Glucagon; Related Peptides Patents (Class 530/308)
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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: 8853159Abstract: The present invention provides fusion peptides having GLP-1 activity and enhanced stability in vivo, in particular resistancy to dipeptidyl peptidase IV. The fusion peptide comprises as component (I) N-terminally a GLP-1(7-35, 7-36 or 7-37) sequence and as component (II) C-terminally a peptide sequence of at least 9 amino acids or a functional fragment, variant or derivative thereof. Component (II) is preferably a full or partial version of IP2 (intervening peptide 2). A preferred embodiment comprises the sequence GLP-1(7-35, 36 or 37)/IP2/GLP-1(7-35, 36 or 37) or GLP-2. The fusion peptide may be produced in engineered cells or synthetically and may be used for preparing a medicament for treating various diseases or disorders, e.g. diabetes type 1 or 2, apoptosis related diseases or neurodegenerative disorders.Type: GrantFiled: May 29, 2012Date of Patent: October 7, 2014Assignee: Biocompatibles UK LtdInventors: Peter Geigle, Christine Wallrapp, Eric Thoenes
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Publication number: 20140296476Abstract: The present invention provides methods and compositions that permit controlled and prolonged drug release in vivo. The compounds are either prodrugs with tunable rates of release, or conjugates of the drug with macromolecules which exhibit tunable controlled rates of release.Type: ApplicationFiled: March 21, 2014Publication date: October 2, 2014Inventors: Daniel V. SANTI, Gary W. ASHLEY
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Patent number: 8846625Abstract: Analogs of glucagon-like peptide 2, a product of glucagon gene expression, have been identified as intestinal tissue growth factors. Their formulation as pharmaceutical, and therapeutic use in treating disorders of the small bowel, are described.Type: GrantFiled: March 11, 2013Date of Patent: September 30, 2014Assignee: 1149336 Ontario Inc.Inventors: Daniel J Drucker, Anna E. Crivici, Martin Sumner-Smith
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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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Publication number: 20140235535Abstract: Compounds are provided having inter alia good duration of action, high potency and/or convenient dosing regimens including oral administration, and reduced immunogenicity. The compounds are engineered polypeptides which incorporate an albumin binding domain in combination with one or more biologically active polypeptides. Also provided are pharmaceutical compositions and methods of treatment for diseases and disorders including obesity and overweight, diabetes, dyslipidemia, hyperlipidemia, Alzheimer's disease, fatty liver disease, Short Bowel Syndrome, Parkinson's disease, and cardiovascular disease.Type: ApplicationFiled: July 3, 2012Publication date: August 21, 2014Inventors: Mary Erickson, David C. Litzinger, Soumitra S. Ghosh, Zijian Guo, Manoj P. Samant, Abhinandini Sharma, Lala Mamedova, Esther Odile Levy, Caroline Ekblad
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Publication number: 20140228288Abstract: The present invention provides pharmaceutical compositions comprising at least one polypeptide having GLP-1 activity wherein an effective dose of said pharmaceutical composition comprises 15 mg, 30 mg, 50 mg or 100 mg of said polypeptide having GLP-1 activity. Also provided are methods of administering the pharmaceutical compositions of the invention.Type: ApplicationFiled: April 25, 2014Publication date: August 14, 2014Applicant: GlaxoSmithKline, LLCInventors: Mark A. BUSH, Murray W. Stewart, Yonghong Yang
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Publication number: 20140221280Abstract: Peptide containing sequence from both the GLP-1 peptide and glucagon peptide, compositions comprising said peptides and methods of using said peptides for the treatment and prevention of metabolic disorders, for example disorders of energy metabolism such as obesity or diabetes, are providedType: ApplicationFiled: July 4, 2011Publication date: August 7, 2014Applicant: IMPERIAL INNOVATIONS LIMITEDInventor: Stephen Robert Bloom
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Publication number: 20140221283Abstract: Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon.Type: ApplicationFiled: June 12, 2012Publication date: August 7, 2014Applicant: Indiana University Research and Technology CorporationInventors: Richard D. Dimarchi, David L. Smiley
