Patents by Inventor LARS LINDEROTH
LARS LINDEROTH 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).
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Publication number: 20230272029Abstract: Peptide co-agonists of the human GLP-1 and GIP receptors suitable for oral delivery, including long-acting derivatives, and their medical use in treatment and/or prevention of obesity, diabetes, and/or liver diseases are described.Type: ApplicationFiled: July 22, 2021Publication date: August 31, 2023Inventors: Patrick J. Knerr, Brian Finan, Richard DiMarchi, Lars Linderoth
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Publication number: 20220177538Abstract: Peptide co-agonists of the human GLP-1 and GIP receptors suitable for oral delivery, including long-acting derivatives, and their medical use in treatment and/or prevention of obesity, diabetes, and/or liver diseases are described.Type: ApplicationFiled: July 22, 2021Publication date: June 9, 2022Inventors: Patrick J. Knerr, Brian Finan, Richard Dimarchi, Lars Linderoth
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Publication number: 20220125940Abstract: Peptide co-agonists of the human GLP-1 and GIP receptors suitable for oral delivery, including long-acting derivatives, and their medical use in treatment and/or prevention of obesity, diabetes, and/or liver diseases are described.Type: ApplicationFiled: January 12, 2022Publication date: April 28, 2022Inventors: Patrick James Knerr, Brian Finan, Richard DiMarchi, Lars Linderoth
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Patent number: 11117947Abstract: 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 esteType: GrantFiled: November 22, 2019Date of Patent: September 14, 2021Assignee: Novo Nordisk A/SInventors: Birgit Wieczorek, Jane Spetzler, Thomas Kruse, Lars Linderoth, Jacob Kofoed
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Patent number: 11034746Abstract: 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 esteType: GrantFiled: May 2, 2018Date of Patent: June 15, 2021Assignee: Novo Nordisk A/SInventors: Birgit Wieczorek, Jane Spetzler, Thomas Kruse, Lars Linderoth, Jacob Kofoed
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Patent number: 10946074Abstract: 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: GrantFiled: March 2, 2017Date of Patent: March 16, 2021Assignee: Novo Nordisk A/SInventors: Jacob Kofoed, Janos Tibor Kodra, Lars Linderoth, Patrick William Garibay
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Publication number: 20200407409Abstract: The invention relates to compounds derived from the EGF(A) domain of LDL-R, in particular compounds comprising a peptide analogue of the wild-type EGF(A) (LDL-R(293-332)) sequence and at least one substituent comprising at least one fatty acid group. The invention also relates to a pharmaceutical composition thereof and use a medicament. The novel EGF(A) compounds of the invention are useful as treatment e.g. in the field of cholesterol lowering, dyslipidaemia and cardiovascular disease.Type: ApplicationFiled: September 17, 2020Publication date: December 31, 2020Inventors: Jianhe Chen, Jesper F. Lau, Janos Tibor Kodra, Birgit Wieczorek, Lars Linderoth, Henning Thoegersen, Salka Elboel Rasmussen, Patrick William Garibay
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Patent number: 10822385Abstract: The invention relates to compounds derived from the EGF(A) domain of LDL-R, in particular compounds comprising a peptide analogue of the wild-type EGF(A) (LDL-R(293-332)) sequence and at least one substituent comprising at least one fatty acid group. The invention also relates to a pharmaceutical composition thereof and use a medicament. The novel EGF(A) compounds of the invention are useful as treatment e.g. in the field of cholesterol lowering, dyslipidaemia and cardiovascular disease.Type: GrantFiled: January 13, 2017Date of Patent: November 3, 2020Assignee: Novo Nordisk A/SInventors: Jianhe Chen, Jesper F. Lau, Janos Tibor Kodra, Birgit Wieczorek, Lars Linderoth, Henning Thoegersen, Salka Elboel Rasmussen, Patrick William Garibay
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Patent number: 10689429Abstract: 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: GrantFiled: April 7, 2015Date of Patent: June 23, 2020Assignee: Novo Nordisk A/SInventors: Lars Linderoth, Jacob Kofoed, Jesper Lau, Paw Bloch, Patrick William Garibay, Janos Tibor Kodra
