此本发明提供制备转谷氨酰胺酶使用工程改造的多肽缀合物的方法。

    MODIFIED FC MOLECULES
    5.
    发明公开
    MODIFIED FC MOLECULES 有权
    经过修饰的Fc分子

    公开(公告)号：EP1928502A2

    公开(公告)日：2008-06-11

    申请号：EP06789737.1

    申请日：2006-08-11

    申请人： Amgen, Inc

    发明人： GEGG, JR., Colin V. ,  WALKER, Kenneth W. ,  MIRANDA, Leslie P. ,  XIONG, Fei

    IPC分类号： A61K47/48

    CPC分类号： A61K47/48369 ,  A61K38/02 ,  A61K47/60 ,  A61K47/68 ,  A61K47/6817 ,  C07K16/00 ,  C07K17/00 ,  C07K2317/40 ,  C07K2317/52

    摘要： Disclosed is a process for preparing a pharmacologically active compound, in which at least one internal conjugation site of an Fc domain sequence is selected that is amenable to conjugation of an additional functional moiety by a defined conjugation chemistry through the side chain of an amino acid residue at the conjugation site. An appropriate amino acid residue for conjugation may be present in a native Fc domain at the conjugation site or may be added by insertion (i.e., between amino acids in the native Fc domain) or by replacement (i.e., removing amino acids and substituting different amino acids). In the latter case, the number of amino acids added need not correspond to the number of amino acids removed from the previously existing Fc domain. This technology may be used to produce useful compositions of matter and pharmaceutical compositions containing them. A DNA encoding the inventive composition of matter, an expression vector containing the DNA, and a host cell containing the expression vector are also disclosed.

    A CONJUGATE COMPRISING OXYNTOMODULIN AND AN IMMUNOGLOBULIN FRAGMENT, AND USE THEREOF
    9.
    发明公开
    A CONJUGATE COMPRISING OXYNTOMODULIN AND AN IMMUNOGLOBULIN FRAGMENT, AND USE THEREOF 审中-公开
    结合奥昔布霉素和免疫球蛋白片段及其用途

    公开(公告)号：EP2721062A4

    公开(公告)日：2014-11-12

    申请号：EP12801247

    申请日：2012-06-15

    申请人： HANMI SCIENCE CO LTD

    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 ,  A61K45/06 ,  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减少食物摄入，抑制胃排空，并且促进无副作用的脂肪分解，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。