Glucagon, Glucagon-like Peptide (e.g., Glp-1, Glp-2, Etc.) Or Derivative Patents (Class 514/11.7)
  • Patent number: 10538569
    Abstract: The present invention relates to a fusion polypeptide containing a glucagon-like peptide (GLP) and an immunoglobulin hybrid Fc, and more specifically, to a fusion polypeptide with an increased half-life and improved efficacy compared to the conventional fusion polypeptide based on the discovery of an immunoglobulin hybrid Fc suitable for GLP or analogs thereof, and a pharmaceutical composition for treating diabetes, inflammatory bowel disease, endoenteritis or diarrhea caused by anticancer chemotherapy, or short bowel syndrome, containing the fusion polypeptide. The fusion polypeptide of the present invention has an increased half-life and improved resistance to DPP-4 enzyme compared to those of GLP-1 and GLP-2, and it thus has improved drug efficacy in treating diabetes, inflammatory bowel disease, endoenteritis or diarrhea caused by anticancer chemotherapy, or short bowel syndrome, compared to those of the conventional drugs.
    Type: Grant
    Filed: December 31, 2015
    Date of Patent: January 21, 2020
    Assignee: GENEXINE, INC.
    Inventors: Young Chul Sung, Se Hwan Yang, Mi Sun Byun, Sang In Yang, Eun Ju Shin
  • Patent number: 10336803
    Abstract: This document provides methods and materials related to insulin secreting polypeptides. For example, polypeptides having the ability to induce insulin secretion and methods and materials for using use such polypeptides to induce insulin secretion and to treat diabetes are provided.
    Type: Grant
    Filed: March 22, 2018
    Date of Patent: July 2, 2019
    Assignee: Mayo Foundation for Medical Education and Research
    Inventors: Horng H. Chen, John C. Burnett, Jr.
  • Patent number: 10286037
    Abstract: The invention is directed to a method for producing a polypeptide composition comprising: combining a polypeptide with a volatile additive to form a liquid mixture and lyophilizing the liquid mixture to obtain a lyophilized polypeptide composition.
    Type: Grant
    Filed: February 9, 2012
    Date of Patent: May 14, 2019
    Assignee: GlaxoSmithKline LLC
    Inventors: James Kranz, Joseph Rinella
  • Patent number: 10279041
    Abstract: The present invention relates to an albumin-free liquid formulation comprising a long-lasting oxyntomodulin conjugate in which an oxyntomodulin peptide comprising a derivative, variant, precursor or fragment of oxyntomodulin is linked to an immunoglobulin Fc region, which can increase the duration of physiological activity of the long-lasting oxyntomodulin conjugate and maintain the in vivo stability thereof for an extended period of time, as compared to native oxyntomodulin, as well as a method for preparing the liquid formulation. The liquid formulation comprises a buffer, a sugar alcohol and a nonionic surfactant and does not contain a human serum albumin and factors that are potentially harmful to the human body, and thus is not susceptible to viral infection.
    Type: Grant
    Filed: June 29, 2017
    Date of Patent: May 7, 2019
    Assignee: Hanmi Pharm Co. Ltd.
    Inventors: Hyun Uk Kim, Hyung Kyu Lim, Myung Hyun Jang, Sang Yun Kim, Sung Min Bae, Se Chang Kwon
  • Patent number: 10238717
    Abstract: This invention relates to compositions of glucagon suitable for administration by manual injection or by an insulin pump or other injection device to treat hypoglycemia. Said compositions comprise glucagon and a sugar, have a final pH between about 1.5 and 3, and are gel-free, chemically-stable at body temperature and pump-able.
    Type: Grant
    Filed: March 30, 2017
    Date of Patent: March 26, 2019
    Assignee: LATITUDE PHARMACEUTICALS, INC.
    Inventor: Andrew Chen
  • Patent number: 10159714
    Abstract: The use of GLP-1 receptor agonists, such as glucagon-like peptide-1 (GLP-1) or exenatide, for the treatment of cancer is described. The GLP-1 receptor agonists are typically delivered using an implanted osmotic delivery device that provides for continuous delivery of the GLP-1 receptor agonist for at least one month. Additional beneficial agents, such as anticancer agents, can also be administered.
