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    DOUBLE-ACYLATED GLP-1 DERIVATIVES
    2.
    发明公开
    DOUBLE-ACYLATED GLP-1 DERIVATIVES 审中-公开
    双酰化GLP-1衍生物

    公开(公告)号：EP3000482A1

    公开(公告)日：2016-03-30

    申请号：EP15188731.2

    申请日：2010-12-16

    申请人： Novo Nordisk A/S

    发明人： SAUERBERG, Per ,  LAU, Jesper ,  LINDEROTH, Lars ,  KODRA, János Tibor ,  SPETZLER, Jane ,  GARIBAY, Patrick William

    IPC分类号： A61K47/48 ,  C07D233/64 ,  C07K14/605

    CPC分类号： C07K14/65 ,  A61K38/00 ,  A61K47/542 ,  A61K47/60 ,  C07K14/605 ,  G01N2333/605

    摘要： The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 37 of GLP-1 (7-37) (SEQ ID NO: 1), a second K residue at a position corresponding to position 26 of GLP-1 (7-37), and a maximum of ten amino acid modifications as compared to GLP-1 (7-37), wherein the first K residue is designated K 37 , and the second K residue is designated K 26 , which derivative comprises two albumin binding moieties attached to K 26 and K 37 , respectively, wherein the albumin binding moiety comprises a protracting moiety selected from:

            Chem. 1:     HOOC-(CH 2 ) x -CO-*

            Chem. 2:     HOOC-C 6 H 4 -O-(CH 2 ) y -CO-*

            Chem. 3:     R 1 -C 6 H 4 -(CH 2 ) z -CO-*

            Chem. 4:     HOOC-C 4 SH 2 -(CH 2 ) w -CO-*

    in which x is an integer in the range of 6-18, y is an integer in the range of 3-17, z is an integer in the range of 1-5, R 1 is a group having a molar mass not higher than 150 Da, and w is an integer in the range of 6-18; with the proviso that when the protracting moiety is Chem. 1, the albumin binding moiety further comprises a linker of formula Chem. 5: *-NH-(CH 2 ) 2 -(O-(CH 2 ) 2 ) k -O-(CH 2 ) n -CO-*, wherein k is an integer in the range of 1-5, and n is an integer in the range of 1-5; or a pharmaceutically acceptable salt, amide, or ester thereof.
    The invention also relates to the pharmaceutical use thereof, for example in the treatment and/or prevention of all forms of diabetes and related diseases, as well as to corresponding novel peptides and side chain intermediates. The derivatives are suitable for oral administration.

    GLP-1 RECEPTOR AGONIST COMPOUNDS WITH A MODIFIED N-TERMINUS
    6.
    发明公开
    GLP-1 RECEPTOR AGONIST COMPOUNDS WITH A MODIFIED N-TERMINUS 审中-公开
    具有修饰的N-末端的GLP-1受体激动剂化合物

    公开(公告)号：EP2512518A1

    公开(公告)日：2012-10-24

    申请号：EP10793244.4

    申请日：2010-12-16

    申请人： Novo Nordisk A/S

    发明人： KODRA, János, Tibor ,  MADSEN, Johnny

    IPC分类号： A61K47/48 ,  C07D233/64 ,  C07K14/605

    CPC分类号： C07K14/65 ,  A61K38/00 ,  A61K47/542 ,  A61K47/60 ,  C07K14/605 ,  G01N2333/605

    摘要： The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 37 of GLP-1 (7-37) (SEQ ID NO: 1), a second K residue at a position corresponding to position 26 of GLP-1 (7-37), and a maximum of ten amino acid modifications as compared to GLP-1 (7-37), wherein the first K residue is designated K 37 , and the second K residue is designated K 26 , which derivative comprises two albumin binding moieties attached to K 26 and K 37 , respectively, wherein the albumin binding moiety comprises a protracting moiety selected from: €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒChem. 1:€ƒ€ƒ€ƒ€ƒ€ƒHOOC-(CH 2 ) x -CO-* €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒChem. 2:€ƒ€ƒ€ƒ€ƒ€ƒHOOC-C 6 H 4 -O-(CH 2 ) y -CO-* €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒChem. 3:€ƒ€ƒ€ƒ€ƒ€ƒR 1 -C 6 H 4 -(CH 2 ) z -CO-* €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒChem. 4:€ƒ€ƒ€ƒ€ƒ€ƒHOOC-C 4 SH 2 -(CH 2 ) w -CO-* in which x is an integer in the range of 6-18, y is an integer in the range of 3-17, z is an integer in the range of 1-5, R 1 is a group having a molar mass not higher than 150 Da, and w is an integer in the range of 6-18; with the proviso that when the protracting moiety is Chem. 1, the albumin binding moiety further comprises a linker of formula Chem. 5: *-NH-(CH 2 ) 2 -(O-(CH 2 ) 2 ) k -O-(CH 2 ) n -CO-*, wherein k is an integer in the range of 1-5, and n is an integer in the range of 1-5; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to the pharmaceutical use thereof, for example in the treatment and/or prevention of all forms of diabetes and related diseases, as well as to corresponding novel peptides and side chain intermediates. The derivatives are suitable for oral administration.

