Glucagon, Glucagon-like Peptide (e.g., Glp-1, Glp-2, Etc.) Or Derivative Patents (Class 514/11.7)
  • Publication number: 20140294977
    Abstract: The present disclosure is directed to a method of making a composition by combining a vehicle, e.g., a single phase vehicle, and an insoluble component comprising a beneficial agent, and sterilizing the composition using ionizing radiation prior to use, wherein the beneficial agent is stable following exposure to a sterilizing dose of ionizing radiation. Related compositions and methods are provided.
    Type: Application
    Filed: November 21, 2012
    Publication date: October 2, 2014
    Applicant: DURECT CORPORATION
    Inventors: Michael Sekar, Su Il Yum, Felix Theeuwes, William van Osdol
  • Publication number: 20140296131
    Abstract: 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: Application
    Filed: June 9, 2014
    Publication date: October 2, 2014
    Applicant: NOVO NORDISK A/S
    Inventors: Jane Spetzler, Lauge Schaeffer, Jesper Lau, Janos T. Kodra, Kjeld Madsen, Patrick W. Garibay, Jacob Kofoed, Steffen Reedtz-Runge, Henning Thoegersen, Ingrid Pettersson
  • Patent number: 8846625
    Abstract: 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: Grant
    Filed: March 11, 2013
    Date of Patent: September 30, 2014
    Assignee: 1149336 Ontario Inc.
    Inventors: Daniel J Drucker, Anna E. Crivici, Martin Sumner-Smith
  • Patent number: 8846618
    Abstract: Pharmaceutical formulations of GLP-1 compounds and methods for preparation thereof.
    Type: Grant
    Filed: May 24, 2010
    Date of Patent: September 30, 2014
    Assignee: Novo Nordisk A/S
    Inventors: James M. Flink, Silke Møller Larsen, Simon Bjerregaard Jensen, Dorthe Kot Engelund
  • Publication number: 20140287998
    Abstract: Glucagon is formulated in hydrochloric acid buffered, mannitol containing formulations that can be readily lyophilized and rapidly reconstituted for use in dual chamber cartridges and auto-injector device technology.
    Type: Application
    Filed: December 7, 2012
    Publication date: September 25, 2014
    Inventors: Richard W. Rylander, JR., Solomon Tse
  • Publication number: 20140271888
    Abstract: Disclosed herein are diketopiperazine microparticles having a specific surface area of less than about 67 m2/g. The diketopiperazine microparticle can be fumaryl diketopiperazine and can comprise a drug such as insulin.
    Type: Application
    Filed: April 11, 2014
    Publication date: September 18, 2014
    Applicant: MannKind Corporation
    Inventors: Marshall L. Grant, Grayson W. Stowell, Paul Menkin
  • Patent number: 8815802
    Abstract: 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: Grant
    Filed: December 16, 2010
    Date of Patent: August 26, 2014
    Assignee: Novo Nordisk A/S
    Inventors: Christoph Kalthoff, Jesper Lau, Jane Spetzler, Patrick William Garibay, Jacob Kofoed, Lars Linderoth
  • Publication number: 20140235535
    Abstract: 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: Application
    Filed: July 3, 2012
    Publication date: August 21, 2014
    Inventors: Mary Erickson, David C. Litzinger, Soumitra S. Ghosh, Zijian Guo, Manoj P. Samant, Abhinandini Sharma, Lala Mamedova, Esther Odile Levy, Caroline Ekblad
  • Publication number: 20140227359
    Abstract: Drug delivery systems have been developed based on the formation of diketopiperazine carboxylate salts and microparticles containing the same. The systems may further comprise a bioactive agent. Related methods for making and using the biologically active agent delivery compositions are also provided. In certain embodiments, the pharmaceutically acceptable salts described can be formed by removal of solvent by methods including distillation, evaporation, spray drying or lyophilization.