    Type: Grant
    Filed: May 17, 2017
    Date of Patent: December 25, 2018
    Assignee: Intarcia Therapeutics, Inc.
    Inventor: Karling Alice Leung
  • Patent number: 10137171
    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: Grant
    Filed: January 19, 2017
    Date of Patent: November 27, 2018
    Assignee: The General Hospital Corporation
    Inventors: Joel F. Habener, Eva Tomas-Falco
  • Patent number: 10118955
    Abstract: C-Terminal Fragments of Glucagon-Like Peptide-1 (GLP 1), and methods of use thereof, e.g., for the treatment of obesity and obesity-related disorders, e.g., diabetes and the metabolic syndrome.
    Type: Grant
    Filed: November 12, 2014
    Date of Patent: November 6, 2018
    Assignee: The General Hospital Corporation
    Inventors: Joel F. Habener, Tatsuya Yano, Eva Tomas Falco
  • Patent number: 10000542
    Abstract: The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue and a second K residue, at positions corresponding to position 26, and 37, respectively, of GLP-1(7-37) (SEQ ID NO: 1), and a maximum of eight amino acid changes as compared to GLP-1(7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 1: HOOC—(CH2)x—CO—*, and Chem. 2: HOOC—C6H4—O—(CH2)y—CO—*, in which x is an integer in the range of 8-16, and y is an integer in the range of 6-13; and the linker comprises Chem. 3: *—NH—(CH2)q—CH[(CH2)w—NR1R2]—CO—*, which is connected at its CO—* end to the epsilon amino group of the first or the second K residue of the GLP-1 analogue, and wherein q is an integer in the range of 0-5, R1 and R2 independently represent *—H or *—CH3, and w is an integer in the range of 0-5; or a pharmaceutically acceptable salt, amide, or ester thereof.
    Type: Grant
    Filed: May 2, 2013
    Date of Patent: June 19, 2018
    Assignee: Novo Nordisk A/S
    Inventors: Jacob Kofoed, Patrick W. Garibay, Jesper Lau
  • Patent number: 9938334
    Abstract: This document provides methods and materials related to insulin secreting polypeptides. For example, polypeptides having the ability to induce insulin secretion and methods and materials for using use such polypeptides to induce insulin secretion and to treat diabetes are provided.
    Type: Grant
    Filed: February 13, 2014
    Date of Patent: April 10, 2018
    Assignee: Mayo Foundation for Medical Education and Research
    Inventors: Horng H. Chen, John C. Burnett, Jr.
  • Patent number: 9809821
    Abstract: There is disclosed a composition and a method for the efficient delivery of a therapeutic RNAi-inducing nucleic acid to cells both in vitro and in vivo through specific formulations of a non viral delivery system using chitosans. Particularly, the composition contains a nucleic acid and a specific chitosan that has the following physico-chemical properties: a number-average molecular weight between 5 kDa and 200 kDa, a degree of deacetylation between 80% and 95% and a chitosan amine to nucleic acid phosphate ratio below 20.
    Type: Grant
    Filed: December 1, 2015
    Date of Patent: November 7, 2017
    Assignee: POLYVALOR, LIMITED PARTNERSHIP
    Inventors: Abderrazzak Merzouki, Michael D. Buschmann
  • Patent number: 9782344
    Abstract: There is provided glucagon formulations suitable for preparing coatings on microneedle patches for the transdermal delivery of glucagon. The coated patches may be used for the treatment of low blood sugar in diabetic patients. Also provided are glucagon loaded patches, methods for their preparation, and methods of their use.
    Type: Grant
    Filed: November 2, 2015
    Date of Patent: October 10, 2017
    Assignee: ZP OPCO, INC.
