Patents by Inventor Patrick W. Garibay
Patrick W. 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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Patent number: 11274135Abstract: 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: GrantFiled: May 2, 2013Date of Patent: March 15, 2022Assignee: Novo Nordisk A/SInventors: Jacob Kofoed, Patrick W. Garibay
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Patent number: 10265384Abstract: The present invention relates to solid pharmaceutical compositions for oral administration comprising a GLP-1 agonist, an absorption enhancer which is a salt of medium-chain fatty acid, and an enteric coating as well as uses thereof.Type: GrantFiled: January 28, 2016Date of Patent: April 23, 2019Assignee: Novo Nordisk A/SInventors: Birgitte Nissen, Flemming S. Nielsen, Patrick W. Garibay
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Patent number: 10000542Abstract: 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: May 2, 2013Date of Patent: June 19, 2018Assignee: Novo Nordisk A/SInventors: Jacob Kofoed, Patrick W. Garibay, Jesper Lau
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Publication number: 20180000903Abstract: The present invention relates to solid pharmaceutical compositions for oral administration comprising a GLP-1 agonist, an absorption enhancer which is a salt of medium-chain fatty acid, and an enteric coating as well as uses thereof.Type: ApplicationFiled: January 28, 2016Publication date: January 4, 2018Inventors: Birgitte Nissen, Flemming S. Nielsen, Patrick W. Garibay
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Patent number: 9657079Abstract: The invention relates to truncated GLP-1 analogs, in particular a GLP-1 analog which is a modified GLP-1(7-35) (SEQ ID No 1) having: i) a total of 2, 3, 4, 5 6, 7, 8, or 9 amino acid substitutions as compared to GLP-1(7-35), including a) a Glu residue at a position equivalent to position 22 of GLP-1(7-35), and b) an Arg residue at a position equivalent to position 26 of GLP-1(7-35); as well as derivatives thereof, and therapeutic uses and compositions. These analogs and derivatives are highly potent, have a good binding affinity to the GLP-1 receptor, also to the extracellular domain of the GLP-1 receptor, which is of potential relevance achieving long-acting, stable GLP-1 compounds with a potential for once weekly administration.Type: GrantFiled: June 9, 2014Date of Patent: May 23, 2017Assignee: Novo Nordisk A/SInventors: Jane Spetzler, Lauge Schaeffer, Jesper Lau, Janos T. Kodra, Kjeld Madsen, Patrick W. Garibay, Jacob Kofoed, Steffen Reedtz-Runge, Ingrid Pettersson
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Patent number: 9409966Abstract: The invention relates to protracted Glucagon-Like Peptide-1 (GLP-1) derivatives and therapeutic uses thereof. The GLP-1 derivative of the invention comprises a modified GLP-1(7-37) sequence having a total of 2-12 amino acid modifications, including Glu22 and Arg26, and being derivatised with an albumin binding residue or pegylated in position 18, 20, 23, 30, 31, 34, 36, 37, or 39. These compounds are useful in the treatment or prevention of diabetes type 2 and related diseases. The compounds are potent, stable, have long half-lives, a high affinity of binding to albumin, and/or a high affinity of binding to the extracellular domain of the GLP-1 receptor (GLP-1R), all of which is of potential relevance for the overall aim of achieving long-acting, stable and active GLP-1 derivatives with a potential for once weekly administration.Type: GrantFiled: October 3, 2014Date of Patent: August 9, 2016Assignee: Novo Nordisk A/SInventors: Jane Spetzler, Lauge Schaeffer, Jesper Lau, Thomas Kruse, Patrick W. Garibay, Steffen Reedtz-Runge, Henning Thoegersen, Ingrid Pettersson
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Publication number: 20150152157Abstract: 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—C6H4-0-(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: ApplicationFiled: May 2, 2013Publication date: June 4, 2015Inventors: Jacob Kofoed, Patrick W. Garibay
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Publication number: 20150133374Abstract: 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: May 2, 2013Publication date: May 14, 2015Inventors: Jacob Kofoed, Patrick W. Garibay, Jesper Lau
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Publication number: 20150025003Abstract: The invention relates to protracted Glucagon-Like Peptide-1 (GLP-1) derivatives and therapeutic uses thereof. The GLP-1 derivative of the invention comprises a modified GLP-1(7-37) sequence having a total of 2-12 amino acid modifications, including Glu22 and Arg26, and being derivatised with an albumin binding residue or pegylated in position 18, 20, 23, 30, 31, 34, 36, 37, or 39. These compounds are useful in the treatment or prevention of diabetes type 2 and related diseases. The compounds are potent, stable, have long half-lives, a high affinity of binding to albumin, and/or a high affinity of binding to the extracellular domain of the GLP-1 receptor (GLP-1R), all of which is of potential relevance for the overall aim of achieving long-acting, stable and active GLP-1 derivatives with a potential for once weekly administration.Type: ApplicationFiled: October 3, 2014Publication date: January 22, 2015Inventors: Jane Spetzler, Lauge Schaeffer, Jesper Lau, Thomas Kruse, Patrick W. Garibay, Steffen Reedtz-Runge, Henning Thoegersen, Ingrid Pettersson
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Publication number: 20140296131Abstract: The invention relates to truncated GLP-1 analogues, in particular a GLP-1 analogue which is a modified GLP-1(7-35) (SEQ ID No 1) having: i) a total of 2, 3, 4, 5 6, 7, 8, or 9 amino acid substitutions as compared to GLP-1(7-35), including a) a Glu residue at a position equivalent to position 22 of GLP-1(7-35), and b) an Arg residue at a position equivalent to position 26 of GLP-1(7-35); as well as derivatives thereof, and therapeutic uses and compositions. These analogues and derivatives are highly potent, have a good binding affinity to the GLP-1 receptor, also to the extracellular domain of the GLP-1 receptor, which is of potential relevance achieving long-acting, stable GLP-1 compounds with a potential for once weekly administration.Type: ApplicationFiled: June 9, 2014Publication date: October 2, 2014Applicant: NOVO NORDISK A/SInventors: Jane Spetzler, Lauge Schaeffer, Jesper Lau, Janos T. Kodra, Kjeld Madsen, Patrick W. Garibay, Jacob Kofoed, Steffen Reedtz-Runge, Henning Thoegersen, Ingrid Pettersson
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Publication number: 20140274903Abstract: This invention relates to novel compounds, methods for selective chemical conjugation of protractor molecules and the use thereof for diagnostic and/or therapeutic purposes.Type: ApplicationFiled: April 29, 2014Publication date: September 18, 2014Applicant: NOVO NORDISK HEALTHCARE AGInventors: Carsten Behrens, Patrick W. Garibay, Magali Zundel, Niels Kristian Klausen, Soeren Bjoern