    Type: Application
    Filed: January 8, 2014
    Publication date: August 14, 2014
    Applicant: MannKind Corporation
    Inventors: Andrea Leone-Bay, Destardi Moye-Sherman, Bryan R. Wilson
  • Patent number: 8802622
    Abstract: The invention provides a powdered composition for nasal administration, comprising a physiologically active peptide and cellulose acetate as the base, and having excellent nasal absorption for physiologically active peptides.
    Type: Grant
    Filed: March 18, 2011
    Date of Patent: August 12, 2014
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Masaru Matsumoto, Shuji Takeda, Kyohei Nobori
  • Publication number: 20140221283
    Abstract: Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon.
    Type: Application
    Filed: June 12, 2012
    Publication date: August 7, 2014
    Applicant: Indiana University Research and Technology Corporation
    Inventors: Richard D. Dimarchi, David L. Smiley
  • Publication number: 20140221282
    Abstract: There are provided compounds having two peptide hormones bound to a central water-soluble polymeric spacer and methods of use thereof.
    Type: Application
    Filed: May 24, 2012
    Publication date: August 7, 2014
    Inventors: Chengzao Sun, Behrouz Bruce Forood
  • Publication number: 20140221280
    Abstract: 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 provided
    Type: Application
    Filed: July 4, 2011
    Publication date: August 7, 2014
    Applicant: IMPERIAL INNOVATIONS LIMITED
    Inventor: Stephen Robert Bloom
  • Publication number: 20140220134
    Abstract: The disclosure provides methods for treating diabetes, treating overweight, treating obesity, reducing body weight, treating cardiovascular diseases, treating fatty liver diseases, treating gastrointestinal diseases, and treating neurodegenerative diseases through the once monthly administration of pharmaceutical formulations containing a non-aqueous carrier and GLP-1 receptor agonists that provides therapeutically effective plasma concentration levels of the GLP-1 receptor agonists over the course of a month.
    Type: Application
    Filed: June 21, 2012
    Publication date: August 7, 2014
    Applicants: Astrazeneca Pharamceuticals LP, Amylin Pharmaceuticals LLC
    Inventors: Matthew L. Zierhut, Brenda B. Cirincione
  • Publication number: 20140221281
    Abstract: 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: Application
    Filed: December 20, 2013
    Publication date: August 7, 2014
    Applicant: Sanofi
    Inventors: Torsten HAACK, Michael Wagner, Bernd Henkel, Siegfried Stengelin, Andreas Evers, Martin Lorenz, Katrin Lorenz
  • Publication number: 20140213518
    Abstract: The invention relates to glucagon-related peptides and their use for the prevention or treatment of disorders involving the large intestine. In particular, it has now been demonstrated that GLP-2 and peptidic agonists of GLP-2 can cause proliferation of the tissue of large intestine. Thus, the invention provides methods of proliferating the large intestine in a subject in need thereof. Further, the methods of the invention are useful to treat or prevent inflammatory conditions of the large intestine, including inflammatory bowel diseases.
    Type: Application
    Filed: November 5, 2013
    Publication date: July 31, 2014
    Applicant: 1149336 Ontario Inc.
    Inventor: Daniel J. Drucker
  • Publication number: 20140213513
    Abstract: 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: Application
    Filed: December 20, 2013
    Publication date: July 31, 2014
    Applicant: Sanofi
    Inventors: Torsten Haack, Michael Wagner, Bernd Henkel, Siegfried Stengelin, Andreas Evers, Martin Lorenz, Katrin Lorenz
  • Publication number: 20140212472
    Abstract: 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: Application
    Filed: July 5, 2012
    Publication date: July 31, 2014
    Applicant: THE GENERAL HOSPITAL CORPORATION
    Inventors: Joel F. Habener, Eva Tomas-Falco
  • Publication number: 20140206609
    Abstract: 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: Application
    Filed: December 20, 2013
    Publication date: July 24, 2014
    Applicant: Sanofi
    Inventors: Torsten Haack, Michael Wagner, Bernd Henkel, Siegfried Stengelin, Andreas Evers, Martin Lorenz, Katrin Lorenz
  • Publication number: 20140206608
    Abstract: 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: Application
    Filed: December 20, 2013
    Publication date: July 24, 2014
    Applicant: Sanofi
    Inventors: Torsten Haack, Michael Wagner, Bernd Henkel, Siegfried Stengelin, Andreas Evers, Martin Lorenz, Katrin Lorenz
  • Publication number: 20140206616
    Abstract: Disclosed is a sustained release lipid pre-concentrate, comprising: a) a sorbitan unsaturated fatty acid ester having a polar head with at least two or more —OH (hydroxyl) groups; b) a phospholipid; and c) a liquid crystal hardener, free of an ionizable group, having a hydrophobic moiety of 15 to 40 carbon atoms with a triacyl group or a carbon ring structure. The lipid pre-concentrate exists as a liquid phase in the absence of aqueous fluid and forms into a liquid crystal in the presence of aqueous fluid. Also, a pharmaceutical composition further comprising a pharmacologically active ingredient plus the pre-concentrate is provided.