    Inventors: Mahmoud Ameri, Peter E. Daddona, Yi Ao
  • Patent number: 9724420
    Abstract: Disclosed are an albumin-free liquid formulation including a long-lasting oxyntomodulin conjugate in which an oxyntomodulin peptide comprising a derivative, variant, precursor or fragment of oxyntomodulin is linked to an immunoglobulin Fc region, which can increase the duration of physiological activity of the long-lasting oxyntomodulin conjugate and maintain the in vivo stability thereof for an extended period of time, as compared to native oxyntomodulin, and a method for preparing the liquid formulation. The liquid formulation contains a buffer, a sugar alcohol and a nonionic surfactant and does not contain a human serum albumin and factors that are potentially harmful to the human body, and thus is not susceptible to viral infection. The oxyntomodulin conjugate contains oxyntomodulin linked to an immunoglobulin Fc region, and thus has a large molecular weight, prolonged physiological activity, and excellent storage stability, compared to native oxyntomodulin.
    Type: Grant
    Filed: November 6, 2013
    Date of Patent: August 8, 2017
    Assignee: Hanmi Pharm. Co., Ltd.
    Inventors: Hyun Uk Kim, Hyung Kyu Lim, Myung Hyun Jang, Sang Yun Kim, Sung Min Bae, Se Chang Kwon
  • Patent number: 9695225
    Abstract: A peptide compound useful in the treatment of hypoglycemia is described.
    Type: Grant
    Filed: December 11, 2014
    Date of Patent: July 4, 2017
    Assignee: Eli Lilly and Company
    Inventors: Jorge Alsina-Fernandez, Robert Chadwick Cummins, Lili Guo
  • Patent number: 9688736
    Abstract: A peptide compound useful in the treatment of hypoglycemia is described.
    Type: Grant
    Filed: December 11, 2014
    Date of Patent: June 27, 2017
    Assignee: Eli Lilly and Company
    Inventors: Jorge Alsina-Fernandez, Robert Chadwick Cummins
  • Patent number: 9657079
    Abstract: The invention relates to truncated GLP-1 analogs, in particular a GLP-1 analog which is a modified GLP-1(7-35) (SEQ ID No 1) having: i) a total of 2, 3, 4, 5 6, 7, 8, or 9 amino acid substitutions as compared to GLP-1(7-35), including a) a Glu residue at a position equivalent to position 22 of GLP-1(7-35), and b) an Arg residue at a position equivalent to position 26 of GLP-1(7-35); as well as derivatives thereof, and therapeutic uses and compositions. These analogs and derivatives are highly potent, have a good binding affinity to the GLP-1 receptor, also to the extracellular domain of the GLP-1 receptor, which is of potential relevance achieving long-acting, stable GLP-1 compounds with a potential for once weekly administration.
    Type: Grant
    Filed: June 9, 2014
    Date of Patent: May 23, 2017
    Assignee: Novo Nordisk A/S
    Inventors: Jane Spetzler, Lauge Schaeffer, Jesper Lau, Janos T. Kodra, Kjeld Madsen, Patrick W. Garibay, Jacob Kofoed, Steffen Reedtz-Runge, Ingrid Pettersson
  • Patent number: 9610329
    Abstract: A formulation composed of a sugar such as glucose and a surfactant such as myristoyl lysophosphocholine (LMPC) has been designed to stabilize both hydrophilic and hydrophobic portions of the glucagon molecule, under prolonged physiological conditions, in a formulation that is sufficiently similar to the pH and osmolarity of plasma so as not to induce or to minimize site irritation. The combination of a simple sugar and an surfactant stabilizes the glucagon molecule in an aqueous solution for seven days at 37° C.
    Type: Grant
    Filed: September 27, 2010
    Date of Patent: April 4, 2017
    Assignee: Albireo Pharma, Inc.
    Inventors: Solomon S. Steiner, Robert Hauser, Ming Li, Robert Feldstein, Roderike Pohl
  • Patent number: 9546205
    Abstract: Peptide analogs of glucagon and peptide analogs of GLP1 are provided herein. Also provided herein are pharmaceutical compositions comprising the analogs, and methods of using the analogs for the treatment and/or prevention of conditions such as obesity and diabetes.
