利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

67 条记录 (耗时 0.045 秒)

    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。

    NOVEL GLUCAGON ANALOGUES
    6.
    发明申请
    NOVEL GLUCAGON ANALOGUES 审中-公开
    新的GLUCAGON ANALOGUES

    公开(公告)号：US20130143798A1

    公开(公告)日：2013-06-06

    申请号：US13637522

    申请日：2011-03-28

    申请人： Jesper F. Lau ,  Thomas Kruse ,  Lars Linderoth ,  Henning Thoegersen

    发明人： Jesper F. Lau ,  Thomas Kruse ,  Lars Linderoth ,  Henning Thoegersen

    IPC分类号： C07K14/605 ,  A61K47/48

    CPC分类号： C07K14/605 ,  A61K38/00 ,  A61K38/26 ,  A61K38/28 ,  A61K47/542 ,  A61K47/545

    摘要： The present invention relates to novel peptide compounds which have an improved physical stability in solution and improved solubility at neutral pH, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of hyperglycemia, diabetes and obesity, as well as a variety of diseases or conditions associated with hyperglycemia, diabetes and obesity.

    摘要翻译： 本发明涉及在溶液中具有改善的物理稳定性和在中性pH下改善的溶解度，化合物在治疗中的用途的新型肽化合物，包括向有需要的患者施用化合物的治疗方法，以及 化合物在制造药物中的用途。 本发明的化合物在治疗高血糖症，糖尿病和肥胖以及与高血糖症，糖尿病和肥胖相关的各种疾病或病症方面特别有意义。

    Novel Glucagon Analogues
    7.
    发明申请
    Novel Glucagon Analogues 审中-公开
    新型胰高血糖素类似物

    公开(公告)号：US20140031278A1

    公开(公告)日：2014-01-30

    申请号：US13984185

    申请日：2012-03-28

    申请人： Jesper F. Lau ,  Thomas Kruse ,  Henning Thoegersen ,  Thomas Nylandsted Krogh ,  Ulrich Sensfuss

    发明人： Jesper F. Lau ,  Thomas Kruse ,  Henning Thoegersen ,  Thomas Nylandsted Krogh ,  Ulrich Sensfuss

    IPC分类号： C07K14/605 ,  A61K45/06 ,  A61K38/26

    CPC分类号： C07K14/605 ,  A61K38/26 ,  A61K45/06 ,  A61K47/64

    摘要： The present invention relates to novel glucagon peptides with improved stability and solubility at neutral pH, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The glucagon peptides of the invention are of particular interest in relation to the treatment of hyperglycemia, diabetes and obesity, as well as a variety of diseases or conditions associated with hyperglycemia, diabetes and obesity.

    摘要翻译： 本发明涉及在中性pH下具有改善的稳定性和溶解度的新型胰高血糖素肽，在治疗中使用该化合物的方法，包括向有需要的患者施用化合物，以及该化合物在 制药。 本发明的胰高血糖素肽与治疗高血糖症，糖尿病和肥胖以及与高血糖症，糖尿病和肥胖相关的各种疾病或病症有特别的关注。

    NOVEL GLUCAGON ANALOGUES
    8.
    发明申请
    NOVEL GLUCAGON ANALOGUES 审中-公开
    新的GLUCAGON ANALOGUES

    公开(公告)号：US20130053310A1

    公开(公告)日：2013-02-28

    申请号：US13637527

    申请日：2011-03-28

    申请人： Jesper F. Lau ,  Thomas Kruse

    发明人： Jesper F. Lau ,  Thomas Kruse

    IPC分类号： C07K14/605 ,  A61P3/08 ,  A61K38/26

    CPC分类号： C07K14/605 ,  A61K38/00

    摘要： The present invention relates to glucagon peptide agonists which have improved solubility and stability, to the use of the peptides in therapy, to methods of treatment comprising administration of the peptides to patients in need thereof, and to the use of the peptides in the manufacture of medicaments. The glucagon peptides of the invention are of particular interest in relation to the treatment of hypoglycemia, diabetes and obesity, as well as a variety of diseases or conditions associated with hypoglycemia, diabetes and obesity.

    摘要翻译： 本发明涉及胰高血糖素肽激动剂，其在治疗中使用肽具有改善的溶解度和稳定性，包括向有需要的患者施用肽以及使用肽来制备 药物。 本发明的胰高血糖素肽与治疗低血糖症，糖尿病和肥胖症以及与低血糖，糖尿病和肥胖相关的各种疾病或病症有特别的关注。

    Double-acylated GLP-1 derivatives with a linker
    9.
    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 WITH A LINKER
    10.
    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。