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: 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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Patent number: 9556250Abstract: The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 37 of GLP-1(7-37) (SEQ ID NO: 1), a second K residue at a position corresponding to position 26 of GLP-1(7-37), and a maximum of ten amino acid modifications as compared to GLP-1(7-37), wherein the first K residue is designated K37, and the second K residue is designated K26, which derivative comprises two albumin binding moieties attached to K26 and K37, respectively, wherein the albumin binding moiety comprises a protracting moiety selected from: Chem. 1, Chem. 2, Chem. 3 or Chem. 4; or a pharmaceutically acceptable salt, amide, or ester thereof.Type: GrantFiled: December 10, 2013Date of Patent: January 31, 2017Assignee: Novo Nordisk A/SInventors: Patrick William Garibay, Jane Spetzler, Lars Linderoth, Jesper Lau, Lauge Schaeffer
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Patent number: 9480753Abstract: The present invention relates to Fibroblast Growth Factor 21 (FGF21), more in particular to derivatives of FGF21 compounds having an albumin binder of the formula A-B-C-D-E- covalently attached. The invention also relates to novel FGF21 analogues, as well as to the pharmaceutical use of these FGF21 derivatives and analogues, in particular for the treatment of diabetes, dyslipidemia, obesity, cardiovascular diseases, metabolic syndrome, and/or Non Alcoholic Fatty Liver Disease (NAFLD). The derivatives of the invention are protracted, e.g. capable of maintaining a low blood glucose level for a longer period of time, capable of increasing the in vivo half-life of FGF21, and/or result in a lower clearance of FGF21. The derivatives of the invention are preferably furthermore of an improved oxidative stability.Type: GrantFiled: January 22, 2010Date of Patent: November 1, 2016Assignee: Novo Nordisk A/SInventors: Tina Møller Tagmose, Patrick William Garibay, Bírgítte Andersen, Henning Thøgersen, Birgit Wieczorek
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Patent number: 9150633Abstract: An acylated insulin analogue wherein the insulin analogue comprises a lysine residue connected C-terminally to the A21 amino acid residue or a peptide residue of up to 4 amino acid residues comprising a lysine residue which peptide residue is connected C-terminally to the A21 amino acid residue, characterized in that an acyl moiety comprising an alkylene glycol moiety is attached to the lysine residue in the A22 position or attached to a lysine residue present in the peptide residue that is attached to the C terminal end of the A21 amino acid residue and wherein there is only one lysine (K, Lys) in the insulin analogue, can conveniently be administered pulmonary.Type: GrantFiled: August 15, 2008Date of Patent: October 6, 2015Assignee: Novo Nordisk A/SInventors: Peter Madsen, Thomas Børglum Kjeldsen, Thomas Hoeg-Jensen, Tina Møller Tagmose, Palle Jakobsen, János Tibor Kodra, Patrick William Garibay, Dorte Xenia Gram
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Publication number: 20150210748Abstract: 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: April 14, 2015Publication date: July 30, 2015Inventors: Peter Madsen, Thomas B. 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: 20150210745Abstract: The invention relates to a derivative of a GLP-1 analogue, which analogue 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 HOOC—(CH2)x-CO—*, and Chem. 1: HOOC—C6H4-0-(CH2)y-CO—*, Chem. 2: in which x is an integer in the range of 6-18, and y is an integer in the range of 3-17; and the linker comprises *—NH—(CH2)q-CH[(CH2)w-NH2]-CO—*, Chem. 3: wherein q is an integer in the range of 0-5, and w is an integer in the range of 0-5; or a pharmaceutically acceptable salt, amide, or ester thereof.Type: ApplicationFiled: January 29, 2015Publication date: July 30, 2015Inventors: Jacob Kofoed, Jesper Lau, Lars Linderoth, Patrick William Garibay, Thomas Kruse
