Glucagon; Related Peptides Patents (Class 530/308)
-
Publication number: 20130338068Abstract: The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 18 of GLP-1(7-37) (SEQ ID NO: 1), a second K residue at another position, and a maximum of twelve amino acid changes as compared to GLP-1(7-37); which derivative comprises two protracting moieties attached to said first and second K residue, respectively, via a linker, wherein the protracting moiety is selected from HOOC—(CH2)x—CO-*, and??Chem. 1: HOOC—C6H4-0-(CH2)y—CO-*,??Chem. 2: in which x is an integer in the range of 6-18, and y is an integer in the range of 3-17; and the linker comprises *-NH—(CH2)q—CH[(CH2)w—NH2]—CO-*,??Chem. 3: wherein q is an integer in the range of 0-5, and w is an integer in the range of 0-5; or a pharmaceutically acceptable salt, amide, or ester thereof.Type: ApplicationFiled: November 9, 2011Publication date: December 19, 2013Applicant: Novo Nordisk A/SInventors: Jacob Kofoed, Jesper Lau, Lars Linderoth, Patrick William Garibay, Thomas Kruse
-
Patent number: 8603972Abstract: The invention relates to protracted GLP-1 compounds and therapeutic uses thereof.Type: GrantFiled: March 20, 2006Date of Patent: December 10, 2013Assignee: Novo Nordisk A/SInventors: Jesper Lau, Florencio Zaragoza Dorwald, Lauge Schaffer, Thomas Kruse Hansen
-
Publication number: 20130324699Abstract: A new method of synthesizing GLP-1 peptide is devised.Type: ApplicationFiled: April 29, 2013Publication date: December 5, 2013Applicant: LONZA AGInventor: Lonza AG
-
Publication number: 20130316941Abstract: The invention provides glucagon analogue peptides and their use for promoting weight loss or preventing weight gain, and the treatment of obesity or excess body weight and associated conditions. The compounds may also be used to improve glycemic control and/or for the treatment of diabetes. The compounds may mediate their effect, inter alia, by having increased selectivity for the GLP-1 receptor as compared to human glucagon.Type: ApplicationFiled: December 19, 2012Publication date: November 28, 2013Applicants: Boehringer Ingelheim International GmbH, Zealand Pharma A/SInventors: Dieter Wolfgang Hamprecht, Jakob Lind Tolborg, Ditte Riber
-
Patent number: 8580919Abstract: Conjugates of a GLP-1 moiety may be covalently attached to one or more water-soluble polymers. For instance, a GLP-1 polymer conjugate may include a GLP-1 moiety releasably attached at its N-terminus to a water-soluble polymer. The GLP-1 polymer conjugate may include a GLP-1 moiety covalently attached to a water-soluble polymer, wherein the GLP-1 moiety possesses an N-methyl substituent.Type: GrantFiled: September 14, 2012Date of Patent: November 12, 2013Assignee: Nektar TherapeuticsInventors: Mary J. Bossard, Zhihao Fang, Tacey X. Viegas, Stewart A. Thompson, Mei-chang Kuo
-
Patent number: 8568781Abstract: Nanoparticles having a core and a corona of ligands covalently linked to the core, wherein peptides are bound to or associated with the nanoparticles.Type: GrantFiled: June 10, 2011Date of Patent: October 29, 2013Assignee: Midatech LimitedInventors: Thomas Rademacher, Phillip Williams, Christof Bachmann, Africa Garcia Barrientos, Esther de Torres Dominguez, Javier del Campo Menoyo
-
Patent number: 8557771Abstract: Provided is a homodimer of insulinotropic peptide analogues and method for preparation thereof and use thereof, wherein the insulinotropic peptide analogue comprises GLP-1 and Exendin-4. The homodimer of insulinotropic peptide analogues of the invention is made by conjugating two identical insulinotropic peptide analogue molecules at the C-terminal Cys residues via disulfide bond or PEG molecule. The homodimer of insulinotropic peptide analogues of the invention has superior stability and biological activity in vivo, and prolonged half-life in the circulation, and can be used for the preparation of hypoglycemic drugs.Type: GrantFiled: March 15, 2010Date of Patent: October 15, 2013Assignee: Chongqing Fagen Biomedical Inc.Inventors: Kai Fan, Zhiquan Zhao, Yong Chen, Chun Zhang, Lin Wang
-
Patent number: 8551946Abstract: 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. Methods 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: GrantFiled: January 26, 2011Date of Patent: October 8, 2013Assignee: Indiana University Research and Technology CorporationInventors: Richard D. Dimarchi, Tao Ma