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Publication number: 20140221281Abstract: The present invention relates to exendin-4 derivatives and their medical use, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, as well as reduction of excess food intake.Type: ApplicationFiled: December 20, 2013Publication date: August 7, 2014Applicant: SanofiInventors: Torsten HAACK, Michael Wagner, Bernd Henkel, Siegfried Stengelin, Andreas Evers, Martin Lorenz, Katrin Lorenz
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Publication number: 20140221282Abstract: There are provided compounds having two peptide hormones bound to a central water-soluble polymeric spacer and methods of use thereof.Type: ApplicationFiled: May 24, 2012Publication date: August 7, 2014Inventors: Chengzao Sun, Behrouz Bruce Forood
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Publication number: 20140212472Abstract: Methods of treating obesity, metabolic syndrome, hepatic and non-hepatic steatosis, and diabetes using a pentapeptide, LVKGRamide, derived from the C-terminus of Glucagon-Like Peptide 1 (GLP-1).Type: ApplicationFiled: July 5, 2012Publication date: July 31, 2014Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: Joel F. Habener, Eva Tomas-Falco
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Publication number: 20140213513Abstract: The present invention relates to exendin-4 derivatives and their medical use, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, as well as reduction of excess food intake.Type: ApplicationFiled: December 20, 2013Publication date: July 31, 2014Applicant: SanofiInventors: Torsten Haack, Michael Wagner, Bernd Henkel, Siegfried Stengelin, Andreas Evers, Martin Lorenz, Katrin Lorenz
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Patent number: 8790704Abstract: Nanoparticles having a core and a corona of ligands covalently linked to the core, wherein differing species of peptides are bound to the nanoparticles and incorporated into various dosage forms.Type: GrantFiled: June 8, 2012Date of Patent: July 29, 2014Assignees: Monosol RX, LLC, Midatech LimitedInventors: Phillip Williams, Thomas Rademacher, Alexander Mark Schobel, Eric Dadey
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Publication number: 20140206609Abstract: The present invention relates to exendin-4 derivatives and their medical use, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, as well as reduction of excess food intake.Type: ApplicationFiled: December 20, 2013Publication date: July 24, 2014Applicant: SanofiInventors: Torsten Haack, Michael Wagner, Bernd Henkel, Siegfried Stengelin, Andreas Evers, Martin Lorenz, Katrin Lorenz
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Publication number: 20140206608Abstract: The present invention relates to exendin-4 derivatives and their medical use, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, as well as reduction of excess food intake.Type: ApplicationFiled: December 20, 2013Publication date: July 24, 2014Applicant: SanofiInventors: Torsten Haack, Michael Wagner, Bernd Henkel, Siegfried Stengelin, Andreas Evers, Martin Lorenz, Katrin Lorenz
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Publication number: 20140206836Abstract: There is provided a novel series of synthetic analogs of hGH-RH(1-29)NH2 (SEQ ID NO: 1) and hGH-RH(1-30)NH2. Of particular interest are those carrying PhAc, N-Me-Aib, Dca, Ac-Ada, Fer, Ac-Amc, Me-NH-Sub, PhAc-Ada, Ac-Ada-D-Phe, Ac-Ada-Phe, Dca-Ada, Dca-Amc, Nac-Ada, Ada-Ada, or CH3—(CH2)10—CO-Ada, at the N-Terminus and ?-Ala, Amc, Apa, Ada, AE2A, AE4P, ?-Lys(?-NH2), Agm, Lys(Oct) or Ahx, at the C-terminus. These analogs inhibit the release of growth hormone from the pituitary in mammals as well as inhibit the proliferation of human cancers, and inhibit the hyperplastic and benign proliferative disorders of various organs, through a direct effect on the cancerous and non-malignant cells. The stronger inhibitory potencies of the new analogs, as compared to previously described ones, result from replacement of various amino acids.Type: ApplicationFiled: February 19, 2014Publication date: July 24, 2014Applicants: U.S.A., represented by the Department of Veterans Affairs, University of MiamiInventors: Andrew V. SCHALLY, Marta ZARANDI, Jozsef L. VARGA, Ren Zhi CAI
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Publication number: 20140206607Abstract: Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon.Type: ApplicationFiled: June 12, 2012Publication date: July 24, 2014Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATIONInventors: Richard D. Dimarchi, David L. Smiley, Bin S. Yang