    Type: Grant
    Filed: September 17, 2013
    Date of Patent: January 17, 2017
    Assignee: IMPERIAL INNOVATIONS LIMITED
    Inventor: Stephen Robert Bloom
  • Patent number: 9498534
    Abstract: The invention relates to derivatives of GLP-1 like peptides which are C-terminally extended analogs of native GLP-1. The derivatives comprise two side chains, one at a position corresponding to position 42, and one at a position corresponding to position 18, 23, 27, 31, 36, or 38, wherein both positions are when compared to GLP-1(7-37). The side chains comprise a C19, C20, or C22 diacid protracting moiety and optionally a linker. The invention also relates to intermediate products in the form of novel GLP-1 analogs incorporated in the derivatives of the invention, as well as pharmaceutical compositions and medical uses of the derivatives. The derivatives have very long half-lives while maintaining a satisfactory potency, which makes them potentially suitable for once-monthly administration.
    Type: Grant
    Filed: July 2, 2014
    Date of Patent: November 22, 2016
    Assignee: Novo Nordisk A/S
    Inventors: Steffen Reedtz-Runge, Jacob Kofoed, Christian Wenzel Tornoee, Per Sauerberg
  • Patent number: 9173924
    Abstract: There is provided glucagon formulations suitable for preparing coatings on microneedle patches for the transdermal delivery of glucagon. The coated patches may be used for the treatment of low blood sugar in diabetic patients. Also provided are glucagon loaded patches, methods for their preparation, and methods of their use.
    Type: Grant
    Filed: August 22, 2014
    Date of Patent: November 3, 2015
    Assignee: ZP OPCO, INC.
    Inventors: Mahmoud Ameri, Peter E. Daddona, Yi Ao
  • Patent number: 9168288
    Abstract: The invention provides a method of treating a subject having, or at risk of developing, a condition in which functioning of the small or large intestine is impaired, enhancing functioning or preventing damage to the small or large intestine in a subject, or ameliorating inflammation of the small or large intestine in a subject, comprising administering to the subject a GLP-1 receptor agonist. A GLP-1 receptor agonist may also be provided in a pharmaceutically acceptable form in an amount effective to treat or prevent conditions of the small or large intestine. Further, pharmaceutical compositions are provided for the treatment or prevention of conditions of the small or large intestine comprising a GLP-1 receptor agonist, together with a pharmaceutically acceptable carrier, excipient or vehicle.
    Type: Grant
    Filed: April 8, 2011
    Date of Patent: October 27, 2015
    Assignee: Mount Sinai Hospital
    Inventors: Daniel J. Drucker, Laurie Lynn Baggio
  • Patent number: 9072794
    Abstract: Disclosed is a novel long-acting glucagon conjugate in which glucagon or its derivative is covalently linked to a polymer carrier via a non-peptide linker, and a pharmaceutical composition comprising the same as an effective ingredient useful for the prevention and treatment of obesity. Since the long-acting glucagon conjugate of the present invention shows improved in vivo durability and stability, when used in combination with an anti-obesity drug, it is possible to induce synergistic effects on the loss of body weight and decrease in food intake without causing any side-effects such as fluctuation in blood glucose level. Accordingly, the long-acting peptide conjugate of the present invention is very effective for the prevention and treatment of obesity.
    Type: Grant
    Filed: July 21, 2011
    Date of Patent: July 7, 2015
    Assignee: HANMI SCIENCE CO., LTD
    Inventors: Young Eun Woo, Jong Soo Lee, Ling Ai Shen, Dae Jin Kim, Sung Youb Jung, In Young Choi, Se Chang Kwon
  • Patent number: 9060992
    Abstract: Intestinal absorption is enhanced in short bowel syndrome patients presenting with colon-in-continuity by treatment with a GLP-2 receptor agonist, such as teduglutide.
    Type: Grant
    Filed: November 2, 2010
    Date of Patent: June 23, 2015
    Assignee: NPS Pharmaceuticals, Inc.
    Inventors: Elizabeth Lemaire Sanguinetti, Thomas B. Marriott, Jennifer Lopansri, Consuelo Maria Blosch
  • Publication number: 20150148289
    Abstract: A composition which includes oxyntomodulin and polyethylene glycol polymer (PEG polymer) linked via a reversible linker such as 9-fluorenylmethoxycarbonyl (Fmoc) or 2-sulfo-9-fluorenylmethoxycarbonyl (FMS) is disclosed. Pharmaceutical compositions comprising the reverse pegylated oxyntomodulin and methods of using same are also disclosed.