-
Patent number: 8546326Abstract: The present invention relates to compositions forming a low viscosity mixture of: a) at least one neutral diacyl lipid, such as a diacyl glycerol; b) at least one phospholipid, such as a phosphatidyl choline; c) at least one biotolerable solvent, such as an oxygen containing solvent; d) at least one GLP-1 analogue; wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The invention further relates to methods of treatment comprising administration of such compositions, especially in treating diabetes, and to pre-filled administration devices and kits containing the formulations.Type: GrantFiled: June 6, 2006Date of Patent: October 1, 2013Assignee: Camurus ABInventors: Fredrik Joabsson, Markus Johnsson, Fredrik Tiberg
-
Patent number: 8546327Abstract: Modified glucagon peptides are disclosed having enhanced potency at the glucagon receptor relative to native glucagon. Further modification of the glucagon peptides by forming intramolecular bridges or the substitution of the terminal carboxylic acid with an amide group produces peptides exhibiting glucagon/GLP-1 receptor co-agonist activity. The solubility and stability of these high potency glucagon analogs can be further improved by modification of the polypeptides by pegylation, acylation, alkylation, substitution of carboxy terminal amino acids, C-terminal truncation, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 26 (GPSSGAPPPS), SEQ ID NO: 27 (KRNRNNIA) and SEQ ID NO: 28 (KRNR).Type: GrantFiled: June 16, 2009Date of Patent: October 1, 2013Assignee: Indiana University Research and Technology CorporationInventors: Richard D. Dimarchi, David L. Smiley, Maria Dimarchi, Joseph Chabenne, Jonathan Day, James Patterson, Brian Ward
-
Patent number: 8536122Abstract: Protracted GLP-1 compounds and therapeutic uses thereof.Type: GrantFiled: March 5, 2012Date of Patent: September 17, 2013Assignee: Novo Nordisk A/SInventors: Jesper Lau, Florencio Zaragoza Doerwald, Paw Bloch, Thomas Kruse Hansen
-
Publication number: 20130217622Abstract: The present disclosure relates to an exendin-4 analogue PEGylated with polyethylene glycol or a derivative thereof, a preparation method, and a pharmaceutical composition for prevention or treatment of diabetes containing the same as an active ingredient. According to the present invention, the yield of an exendin-4 analogue can be increased via the selective PEGylation by using exendin-4 in which a cysteine is introduced into #40 site of the C-terminal, and treatment effect of medications can be increased, so that the exendin-4 analogue can be usefully applied as a composition for prevention or treatment of diseases caused by insulin hypersecretion.Type: ApplicationFiled: June 28, 2012Publication date: August 22, 2013Applicant: B & L DELIPHARM, CORP.Inventors: Sung Kwon Lee, Won Bae Kim, Seulki Lee, Tae Hyung Kim
-
Patent number: 8513188Abstract: This invention relates to the use of a cyclic compound of formula (I) wherein A, B independently in each occurrence is alkane-i,j-diyl having k carbon atoms, i and independently j being less than or equal k and k being selected from 1 to 10, wherein said alkane-i,j-diyl (i) may comprise one or more double bonds; (ii) is optionally substituted; and/or (iii) comprises a cycle, wherein the total number of cycles being cyclic sugars in said compound is selected from 0 to 4 and is less than p·(n+m); X,Y independently in each occurrence is a biocompatible functional group comprising at least one oxygen atom or two sulphur atoms; n, m independently of each other are selected from 0 to 20; p is selected from 1 to 10; n+m is equal or greater than 1; and p·(n+m) is selected from 3 to 30; wherein said compound is capable of forming a complex with a protonated primary and/or protonated secondary amino group and/or a protonated guanidinium group for the manufacture of a pharmaceutical or diagnostic composition.Type: GrantFiled: September 27, 2007Date of Patent: August 20, 2013Inventor: Paolo Botti
-
Publication number: 20130203673Abstract: 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: ApplicationFiled: March 11, 2013Publication date: August 8, 2013Applicants: 1149336 Ontario, Inc., NPS Pharmaceuticals, Inc.Inventors: NPS Pharmaceuticals, Inc., 1149336 Ontario, Inc.