    Type: Application
    Filed: August 28, 2012
    Publication date: July 24, 2014
    Applicant: Chong Kun Dang Pharmaceutical Corp.
    Inventors: Jin Young Ko, Ji Yeon Kim, So Hyun Park, Sung Won An, Min Hyo Ki
  • Publication number: 20140206607
    Abstract: Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon.
    Type: Application
    Filed: June 12, 2012
    Publication date: July 24, 2014
    Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
    Inventors: Richard D. Dimarchi, David L. Smiley, Bin S. Yang
  • Publication number: 20140206615
    Abstract: Methods and uses for the treatment and prevention of cardiac and cardiovascular diseases comprising administration of a GLP-1 agonist.
    Type: Application
    Filed: March 28, 2014
    Publication date: July 24, 2014
    Applicant: NOVO NORDISK A/S
    Inventors: Liselotte Bjerre Knudsen, Bidda Charlotte Rolin, Richard David Carr, Johan Selmer, Jens Larsen, Bodil Elbrond, Lars Bo Nielsen, Christina Christoffersen
  • Publication number: 20140200183
    Abstract: Compositions of the invention, including compounds that bind to a receptor for a glucagon-like peptide-1, an incretin, a glucagon-like peptide-1 (GLP-1), an exendin, or an agonist, an analog (preferably an agonist analog), a derivative, or a variant of any of aforementioned compounds, are used in the prevention and treatment of arrhythmias associated with cardiac ischemia, cardiac ischemia-perfusion and/or congestive heart failure. The invention relates to both the method and compositions for such treatment.
    Type: Application
    Filed: March 21, 2014
    Publication date: July 17, 2014
    Applicants: ASTRAZENECA PHARMACEUTICALS LP, AMYLIN PHARMACEUTICALS, LLC
    Inventors: David R. HATHAWAY, Alain D. BARON
  • Patent number: 8778403
    Abstract: Disclosed herein are diketopiperazine microparticles having a specific surface area of less than about 67 m2/g. The diketopiperazine microparticle can be fumaryl diketopiperazine and can comprise a drug such as insulin.
    Type: Grant
    Filed: September 3, 2013
    Date of Patent: July 15, 2014
    Assignee: Mannkind Corporation
    Inventors: Marshall L. Grant, Grayson W. Stowell, Paul Menkin
  • Publication number: 20140193365
    Abstract: The present disclosure provides a biodegradable drug delivery composition including a vehicle and an insoluble component comprising beneficial agent dispersed in the vehicle. Typically, the composition is not an emulsion, but has a low viscosity and further provides for minimized initial burst and sustained release of the beneficial agent over time. Also provided, are kits including the biodegradable drug delivery composition or components thereof, as well as methods of making and using the biodegradable drug delivery composition.
