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    DOUBLE-ACYLATED GLP-1 DERIVATIVES WITH A LINKER
    1.
    发明申请
    DOUBLE-ACYLATED GLP-1 DERIVATIVES WITH A LINKER 有权
    具有连接子的双取代的GLP-1衍生物

    公开(公告)号：US20130338068A1

    公开(公告)日：2013-12-19

    申请号：US13883946

    申请日：2011-11-09

    申请人： Jacob Kofoed ,  Jesper Lau ,  Lars Linderoth ,  Patrick William Garibay ,  Thomas Kruse

    发明人： Jacob Kofoed ,  Jesper Lau ,  Lars Linderoth ,  Patrick William Garibay ,  Thomas Kruse

    IPC分类号： C07K14/605

    CPC分类号： C07K14/605 ,  A61K47/542

    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 18 of GLP-1(7-37) (SEQ ID NO: 1), a second K residue at another position, and a maximum of twelve amino acid changes as compared to GLP-1(7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from HOOC—(CH2)x—CO-*, and  Chem. 1: HOOC—C6H4-0-(CH2)y—CO-*,  Chem. 2: in which x is an integer in the range of 6-18, and y is an integer in the range of 3-17; and the linker comprises *-NH—(CH2)q—CH[(CH2)w—NH2]—CO-*,  Chem. 3: wherein q is an integer in the range of 0-5, and w is an integer in the range of 0-5; 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 potent, protracted, and suitable for oral administration.

    摘要翻译： 本发明涉及GLP-1类似物的衍生物，其类似物包含在对应于GLP-1（7-37）（SEQ ID NO：1）的第18位的位置处的第一个K残基，另一个的第二个K残基 位置和与GLP-1（7-37）相比最多12个氨基酸变化; 该衍生物分别包含通过接头分别连接到所述第一和第二K残基的两个伸长部分，其中伸长部分选自HOOC-（CH 2）x -CO- *和Chem。 1：HOOC-C6H4-0-（CH2）y-CO- *，Chem。 2：其中x是6-18的整数，y是3-17的整数; 并且连接体包含* -NH-（CH 2）q-CH [（CH 2）w -NH 2] -CO - *， 3：其中q是0-5的整数，w是0-5的整数; 或其药学上可接受的盐，酰胺或酯。 本发明还涉及其药物用途，例如用于治疗和/或预防所有形式的糖尿病和相关疾病，以及相应的新型肽和侧链中间体。 衍生物有效，延长，适合口服。

    Double-acylated GLP-1 derivatives with a linker
    3.
    发明授权
    Double-acylated GLP-1 derivatives with a linker 有权
    具有接头的双酰化GLP-1衍生物

    公开(公告)号：US09006178B2

    公开(公告)日：2015-04-14

    申请号：US13883946

    申请日：2011-11-09

    申请人： Jacob Kofoed ,  Jesper Lau ,  Lars Linderoth ,  Patrick William Garibay ,  Thomas Kruse

    发明人： Jacob Kofoed ,  Jesper Lau ,  Lars Linderoth ,  Patrick William Garibay ,  Thomas Kruse

    IPC分类号： A61K38/26 ,  A61P3/10 ,  A61P7/12 ,  C07K14/605 ,  A61K38/28 ,  C07K5/00 ,  C07K7/00 ,  C07K16/00 ,  C07K17/00 ,  A61K47/48

    CPC分类号： C07K14/605 ,  A61K47/542

    摘要： The invention relates to a derivative of a GLP-1 analog, which analog comprises a first K residue at a position corresponding to position 18 of GLP-1(7-37) (SEQ ID NO: 1), a second K residue at another position, and a maximum of twelve amino acid changes as compared to GLP-1(7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 1: HOOC—(CH2)x—CO—*, and Chem. 2: HOOC—C6H4-0-(CH2)y—CO—*, in which x is an integer in the range of 6-18, and y is an integer in the range of 3-17; and the linker comprises Chem. 3: *—NH—(CH2)q—CH[(CH2)w—NH2]—CO—*, wherein q is an integer in the range of 0-5, and w is an integer in the range of 0-5; 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 potent, protracted, and suitable for oral administration.

    摘要翻译： 本发明涉及GLP-1类似物的衍生物，其类似物包含在对应于GLP-1（7-37）（SEQ ID NO：1）的第18位的位置处的第一个K残基，另一个的第二个K残基 位置和与GLP-1（7-37）相比最多12个氨基酸变化; 该衍生物分别包含通过接头分别连接到所述第一和第二K残基的两个伸长部分，其中伸长部分选自Chem。 1：HOOC-（CH 2）x-CO- *，和Chem。 2：HOOC-C6H4-0-（CH2）y-CO- *，其中x是6-18的整数，y是3-17的整数; 连接体包括Chem。 3：* -NH-（CH 2）q-CH [（CH 2）w -NH 2] -CO- *，其中q是0-5的整数，w是0-5的整数 ; 或其药学上可接受的盐，酰胺或酯。 本发明还涉及其药物用途，例如用于治疗和/或预防所有形式的糖尿病和相关疾病，以及相应的新型肽和侧链中间体。 衍生物有效，延长，适合口服。