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Publication number: 20200079834Abstract: 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 esteType: ApplicationFiled: November 22, 2019Publication date: March 12, 2020Inventors: Birgit Wieczorek, Jane Spetzler, Thomas Kruse, Lars Linderoth, Jacob Kofoed
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Publication number: 20190038721Abstract: 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: ApplicationFiled: March 2, 2017Publication date: February 7, 2019Inventors: Jacob Kofoed, Janos Tibor Kodra, Lars Linderoth, Patrick William Garibay
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Publication number: 20190016768Abstract: The invention relates to compounds derived from the EGF(A) domain of LDL-R, in particular compounds comprising a peptide analogue of the wild-type EGF(A) (LDL-R(293-332)) sequence and at least one substituent comprising at least one fatty acid group. The invention also relates to a pharmaceutical composition thereof and use a medicament. The novel EGF(A) compounds of the invention are useful as treatment e.g. in the field of cholesterol lowering, dyslipidaemia and cardiovascular disease.Type: ApplicationFiled: January 13, 2017Publication date: January 17, 2019Inventors: Jianhe Chen, Jesper F. Lau, Janos Tibor Kodra, Birgit Wieczorek, Lars Linderoth, Henning Thoegersen, Salka Elboel Rasmussen, Patrick William Garibay
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Publication number: 20180251512Abstract: 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 esteType: ApplicationFiled: May 2, 2018Publication date: September 6, 2018Inventors: Birgit Wieczorek, Jane Spetzler, Thomas Kruse, Lars Linderoth, Jacob Kofoed
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Patent number: 10005827Abstract: 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 thType: GrantFiled: November 8, 2016Date of Patent: June 26, 2018Assignee: Novo Nordisk A/SInventors: Jane Spetzler, Thomas Kruse, Lars Linderoth, Jacob Kofoed
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Publication number: 20180016319Abstract: 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.Type: ApplicationFiled: July 26, 2017Publication date: January 18, 2018Inventors: Jesper F. Lau, Thomas Kruse, Lars Linderoth, Henning Thoegersen
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Patent number: 9708383Abstract: 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, Chem. 2, and Chem. 3: HOOC—(CH2)x—CO—*??Chem. 1: HOOC—C6H4—O—(CH2)y—CO—*??Chem. 2: R2—C6H4—(CH2)z—CO—*,??Chem. 3: 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 *—NH—(CH2)2—(O—(CH2)2)k—O—(CH2)n—CO—*.??Chem. 4: 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: GrantFiled: November 9, 2011Date of Patent: July 18, 2017Assignee: Novo Nordisk A/SInventors: Alice Ravn Madsen, Birgit Wieczorek, Jacob Kofoed, Jesper Lau, Jane Spetzler, Janos Tibor Kodra, Lars Linderoth, Patrick William Garibay, Per Sauerberg, Thomas Kruse
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Publication number: 20170190757Abstract: The present invention relates to novel peptide compounds which have a protracted profile of action and improved solubility and stability, 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.Type: ApplicationFiled: March 13, 2017Publication date: July 6, 2017Inventors: Jesper F. Lau, Thomas Kruse, Lars Linderoth, Henning Thoegersen, Jacob Kofoed, Kirsten Dahl
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Publication number: 20170114116Abstract: 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.Type: ApplicationFiled: April 7, 2015Publication date: April 27, 2017Inventors: Lars Linderoth, Jacob Kofoed, Jesper Lau, Paw Bloch, Patrick William Garibay, Janos Tibor Kodra
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Publication number: 20170058014Abstract: 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 esteType: ApplicationFiled: November 8, 2016Publication date: March 2, 2017Inventors: Birgit Wieczorek, Jane Spetzler, Thomas Kruse, Lars Linderoth, Jacob Kofoed
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Publication number: 20170051034Abstract: The present invention relates to novel peptide compounds which have a protracted profile of action and improved solubility and stability, 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.Type: ApplicationFiled: September 12, 2016Publication date: February 23, 2017Inventors: Jesper F. Lau, Thomas Kruse, Lars Linderoth, Henning Thoegersen, Jacob Kofoed, Kirsten Dahl