知搜-全球专利检索

  1. 登录
  2. 注册

搜索结果

9 条记录 (耗时 0.021 秒)

    Compounds for treatment of obesity
    1.
    发明授权
    Compounds for treatment of obesity 有权

    公开(公告)号：US11753455B2

    公开(公告)日：2023-09-12

    申请号：US17253708

    申请日：2019-06-20

    申请人： Novo Nordisk A/S

    发明人： Nikolaj Kulahin Roed ,  Michael Paolo Bastner Sandrini ,  Jesper Lau ,  Paw Bloch ,  Anna Secher ,  Adam Paul Chambers ,  Jim McGuire ,  Lotte Bjerre Knudsen

    IPC分类号： C07K14/575 ,  A61K47/62 ,  A61K38/00

    CPC分类号： C07K14/575 ,  A61K47/62 ,  A61K38/00 ,  C07K2319/74

    摘要： The invention relates to a construct comprising a compound targeting areas in the brain involved in the regulation of body weight and an allosteric ligand to a receptor located in the blood-brain barrier (BBB). The invention also relates to compositions and uses of such construct, for example in the prevention or treatment of overweight and obesity. Preferred compounds for regulation of body weight include GLP-1 receptor agonists (GLP-1RA), and preferred receptors located in the BBB include the transferrin receptor (TfR). Exemplary fusions and conjugates of GLP-1 RA's and anti TfR-Fab's exhibit an increased binding to brain regions expressing the GLP-1 receptor as compared to fusions or conjugates with inactive control Fab's, in particular in brain areas protected by the BBB. In vivo mice studies confirm increased reduction in food intake as well as weight loss for the active construct compared to the inactive one.

    NOVEL COMPOUNDS FOR TREATMENT OF OBESITY
    2.
    发明申请
    NOVEL COMPOUNDS FOR TREATMENT OF OBESITY 有权

    公开(公告)号：US20210261641A1

    公开(公告)日：2021-08-26

    申请号：US17253708

    申请日：2019-06-20

    申请人： Novo Nordisk A/S

    发明人： Nikolaj Kulahin Roed ,  Michael Paolo Bastner Sandrini ,  Jesper Lau ,  Paw Bloch ,  Anna Secher ,  Adam Paul Chambers ,  Jim McGuire ,  Lotte Bjerre Knudsen

    IPC分类号： C07K14/575 ,  A61K47/62

    摘要： The invention relates to a construct comprising a compound targeting areas in the brain involved in the regulation of body weight and an allosteric ligand to a receptor located in the blood-brain barrier (BBB). The invention also relates to compositions and uses of such construct, for example in the prevention or treatment of overweight and obesity. Preferred compounds for regulation of body weight include GLP-1 receptor agonists (GLP-1RA), and preferred receptors located in the BBB include the transferrin receptor (TfR). Exemplary fusions and conjugates of GLP-1 RA's and anti TfR-Fab's exhibit an increased binding to brain regions expressing the GLP-1 receptor as compared to fusions or conjugates with inactive control Fab's, in particular in brain areas protected by the BBB. In vivo mice studies confirm increased reduction in food intake as well as weight loss for the active construct compared to the inactive one.

    Double-acylated GLP-1 compounds
    4.
    发明授权
    Double-acylated GLP-1 compounds 有权

    公开(公告)号：US10689429B2

    公开(公告)日：2020-06-23

    申请号：US15301960

    申请日：2015-04-07

    申请人： Novo Nordisk A/S

    发明人： Lars Linderoth ,  Jacob Kofoed ,  Jesper Lau ,  Paw Bloch ,  Patrick William Garibay ,  Janos Tibor Kodra