    Double-Acylated GLP-1 Derivatives
    4.
    发明申请
    Double-Acylated GLP-1 Derivatives 有权
    双酰化GLP-1衍生物

    公开(公告)号：US20130288960A1

    公开(公告)日：2013-10-31

    申请号：US13882947

    申请日：2011-11-09

    申请人： Alice Ravn Madsen ,  Birgit Wieczorek ,  Jacob Kofoed ,  Jesper Lau ,  Jane Spetzler ,  Janos Tibor Kodra ,  Lars Linderoth ,  Patrick William Garibay ,  Per Sauerberg ,  Thomas Kruse

    发明人： Alice Ravn Madsen ,  Birgit Wieczorek ,  Jacob Kofoed ,  Jesper Lau ,  Jane Spetzler ,  Janos Tibor Kodra ,  Lars Linderoth ,  Patrick William Garibay ,  Per Sauerberg ,  Thomas Kruse

    IPC分类号： C07K14/605

    CPC分类号： C07K14/605 ,  A61K47/542

    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 18 of GLP-1 (7-37) (SEQ ID NO: 1), a second K residue at another position, and a maximum of twelve amino acid changes as compared to GLP-1 (7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 1, Chem. 2, and Chem. 3: Chem.: HOOC—(CH2)x—CO—* Chem. 2: HOOC—C6H4-0-(CH2)y—CO—* Chem. 3: R2—C6H4—(CH2)z—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, and R2 is a group having a molar mass not higher than 150 Da; and the linker comprises Chem. 4: *—NH—(CH2)2-(0-(CH2)2)k-0-(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 peptides and side chain intermediates. The derivatives are suitable for oral administration.

    摘要翻译： 本发明涉及GLP-1类似物的衍生物，其类似物包含在对应于GLP-1（7-37）（SEQ ID NO：1）的第18位的位置处的第一个K残基，另一个的第二个K残基 位置和与GLP-1（7-37）相比最多12个氨基酸变化; 该衍生物分别包含通过接头分别连接到所述第一和第二K残基的两个伸长部分，其中伸长部分选自Chem。 1，Chem。 2和Chem。 3：化学式：HOOC-（CH2）x-CO- * 2：HOOC-C6H4-0-（CH2）y-CO- * Chem。 3：R2-C6H4-（CH2）z-CO- *，其中x是6-18的整数，y是3-17的整数，z是1的整数 -5和R2是摩尔质量不高于150Da的基团; 连接体包括Chem。 4：* -NH-（CH 2）2 - （O-（CH 2）2）k -O-（CH 2）n -CO- *。 其中k是1-5的整数，n是1-5的整数; 或其药学上可接受的盐，酰胺或酯。 本发明还涉及其药物用途，例如用于治疗和/或预防所有形式的糖尿病和相关疾病，以及相应的新型肽和侧链中间体。 该衍生物适用于口服给药。

    GLP-1 ANALOGUES AND DERIVATIVES
    5.
    发明申请
    GLP-1 ANALOGUES AND DERIVATIVES 有权
    GLP-1类似物和衍生物

    公开(公告)号：US20130053311A1

    公开(公告)日：2013-02-28

    申请号：US13516312

    申请日：2010-12-16

    申请人： Christoph Kalthoff ,  Jesper Lau ,  Jane Spetzler ,  Patrick William Garibay ,  Jacob Kofoed ,  Lars Linderoth

    发明人： Christoph Kalthoff ,  Jesper Lau ,  Jane Spetzler ,  Patrick William Garibay ,  Jacob Kofoed ,  Lars Linderoth

    IPC分类号： A61K38/26 ,  A61P3/10 ,  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 GLP-1 analogue which comprises a histidine (H) residue at a position corresponding to position 31 of GLP-1 (7-37) (SEQ ID NO: 1), a glutamine (Q) residue at a position corresponding to position 34 of GLP-1 (7-37) (SEQ ID NO: 1), and a maximum of ten amino acid modifications as compared to GLP-1 (7-37) (SEQ ID NO: 1); wherein the H residue is designated H31, and the Q residue is designated Q34; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to derivatives thereof, as well as the pharmaceutical use of these analogues and derivatives, for example in the treatment and/or prevention of all forms of diabetes and related diseases. The invention furthermore relates to corresponding novel side chain intermediates. The derivatives are suitable for oral administration.