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Patent number: 8772232Abstract: Novel protracted exendin-4 compounds and therapeutic uses thereof.Type: GrantFiled: August 18, 2011Date of Patent: July 8, 2014Assignee: Novo Nordisk A/SInventors: Jesper Lau, Thomas Kruse Hansen
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Publication number: 20140187490Abstract: A method of treating functional dyspepsia and/or irritable bowel syndrome in mammals in need of treatment is disclosed herein. The method comprises administering to the mammal a formulation by inhalation, wherein the formulation avoids first pass metabolism of the active ingredient. The method comprises administering a formulation by pulmonary inhalation comprising a diketopiperazine and a glucagon-like peptide (GLP-1), analog, ROSE-010.Type: ApplicationFiled: December 23, 2013Publication date: July 3, 2014Applicants: Rose Pharma A/S, MannKind CorporationInventors: Peter Richardson, Edna Kenny, Per Hellstrom, Marshall L. Grant, Grayson W. Stowell, Scott Daniels, Anthony Smithson, Stephanie Greene
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Patent number: 8759295Abstract: Peptide-peptidase inhibitor conjugate molecules are disclosed. These conjugate molecules are useful as agents for the treatment and prevention of metabolic and cardiovascular diseases, disorders, and conditions. Such diseases, conditions and disorders include, but are not limited to, hypertension, dyslipidemia, cardiovascular disease, eating disorders, insulin-resistance, obesity, and diabetes mellitus of any kind, and other diabetes-related disorders.Type: GrantFiled: May 21, 2010Date of Patent: June 24, 2014Assignees: Amylin Pharmaceuticals, LLC, Astrazeneca Pharmaceuticals LPInventors: Soumitra S. Ghosh, Josue Alfaro-Lopez, Lawrence J. D'Souza, Odile Esther Levy, Qing Lin, Christopher J. Soares
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Publication number: 20140171364Abstract: The delivery of biopharmaceutical and other therapeutic agents parenterally to an animal via a minimally invasive, low pain administration is provided. The agents are delivered to the patient via, e.g., the epidermal, dermal, or subcutaneous layer of the skin in a concentrated form of injectable glucagon that is dissolved in a pharmaceutically acceptable carrier.Type: ApplicationFiled: February 21, 2014Publication date: June 19, 2014Inventors: Steven Prestrelski, Wei-Jie Fang, John F. Carpenter, John Kinzell
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Publication number: 20140162943Abstract: The disclosure provides N-terminus conformationally constrained compounds, which may comprise peptide mimetics and/or amino acid substitutions, which may be used in peptides, such as GLP-1 receptor agonist compounds, to induce ?-turn secondary structure at the N-terminus. The N-terminus conformationally constrained compounds may be used for research purposes; to produce GLP-1 receptor agonist compounds having improved GLP-1 receptor binding activity, enzymatic stability, or in vivo glucose lowering activity; and to develop GLP-1 receptor agonist compounds which have fewer amino acid residues. The disclosure also provides GLP-1 receptor agonist compounds, such as exendins, exendin analogs, GLP-1(7-37), GLP-1(7-37) analogs, comprising the N-terminus conformationally constrained compounds. The compounds are useful for treating various diseases, such as diabetes and obesity. The disclosure also provides methods for chemically synthesizing the N-terminus conformationally constrained compounds.Type: ApplicationFiled: January 28, 2014Publication date: June 12, 2014Applicants: ASTRAZENECA PHARMACEUTICALS, LP, AMYLIN PHARMACEUTICALS, LLCInventors: Josue ALFARO-LOPEZ, Abhinandini SHARMA, Soumitra S. GHOSH
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Patent number: 8748376Abstract: Stable pharmaceutical composition comprising insulinotropic peptide.Type: GrantFiled: December 21, 2009Date of Patent: June 10, 2014Assignee: Novo Nordisk A/SInventors: Svend Ludvigsen, Morten Schlein, Tine Elisabeth Gottschalk Bøving, Claude Bonde, Anne-Mette Lilleøre, Dorthe Kot Engelund, Bjarne Rønfeldt Nielsen