    Type: Application
    Filed: December 10, 2013
    Publication date: July 10, 2014
    Applicant: Durect Corporation
    Inventors: William W. van Osdol, Su Il Yum, Felix Theeuwes, Michael Sekar, John W. Gibson, Keith E. Branham, Huey-Ching Su
  • Publication number: 20140187489
    Abstract: The present invention provides a composition comprising or consisting of components (a) (i) at least one mono-alkanoyl glycerol ester, wherein alkanoyl is selected from C4 to C21 alkanoyl, preferably from octanoyl and decanoyl; and (b) (i) at least one compound selected from cholesterol, phosphatidyl cholines and phosphatidyl glycerols, wherein the acyl moieties of the phosphatidyl moieties are independently selected from C6 to C21 alkanoyl and C6 to C21 alkenoyl.
    Type: Application
    Filed: May 25, 2012
    Publication date: July 3, 2014
    Applicant: ARISGEN SA
    Inventors: Paolo Botti, Sylvie Tchertchian
  • Publication number: 20140187490
    Abstract: 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: Application
    Filed: December 23, 2013
    Publication date: July 3, 2014
    Applicants: Rose Pharma A/S, MannKind Corporation
    Inventors: Peter Richardson, Edna Kenny, Per Hellstrom, Marshall L. Grant, Grayson W. Stowell, Scott Daniels, Anthony Smithson, Stephanie Greene
  • Patent number: 8765668
    Abstract: The present invention relates to process to prepare ?-aminobutyryl compounds having ?-amino acid core structural moieties and optionally having ?-phenyl and/or heterocyclic structural moieties. Such compounds are useful as key structure framework of modern drug chemistry.
    Type: Grant
    Filed: June 3, 2011
    Date of Patent: July 1, 2014
    Assignee: Lek Pharmaceuticals D.D.
    Inventors: Damjan Sterk, Matjaz Ustar, Marko Zlicar
  • Patent number: 8765669
    Abstract: Oligosaccharide chain added GLP-1 peptides are more stable in blood and more active in controlling blood-sugar levels than GLP-1 peptides without added oligosaccharides. Oligosaccharide chain added GLP-1 peptides having GLP-1 activity include at least one or at least two amino acids each substituted with an oligosaccharide chain added amino acid in GLP-1; a peptide having the amino acid sequence of GLP-1 with deletion, substitution or addition of one or several amino acids; or a GLP-1 analog. Oligosaccharide chain added GLP-1 peptides with at least one amino acid substituted with an oligosaccharide chain added amino acid include an oligosaccharide chain with oligo hyaluronic acid. Oligosaccharide chain added amino acids include oligosaccharide chains attached to amino acids via linkers.
    Type: Grant
    Filed: June 15, 2009
    Date of Patent: July 1, 2014
    Assignee: Glytech, Inc.
    Inventors: Yasuhiro Kajihara, Takashi Tsuji, Izumi Sakamoto, Yuri Nambu, Naohiro Hayashi, Kazuyuki Ishii, Kazuhiro Fukae, Katsunari Tezuka, Hiroaki Asai
  • Patent number: 8759290
    Abstract: The present invention relates to the field of metabolic compound conjugates, methods of forming said conjugates and uses of these conjugates in the treatment of diabetes and conditions related to this condition. The metabolic compound conjugates of this invention include a metabolic peptide having a glucagon-like peptide (GLP-1) receptor binding motif for action on a GLP-1 receptor and at least one oligomer conjugation site for binding with at least one oligomer, wherein the oligomer includes a polyethylene glycol moiety (PEG), and/or alkyl moiety.
    Type: Grant
    Filed: October 18, 2006
    Date of Patent: June 24, 2014
    Assignee: Biocon Limited
    Inventor: Kenneth D. James
  • Patent number: 8759291
    Abstract: Methods for increasing urine flow are disclosed, comprising administration of an effective amount of GLP-1, an exendin, or an exendin or GLP-1 agonist. Methods for increasing urinary sodium excretion and decreasing urinary potassium concentration are also disclosed. The methods are useful for treating conditions or disorders associated with toxic hypervolemia, such as renal failure, congestive heart failure, nephrotic syndrome, cirrhosis, pulmonary edema, and hypertension. The present invention also relates to methods for inducing an inotropic response comprising administration of an effective amount of GLP-1, an exendin, or an exendin or GLP-1 agonist. These methods are useful for treating conditions or disorders that can be alleviated by an increase in cardiac contractility such as congestive heart failure. Pharmaceutical compositions for use in the methods of the invention are also disclosed.