    IPC分类号： C07K14/605 ,  C07C235/20 ,  A61K38/00

    摘要： The invention relates to a derivative of a GLP-1 peptide, which peptide comprises a first Lys residue at a position corresponding to position 36 of GLP-1(7-37) (SEQ ID NO: 1), a second Lys residue at a position corresponding to position 37 of GLP-1(7-37) (SEQ ID NO: 1), and a maximum of seven amino acid changes as compared to GLP-1(7-37) (SEQ ID NO: 1); which derivative comprises two protractors attached to said first and second Lys residue, respectively, each via a linker; wherein the protractor is selected from: HOOC—C6H4—O—(CH2)y—CO—*, and  Chem. 1: HOOC—(CH2)x—CO—*,  Chem. 2: wherein y is an integer in the range of 8-11, and x is 12; and the linker comprises at least one of: *—NH—CH(COOH)—(CH2)2—CO—*,  Chem. 3: *—NH—CH((CH2)2—COOH)—CO—*, and/or  Chem. 4: *—NH—(CH2)2—[O—(CH2)2]k—O—[CH2]n—CO—*,  Chem. 5: 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 uses thereof, such as for the treatment of diabetes and obesity, as well as to the GLP-1 peptides forming part of these derivatives which have Lys residues at positions 36 and 37 and no other Lys residues, and the GLP-1(9-37) fragments thereof. The invention furthermore relates to an intermediate product comprising 3-carboxyphenoxy-nonanoic acid with a protection group at the carboxy group of the nonanoic acid, optionally via a linker. The derivatives have a very good potency and a long half-life which makes them potentially useful for, e.g., oral administration.

    GLP-1 derivatives
    5.
    发明授权
    GLP-1 derivatives 有权

    公开(公告)号：US10308700B2

    公开(公告)日：2019-06-04

    申请号：US15404808

    申请日：2017-01-12

    申请人： Novo Nordisk A/S

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

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

    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 gGlu-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.

    GLP-1 Derivatives
    7.
    发明申请
    GLP-1 Derivatives 审中-公开

    公开(公告)号：US20170145069A1

    公开(公告)日：2017-05-25

    申请号：US15404808

    申请日：2017-01-12

    申请人： Novo Nordisk A/S

    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 gGlu-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.

    Double-Acylated GLP-1 Compounds
    8.
    发明申请
    Double-Acylated GLP-1 Compounds 审中-公开

    公开(公告)号：US20170114116A1

    公开(公告)日：2017-04-27

    申请号：US15301960

    申请日：2015-04-07

    申请人： Novo Nordisk A/S

    发明人： Lars Linderoth ,  Jacob Kofoed ,  Jesper Lau ,  Paw Bloch ,  Patrick William Garibay ,  Janos Tibor Kodra

    IPC分类号： C07K14/605 ,  C07C235/20

    摘要： The invention relates to a derivative of a GLP-1 peptide, which peptide comprises a first Lys residue at a position corresponding to position 36 of GLP-1(7-37) (SEQ ID NO:1), a second Lys residue at a position corresponding to position 37 of GLP-1(7-37) (SEQ ID NO: 1), and a maximum of seven amino acid changes as compared to GLP-1(7-37) (SEQ ID NO: 1); which derivative comprises two protractors attached to said first and second Lys residue, respectively, each via a linker; wherein the protractor is selected from: Chem. 1: HOOC—C6H4-0-(CH2)y—CO—*, and Chem. 2: HOOC—(CH2)x—CO—*, wherein y is an integer in the range of 8-11, and x is 12; and the linker comprises at least one of: Chem. 3: *—NH—CH(COOH)—(CH2)2—CO—*, Chem. 4: *—NH—CH((CH2)2—COOH)—CO—*, and/or Chem. 5: *—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 uses thereof, such as for the treatment of diabetes and obesity, as well as to the GLP-1 peptides forming part of these derivatives which have Lys residues at positions 36 and 37 and no other Lys residues, and the GLP-1(9-37) fragments thereof. The invention furthermore relates to an intermediate product comprising 3-carboxyphenoxy-nonanoic acid with a protection group at the carboxy group of the nonanoic acid, optionally via a linker. The derivatives have a very good potency and a long half-life which makes them potentially useful for, e.g., oral administration.