Patents by Inventor Jacob Kofoed

Jacob Kofoed has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 11572398
    Abstract: The invention relates to a derivative of a GLP-1 analogue of a general Formula I, which derivative comprises a side chain attached to a Lys residue at position 34, 35, 36, 37, or 38 of the GLP-1 analogue, which side chain comprises a Branched linker, a 1st and a 2nd Protractor selected from C18 diacid, C20 diacid, and sulfonic acid C16, and at least one Linker element-1 incorporating ethylene glycol units. Linker element-1 may be incorporated in an optional Pre-linker, and/or in a 1st or 2nd Post-linker. The invention also relates to novel GLP-1 analogues, novel side chain intermediate products and their manufacture and use to prepare derivatives of biologically active peptides and proteins, as well as pharmaceutical compositions and medical uses of the analogues and derivatives. The derivatives have very long half-lives while maintaining a satisfactory potency, which makes them potentially suitable for once-monthly administration.
    Type: Grant
    Filed: November 26, 2015
    Date of Patent: February 7, 2023
    Assignee: Novo Nordisk A/S
    Inventors: Per Sauerberg, Jacob Kofoed
  • Patent number: 11518795
    Abstract: The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue and a second K residue, at positions corresponding to position 26, and 37, respectively, of GLP-1(7-37) (SEQ ID NO: 1), and a maximum of eight 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—O—(CH2)y—CO—*, in which x is an integer in the range of 8-16, and y is an integer in the range of 6-13; and the linker comprises Chem. 3: *—NH—(CH2)q—CH[(CH2)w—NR1R2]—CO—*, which is connected at its CO—* end to the epsilon amino group of the first or the second K residue of the GLP-1 analogue, and wherein q is an integer in the range of 0-5, R1 and R2 independently represent *—H or *—CH3, and w is an integer in the range of 0-5; or a pharmaceutically acceptable salt, amide, or ester thereof.
    Type: Grant
    Filed: December 17, 2019
    Date of Patent: December 6, 2022
    Assignee: Novo Nordisk A/S
    Inventors: Jacob Kofoed, Patrick William Garibay, Jesper Lau
  • Patent number: 11274135
    Abstract: The invention relates to a derivative of a GLP-1 peptide, which peptide comprises a first K residue and a second K residue, at positions corresponding to position 26, and 34, respectively, of GLP-1(7-37) (SEQ ID NO:1), and a maximum of eight 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 Chem. 2: HOOC—C6H4—O—(CH2)y—CO—*, in which y is an integer in the range of 6-13; and the linker comprises Chem. 3a: *—NH—(CH2)q—CH[(CH2)w—NR1R2]—CO—*, wherein q is an integer in the range of 0-5, R1 and R2 independently represent *—H or *—CH3, 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 peptide and linker intermediates.
    Type: Grant
    Filed: May 2, 2013
    Date of Patent: March 15, 2022
    Assignee: Novo Nordisk A/S
    Inventors: Jacob Kofoed, Patrick W. Garibay
  • Patent number: 11117947
    Abstract: 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 este
    Type: Grant
    Filed: November 22, 2019
    Date of Patent: September 14, 2021
    Assignee: Novo Nordisk A/S
    Inventors: Birgit Wieczorek, Jane Spetzler, Thomas Kruse, Lars Linderoth, Jacob Kofoed
  • Patent number: 11034746
    Abstract: 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)2—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 este
    Type: Grant
    Filed: May 2, 2018
    Date of Patent: June 15, 2021
    Assignee: Novo Nordisk A/S
    Inventors: Birgit Wieczorek, Jane Spetzler, Thomas Kruse, Lars Linderoth, Jacob Kofoed
  • Patent number: 10946074
    Abstract: The invention relates to GLP-1 analogues and derivatives having a Trp at a position corresponding to position 8 of GLP-1(7-37), and their pharmaceutical use e.g. in the treatment of type 2 diabetes. These Trp8 compounds are very stable against degradation by DPP-IV, while maintaining the capability to bind to and activate the GLP-1 receptor. The derivatives have one or two substituents (P-L) attached to a Lys residue of the GLP-1 analogue via an optional Branching group (B), wherein P is a Protracting moiety such as a fatty diacid, and L is a linker consisting of one or more linker elements such as, for example, 8-amino-3,6-dioxaoctanoic acid. Examples of compounds of the invention include the 8W variants of liraglutide and dulaglutide.
    Type: Grant
    Filed: March 2, 2017
    Date of Patent: March 16, 2021
    Assignee: Novo Nordisk A/S
    Inventors: Jacob Kofoed, Janos Tibor Kodra, Lars Linderoth, Patrick William Garibay
  • Patent number: 10689429
    Abstract: 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.