    Type: Application
    Filed: June 4, 2013
    Publication date: May 28, 2015
    Inventors: Udi Eyal Fima, Oren Hershkovitz
  • Publication number: 20150147390
    Abstract: Embodiments of the invention provide swallowable devices, preparations and methods for delivering drugs and other therapeutic agents within the GI tract. Many embodiments provide a swallowable device for delivering the agents. Particular embodiments provide a swallowable device such as a capsule for delivering drugs into the intestinal wall or other GI lumen. Embodiments also provide various drug preparations that are configured to be contained within the capsule, advanced from the capsule into the intestinal wall and degrade to release the drug into the bloodstream to produce a therapeutic effect. The preparation can be operably coupled to delivery means having a first configuration where the preparation is contained in the capsule and a second configuration where the preparation is advanced out of the capsule into the intestinal wall. Embodiments of the invention are particularly useful for the delivery of drugs which are poorly absorbed, tolerated and/or degraded within the GI tract.
    Type: Application
    Filed: January 27, 2015
    Publication date: May 28, 2015
    Inventor: Mir Imran
  • Patent number: 9040481
    Abstract: Methods for treating fatty liver disease, e.g., hepatic steatosis, using peptide fragments of the C-terminal end of glucagon-like peptide-1 (GLP-1), e.g., GLP-1(28-36).
    Type: Grant
    Filed: November 2, 2011
    Date of Patent: May 26, 2015
    Assignee: The General Hospital Corporation
    Inventors: Joel F. Habener, Eva Tomas-Falco
  • Publication number: 20150133374
    Abstract: The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue and a second K residue, at positions corresponding to position 26, and 37, respectively, of GLP-1(7-37) (SEQ ID NO: 1), and a maximum of eight amino acid changes as compared to GLP-1(7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 1: HOOC—(CH2)x—CO—*, and Chem. 2: HOOC—C6H4—O—(CH2)y—CO—*, in which x is an integer in the range of 8-16, and y is an integer in the range of 6-13; and the linker comprises Chem. 3: *—NH—(CH2)q—CH[(CH2)w—NR1R2]—CO—*, which is connected at its CO—* end to the epsilon amino group of the first or the second K residue of the GLP-1 analogue, and wherein q is an integer in the range of 0-5, R1 and R2 independently represent *—H or *—CH3, and w is an integer in the range of 0-5; or a pharmaceutically acceptable salt, amide, or ester thereof.
    Type: Application
    Filed: May 2, 2013
    Publication date: May 14, 2015
    Inventors: Jacob Kofoed, Patrick W. Garibay, Jesper Lau
  • Publication number: 20150133384
    Abstract: C-Terminal Fragments of Glucagon-Like Peptide-1 (GLP 1), and methods of use thereof, e.g., for the treatment of obesity and obesity-related disorders, e.g., diabetes and the metabolic syndrome.
    Type: Application
    Filed: November 12, 2014
    Publication date: May 14, 2015
    Inventors: Joel F. Habener, Tatsuya Yano, Eva Tomas Falco
  • Publication number: 20150125431
    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 altered GLP-1 activity, and their medical use. The analogues are particularly useful for the prophylaxis, treatment or ameliorating of the gastro-intestinal associated side effects of diabetes.
    Type: Application
    Filed: May 3, 2013
    Publication date: May 7, 2015
    Inventors: Rasmus Just, Kirsten Lindegaard Bovbjerg, Ditte Riber, Wayne Shaun Russell
  • Patent number: 9023985
    Abstract: There is provided according to the invention an aqueous composition having pH between 4 and 7 comprising (i) glucagon at a concentration of 0.05% w/v or more and (ii) a cationic surfactant selected from benzalkonium salts and benzethonium salts as solubilizing agent in an amount sufficient to dissolve the glucagon in the composition.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: May 5, 2015
    Assignee: Arecor Ltd.