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Publication number: 20140154214Abstract: GLP-2 analogues are disclosed which comprise one of more substitutions as compared to h[Gly2]GLP-2 and which may have the property of an increased small intestine/colon and stomach/colon selectivity. More particularly, preferred GLP-2 analogues disclosed herein comprise substitutions at one or more of positions 11, 16, 20, 24 and/or 28 of the wild-type GLP-2 sequence, optionally in combination with further substitutions at position 2 and one or more of positions 3, 5, 7, and 10, and/or a deletion of one or more of amino acids 31 to 33 and/or the addition of a N-terminal or C-terminal stabilizing peptide sequence. The analogues are particularly useful for the prophylaxis or treatment of stomach and bowel-related disorders and for ameliorating side effects of chemotherapy.Type: ApplicationFiled: February 4, 2014Publication date: June 5, 2014Inventors: Bjarne Due LARSEN, Yvette Miata Petersen
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Publication number: 20140142037Abstract: The invention discloses site-specific mono-PEGylated Exendin analogs in which any amino groups can be mono-PEGylated as well as their preparation method and use. The method of the present invention adopts a more stable protective group Dde (N-?-1-(4,4-dimethyl-2,6-dioxo-cyclohexylene)) to avoid multi-PEGylated side reactions rendered by unstable protecting groups, achieving mono-PEGylated Exendin analogs at a high recovery with a low reaction molar ratio.Type: ApplicationFiled: September 30, 2013Publication date: May 22, 2014Applicant: SHANGHAI HUAYI BIO-LAB CO., LTD.Inventor: Peng YUE
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Patent number: 8729017Abstract: Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon.Type: GrantFiled: June 12, 2012Date of Patent: May 20, 2014Assignee: Indiana University Research and Technology CorporationInventors: Richard D. DiMarchi, David L. Smiley, Bin Yang
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Publication number: 20140121159Abstract: The present disclosure provides inter alia conjugates of formula (I): wherein n, R1, R2, Rx, Z, X, Y and Z are as defined herein. A conjugate of formula (I) can also be converted to a conjugate of formulae (II) or (III) as described herein. Without limitation, the conjugates can be used to make controlled release materials and chemical sensors.Type: ApplicationFiled: December 3, 2013Publication date: May 1, 2014Applicant: SmartCells, Inc.Inventors: Todd C. Zion, Thomas M. Lancaster
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Publication number: 20140121154Abstract: This invention relates to novel compositions comprising analogs of glucagon, wherein the analog comprises an ?-amino acid and at least one ?-amino acid. Administration of the compositions may be used for effecting treatment or prevention of a plurality of disease states caused by dysfunctional biochemical or biological pathways, including diabetes and other metabolic disorders. The compositions and methods of this invention are particularly useful to identify novel therapeutic modulators of in-vivo receptor activity with extended half-lives and relevant bioactivity as compared to the naturally translated polypeptides upon which the analogs are derived.Type: ApplicationFiled: April 5, 2012Publication date: May 1, 2014Applicant: Longevity Biotech, Inc.Inventors: Scott Shandler, Samuel H. Gellman
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Use of tris(hydroxymethyl) aminomethane for the stabilization of peptides, polypeptides and proteins
Patent number: 8710181Abstract: The present invention is directed to a method for reducing the onset or incidence of gelation/fibrillation/aggregation during the up- and down-stream processing and purification of peptides, polypeptides and proteins analogs and/or derivatives thereof, including Glucagon-Like Peptides (GLPs). More particularly, the present invention relates to methods of processing and purifying such peptides, polypeptides and proteins in the presence of tris(hydroxymethyl)aminomethane.Type: GrantFiled: August 26, 2005Date of Patent: April 29, 2014Assignee: Novo Nordisk A/SInventors: Ingun Christiansen, Arne Staby -
Patent number: 8703907Abstract: The invention relates to compositions that comprise dendrimers useful in medical and veterinary applications that provide controlled release of drugs, such as peptides, nucleic acids and small molecules. The drugs are covalently coupled to the dendrimer through a linkage that releases the drug or a prodrug through controlled beta elimination.Type: GrantFiled: May 5, 2011Date of Patent: April 22, 2014Assignee: Prolynx LLCInventors: Gary Ashley, Daniel V. Santi