    摘要翻译： 本发明涉及GLP-1类似物，其包含在对应于GLP-1（7-37）（SEQ ID NO：1）的第31位的位置处的组氨酸（H）残基，位置上的谷氨酰胺（Q）残基 对应于GLP-1（7-37）（SEQ ID NO：1）的位置34，与GLP-1（7-37）（SEQ ID NO：1）相比最多为10个氨基酸修饰。 其中H残基指定为H31，Q残基指定为Q34; 或其药学上可接受的盐，酰胺或酯。 本发明还涉及其衍生物，以及这些类似物和衍生物的药物用途，例如用于治疗和/或预防所有形式的糖尿病和相关疾病。 本发明还涉及相应的新型侧链中间体。 该衍生物适用于口服给药。

    GLP-1 analogues and derivatives
    6.
    发明授权
    GLP-1 analogues and derivatives 有权
    GLP-1类似物和衍生物

    公开(公告)号：US08815802B2

    公开(公告)日：2014-08-26

    申请号：US13516312

    申请日：2010-12-16

    申请人： Christoph Kalthoff ,  Jesper Lau ,  Jane Spetzler ,  Patrick William Garibay ,  Jacob Kofoed ,  Lars Linderoth

    发明人： Christoph Kalthoff ,  Jesper Lau ,  Jane Spetzler ,  Patrick William Garibay ,  Jacob Kofoed ,  Lars Linderoth

    IPC分类号： A61K38/26 ,  A61P3/10 ,  C07K14/605 ,  A61K38/00 ,  C07K14/65

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

    摘要： The invention relates to a GLP-1 analog which comprises a histidine (H) residue at a position corresponding to position 31 of GLP-1(7-37) (SEQ ID NO: 1), a glutamine (Q) residue at a position corresponding to position 34 of GLP-1 (7-37) (SEQ ID NO: 1), and a maximum of ten amino acid modifications as compared to GLP-1 (7-37) (SEQ ID NO: 1); wherein the H residue is designated H31, and the Q residue is designated Q34; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to derivatives thereof, as well as the pharmaceutical use of these analogs and derivatives, for example in the treatment and/or prevention of all forms of diabetes and related diseases. The invention furthermore relates to corresponding novel side chain intermediates. The derivatives are suitable for oral administration.

    摘要翻译： 本发明涉及GLP-1类似物，其在对应于GLP-1（7-37）（SEQ ID NO：1）的位置31的位置处的组氨酸（H）残基，位置上的谷氨酰胺（Q）残基 对应于GLP-1（7-37）（SEQ ID NO：1）的位置34，与GLP-1（7-37）（SEQ ID NO：1）相比最多为10个氨基酸修饰。 其中H残基指定为H31，Q残基指定为Q34; 或其药学上可接受的盐，酰胺或酯。 本发明还涉及其衍生物，以及这些类似物和衍生物的药物用途，例如用于治疗和/或预防所有形式的糖尿病和相关疾病。 本发明还涉及相应的新型侧链中间体。 该衍生物适用于口服给药。

    GLP-1 Derivatives
    7.
    发明申请
    GLP-1 Derivatives 有权
    GLP-1衍生物

    公开(公告)号：US20140303083A1

    公开(公告)日：2014-10-09

    申请号：US14343152

    申请日：2012-09-06

    申请人： Jesper Lau ,  Paw Bloch ,  Jacob Kofoed ,  Patrick William Garibay

    发明人： Jesper Lau ,  Paw Bloch ,  Jacob Kofoed ,  Patrick William Garibay

    IPC分类号： C07K14/605

    CPC分类号： C07K14/605 ,  A61K38/00 ,  A61K38/26

    摘要： The invention relates to a derivative of a GLP-1 peptide, which peptide has two Lys residues, namely a first and a second Lys residue, and a maximum of eight amino acid changes as compared to GLP-1(7-37) (SEQ ID NO: 3), which derivative comprises two protracting moieties attached to the epsilon amino group of said first and second Lys residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 15: HOOC—(CH2)x-CO—*, and Chem. 16: HOOC—C6H4-O—(CH2)y-CO—*, in which x is an integer in the range of 10-16, and y is an integer in the range of 8-12; and the linker comprises a first linker element *—NH—CH(CH2OH)—CO—*. A preferred linker is g Glu-Ser-Ser-Gly-Ser-Ser-Gly (SEQ ID NO: 2). The derivative of the invention has a very good potency, and a very good binding to the GLP-1 receptor. The invention also relates to the pharmaceutical use of the derivative, for example in the treatment and/or prevention of all forms of diabetes and related diseases.

    摘要翻译： 本发明涉及GLP-1肽的衍生物，该肽与GLP-1（7-37）（SEQ）相比具有两个Lys残基，即第一和第二Lys残基，最多八个氨基酸变化 SEQ ID NO：3），该衍生物分别包含通过接头分别连接到所述第一和第二Lys残基的ε氨基的两个伸长部分，其中伸长部分选自Chem。 15：HOOC-（CH 2）x-CO- *，和Chem。 16：HOOC-C6H4-O-（CH2）y-CO- *，其中x是10-16的整数，y是8-12的整数; 并且连接体包含第一连接体元件* -NH-CH（CH 2 OH）-CO- *。 优选的接头是g Glu-Ser-Ser-Gly-Ser-Ser-Gly（SEQ ID NO：2）。 本发明的衍生物具有非常好的效力，并且与GLP-1受体具有非常好的结合。 本发明还涉及衍生物的药物用途，例如用于治疗和/或预防所有形式的糖尿病和相关疾病。