-
Publication number: 20130203659Abstract: GLP-1 compounds comprising GLP-1 analogs and methods of using the GLP-1 compounds for treating metabolic disorders, enhancing insulin expression, and promoting insulin secretion in a patient are provided.Type: ApplicationFiled: October 15, 2012Publication date: August 8, 2013Inventors: Leslie P. MIRANDA, Katherine Ann WINTERS, Murielle VENIANT-ELLISON
-
Publication number: 20130203660Abstract: Modified glucagon peptides are disclosed having enhanced potency at the glucagon receptor relative to native glucagon. Further modification of the glucagon peptides by forming lactam bridges or the substitution of the terminal carboxylic acid with an amide group produces peptides exhibiting glucagon/GLP-1 receptor co-agonist activity. The solubility and stability of these high potency glucagon analogs can be further improved by modification of the polypeptides by pegylation, substitution of carboxy terminal amino acids, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 26 (GPSSGAPPPS), SEQ ID NO: 27 (KRNRNNIA) and SEQ ID NO: 28 (KRNR).Type: ApplicationFiled: January 9, 2013Publication date: August 8, 2013Applicant: Indiana University Research and Technology CorporationInventor: Indiana University Research and Technology Corporation
-
Patent number: 8497240Abstract: The present invention relates generally to novel GIP analogs and GIP hybrid polypeptides with selectable properties, useful as agents for the treatment and prevention of metabolic diseases and disorders, for example those which can be alleviated by control plasma glucose levels, insulin levels, and/or insulin secretion, positive inotropic effects, reduction of catabolic effects, slowing of gastric emptying. Such conditions and disorders include, but are not limited to, hypertension, dyslipidemia, cardiovascular disease, eating disorders, critical care, insulin-resistance, obesity, and diabetes mellitus of any kind, including type 1, type 2, and gestational diabetes.Type: GrantFiled: August 17, 2007Date of Patent: July 30, 2013Assignees: Amylin Pharmaceuticals, LLC, AstraZeneca Pharmaceuticals LPInventors: Odile Esther Levy, Alain D. Baron, Lawrence J. D'Souza, Mary Erickson, Soumitra S. Ghosh, Michael R. Hanley, Samuel Janssen, Carolyn M. Jodka, Diana Y. Lewis, Christine M. Mack, David G. Parkes, Richard A. Pittner, Christopher J. Soares, Ved Srivastava, Andrew A. Young, Thao Le
-
Publication number: 20130184203Abstract: The disclosure provides GLP-1 receptor agonist compounds having stabilized regions corresponding to alpha-helical regions of the natural peptide compounds. The disclosure also provides benzamide-containing exendin-4 analogs and alkene-constrained exendin-4 analogs, both of which have stabilized regions corresponding to alpha-helical regions of exendin-4.Type: ApplicationFiled: July 27, 2011Publication date: July 18, 2013Applicants: AstraZeneca Pharmaceuticals LP, Amylin Pharmaceuticals, LLCInventors: Josue Alfaro-Lopez, Abhinandini Sharma, Christopher J. Soares, Eugene Coats, Soumitra S. Ghosh
-
Publication number: 20130178416Abstract: Therapeutic compositions containing fusion proteins (FPs) including elastin-like peptides (ELPs) and peptide active therapeutic agents, and methods of making and using such compositions and fusion proteins. Therapeutic compositions of such type enable improved efficacy of the peptide active therapeutic agent to be achieved, in relation to the peptide active therapeutic agent alone. Enhanced efficacy of the peptide active therapeutic agent in the therapeutic composition may include improved solubility, bioavailability, bio-unavailability, half-life, etc., as compared to corresponding compositions containing the same peptide active therapeutic agent without associated ELPs.Type: ApplicationFiled: March 12, 2013Publication date: July 11, 2013Applicant: PHASEBIO PHARMACEUTICALS, INC.Inventor: PHASEBIO PHARMACEUTICALS, INC.