    Inventors: Jan Jezek, Barry Kingston Derham
  • Publication number: 20150111817
    Abstract: 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: Application
    Filed: October 16, 2014
    Publication date: April 23, 2015
    Inventors: Ditte RIBER, Jakob Lind TOLBORG, Dieter Wolfgang HAMPRECHT
  • Publication number: 20150111826
    Abstract: 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 acylated 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: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Inventors: Ditte RIBER, Jakob Lind TOLBORG, Dieter Wolfgang HAMPRECHT, Wolfgang RIST
  • Patent number: 9006178
    Abstract: 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: Grant
    Filed: November 9, 2011
    Date of Patent: April 14, 2015
    Assignee: Novo Nordisk A/S
    Inventors: Jacob Kofoed, Jesper Lau, Lars Linderoth, Patrick William Garibay, Thomas Kruse
  • Patent number: 8999930
    Abstract: The present invention relates to a soluble hydrophobic-core carrier composition comprising (i) a linear polymeric backbone; (ii) a plurality of hydrophilic polymeric protective chains covalently linked and pendant to the polymeric backbone and (iii) at least one hydrophobic moiety covalently linked and pendant to the polymeric backbone. In certain embodiments, the weight ratio of hydrophilic protective chains to hydrophobic moieties in the carrier is at least 15:1. In other embodiments, at least 90% of the residues of the polymeric backbone are coupled to a hydrophilic polymeric protective chain or a hydrophobic moiety. In other embodiments, the composition further comprises (iv) a hydrophobic load molecule dissociably linked to the hydrophobic moiety of the carrier.
    Type: Grant
    Filed: February 24, 2010
    Date of Patent: April 7, 2015
    Assignee: PharmaIN Corporation
    Inventors: Gerardo M. Castillo, Elijah M. Bolotin
  • Publication number: 20150086618
    Abstract: The invention generally relates to compositions and methods for the reduction or neutralization of toxins associated with a bacterial, mycobacterial, fungal, viral, or protozoal agent. More particularly, the invention is directed to sterically stabilized phospholipid micellar and liposomal compositions, which interact with the toxins to decrease or neutralize their toxicity. Additionally, the invention includes the use of sterically stabilized phospholipid micellar compositions comprising one or more water-insoluble antibiotic, antifungal, antiviral, antiprotozoal, or anti-inflammatory agent(s), wherein the micellar or liposomal composition inhibits the formation of aggregates. The invention further includes the use of sterically stabilized micelle and liposomal compositions to deliver compounds to the site of action, and in some cases targets the compound to the site of action, for the treatment of inflammation and infection.
    Type: Application
    Filed: September 30, 2014
    Publication date: March 26, 2015
    Inventors: HAYAT ONYUKSEL, ISRAEL RUBENSTEIN
  • Publication number: 20150080307
    Abstract: Methods for reducing gastric motility and delaying gastric emptying for therapeutic and diagnostic purposes are disclosed which comprise administration of an effective amount of an exendin or an exendin agonist. Methods for treating conditions associated with elevated, inappropriate, or undesired post-prandial blood glucose levels are disclosed which comprise administration of an effective amount of an exendin or an exendin agonist alone or in conjunction with other anti-gastric emptying agents.
    Type: Application
    Filed: November 21, 2014
    Publication date: March 19, 2015
    Inventors: Andrew A. YOUNG, Bronislava GEDULIN
  • Publication number: 20150080308
    Abstract: Provided herein are formulations containing exendins, exendin agonists and/or exendin analogs and methods of using the exendins, exendin agonists and/or exendin analogs and formulations thereof to treat glucagonoma and necrolytic migratory erythema, or to suppress glucagon secretion.
