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22 条记录 (耗时 0.025 秒)

    FGF21 derivatives and uses thereof
    4.
    发明授权
    FGF21 derivatives and uses thereof 有权

    公开(公告)号：US10124039B2

    公开(公告)日：2018-11-13

    申请号：US15849920

    申请日：2017-12-21

    申请人： Novo Nordisk A/S

    发明人： Birgit Wieczorek ,  Tina Moeller Tagmose ,  Kristian Sass-Oerum ,  Birgitte Andersen ,  Joergen Olsen

    IPC分类号： A61K38/00 ,  A61K38/18 ,  C07K14/50 ,  A61K47/54

    摘要： The invention relates to a derivative of a FGF21 protein having a cysteine residue at a position corresponding to position 167, 169, 170, 171, 172, 173, 174, 175 and in particular position 180 or position 181 of mature human FGF21 and derivatives thereof having a side chain attached to this cysteine. The FGF21 derivatives of the invention display high potency towards the FGF receptors. The invention also relates to pharmaceutical compositions comprising such FGF21 derivatives and pharmaceutically acceptable excipients, as well as the medical use of the FGF21 derivatives.

    Double-acylated GLP-1 derivatives
    8.
    发明授权
    Double-acylated GLP-1 derivatives 有权

    公开(公告)号：US11117947B2

    公开(公告)日：2021-09-14

    申请号：US16692260

    申请日：2019-11-22

    申请人： Novo Nordisk A/S

    发明人： Birgit Wieczorek ,  Jane Spetzler ,  Thomas Kruse ,  Lars Linderoth ,  Jacob Kofoed

    IPC分类号： A61K38/26 ,  A61K47/54 ,  C07K14/605 ,  A61K47/60 ,  A61K38/00

    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 27 of GLP-1(7-37) (SEQ ID NO: 1); a second K residue at a position corresponding to position T of GLP-1(7-37), where T is an integer in the range of 7-37 except 18 and 27; and a maximum of ten amino acid changes as compared to GLP-1(7-37); wherein the first K residue is designated K27, and the second K residue is designated KT; which derivative comprises two albumin binding moieties attached to K27 and KT, respectively, via a linker, wherein the albumin binding moiety comprises a protracting moiety selected from HOOC—(CH2)x—CO— and HOOC—C6H4—O—(CH2)y—CO—; in which x is an integer in the range of 6-16, and y is an integer in the range of 3-17; wherein the linker comprises an element of the formula —NH—(CH2)2—(O—(CH2)2)k—O—(CH2)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 GLP-1 analogues. The derivatives are suitable for oral administration.