Patents by Inventor Patrick William Garibay
Patrick William Garibay 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: 20230233650Abstract: Ucn2 derivatives comprising a peptide and a substituent with high potency, high physical and high chemical stability, suitable for administration to humans, and their medical use in treatment and/or prevention of obesity and/or diabetes.Type: ApplicationFiled: July 15, 2022Publication date: July 27, 2023Inventors: Chien Li, Nicholas Raymond Cox, Jason O'Neil, Patrick William Garibay, Berit Christoffersen Gyrstinge, Hans Dennis Aasberg, Lennart Lykke, Nikolaj Kulahin Roed
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Patent number: 11518795Abstract: 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: GrantFiled: December 17, 2019Date of Patent: December 6, 2022Assignee: Novo Nordisk A/SInventors: Jacob Kofoed, Patrick William Garibay, Jesper Lau
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Publication number: 20220265777Abstract: The invention relates to solid pharmaceutical compositions comprising a GLP-1 agonist, an SGLT2 inhibitor and a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid. The invention further relates to processes for the preparation of such compositions, and their use in medicine.Type: ApplicationFiled: August 6, 2020Publication date: August 25, 2022Inventors: Betty Lomstein Pedersen, Birgitte Nissen, Patrick William Garibay, Kaisa Naelapaeae, Andreas Vegge
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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: 20200123215Abstract: 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: ApplicationFiled: December 17, 2019Publication date: April 23, 2020Inventors: Jacob Kofoed, Patrick William Garibay, Jesper Lau
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Patent number: 10604554Abstract: 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: GrantFiled: April 30, 2018Date of Patent: March 31, 2020Assignee: Novo Nordisk A/SInventors: Jacob Kofoed, Patrick William Garibay, Jesper Lau
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Patent number: 10308700Abstract: 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: GrantFiled: January 12, 2017Date of Patent: June 4, 2019Assignee: Novo Nordisk A/SInventors: Jesper Lau, Paw Bloch, Jacob Kofoed, Patrick William Garibay
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Publication number: 20190112348Abstract: Novel acylated insulin analogues exhibiting resistance towards proteases can, effectively, be administered pulmonary or orally. The insulin analogues contain B25H and A14E or A14H.Type: ApplicationFiled: December 14, 2018Publication date: April 18, 2019Inventors: Peter Madsen, Thomas Boerglum Kjeldsen, Thomas Hoeg-Jensen, Palle Jakobsen, Tina Moeller Tagmose, Tine Glendorf, Janos Tibor Kodra, Patrick William Garibay, Jacob Sten Petersen
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Patent number: 10259856Abstract: Novel acylated insulin analogues exhibiting resistance towards proteases can, effectively, be administered pulmonary or orally. The insulin analogues contain B25H and A14E or A14H.Type: GrantFiled: April 14, 2015Date of Patent: April 16, 2019Assignee: Novo Nordisk A/SInventors: Peter Madsen, Thomas Boerglum Kjeldsen, Thomas Hoeg-Jensen, Palle Jakobsen, Tina Moeller Tagmose, Tine Glendorf, Janos Tibor Kodra, Patrick William Garibay, Jacob Sten Petersen
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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: 20180244742Abstract: 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: ApplicationFiled: April 30, 2018Publication date: August 30, 2018Inventors: Jacob Kofoed, Patrick William Garibay, Jesper Lau
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Patent number: 9758560Abstract: 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.Type: GrantFiled: September 6, 2012Date of Patent: September 12, 2017Assignee: Novo Nordisk A/SInventors: Jesper Lau, Paw Bloch, Patrick William Garibay
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Patent number: 9732137Abstract: A semi-recombinant method for the production of GLP-1 analogues and derivatives with non-proteogenic amino acids in the N-terminal part combining the use of recombinant expression techniques and chemical peptide synthesis.Type: GrantFiled: December 22, 2008Date of Patent: August 15, 2017Assignee: Novo Nordisk A/SInventors: Jesper Færgeman Lau, Asser Sloth Andersen, Paw Bloch, Jesper Lau, Patrick William Garibay, Thomas Kruse, Inga Sig Nielsen Nørby, Claus Ulrich Jessen, Caspar Christensen, Jens Christian Norrild
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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: 20170145069Abstract: 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: ApplicationFiled: January 12, 2017Publication date: May 25, 2017Inventors: Jesper Lau, Paw Bloch, Jacob Kofoed, Patrick William Garibay
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Patent number: 9655974Abstract: Analogs of FGF21 carrying a modifying, substituted ethylene or benzyl group can be used for treatment or prevention of diabetes, dyslipidemia, obesity, cardiovascular diseases, metabolic syndrome, and/or Non Alcoholic Fatty Liver Disease (NAFLD).Type: GrantFiled: July 18, 2011Date of Patent: May 23, 2017Assignee: Novo Nordisk A/SInventors: Tina Moeller Tagmose, Patrick William Garibay, Xujia Zhang, Henning Thoegersen, Peter Kresten Nielsen, Kristian Sass Bak-Jensen, Helle Fabricius Woeldike