Patents by Inventor Paw Bloch
Paw Bloch 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: 11753455Abstract: The invention relates to a construct comprising a compound targeting areas in the brain involved in the regulation of body weight and an allosteric ligand to a receptor located in the blood-brain barrier (BBB). The invention also relates to compositions and uses of such construct, for example in the prevention or treatment of overweight and obesity. Preferred compounds for regulation of body weight include GLP-1 receptor agonists (GLP-1RA), and preferred receptors located in the BBB include the transferrin receptor (TfR). Exemplary fusions and conjugates of GLP-1 RA's and anti TfR-Fab's exhibit an increased binding to brain regions expressing the GLP-1 receptor as compared to fusions or conjugates with inactive control Fab's, in particular in brain areas protected by the BBB. In vivo mice studies confirm increased reduction in food intake as well as weight loss for the active construct compared to the inactive one.Type: GrantFiled: June 20, 2019Date of Patent: September 12, 2023Assignee: Novo Nordisk A/SInventors: Nikolaj Kulahin Roed, Michael Paolo Bastner Sandrini, Jesper Lau, Paw Bloch, Anna Secher, Adam Paul Chambers, Jim McGuire, Lotte Bjerre Knudsen
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Publication number: 20210261641Abstract: The invention relates to a construct comprising a compound targeting areas in the brain involved in the regulation of body weight and an allosteric ligand to a receptor located in the blood-brain barrier (BBB). The invention also relates to compositions and uses of such construct, for example in the prevention or treatment of overweight and obesity. Preferred compounds for regulation of body weight include GLP-1 receptor agonists (GLP-1RA), and preferred receptors located in the BBB include the transferrin receptor (TfR). Exemplary fusions and conjugates of GLP-1 RA's and anti TfR-Fab's exhibit an increased binding to brain regions expressing the GLP-1 receptor as compared to fusions or conjugates with inactive control Fab's, in particular in brain areas protected by the BBB. In vivo mice studies confirm increased reduction in food intake as well as weight loss for the active construct compared to the inactive one.Type: ApplicationFiled: June 20, 2019Publication date: August 26, 2021Inventors: Nikolaj Kulahin Roed, Michael Paolo Bastner Sandrini, Jesper Lau, Paw Bloch, Anna Secher, Adam Paul Chambers, Jim McGuire, Lotte Bjerre Knudsen
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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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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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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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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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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: 20160108102Abstract: Novel polypeptide derivatives having protracted profile of action.Type: ApplicationFiled: June 25, 2015Publication date: April 21, 2016Inventors: Jesper Lau, Thomas K. Hansen, Kjeld Madsen, Paw Bloch, Florencio Z. Dorwald, Niels L. Johansen
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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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Publication number: 20130244931Abstract: Novel polypeptide derivatives having protracted profile of action.Type: ApplicationFiled: May 28, 2013Publication date: September 19, 2013Inventors: Jesper Lau, Thomas Kruse Hansen, Kjeld Madsen, Paw Bloch, Florencio Zaragoza Dorwald, Niels Langeland Johansen
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Patent number: 8536122Abstract: Protracted GLP-1 compounds and therapeutic uses thereof.Type: GrantFiled: March 5, 2012Date of Patent: September 17, 2013Assignee: Novo Nordisk A/SInventors: Jesper Lau, Florencio Zaragoza Doerwald, Paw Bloch, Thomas Kruse Hansen
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Publication number: 20130053315Abstract: Novel polypeptide derivatives having protracted profile of action.Type: ApplicationFiled: March 22, 2012Publication date: February 28, 2013Inventors: Jesper Lau, Thomas Kruse Hansen, Kjeld Madsen, Paw Bloch, Florencio Zaragoza Dorwald, Nils Langeland Johansen
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Publication number: 20130040884Abstract: Novel polypeptide derivatives having protracted profile of action.Type: ApplicationFiled: March 22, 2012Publication date: February 14, 2013Inventors: Jesper Lau, Thomas Kruse Hansen, Kjeld Madsen, Paw Bloch, Florencio Zaragoza Dorwald, Nils Langeland Johansen
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Publication number: 20120295847Abstract: Protracted GLP-1 compounds and therapeutic uses thereof.Type: ApplicationFiled: March 5, 2012Publication date: November 22, 2012Applicant: Novo Nordisk A/SInventors: Jesper Lau, Florencio Zaragoza Dörwald, Henrik Stephensen, Paw Bloch, Thomas Kruse Hansen, Kjeld Madsen
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Patent number: 8129343Abstract: Protracted GLP-1 compounds and therapeutic uses thereof.Type: GrantFiled: March 20, 2006Date of Patent: March 6, 2012Assignee: Novo Nordisk A/SInventors: Jesper Lau, Paw Bloch, Thomas Kruse Hansen
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Publication number: 20110301158Abstract: This invention relates to aryl carbonyl derivatives which are activators of glucokinase which may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.Type: ApplicationFiled: August 15, 2011Publication date: December 8, 2011Applicant: Novo Nordisk A/SInventors: Dharma Rao Polisetti, Janos Tibor Kodra, Jesper Lau, Paw Bloch, Maria Carmen Valcarce-Lopez, Niels Blume, Mustafa Guzel, Kalpathy Chidambareswaran Santhosh, Adnan M.M. Mjalli, Robert Carl Andrews, Govindan Subramanian, Michael Ankersen, Per Vedso, Anthony Murray, Lone Jeppesen
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Patent number: 8063081Abstract: This invention relates to aryl carbonyl derivatives which are activators of glucokinase which may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.Type: GrantFiled: October 31, 2007Date of Patent: November 22, 2011Assignee: Novo Nordisk A/SInventors: Dharma Rao Polisetti, Janos Tibor Kodra, Jesper Lau, Paw Bloch, Maria Carmen Valcarce Lopez, Niels Blume, Mustafa Guzel, Kalpathy Chidambareswaran Santhosh, Adnan M. M. Mjalli, Robert Carl Andrews, Govindan Subramanian, Michael Ankersen, Per Vedso, Anthony Murray, Lone Jeppesen
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Patent number: 7897628Abstract: This invention relates to aryl carbonyl derivatives which are activators of glucokinase which may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.Type: GrantFiled: October 31, 2007Date of Patent: March 1, 2011Assignee: Novo Nordisk A/SInventors: Dharma Rao Polisetti, Janos Tibor Kodra, Jesper Lau, Paw Bloch, Maria Carmen Valcarce Lopez, Niels Blume, Mustafa Guzel, Kalpathy Chidambareswaran Santhosh, Adnan M.M. Mjalli, Robert Carl Andrews, Govindan Subramanian, Michael Ankersen, Per Vedso, Anthony Murray, Lone Jeppesen
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Patent number: RE45670Abstract: This invention relates to aryl carbonyl derivatives which are activators of glucokinase which may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.Type: GrantFiled: December 20, 2013Date of Patent: September 15, 2015Assignee: NOVO NORDISK A/SInventors: Dharma Rao Polisetti, Janos Tibor Kodra, Jesper F. Lau, Paw Bloch, Mustafa Guzel, Santhosh Chidambareswaran Kalpathy, Adnan M. M. Mjalli, Robert Carl Andrews, Govindan Subramanian, Michael Ankersen, Per Vedso, Anthony Murray, Lone Jeppesen, Jesper Lau