    Type: Application
    Filed: November 25, 2014
    Publication date: March 19, 2015
    Inventors: Orville G. KOLTERMAN, Andrew A. YOUNG, James J. L'ITALIEN
  • Publication number: 20150080295
    Abstract: 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: Application
    Filed: March 3, 2014
    Publication date: March 19, 2015
    Applicant: Zealand Pharma A/S
    Inventors: Eddi MEIER, Ditte Riber, Marie Skovgaard, Bjarne Due Larsen, Jens Rosengren Daugaard
  • Publication number: 20150071879
    Abstract: An aqueous composition having increased protein stability is obtained by: a. determining a pH at which the protein has stability at the desired temperature; b. adding to the composition at least one displacement buffer wherein the displacement buffer has a pKa that is at least 1 unit greater or less than the pH of step (a); and c. adjusting the pH of the composition to the pH of step (a); wherein the aqueous composition does not comprise a conventional buffer at a concentration greater than about 2 mM and wherein the conventional buffer has a pKa that is within 1 unit of the pH of step (a).
    Type: Application
    Filed: October 17, 2014
    Publication date: March 12, 2015
    Inventor: Jan JEZEK
  • Publication number: 20150072930
    Abstract: The invention relates to novel polypeptide analogs of GLP-1 and exendin-4. The polypeptide, in a preferred embodiment, is insulinotropic and long-acting. Preferably, the polypeptide's insulinotropic effect is comparable to or exceeds the effect of an equimolar amount of GLP-1 or exendin-4. The invention also relates to a method of treating a subject with diabetes, comprising administering to the subject the polypeptide of the invention in an amount that has an insulinotropic effect. The invention also relates to methods of using GLP-1, exendin-4, and polypeptide analogs thereof for neuroprotective and neurotrophic effects.
    Type: Application
    Filed: August 27, 2014
    Publication date: March 12, 2015
    Inventors: Nigel H. Greig, Josephine M. Egan, Maire Doyle, Harold W. Holloway, Tracy Perry
  • Publication number: 20150072926
    Abstract: The invention relates to pharmaceutical compositions comprising a first type of granules and a second type of granules, wherein said first type of granules comprises a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and no GLP-1 peptide, and wherein said second type of granules comprises a GLP-1 peptide and no salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, as well as the intermediate granules, processes for the preparation of the granules and compositions, and use thereof in medicine.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 12, 2015
    Inventors: Thomas Vilhelmsen, Helle Eliasen, Tue Hansen
  • Patent number: 8975227
    Abstract: The present invention provides a composition (e.g., a pharmaceutical composition) comprising at least one delivery agent compound and glucagon. Preferably, the composition includes a therapeutically effective amount of glucagon and the delivery agent compound. The composition of the present invention facilitates the delivery of glucagon and increases its bioavailability compared to administration without the delivery agent compound.
    Type: Grant
    Filed: July 17, 2006
    Date of Patent: March 10, 2015
    Assignee: Emisphere Technologies, Inc.
    Inventors: Nai Fang Wang, Puchun Liu, Steven Dinh, Michael M. Goldberg, Ehud Arbit
  • Publication number: 20150065422
    Abstract: Disclosed are drug delivery systems for the delivery of small molecule and macromolecular drugs. More particularly, disclosed are substituted analogs of 3,6-di(alkyl-4 aminobutyl)-2,5-diketopiperazine (which may also be referred to DKP), their use in the formulation of both small molecule and macromolecular drugs including therapeutic, prophylactic and diagnostic agents, stabilizing agents and systems for their delivery.
    Type: Application
    Filed: November 7, 2014
    Publication date: March 5, 2015
    Inventor: Kelly Sullivan Kraft
  • Patent number: 8969288
    Abstract: Prodrug formulations of glucagon superfamily peptides are provided wherein the glucagon superfamily peptide has been modified by the linkage of a dipeptide to the glucagon superfamily through an amide bond linkage. The prodrugs disclosed herein have extended half lives and are converted to the active form at physiological conditions through a non-enzymatic reaction driven by chemical instability.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: March 3, 2015
    Assignee: Indiana University Research and Technology Corporation
    Inventors: Richard D. DiMarchi, Binbin Kou
  • Patent number: 8968716
    Abstract: Disclosed herein are an in situ-forming, bioadhesive hydrogel and the medical uses thereof. Being formed by in situ crosslinking through an enzymatic reaction, the hydrogel has an advantage over conventional bioadhesive hydrogels in terms of biocompatibility. In addition, the in situ-forming bioadhesive hydrogel has excellent biocompatibility and mechanical strength and has excellent tissue adhesiveness thanks to modification with/without dopa derivatives. The hydrogel finds a variety of applications in the biomedical field, including bioadhesives or hemostats, implant substances for tissue regeneration and augmentation, carriers for delivering biologically active materials or drugs, etc.