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Publication number: 20140107019Abstract: Compounds are provided having inter alia good duration of action, high potency and/or convenient dosing regimens including oral administration. The compounds are engineered polypeptides which incorporate an albumin binding domain in combination with one or more biologically active polypeptides. Also provided are pharmaceutical compositions and methods of treatment for diseases and disorders including obesity and overweight, diabetes, dyslipidemia, hyperlipidemia, Alzheimer's disease, fatty liver disease, short bowel syndrome, Parkinson's disease, cardiovascular disease, and other and disorders of the central nervous system.Type: ApplicationFiled: March 28, 2013Publication date: April 17, 2014Applicants: ASTRAZENECA PHARMACEUTICALS LP, AMYLIN PHARMACEUTICALS, LLCInventors: Amylin Pharmaceuticals, LLC, Astrazeneca Pharmaceuticals LP
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Publication number: 20140107021Abstract: Provided herein are peptide combinations comprising a GIP agonist peptide and a glucagon antagonist peptide. In some embodiments, the peptide combination is provided as a composition, e.g., a pharmaceutical composition, while in other embodiments, the peptide combination is provided as a kit. In yet other embodiments, the peptide combination is provided as a conjugate, e.g., a fusion peptide, a heterodimer. In specific aspects, the GIP agonist peptide is an analog of native human glucagon. In specific aspects, the glucagon antagonist peptide is an analog of native human glucagon. In some embodiments, the GIP agonist peptide is covalently attached to the glucagon antagonist peptide via a linker. Method of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the peptide compositions described herein are further provided.Type: ApplicationFiled: September 13, 2013Publication date: April 17, 2014Applicant: Indiana University Research and Technology CorporationInventors: Richard D. DiMARCHI, Tao MA
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Patent number: 8697648Abstract: The 30 amino acid peptide GLP-1 has been integrated into the stable host protein human calbindin D9k. The fusion protein binds to GLP-1R. The fusion protein agents can be useful for both diabetes treatment and GLP-1R receptor targeting MR imaging. The fusion protein comprises a first peptide that selectively binds to a site of a target cell and linked to a second peptide, where the fusion protein is more stable than the first peptide alone and may further comprise a detectable label. The first peptide of the fusion protein may be glucagon-like peptide-1 (GLP-1), glucagon-like peptide-1 (GLP-1)(7-36), or glucagon-like peptide-1 (GLP-1) (9-36), or a conservative variant thereof.Type: GrantFiled: October 20, 2010Date of Patent: April 15, 2014Assignee: Georgia State University Research Foundation, Inc.Inventors: Zhi-Ren Liu, Jie Yang, Bing Xu, Wangda Zhou, Shenghui Xue
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Publication number: 20140100156Abstract: The present invention relates to exendin-4 derivatives and their medical use, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, as well as reduction of excess food intake.Type: ApplicationFiled: October 9, 2013Publication date: April 10, 2014Applicant: SANOFIInventors: Torsten HAACK, Michael WAGNER, Bernd HENKEL, Siegfried STENGELIN, Andreas EVERS, Martin BOSSART
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Patent number: 8680315Abstract: The present invention provides methods and compositions that permit controlled and prolonged drug release in vivo. The compounds are either prodrugs with tunable rates of release, or conjugates of the drug with macromolecules which exhibit tunable controlled rates of release.Type: GrantFiled: June 26, 2009Date of Patent: March 25, 2014Assignee: Prolynx, LLCInventors: Daniel V. Santi, Gary W. Ashley
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Publication number: 20140080757Abstract: The invention provides materials and methods for the treatment of obesity and excess weight, diabetes, and other associated metabolic disorders. In particular, the invention provides novel glucagon analogue peptides effective in such methods. The peptides may mediate their effect by having increased selectivity for the GLP-1 receptor as compared to human glucagon.Type: ApplicationFiled: September 17, 2013Publication date: March 20, 2014Applicants: Boehringer Ingelheim International GmbH, Zealand Pharma A/SInventors: Jakob Lind TOLBORG, Keld Fosgerau, Pia Nørregaard, Rasmus Just, Ditte Riber, Dieter Wolfgang Hamprecht, Robert Augustin, Leo Thomas