    Type: Grant
    Filed: April 5, 2011
    Date of Patent: June 24, 2014
    Assignees: Amylin Pharmaceuticals, LLC, AstraZeneca Pharmaceuticals LP
    Inventors: Andrew A. Young, Will Vine, Kathryn Prickett, Nigel R.A. Beeley
  • Publication number: 20140171364
    Abstract: 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: Application
    Filed: February 21, 2014
    Publication date: June 19, 2014
    Inventors: Steven Prestrelski, Wei-Jie Fang, John F. Carpenter, John Kinzell
  • Publication number: 20140171370
    Abstract: The present invention provides pharmaceutical formulations for sustained release, and methods for delivering a treatment regimen with a combination of sustained release and long half-life formulations. The invention provides improved pharmacokinetics for peptide and small molecule drugs.
    Type: Application
    Filed: December 6, 2013
    Publication date: June 19, 2014
    Applicant: PhaseBio Pharmaceuticals, Inc.
    Inventors: Susan Arnold, Christopher Prior
  • Publication number: 20140171362
    Abstract: Stable formulations for parenteral injection of peptide drugs and methods of using such stable formulations are provided. In particular, the present invention provides stable formulations for parenteral injection of glucagon and methods of using such glucagon formulations to treat hypoglycemia, especially severe hypoglycemia in emergency situations.
    Type: Application
    Filed: February 24, 2014
    Publication date: June 19, 2014
    Applicant: Xeris Pharmaceuticals, Inc.
    Inventors: Steven Prestrelski, John Kinzell
  • Publication number: 20140162943
    Abstract: 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: Application
    Filed: January 28, 2014
    Publication date: June 12, 2014
    Applicants: ASTRAZENECA PHARMACEUTICALS, LP, AMYLIN PHARMACEUTICALS, LLC
    Inventors: Josue ALFARO-LOPEZ, Abhinandini SHARMA, Soumitra S. GHOSH
  • Publication number: 20140154214
    Abstract: 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: Application
    Filed: February 4, 2014
    Publication date: June 5, 2014
    Inventors: Bjarne Due LARSEN, Yvette Miata Petersen
  • Patent number: 8729019
    Abstract: Methods are provided for coating crystalline microparticles with an active agent by altering the surface properties of the microparticles in order to facilitate favorable association on the microparticle by the active agent. Type of surface properties that are altered by the disclosed methods include by electrostatic properties, hydrophobic properties and hydrogen bonding properties.
    Type: Grant
    Filed: July 6, 2010
    Date of Patent: May 20, 2014
    Assignee: Mannkind Corporation
    Inventors: Keith A. Oberg, Joseph Sulner
  • Patent number: 8729018
    Abstract: The present invention provides therapeutic agents and compositions comprising elastic peptides and therapeutic proteins. Such peptides exhibit a flexible, extended conformation. In some embodiments, the therapeutic protein is a GLP-1 receptor agonist (e.g., GLP-1, exendin), insulin, or Factor VII/VIIa, including functional analogs. The present invention further provides encoding polynucleotides, as well as methods of making and using the therapeutic agents. The therapeutic agents have improvements in relation to their use as therapeutics, including, inter alia, one or more of half-life, clearance and/or persistance in the body, solubility, and bioavailability.
    Type: Grant
    Filed: March 12, 2013
    Date of Patent: May 20, 2014
    Assignee: Duke University
    Inventor: Ashutosh Chilkoti
  • Patent number: 8729017
    Abstract: Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon.