-
Publication number: 20130165624Abstract: Compounds which can include an active (drug) moiety have the general formula (I): wherein: SA is a pentapeptide aa1-aa2-aa3-aa4-aa5, wherein at least one of aa1, aa2, aa3, aa4, and aa5 is L, I, E, D, and I, respectively, wherein L, I, E, and D are eponymous amino acids; SB is a dipeptide aa6-aa7, wherein at least one of aa6 and aa7 is L and W, respectively, wherein W and L are eponymous amino acids; R1 and R5 are N-, and C-terminal moieties, respectively; R3 and R4 are independently a linker selected from a substituted or unsubstituted methylene, an amino acid, a peptide, and a peptide bond; and S is a scaffold moiety, a bond, a peptide bond, an amino acid, or a peptide of up to three residues, wherein R3, S, and R4 together form a turn in the compound, and the compound selectively binds a serum albumin.Type: ApplicationFiled: December 22, 2012Publication date: June 27, 2013Applicant: SRI INTERNATIONALInventor: Hendrik Mario Geysen
-
Publication number: 20130157929Abstract: The invention provides materials and methods for promoting weight loss or preventing weight gain and for treating diabetes and associated metabolic disorders. In particular, the invention provides novel glucagon analogue peptide compounds effective in such methods. The compounds may mediate their effect by having, for example, increased selectivity for the GLP-1 receptor compared to human glucagon.Type: ApplicationFiled: June 24, 2011Publication date: June 20, 2013Applicant: ZEALAND PHARMA A/SInventors: Ditte Riber, Eddi Meier
-
Publication number: 20130157935Abstract: The invention provides materials and methods for promoting weight loss or preventing weight gain without affecting glycemic control. 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: June 23, 2011Publication date: June 20, 2013Applicant: Zealand Pharma A/SInventors: Eddi Meier, Ditte Riber, Jens Rosengren Daugaard, Marie Skovgaard
-
Publication number: 20130157934Abstract: Provided herein are glucagon superfamily peptides conjugated with GR ligands that are capable of acting at a glucocorticoid receptor. Also provided herein are pharmaceutical compositions and kits of the conjugates of the invention. Further provided herein are methods of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the conjugates of the invention.Type: ApplicationFiled: November 16, 2012Publication date: June 20, 2013Applicant: Indiana University Research and Technology CorporationInventor: Indiana University Research and Technology Corp
-
Publication number: 20130143798Abstract: The present invention relates to novel peptide compounds which have an improved physical stability in solution and improved 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 compounds 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, 2011Publication date: June 6, 2013Applicant: NOVO NORDISK A/SInventors: Jesper F. Lau, Thomas Kruse, Lars Linderoth, Henning Thoegersen
-
Patent number: 8455433Abstract: Disclosed is a method of preparing a GLP-1 compound that is soluble in aqueous solution at pH 7.4 from a GLP-1 compound that is substantially insoluble in aqueous solution at pH 7.4. The insoluble GLP-1 compound is dissolved in aqueous base or in aqueous acid to form a GLP-1 solution. The GLP-1 solution is then neutralized to a pH at which substantially no amino acid racemization of the GLP-1 compounds occurs, after which the soluble GLP-1 compound is isolated from the neutralized solution.Type: GrantFiled: August 10, 2012Date of Patent: June 4, 2013Assignee: Eli Lilly and CompanyInventors: Walter Francis Prouty, Jr., Joseph Vincent Rinella, Jr.