    Type: Grant
    Filed: April 7, 2015
    Date of Patent: June 23, 2020
    Assignee: Novo Nordisk A/S
    Inventors: Lars Linderoth, Jacob Kofoed, Jesper Lau, Paw Bloch, Patrick William Garibay, Janos Tibor Kodra
  • Publication number: 20200123215
    Abstract: The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue and a second K residue, at positions corresponding to position 26, and 37, respectively, of GLP-1(7-37) (SEQ ID NO: 1), and a maximum of eight 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—O—(CH2)y—CO—*, in which x is an integer in the range of 8-16, and y is an integer in the range of 6-13; and the linker comprises Chem. 3: *—NH—(CH2)q—CH[(CH2)w—NR1R2]—CO—*, which is connected at its CO—* end to the epsilon amino group of the first or the second K residue of the GLP-1 analogue, and wherein q is an integer in the range of 0-5, R1 and R2 independently represent *—H or *—CH3, and w is an integer in the range of 0-5; or a pharmaceutically acceptable salt, amide, or ester thereof.
    Type: Application
    Filed: December 17, 2019
    Publication date: April 23, 2020
    Inventors: Jacob Kofoed, Patrick William Garibay, Jesper Lau
  • Patent number: 10604554
    Abstract: The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue and a second K residue, at positions corresponding to position 26, and 37, respectively, of GLP-1(7-37) (SEQ ID NO: 1), and a maximum of eight 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—O—(CH2)y—CO—*, in which x is an integer in the range of 8-16, and y is an integer in the range of 6-13; and the linker comprises Chem. 3: *—NH—(CH2)q—CH[(CH2)w—NR1R2]—CO—*, which is connected at its CO—* end to the epsilon amino group of the first or the second K residue of the GLP-1 analogue, and wherein q is an integer in the range of 0-5, R1 and R2 independently represent *—H or *—CH3, and w is an integer in the range of 0-5; or a pharmaceutically acceptable salt, amide, or ester thereof.
    Type: Grant
    Filed: April 30, 2018
    Date of Patent: March 31, 2020
    Assignee: Novo Nordisk A/S
    Inventors: Jacob Kofoed, Patrick William Garibay, Jesper Lau
  • Publication number: 20200079834
    Abstract: 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 este
    Type: Application
    Filed: November 22, 2019
    Publication date: March 12, 2020
    Inventors: Birgit Wieczorek, Jane Spetzler, Thomas Kruse, Lars Linderoth, Jacob Kofoed
  • Patent number: 10392428
    Abstract: The invention relates to a derivative of a GLP-1 analog of a general Formula I, which derivative comprises a side chain attached to a Lys residue at position 34, 35, 36, 37, 38, or 39 of the GLP-1 analog. The side chain comprises a Branched linker, a 1st and a 2nd Protractor and a Pre-linker. The Branched linker is connected to the Lys residue of the GLP-1 analog via the Pre-linker and to the 1st and the 2nd Protractor via a 1st and 2nd Post-linker, respectively. The Branched linker may, e.g., be a tri-radical of Lys. The 1st and the 2nd Protractor is C20 diacid. Various linker elements may be used in the Prelinker as well as the two Post-linkers. The invention also relates to novel GLP-analogs, novel side chain intermediates and their manufacture and use to prepare derivatives of biologically active peptides and proteins, as well as pharmaceutical compositions and medical uses of the analogs and derivatives.
    Type: Grant
    Filed: December 17, 2015
    Date of Patent: August 27, 2019
    Assignee: Novo Nordisk A/S
    Inventor: Jacob Kofoed
  • Patent number: 10308700
    Abstract: 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.
    Type: Grant
    Filed: January 12, 2017
    Date of Patent: June 4, 2019
    Assignee: Novo Nordisk A/S
    Inventors: Jesper Lau, Paw Bloch, Jacob Kofoed, Patrick William Garibay
  • Patent number: 10266577
    Abstract: The present invention relates to tri-acylated GLP-1 derivatives, acylated at positions corresponding to positions (18, 22, 30), (18, 26, 37), (18, 27, 37), (26, 30, 37), or (27, 30, 37) of the native human glucagon-like peptide 1 (GLP-1 (7-37) (SEQ ID NO: 1); or pharmaceutically acceptable salts, amides, or esters thereof. The acylated side chains comprise a protracting moiety selected from Chem. 1: HOOC—(CH2)16—CO—*, Chem. 1a: HOOC—(CH2)18—CO—*, and Chem. 2: HO3S—(CH2)15—CO—*, and the protracting moieties are connected, via a linker, to a Lys residue of the GLP-1 peptide. The GLP-1 peptide has a maximum of seven amino acid changes as compared to GLP-1 (7-37) (SEQ ID NO: 1). The invention also relates to intermediate products in the form of novel GLP-1 analogs, as well as to pharmaceutical compositions and uses of the derivatives and analogs, in particular for the treatment of type 2 diabetes.