    Type: Grant
    Filed: June 12, 2012
    Date of Patent: May 20, 2014
    Assignee: Indiana University Research and Technology Corporation
    Inventors: Richard D. DiMarchi, David L. Smiley, Bin Yang
  • Publication number: 20140121159
    Abstract: 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: Application
    Filed: December 3, 2013
    Publication date: May 1, 2014
    Applicant: SmartCells, Inc.
    Inventors: Todd C. Zion, Thomas M. Lancaster
  • Publication number: 20140121154
    Abstract: 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: Application
    Filed: April 5, 2012
    Publication date: May 1, 2014
    Applicant: Longevity Biotech, Inc.
    Inventors: Scott Shandler, Samuel H. Gellman
  • Patent number: 8697644
    Abstract: Stable formulations for parenteral injection of peptide drugs and methods of using such stable formulations are provided. In particular, the present invention provides stable formulations for parenteral injection of glucagon and methods of using such glucagon formulations to treat hypoglycemia, especially severe hypoglycemia in emergency situations.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: April 15, 2014
    Assignee: Xeris Pharmaceuticals, Inc.
    Inventors: Steven Prestrelski, John Kinzell
  • Patent number: 8697648
    Abstract: 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: Grant
    Filed: October 20, 2010
    Date of Patent: April 15, 2014
    Assignee: Georgia State University Research Foundation, Inc.
    Inventors: Zhi-Ren Liu, Jie Yang, Bing Xu, Wangda Zhou, Shenghui Xue
  • Publication number: 20140100156
    Abstract: 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: Application
    Filed: October 9, 2013
    Publication date: April 10, 2014
    Applicant: SANOFI
    Inventors: Torsten HAACK, Michael WAGNER, Bernd HENKEL, Siegfried STENGELIN, Andreas EVERS, Martin BOSSART
  • Patent number: 8691763
    Abstract: The present invention provides methods for treating, preventing and/or ameliorating at least one cardiovascular disorder in a human in need thereof comprising administering to said human a pharmaceutical composition comprising at least one polypeptide having at least one GLP-1 activity and/or at least one GLP-1 agonist.
    Type: Grant
    Filed: May 4, 2011
    Date of Patent: April 8, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Beat M. Jucker, John J. Lepore, Eric J. Olson
  • Publication number: 20140094407
    Abstract: The invention relates to a therapeutic device for the delivery of therapeutic agents, e.g. a peptide such as leuprolide, via the vagina to a female mammal. In some embodiments, the invention also relates to methods for the treatment of obesity and eating disorders, diabetes, multiple sclerosis (MS), endometriosis, uterine fibroids, polycystic ovarian disease, various cancers such as breast cancer, acne, hirsutism, microbial or fungal or viral infections such as bacterial vaginosis or AIDS/HIV, and chronic diseases using a disclosed vaginal device.
    Type: Application
    Filed: December 4, 2013
    Publication date: April 3, 2014
    Applicant: Combinent Biomedical Systems, Inc.
    Inventors: Eyal S. Ron, William F. Crowley, JR., Robert S. Langer, Surajit K. Biswas, Quentin Baca, Armen Tashjian
  • Publication number: 20140087996
    Abstract: The invention relates to a pharmaceutical composition according to the claim 1 comprising an SGLT2 inhibitor and a GLP-1 receptor agonist which is suitable in the treatment or prevention of diabetes mellitus, impaired glucose tolerance, hyperglycemia or other conditions. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions.
    Type: Application
    Filed: December 4, 2013
    Publication date: March 27, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Thomas KLEIN, Rolf GREMPLER, Michael MARK
  • Publication number: 20140086910
    Abstract: The present invention provides indane acetic acid and their derivatives and methods for the treating and/or preventing of Alzheimer's diseases.
    Type: Application
    Filed: August 29, 2013
    Publication date: March 27, 2014
    Applicant: DARA BIOSCIENCES, INC.
    Inventor: Mary Katherine Delmedico
  • Patent number: 8680315
    Abstract: 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: Grant
    Filed: June 26, 2009
    Date of Patent: March 25, 2014
    Assignee: Prolynx, LLC
    Inventors: Daniel V. Santi, Gary W. Ashley