-
Publication number: 20130123462Abstract: 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: ApplicationFiled: June 14, 2011Publication date: May 16, 2013Applicant: Indiana University Research and Technology CorporationInventors: Richard D. Dimarchi, Binbin Kou
-
Publication number: 20130123461Abstract: 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: ApplicationFiled: May 5, 2011Publication date: May 16, 2013Applicant: PROLYNX LLCInventors: Gary Ashley, Daniel V. Santi
-
Publication number: 20130123460Abstract: The present invention aims at providing a peptide fragment capable of improving biostability of a bioactive substance while maintaining the activity of the bioactive substance, and a bioactive substance to which the peptide fragment is added. The present invention relates to a partial peptide of a GA module having 5 to 25 amino acids, including a partial sequence of a GA module (SEQ ID NO: 1) and the amino acid sequence Ile-Asp-Glu-Ile-Leu (SEQ ID NO: 2), and a bioactive complex in which the partial peptide of the GA module is bound to a bioactive substance. The bioactive substance includes GLP-1, GLP-2, GIP, VIP, somatostatin, amylin, ghrelin, derivatives thereof, and the like.Type: ApplicationFiled: April 28, 2011Publication date: May 16, 2013Applicant: SANWA KAGAKU KENKYUSHO CO., LTD.Inventors: Masayuki Okamoto, Ryuhji Okamoto, Tomohiro Shigemori, Takayo Murase, Atsushi Miyachi, Mitsuaki Takeuchi, Miyuki Tamura, Hiroshi Kinoshita
-
Publication number: 20130123178Abstract: Provided herein are glucagon superfamily peptides conjugated with NHR ligands that are capable of acting at a nuclear hormone receptor. Also provided herein are pharmaceutical compositions and kits of the conjugates of the invention. Further provided herein are methods of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the conjugates of the invention.Type: ApplicationFiled: May 10, 2011Publication date: May 16, 2013Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATIONInventors: Richard D. DiMarchi, Bin Yang, Brian Finan
-
Publication number: 20130116173Abstract: 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: December 27, 2012Publication date: May 9, 2013Applicant: Indiana University Research and Technology CorporationInventor: Indiana University Research and Technology Corporation
-
Publication number: 20130116172Abstract: Provided herein are glucagon superfamily peptides conjugated with GPCR ligands that are capable of acting at a G protein-coupled receptor. Also provided herein are pharmaceutical compositions and kits of the conjugates of the invention. Further provided herein are methods of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the conjugates of the invention.Type: ApplicationFiled: May 10, 2011Publication date: May 9, 2013Applicant: MARCADIA BIOTECH, INC.Inventors: Richard D. Dimarchi, Lianshan Zhang
-
Publication number: 20130096060Abstract: The present invention relates to a pharmaceutical composition for use in the treatment of a disease or condition, wherein said disease or condition is associated with stenosis or/and obstruction located in the pancreatic duct system, said composition comprising at least one GLP-1 agonist and optionally a pharmaceutically acceptable carrier, diluent or/and auxiliary substance.Type: ApplicationFiled: October 2, 2012Publication date: April 18, 2013Inventors: Jens STECHL, Irene NOWOTNY, Claudia PFEIFFER, Jean-Louis PINQUIER, Jerome MSIHID
-
Publication number: 20130095037Abstract: In the current invention peptides, which are derived from GLP-1 (glucagon-like peptide-1) and exendin-3 and/or exendin-4, are provided which bond to the GLP-1 receptor and can be used, labeled or unlabeled, for the production of an agent for diagnostic and therapy of benign and malignant diseases, in which GLP-1 receptor expression plays a role.Type: ApplicationFiled: August 24, 2012Publication date: April 18, 2013Applicant: Philipps-Universitat MarburgInventors: Martin GOTTHARDT, Martin Béhé, Thomas Behr, Burkhard J. Göke
-
Publication number: 20130096059Abstract: The present invention relates to a pharmaceutical composition for use in the treatment of a disease or condition, wherein said disease or condition is associated (a) stenosis or/and obstruction located in the biliary tract, or/and (b) biliary dyskinesia, said composition comprising at least one GLP-1 agonist and optionally a pharmaceutically acceptable carrier, diluent or/and auxiliary substance.Type: ApplicationFiled: October 2, 2012Publication date: April 18, 2013Inventors: Jens STECHL, Irene NOWOTNY, Claudia PFEIFFER, Jean-Louis PINQUIER, Jerome MSIHID
-