    Type: Grant
    Filed: September 2, 2010
    Date of Patent: March 3, 2015
    Assignee: Ajou University Industry-Academic Cooperation Foundation
    Inventors: Ki-Dong Park, Yoon-Ki Joung, Kyung-Min Park, Eu-Gene Lih
  • Publication number: 20150057221
    Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising a drug linker conjugate D-L, wherein -D is an amine containing biologically active moiety; and -L is a non-biologically active linker moiety -L1 represented by formula (I): wherein the dashed line indicates the attachment to the amine of the biologically active moiety and wherein R1, R1a, R2, R2a, R3, R3a, X, X1, X2, X3 have the meaning as indicated in the description and the claims and wherein L1 is substituted with one to four groups L2-Z and optionally further substituted, provided that the hydrogen marked with the asterisk in formula (I) is not replaced by a substituent; wherein L2 is a single chemical bond or a spacer; and Z is a carrier group. The invention also relates to A-L, wherein A is a leaving group, pharmaceutical composition comprising said prodrugs and their use as medicaments.
    Type: Application
    Filed: October 30, 2014
    Publication date: February 26, 2015
    Inventors: Felix Cleemann, Ulrich Hersel, Silvia Kaden, Harald Rau, Thomas Wegge
  • Publication number: 20150057220
    Abstract: Fused aromatic phosphonates of structural formula I are precursors to inhibitors of protein tyrosine phosphatase-1B (PTP-1B). The compounds of the present invention are therefore useful for the treatment in a mammal of a disorder, condition, or disease responsive to inhibition of protein tyrosine phosphatase-1B, including Type 2 diabetes, insulin resistance, a lipid disorder, obesity, Metabolic Syndrome, and cancer.
    Type: Application
    Filed: April 16, 2013
    Publication date: February 26, 2015
    Inventors: Michel Therien, Yves Leblanc, Yongxin Han
  • Publication number: 20150057605
    Abstract: There is provided glucagon formulations suitable for preparing coatings on microneedle patches for the transdermal delivery of glucagon. The coated patches may be used for the treatment of low blood sugar in diabetic patients. Also provided are glucagon loaded patches, methods for their preparation, and methods of their use.
    Type: Application
    Filed: August 22, 2014
    Publication date: February 26, 2015
    Inventors: Mahmoud Ameri, Peter E. Daddona, Yi Ao
  • Publication number: 20150056167
    Abstract: Human proIslet Peptides (HIP) and HIP analogs and derivatives thereof, derived from or homologous in sequence to the human REG3A protein, chromosome 2p12, are able to induce islet neogenesis from endogenous pancreatic progenitor cells. Human proIslet Peptides are used either alone or in combination with other pharmaceuticals in the treatment of type 1 and type 2 diabetes and other pathologies related to aberrant glucose, carbohydrate, andor lipid metabolism, insulin resistance, overweight, obesity, polycystic ovarian syndrome, eating disorders and the metabolic syndrome.
    Type: Application
    Filed: September 4, 2014
    Publication date: February 26, 2015
    Inventors: Claresa S. Levetan, Loraine V. Upham
  • Publication number: 20150056160
    Abstract: An invention relating to therapeutic pharmacological agents and methods to chemically induce intracellular hyperthermia and/or free radicals for the diagnosis and treatment of infections, malignancy and other medical conditions. The invention relates to a process and composition for the diagnosis or killing of cancer cells and inactivation of susceptible bacterial, parasitic, fungal, and viral pathogens by chemically generating heat, and/or free radicals and/or hyperthermia—inducible immunogenic determinants by using mitochondrial uncoupling agents, especially 2,4 dinitrophenol and, their conjugates, either alone or in combination with other drugs, hormones, cytokines and radiation.
    Type: Application
    Filed: February 24, 2014
    Publication date: February 26, 2015
    Inventors: Nicholas Bachynsky, Woodie Roy