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Patent number: 8669228Abstract: Modified glucagon peptides are disclosed having improved solubility while retaining glucagon agonist activity. The glycogen peptides have been modified by substitution of native amino acids with, and/or addition of, charged amino acids to the carboxy terminus of the peptide. The modified glucagon agonists can be further modified by pegylation, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 20, SEQ ID NO: 21, SEQ ID NO: 23, or both to further enhance the solubility of the glucagon agonist analogs.Type: GrantFiled: January 3, 2008Date of Patent: March 11, 2014Assignee: Indiana University Research and Technology CorporationInventors: Richard D. Dimarchi, Maria Dimarchi, Joseph Chabenne
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Publication number: 20140056812Abstract: The present disclosure provides compositions and methods based on peptide-detectable agent conjugates that are useful for imaging beta cell mass.Type: ApplicationFiled: June 27, 2011Publication date: February 27, 2014Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: Ralph Weissleder, Thomas Reiner, Edmund J. Keliher
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Publication number: 20140038891Abstract: Novel modified exendins and exendin agonists having an exendin or exendin agonist linked to one or more polyethylene glycol polymers, for example, and related formulations and dosages and methods of administration thereof are provided. These modified exendins and exendin agonists, compositions and methods are useful in treating diabetes and conditions that would be benefited by lowering plasma glucose or delaying and/or slowing gastric emptying or inhibiting food intake.Type: ApplicationFiled: May 17, 2013Publication date: February 6, 2014Applicants: AstraZeneca Pharmaceuticals LP, Amylin Pharmaceuticals, LLCInventors: Kathryn S. Prickett, Andrew A. Young
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Patent number: 8642544Abstract: The disclosure provides N-terminus conformationally constrained compounds, which may comprise peptide mimetics and/or amino acid substitutions, which may be used in peptides, such as GLP-1 receptor agonist compounds, to induce a ?-turn secondary structure at the N-terminus. The N-terminus conformationally constrained compounds may be used for research purposes; to produce GLP-1 receptor agonist compounds having improved GLP-1 receptor binding activity, enzymatic stability, or in vivo glucose lowering activity; and to develop GLP-1 receptor agonist compounds which have fewer amino acid residues. The disclosure also provides GLP-1 receptor agonist compounds, such as exendins, exendin analogs, GLP-1 (7-37), GLP-1 (7-37) analogs, comprising the N-terminus conformationally constrained compounds. The compounds are useful for treating various diseases, such as diabetes and obesity. The disclosure also provides methods for chemically synthesizing the N-terminus conformationally constrained compounds.Type: GrantFiled: March 26, 2010Date of Patent: February 4, 2014Assignees: Amylin Pharmaceuticals, LLC, AstraZeneca Pharmaceuticals LPInventors: Josue Alfaro-Lopez, Abhinandini Sharma, Soumitra S. Ghosh
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Patent number: 8642727Abstract: GLP-2 analogues are disclosed which comprise one of more substitutions as compared to h[Gly2]GLP-2 and which may have the property of an increased small intestine/colon and stomach/colon selectivity. More particularly, preferred GLP-2 analogues disclosed herein comprise substitutions at one or more of positions 11, 16, 20, 24 and/or 28 of the wild-type GLP-2 sequence, optionally in combination with further substitutions at position 2 and one or more of positions 3, 5, 7, and 10, and/or a deletion of one or more of amino acids 31 to 33 and/or the addition of a N-terminal or C-terminal stabilizing peptide sequence. The analogues are particularly useful for the prophylaxis or treatment of stomach and bowel-related disorders and for ameliorating side effects of chemotherapy.Type: GrantFiled: November 8, 2007Date of Patent: February 4, 2014Assignee: Zealand Pharma A/SInventors: Bjarne Due Larsen, Yvette Miata Petersen
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Patent number: 8642540Abstract: The invention provides materials and methods for promoting weight loss or preventing weight gain, and in the treatment of diabetes, metablic syndrome and associated disorders. In particular, the invention provides novel glucagon analogue peptides effective in such methods. The peptides may mediate their effect by having increased selectivity for the GLP-1 receptor as compared to human glucagon.Type: GrantFiled: December 15, 2008Date of Patent: February 4, 2014Assignee: Zealand Pharma A/SInventors: Eddi Meier, Ditte Riber, Marie Skovgaard, Bjarne Due Larsen, Jens Rosengren Daugaard