Patent number: 8420598Abstract: Disclosed herein are exendin singly modified with polyethylene glycole or a derivative thereof, a method for the preparation of the same, and uses thereof. Exendin modified at lysine (27) with polyethylene glycol shows biological activity similar to that of natural exendin, but is improved in half life. In addition, the modification position and the number of PEG or its derivative are restricted so as to minimize the side effects caused by a variety of combinations of such factors. The exendin is useful in the prevention and treatment of diseases caused by the over-secretion of insulin, or diseases caused due to a decrease in plasma glucose level, the inhibition of gastric or intestinal motility, the promotion of satiety, or the inhibition of food intake, especially diabetes, obesity and irritable colon syndrome.Type: GrantFiled: April 20, 2007Date of Patent: April 16, 2013Assignee: B & L Delipharm Corp.Inventors: Kang Choon Lee, Chan Woong Park, Yu Seok Youn, Su Young Chae
-
Publication number: 20130090286Abstract: Modified glucagon peptides are disclosed having enhanced potency at the glucagon receptor relative to native glucagon. Further modification of the glucagon peptides by forming intramolecular bridges or the substitution of the terminal carboxylic acid with an amide group produces peptides exhibiting glucagon/GLP-1 receptor co-agonist activity. The solubility and stability of these high potency glucagon analogs can be further improved by modification of the polypeptides by pegylation, acylation, alkylation, substitution of carboxy terminal amino acids, C-terminal truncation, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 26 (GPSSGAPPPS), SEQ ID NO: 27 (KRNRNNIA) and SEQ ID NO: 28 (KRNR).Type: ApplicationFiled: August 6, 2012Publication date: April 11, 2013Inventors: Elisabetta Bianchi, Antonello Pessi, Jonathan Day, Richard Dimarchi, David Smiley
-
Publication number: 20130079278Abstract: The present invention relates to novel glucagon peptides, to the use of said glucagon peptides in therapy, to methods of treatment comprising administration of said glucagon peptides to patients in need thereof, and to the use of said glucagon peptides in the manufacture of medicaments. The glucagon peptides of the present 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: September 21, 2012Publication date: March 28, 2013Applicant: NOVO NORDISK A/SInventor: Novo Nordisk A/S
-
Publication number: 20130072658Abstract: Disclosed is a method of preparing a GLP-1 compound that is soluble in aqueous solution at pH 7.4 from a GLP-1 compound that is substantially insoluble in aqueous solution at pH 7.4. The insoluble GLP-1 compound is dissolved in aqueous base or in aqueous acid to form a GLP-1 solution. The GLP-1 solution is then neutralized to a pH at which substantially no amino acid racemization of the GLP-1 compounds occurs, after which the soluble GLP-1 compound is isolated from the neutralized solution.Type: ApplicationFiled: August 10, 2012Publication date: March 21, 2013Applicant: ELI LILLY AND COMPANYInventors: Walter Francis Prouty, JR., Joseph Vincent Rinella, JR.
-
Publication number: 20130059780Abstract: The present invention provides polypeptides that include an O-linked glycoconjugate in which a species such as a water-soluble polymer, a therapeutic agent of a biomolecule is covalently linked through an intact O-linked glycosyl residue to the polypeptide. The polypeptides of the invention include wild-type peptides and mutant peptides that include an O-linked glycosylation site that is not present in the wild-type peptide. Also provided are methods of making the peptides of the invention and methods, pharmaceutical compositions containing the peptides and methods of treating, ameliorating or preventing diseased in mammals by administering an amount of a peptide of the invention sufficient to achieve the desired response.Type: ApplicationFiled: July 3, 2012Publication date: March 7, 2013Applicant: BIOGENERIX AGInventor: Shawn DeFrees
-
Patent number: 8389473Abstract: 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: GrantFiled: March 30, 2010Date of Patent: March 5, 2013Assignees: Amylin Pharmaceuticals, LLC, AstraZeneca Pharmaceuticals LPInventors: David R. Hathaway, Alain D. Baron
-
Publication number: 20130052130Abstract: Disclosed are general and “substantially pure” branched discrete polyethylene glycol constructs useful in attaching to a variety of biologically active groups, for example, preferential locators, as well as biologics like enzymes, for use in diagnostics, e.g. imaging, therapeutics, theranostics, and moieties specific for other applications. In its simplest intermediate state, a branched discrete polyethylene glycol construct is terminated at one end by a chemically reactive moiety, “A”, a group that is reactive with a biologic material that creates “A”, which is a biologically reactive group, connected through to a branched core (BC) which has attached at least two dPEG-containing chains, indicated by the solid line, , having terminal groups, which can be charged, non-reactive or reactable moieties and containing between about 2 and 64 dPEG residues.Type: ApplicationFiled: August 30, 2012Publication date: February 28, 2013Applicants: UNIVERSITY OF WASHINGTON, QUANTA BIODESIGN, LTD.Inventors: Paul D. Davis, D. Scott Wilbur