    摘要翻译： 本发明涉及具有修饰的N-末端的GLP-1受体激动剂化合物。 该化合物具有式Chem。 1：Y-Z-P，其中P代表缺乏两个N端氨基酸残基的GLP-1受体激动剂肽的片段; 而Y-Z代表新型His-Ala模拟物。 GLP-1受体激动剂化合物的实例衍生自人GLP-1（7-37），毒蜥外泌肽-4（1-39）或GLP-1A（1-37）。 本发明还涉及这些化合物的衍生物，特别是具有能够延长这些化合物的体内作用持续时间的一种或多种白蛋白结合侧链的化合物。 本发明的肽和衍生物具有良好的效力，长期的药代动力学特征，对胃肠酶降解稳定，和/或具有高的口服生物利用度。 这些性质对于开发用于皮下，静脉内和/或特别是口服给药的GLP-1受体激动剂化合物是重要的。 本发明还涉及用于制备本发明的GLP-1受体激动剂化合物的中间产物。

    Glucagon-like peptide-2 and its therapeutic use
    7.
    发明公开
    Glucagon-like peptide-2 and its therapeutic use 失效
    Glucagon-artiges Peptid-2和seine therapeutische Verwendung

    公开(公告)号：EP2277530A1

    公开(公告)日：2011-01-26

    申请号：EP10012215.9

    申请日：1996-04-12

    申请人： 1149336 ONTARIO INC.

    发明人： Drucker, Daniel

    IPC分类号： A61K38/25 ,  C07K14/605 ,  G01N33/68

    CPC分类号： G01N33/74 ,  A61K38/00 ,  C07K14/605 ,  G01N2333/605 ,  G01N2500/00

    摘要： Glucagon-like peptide-2, a product of glucagon gene expression, and analogs of glucagon-like peptide-2, have been identified as gastrointestinal tissue growth factors. Their effects on the growth of small bowel and pancreatic islets are described. Their formulation as a pharmaceutical, and their therapeutic use in treating disorders of the bowel, are described.

    摘要翻译： 胰高血糖素样肽-2，胰高血糖素基因表达的产物和胰高血糖素样肽-2的类似物已被鉴定为胃肠组织生长因子。 描述了它们对小肠和胰岛生长的影响。 描述了其作为药物的制剂及其在治疗肠道疾病中的治疗用途。

    Glucagon receptors
    9.
    发明公开
    Glucagon receptors 失效
    Glucagonrezeptoren

    公开(公告)号：EP1514932A2

    公开(公告)日：2005-03-16

    申请号：EP04026892.2

    申请日：1993-08-30

    申请人： NOVO NORDISK A/S

    发明人： Kindsvogle, Wayne R. ,  Sheppard, Paul O. ,  Grant, Francis J. ,  Lok, Si ,  Jelinek, Laura J. ,  Kuijper, Joseph L. ,  Foster, Donald C. ,  O'Hara, Patrick J.

    IPC分类号： C12N15/12 ,  C12N15/62 ,  C12N5/10 ,  C07K14/72 ,  C07K16/28 ,  C12N15/06 ,  C12Q1/68 ,  C12Q1/66 ,  G01N33/74

    CPC分类号： C07K14/72 ,  C07K2319/00 ,  C07K2319/02 ,  C12Q1/66 ,  G01N33/74 ,  G01N2333/605 ,  G01N2333/72

    摘要： The present invention provides isolated DNA molecules comprising a DNA segment encoding a glucagon receptor. Also provided are DNA constructs comprising a first DNA segment encoding a glucagon receptor operably linked to additional DNA segments required for the expression of the first DNA segment, as well as host cells containing such DNA constructs. The present invention also provides a method for detecting the presence of glucagon antagonists, comprising the steps (a) exposing a compound in the presence of a glucagon agonist to a recombinant glucagon receptor coupled to a response pathway under conditions and for time sufficient to allow binding of the compound to the receptor and an associated response through the pathway, and (b) detecting a reduction to the stimulation of the response pathway resulting from the binding of the compound to the glucagon receptor, relative to the stimulation of the response pathway by the glucagon agonist alone and therefrom determining the presence of a glucagon antagonist.

    摘要翻译： 本发明提供了分离的DNA分子，其包含编码胰高血糖素受体的DNA区段。 还提供了DNA构建体，其包含编码与第一DNA区段表达所需的另外的DNA区段可操作地连接的胰高血糖素受体的第一DNA区段，以及含有该DNA构建体的宿主细胞。 本发明还提供了一种用于检测胰高血糖素拮抗剂的存在的方法，其包括以下步骤：（a）将在胰高血糖素激动剂存在下的化合物暴露于在足以允许结合的条件和时间的情况下，与重要的胰高血糖素受体偶联至应答途径 的化合物与受体的相关应答和通过该途径的相关应答，和（b）相对于由该化合物与胰高血糖素受体结合的刺激反应路径的刺激， 胰高血糖素激动剂单独和由此决定胰高血糖素拮抗剂的存在。