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Publication number: 20150210747Abstract: 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: April 13, 2015Publication date: July 30, 2015Inventors: Peter Madsen, Thomas B. 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: 9067977Abstract: The invention relates to protracted peptide derivatives such as Glucagon-Like Peptide-1 (GLP-1), exendin-4, and analogs thereof, as well as therapeutic uses thereof. The peptide derivative of the invention comprises a peptide wherein at least one amino acid residue is derivatized with A-B-C-, or A-B-C-D-. These compounds are useful in the treatment or prevention of diabetes type 2 and related diseases. The compounds are potent, have a low ratio of binding affinity to the GLP-1 receptor in the presence of high/low albumin concentrations, have long half-lives, and have a high affinity of binding to albumin, 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: June 28, 2013Date of Patent: June 30, 2015Assignee: Novo Nordisk A/SInventors: Jane Spetzler, Lauge Schaeffer, Jesper Lau, Thomas Kruse, Patrick William Garibay, Soeren Oestergaard, Steffen Reedtz-Runge, Henning Thoegersen
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Patent number: 9045560Abstract: 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: August 22, 2013Date of Patent: June 2, 2015Assignee: NOVO NORDISK A/SInventors: Peter Madsen, Thomas Boerglum Kjeldsen, Thomas Hoeg-Jensen, Palle Jakobsen, Tina Moeller Tagmose, Tine Glendorf, Jaanos Tibor Kodra, Patrick William Garibay, Jacob Sten Petersen
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Patent number: 9006178Abstract: 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: HOOC—(CH2)x—CO—*, and Chem. 2: HOOC—C6H4-0-(CH2)y—CO—*, in which x is an integer in the range of 6-18, and y is an integer in the range of 3-17; and the linker comprises Chem. 3: *—NH—(CH2)q—CH[(CH2)w—NH2]—CO—*, wherein q is an integer in the range of 0-5, and w is an integer in the range of 0-5; or a pharmaceutically acceptable salt, amide, or ester thereof.Type: GrantFiled: November 9, 2011Date of Patent: April 14, 2015Assignee: Novo Nordisk A/SInventors: Jacob Kofoed, Jesper Lau, Lars Linderoth, Patrick William Garibay, Thomas Kruse
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Patent number: 8933021Abstract: The present invention relates to novel human insulin derivatives which are soluble at physiological pH values and have a prolonged profile of action. The invention also relates to methods of providing such derivatives, to pharmaceutical compositions containing them, to methods of treating diabetes and hyperglycaemia using the insulin derivatives of the invention and to the use of such insulin derivatives in the treatment of diabetes and hyperglycaemia.Type: GrantFiled: May 8, 2007Date of Patent: January 13, 2015Assignee: Novo Nordisk A/SInventors: Frantisek Hubalek, Thomas Hoeg-Jensen, Ib Jonassen, Patrick William Garibay, Palle Jakobsen, Svend Havelund, Janos Tibor Kodra
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Patent number: 8895694Abstract: 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: September 5, 2008Date of Patent: November 25, 2014Assignee: Novo Nordisk A/SInventors: Jane Spetzler, Lauge Schäffer, Jesper Lau, Thomas Kruse, Patrick William Garibay, Steffen Reedtz-Runge, Henning Thøgersen, Ingrid Pettersson
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Patent number: 8865868Abstract: The invention relates to conjugated proteins, in particular but not exclusively, blood coagulation factors, to processes for preparing the conjugated proteins which contain the steps of reacting a protein or glycoprotein, such as factor VIIa or human growth hormone, with a water insoluble albumin binder in the presence of an optionally substituted cyclodextrin molecule, to pharmaceutical compositions comprising the protein conjugates and to the use of the protein conjugates in therapy, in particular but not exclusively, for the treatment of diseases alleviated by blood coagulation factors such as the prophylactic treatment of hemophilia.Type: GrantFiled: August 6, 2009Date of Patent: October 21, 2014Assignee: Novo Nordisk Healthcare AGInventors: Carsten Behrens, Patrick William Garibay, Søren Østergaard, Henrik Sune Andersen, Nils Langeland Johansen, Bernd Peschke, Sonja Bak
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Patent number: 8859493Abstract: The present invention is related to insulin derivatives having a side chain attached either to the ?-amino group of the N-terminal amino acid residue of B chain or to an ?-amino group of a Lys residue present in the B chain of the parent insulin molecule via an amide bond which side chain comprises one or more residues of ethyleneglycol, propyleneglycol and/or butyleneglycol containing independently at each termini a group selected from —NH2 and —COOH; a fatty diacid moiety with 4 to 22 carbon atoms, at least one free carboxylic acid group or a group which is negatively charged at neutral pH; and possible linkers which link the individual components in the side chain together via amide or ether bonds, said linkers optionally comprising a free carboxylic acid group.Type: GrantFiled: April 9, 2012Date of Patent: October 14, 2014Assignee: Novo Nordisk A/SInventors: Patrick William Garibay, Thomas Hoeg-Jensen, Ib Jonassen, Svend Havelund, Peter Madsen, Palle Jakobsen