-
Publication number: 20130053310Abstract: The present invention relates to glucagon peptide agonists which have improved solubility and stability, to the use of the peptides in therapy, to methods of treatment comprising administration of the peptides to patients in need thereof, and to the use of the peptides in the manufacture of medicaments. The glucagon peptides of the invention are of particular interest in relation to the treatment of hypoglycemia, diabetes and obesity, as well as a variety of diseases or conditions associated with hypoglycemia, diabetes and obesity.Type: ApplicationFiled: March 28, 2011Publication date: February 28, 2013Applicant: NOVO NORDISK A/SInventors: Jesper F. Lau, Thomas Kruse
-
Publication number: 20130053315Abstract: Novel polypeptide derivatives having protracted profile of action.Type: ApplicationFiled: March 22, 2012Publication date: February 28, 2013Inventors: Jesper Lau, Thomas Kruse Hansen, Kjeld Madsen, Paw Bloch, Florencio Zaragoza Dorwald, Nils Langeland Johansen
-
Publication number: 20130053301Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof, comprising a drug linker conjugate D-L, wherein D being a biologically active moiety containing an aliphatic amine group is conjugated to one or more polymeric carriers via dipeptide-containing linkers L. Such carrier-linked prodrugs achieve drug releases with therapeutically useful half-lives. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.Type: ApplicationFiled: January 21, 2011Publication date: February 28, 2013Applicant: Ascendis Pharma A/SInventors: Harald Rau, Torben Lessmann
-
Publication number: 20130053304Abstract: Provided is a glucagon-like peptide-1 (GLP-1) analogue shown as the following formula, wherein X is selected from glycine and glycinamide. The GLP-1 analogue has a non-proteogenic amino acid residue in position 8 relative to the sequence GLP-1, and is acylated with a moiety comprising two acidic groups to the lysine residue in position 26. The GLP-1 analogue is resistant to dipeptidyl peptidase IV so as to have an extended half-life in vivo. Also provided is a use of the GLP-1 analogue in conquering blood sugar.Type: ApplicationFiled: April 29, 2011Publication date: February 28, 2013Inventors: Yinxiang Wang, Fenlai Tan, Shaojing Hu, Xiangdong Zhao, Cunbo Ma, Yanping Wang, Xiaoyan Shen, Lieming Ding, Yunyan Hu, Hong Cao, Wei Long
-
Publication number: 20130053311Abstract: The invention relates to a GLP-1 analogue 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 analogues 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: ApplicationFiled: December 16, 2010Publication date: February 28, 2013Applicant: Novo Nordisk A/SInventors: Christoph Kalthoff, Jesper Lau, Jane Spetzler, Patrick William Garibay, Jacob Kofoed, Lars Linderoth
-
Patent number: 8377869Abstract: A method for preventing or reducing adverse effects such as profuse sweating, nausea and vomiting, which normally are associated with subcutaneous and intravenous administration of glucagon-like peptide 1 (GLP-1) therapy is provided. In particular, the method comprises the rapid administration of a GLP-1 formulation into the pulmonary circulation such as by inhalation, directly into pulmonary alveolar capillaries using a dry powder drug delivery system.Type: GrantFiled: October 24, 2008Date of Patent: February 19, 2013Assignee: MannKind CorporationInventors: Peter Richardson, Robert A. Baughman, Donald Costello
-
Publication number: 20130040884Abstract: Novel polypeptide derivatives having protracted profile of action.Type: ApplicationFiled: March 22, 2012Publication date: February 14, 2013Inventors: Jesper Lau, Thomas Kruse Hansen, Kjeld Madsen, Paw Bloch, Florencio Zaragoza Dorwald, Nils Langeland Johansen
-
Publication number: 20130035285Abstract: The present invention relates to novel peptide compounds which have a protracted profile of action and improved solubility and stability, 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 compounds 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, 2011Publication date: February 7, 2013Applicant: Novo Nordisk A/SInventors: Jesper F. Lau, Thomas Kruse, Lars Linderoth, Henning Thoegersen, Jacob Kofoed, Kirsten Dahl
-
Patent number: 8367607Abstract: The present invention provides an Oxyntomodulin peptide analogue useful in the treatment of diabetes and/or obesity.Type: GrantFiled: December 15, 2010Date of Patent: February 5, 2013Assignee: Eli Lilly and CompanyInventors: Jorge Alsina-Fernandez, Wayne David Kohn