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Patent number: 8642541Abstract: The invention provides materials and methods for promoting weight loss or preventing weight gain, and in the treatment of diabetes, metabolic syndrome and associated disorders. In particular, the invention provides novel glucagon analogue peptides effective in such methods. The peptides may mediate their effect by having increased selectivity for the GLP-1 receptor as compared to human glucagon.Type: GrantFiled: December 15, 2008Date of Patent: February 4, 2014Assignee: Zealand Pharma A/SInventors: Eddi Meier, Ditte Riber, Marie Skovgaard, Bjarne Due Larsen, Jens Rosengren Daugaard, Trine Skovlund Ryge Neerup
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Publication number: 20140031278Abstract: The present invention relates to novel glucagon peptides with improved stability and 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 glucagon peptides 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 28, 2012Publication date: January 30, 2014Applicant: NOVO NORDISK A/SInventors: Jesper F. Lau, Thomas Kruse, Henning Thoegersen, Thomas Nylandsted Krogh, Ulrich Sensfuss
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Publication number: 20140024585Abstract: A composition containing at least two of the following active substances A, B, C, wherein: A=at least one hormone stimulating the production of cAMP; B=at least one substance inhibiting the degradation of a cyclic nucleotide; C=at least one hormone stimulating the production of cGMP.Type: ApplicationFiled: April 11, 2011Publication date: January 23, 2014Inventors: Wolf Georg Forssmann, Rudolf Richter, Knut Adermann, Markus Meyer
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Publication number: 20140011738Abstract: Provided herein are glucagon analogs which exhibit potent activity at the GIP receptor, and, as such are contemplated for use in treating diabetes and obesity. In exemplary embodiments, the glucagon analog of the present disclosures exhibit an EC50 at the GIP receptor which is within the nanomolar or picomolar range.Type: ApplicationFiled: June 18, 2013Publication date: January 9, 2014Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATIONInventor: Richard D. DiMARCHI
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Publication number: 20130345129Abstract: The present invention relates to an oligosaccharide chain added GLP-1 peptide that has higher stability in blood than that of GLP-1 and, preferably, exhibits higher activity of controlling blood-sugar levels than that of GLP-1. The present invention relates to an oligosaccharide chain added GLP-1 peptide having GLP-1 activity, wherein at least one amino acid is substituted with an oligosaccharide chain added amino acid, in: (a) GLP-1; (b) a peptide having the amino acid sequence of GLP-1 with deletion, substitution or addition of one or several amino acids; or (c) a GLP-1 analog.Type: ApplicationFiled: June 7, 2013Publication date: December 26, 2013Applicant: GLYTECH, INC.Inventors: YASUHIRO KAJIHARA, TAKASHI TSUJI, IZUMI SAKAMOTO, YURI NAMBU, KAZUHIRO FUKAE, KATSUNARI TEZUKA, HIROAKI ASAI
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Patent number: 8614181Abstract: Method for increasing the shelf-life of a pharmaceutical composition for parenteral administration comprising a glucagon-like peptide which is prepared from a peptide product that has been subjected to treatment at a pH above neutral pH.Type: GrantFiled: November 5, 2009Date of Patent: December 24, 2013Assignee: Novo Nordisk A/SInventors: Claus Juul-Mortensen, Dorte Kot Engelund
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Patent number: 8614182Abstract: This invention discloses GLP-1 analogues and their pharmaceutical salts, wherein the GLP-1 analogue comprises an amino acid sequence of general formula (I), wherein Lys represents a modified lysine with a lipophilic acid. The GLP-1 analogues provided by this invention have the function of human GLP-1, and a longer half-life in vivo compared with the human GLP-1. Uses of such compounds and compositions include treating non-insulin-dependent diabetes, insulin-dependent diabetes, and obesity.Type: GrantFiled: January 31, 2012Date of Patent: December 24, 2013Assignee: Jiangsu Hansoh Pharmaceuticals Co., Ltd.Inventors: Yali Wang, Aifeng Lü, Changan Sun, Hengli Yuan