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Publication number: 20140303083Abstract: 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: ApplicationFiled: September 6, 2012Publication date: October 9, 2014Applicant: NOVO NORDISK A/SInventors: Jesper Lau, Paw Bloch, Jacob Kofoed, Patrick William Garibay
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Patent number: 8815802Abstract: The invention relates to a GLP-1 analog which comprises a histidine (H) residue at a position corresponding to position 31 of GLP-1(7-37) (SEQ ID NO: 1), a glutamine (Q) residue at a position corresponding to position 34 of GLP-1 (7-37) (SEQ ID NO: 1), and a maximum of ten amino acid modifications as compared to GLP-1 (7-37) (SEQ ID NO: 1); wherein the H residue is designated H31, and the Q residue is designated Q34; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to derivatives thereof, as well as the pharmaceutical use of these analogs and derivatives, for example in the treatment and/or prevention of all forms of diabetes and related diseases. The invention furthermore relates to corresponding novel side chain intermediates. The derivatives are suitable for oral administration.Type: GrantFiled: December 16, 2010Date of Patent: August 26, 2014Assignee: Novo Nordisk A/SInventors: Christoph Kalthoff, Jesper Lau, Jane Spetzler, Patrick William Garibay, Jacob Kofoed, Lars Linderoth
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Patent number: 8796205Abstract: Novel human insulin derivatives are described which are soluble at physiological pH values and have a prolonged profile of action.Type: GrantFiled: May 8, 2007Date of Patent: August 5, 2014Assignee: Novo Nordisk A/SInventors: Ib Jonassen, Patrick William Garibay, Janos Tibor Kodra
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Publication number: 20140179899Abstract: The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 37 of GLP-1(7-37) (SEQ ID NO: 1), a second K residue at a position corresponding to position 26 of GLP-1(7-37), and a maximum of ten amino acid modifications as compared to GLP-1(7-37), wherein the first K residue is designated K37, and the second K residue is designated K26, which derivative comprises two albumin binding moieties attached to K26 and K37, respectively, wherein the albumin binding moiety comprises a protracting moiety selected from: Chem. 1, Chem. 2, Chem. 3 or Chem. 4; or a pharmaceutically acceptable salt, amide, or ester thereof.Type: ApplicationFiled: December 10, 2013Publication date: June 26, 2014Applicant: NOVO NORDISK A/SInventors: Patrick William Garibay, Jane Spetzler, Janos Tibor Kodra, Lars Linderoth, Jesper Lau, Per Sauerberg
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Patent number: 8722620Abstract: The present invention is related to insulin derivatives having a side chain attached to an ?-amino group of a Lys residue present in the A-chain or to an ?-amino group of a Lys residue in the B-chain.Type: GrantFiled: February 27, 2007Date of Patent: May 13, 2014Assignee: Novo Nordisk A/SInventors: Charlotte Harkjaer Fynbo, Ib Jonassen, Thomas Børglum Kjeldsen, Peter Madsen, Patrick William Garibay, Janos Tibor Kodra, Thomas Hoeg-Jensen, Tina Møller Tagmose
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Patent number: RE46170Abstract: The present invention relates to insulin derivatives having a side chain attached either to the ?-amino group of the N-terminal amino acid residue of the B chain or to the ?-amino group of a Lys residue present in the B chain of the parent insulin via an amide bond which side chain comprises at least one aromatic group; at least one free carboxylic acid group or a group which is negatively charged at neutral pH, a fatty acid moiety with 4 to 22 carbon atoms in the carbon chain; and possible linkers which link the individual components in the side chain together via amide bonds.Type: GrantFiled: June 26, 2014Date of Patent: October 4, 2016Assignee: Novo Nordisk A/SInventors: Janos Tibor Kodra, Patrick William Garibay, Thomas Hoeg-Jensen, Ib Jonassen, Peter Madsen, Tina Moeller Tagmose