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    GLP-1 DERIVATIVES AND USES THEREOF
    8.
    发明公开
    GLP-1 DERIVATIVES AND USES THEREOF 有权
    GLP-1衍生物及其用途

    公开(公告)号：EP3010546A1

    公开(公告)日：2016-04-27

    申请号：EP14731951.1

    申请日：2014-06-19

    申请人： Novo Nordisk A/S

    发明人： REEDTZ-RUNGE, Steffen ,  SAUERBERG, Per ,  KOFOED, Jacob ,  PETTERSSON, Ingrid ,  TORNØE, Christian, Wenzel

    IPC分类号： A61K47/48 ,  C07K14/605

    CPC分类号： A61K38/26 ,  A61K47/54 ,  A61K47/542 ,  A61K47/56 ,  A61K47/60 ,  C07K14/605

    摘要： The invention relates to a derivative of a GLP-1 analogue, optionally C-terminally extended, which derivative comprises a first and a second protracting moiety in the form of a C20 or C22 diacid radical, a bis-amino branched linker, and a first and a second further linker each comprising an OEG-like linker element; wherein these elements are interconnected via amide bonds and attached to a Lys residue of the GLP-1 analogue. The invention also relates to intermediate products in the form of novel GLP-1 analogues incorporated in the derivatives of the invention, as well pharmaceutical compositions and medical uses of the derivatives. The derivatives have very long half-lives while maintaining a satisfactory potency, which makes them potentially suitable for once-monthly administration.

    摘要翻译： 本发明涉及任选C端延伸的GLP-1类似物的衍生物，所述衍生物包含呈C20或C22二酸基团形式的第一和第二延伸部分，双氨基分支连接子和第一 和第二个另外的接头，每个接头都包含OEG样接头元件; 其中这些元件通过酰胺键相互连接并连接到GLP-1类似物的Lys残基上。 本发明还涉及掺入本发明衍生物中的新型GLP-1类似物形式的中间产物，以及该衍生物的药物组合物和医学用途。 衍生物具有很长的半衰期，同时保持令人满意的效力，这使得它们可能适用于每月一次的施用。

    DOUBLE-ACYLATED GLP-1 DERIVATIVES
    9.
    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.