    Type: Grant
    Filed: August 14, 2014
    Date of Patent: April 23, 2019
    Assignee: Novo Nordisk A/S
    Inventors: Per Sauerberg, Jacob Kofoed
  • Publication number: 20190038721
    Abstract: The invention relates to GLP-1 analogues and derivatives having a Trp at a position corresponding to position 8 of GLP-1(7-37), and their pharmaceutical use e.g. in the treatment of type 2 diabetes. These Trp8 compounds are very stable against degradation by DPP-IV, while maintaining the capability to bind to and activate the GLP-1 receptor. The derivatives have one or two substituents (P-L) attached to a Lys residue of the GLP-1 analogue via an optional Branching group (B), wherein P is a Protracting moiety such as a fatty diacid, and L is a linker consisting of one or more linker elements such as, for example, 8-amino-3,6-dioxaoctanoic acid. Examples of compounds of the invention include the 8W variants of liraglutide and dulaglutide.
    Type: Application
    Filed: March 2, 2017
    Publication date: February 7, 2019
    Inventors: Jacob Kofoed, Janos Tibor Kodra, Lars Linderoth, Patrick William Garibay
  • Patent number: 10195255
    Abstract: 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.
    Type: Grant
    Filed: June 19, 2014
    Date of Patent: February 5, 2019
    Assignee: Novo Nordisk A/S
    Inventors: Steffen Reedtz-Runge, Per Sauerberg, Jacob Kofoed, Ingrid Pettersson, Christian W. Tornoee
  • Publication number: 20180258153
    Abstract: The invention relates to a derivative of a GLP-1 analogue of a general Formula I, which derivative comprises a side chain attached to a Lys residue at position 34, 35, 36, 37, 38, or 39 of the GLP-1 analogue. The side chain comprises a Branched linker, a 1st and a 2nd Protractor and a Pre-linker. The Branched linker is connected to the Lys residue of the GLP-1 analogue via the Pre-linker and to the 1st and the 2nd Protractor via a 1st and 2nd Post-linker, respectively. The Branched linker may, e.g., be a tri-radical of Lys. The 1st and the 2nd Protractor is C20 diacid. Various linker elements may be used in the Prelinker as well as the two Post-linkers. The invention also relates to novel GLP-analogues, novel side chain intermediates and their manufacture and use to prepare derivatives of biologically active peptides and proteins, as well as pharmaceutical compositions and medical uses of the analogues and derivatives.
    Type: Application
    Filed: December 17, 2015
    Publication date: September 13, 2018
    Applicants: Novo Nordisk A/S, Novo Nordisk A/S
    Inventor: Jacob Kofoed
  • Publication number: 20180251512
    Abstract: 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)2—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 este
    Type: Application
    Filed: May 2, 2018
    Publication date: September 6, 2018
    Inventors: Birgit Wieczorek, Jane Spetzler, Thomas Kruse, Lars Linderoth, Jacob Kofoed
  • Publication number: 20180244742
    Abstract: The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue and a second K residue, at positions corresponding to position 26, and 37, respectively, of GLP-1(7-37) (SEQ ID NO: 1), and a maximum of eight 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—O—(CH2)y—CO-*, in which x is an integer in the range of 8-16, and y is an integer in the range of 6-13; and the linker comprises Chem. 3: *—NH—(CH2)q—CH[(CH2)w—NR1R2]—CO-*, which is connected at its CO-* end to the epsilon amino group of the first or the second K residue of the GLP-1 analogue, and wherein q is an integer in the range of 0-5, R1 and R2 independently represent *—H or *—CH3, and w is an integer in the range of 0-5; or a pharmaceutically acceptable salt, amide, or ester thereof.
    Type: Application
    Filed: April 30, 2018
    Publication date: August 30, 2018
    Inventors: Jacob Kofoed, Patrick William Garibay, Jesper Lau
  • Patent number: 10010614
    Abstract: The invention relates to derivatives of GLP-1 like peptides which are C-terminally extended analogs of native GLP-1. The derivatives comprise two side chains, one at a position corresponding to position 42, and one at a position corresponding to position 18, 23, 27, 31, 36, or 38, wherein both positions are when compared to GLP-1(7-37). The side chains comprise a C19, C20, or C22 diacid protracting moiety and optionally a linker. The invention also relates to intermediate products in the form of novel GLP-1 analogs incorporated in the derivatives of the invention, as well as 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.
    Type: Grant
    Filed: September 28, 2016
    Date of Patent: July 3, 2018
    Assignee: Novo Nordisk A/S
    Inventors: Steffen Reedtz-Runge, Jacob Kofoed
  • Patent number: 10005827
    Abstract: The invention relates to a derivative of a GLP-1 analog, which analog 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 th
    Type: Grant
    Filed: November 8, 2016
    Date of Patent: June 26, 2018
    Assignee: Novo Nordisk A/S
    Inventors: Jane Spetzler, Thomas Kruse, Lars Linderoth, Jacob Kofoed