Peptide Hormone Or Derivative Utilizing Patents (Class 514/5.3)
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Publication number: 20140018291Abstract: Methods are provided for administering an extended half-life GLP-1/GIP coagonist peptide to a patient in need thereof for reducing weight gain, inducing weight loss, treating hyperglycemia, reducing blood glucose levels, or normalizing blood glucose levels in said patient.Type: ApplicationFiled: December 22, 2011Publication date: January 16, 2014Applicant: MARCADIA BIOTECH, INC.Inventors: Louis Vignati, Richard D. Dimarchi
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Publication number: 20140011738Abstract: Provided herein are glucagon analogs which exhibit potent activity at the GIP receptor, and, as such are contemplated for use in treating diabetes and obesity. In exemplary embodiments, the glucagon analog of the present disclosures exhibit an EC50 at the GIP receptor which is within the nanomolar or picomolar range.Type: ApplicationFiled: June 18, 2013Publication date: January 9, 2014Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATIONInventor: Richard D. DiMARCHI
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Publication number: 20140011733Abstract: The invention relates to methods for treating metabolic disorders, including diabetes by using a combination of an acylated glucagon analogue and an insulin analogue. The invention also features a kit that includes an acylated glucagon analogue and an insuline analogue.Type: ApplicationFiled: January 20, 2012Publication date: January 9, 2014Applicant: Zealand Pharma A/SInventors: Keld Fosgerau, Ditte Riber
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Publication number: 20140005106Abstract: The invention relates to formulations that demonstrate the feasibility of oral absorption comprising glucose-like peptide-1 compounds and specified delivery agents, and to methods of stimulating GLP-1 receptor in a subject in need of such stimulation, by administration of the formulation of the present invention.Type: ApplicationFiled: July 16, 2013Publication date: January 2, 2014Applicant: Emisphere Technologies, Inc.Inventors: Mohammed Amin KHAN, Bryan Edward Jones, John Mcneill McGill
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Publication number: 20130331317Abstract: The present invention relates to a chimeric protein that includes an N-terminus coupled to a C-terminus, where the N-terminus includes a portion of a paracrine fibroblast growth factor (“FGF”) and the C-terminus includes a C-terminal portion of an FGF19 molecule. The portion of the paracrine FGF is modified to decrease binding affinity for heparin and/or heparan sulfate compared to the portion without the modification. The present invention also relates to pharmaceutical compositions including chimeric proteins according to the present invention, methods for treating a subject suffering from diabetes, obesity, or metabolic syndrome, and methods of screening for compounds with enhanced binding affinity for the ?Klotho-FGF receptor complex involving the use of chimeric proteins of the present invention.Type: ApplicationFiled: March 15, 2013Publication date: December 12, 2013Applicant: New York UniversityInventors: Moosa MOHAMMADI, Regina Goetz
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Publication number: 20130331316Abstract: The present invention relates to a chimeric protein that includes an N-terminus coupled to a C-terminus, where the N-terminus includes a portion of a paracrine fibroblast growth factor (“FGF”) and the C-terminus includes a C-terminal portion of an FGF21 molecule. The portion of the paracrine FGF is modified to decrease binding affinity for heparin and/or heparan sulfate compared to the portion without the modification. The present invention also relates to pharmaceutical compositions including chimeric proteins according to the present invention, methods for treating a subject suffering from diabetes, obesity, or metabolic syndrome, and methods of screening for compounds with enhanced binding affinity for the ?Klotho-FGF receptor complex involving the use of chimeric proteins of the present invention.Type: ApplicationFiled: March 15, 2013Publication date: December 12, 2013Applicant: New York UniversityInventors: Moosa MOHAMMADI, Regina GOETZ
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Publication number: 20130324463Abstract: The present invention relates to the use of a certain DPP-4 inhibitor for modifying food intake and regulating food preference.Type: ApplicationFiled: May 21, 2013Publication date: December 5, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thomas KLEIN, Michael MARK
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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
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Publication number: 20130303436Abstract: Disclosed herein are methods and compositions for the treatment and/or prevention of diseases or conditions comprising administration of GLP-1, and/or naturally or artificially occurring variants or analogues of GLP-1, or pharmaceutically acceptable salts thereof, alone or in combination with one or more active agents (e.g., an aromatic-cationic peptide such as D-Arg-2?6?-Dmt-Lys-Phe-NH2).Type: ApplicationFiled: April 11, 2013Publication date: November 14, 2013Inventor: D. Travis WILSON
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Publication number: 20130288958Abstract: 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: July 9, 2013Publication date: October 31, 2013Inventors: Jesper F. Lau, Thomas Kruse, Henning Thoegersen, Ulrich Sensfuss, Peter Kresten Nielsen
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Publication number: 20130274182Abstract: Compounds are provided having inter alia good duration of action, high potency and/or convenient dosing regimens including once weekly administration. The compounds are engineered polypeptides which incorporate an albumin binding domain in combination with one or more biologically active polypeptides. Also provided are pharmaceutical compositions and methods of treatment for diseases and disorders including lipodystrophy, dyslipidemia, hyperlipidemia, overweight, obesity, hypothalamic amenorrhea, Alzheimer's disease, leptin deficiency, fatty liver disease or diabetes (including type I and type II). Additional diseases and disorders which can be treated by the compounds and methods described herein include nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD), metabolic syndrome X and Huntington's Disease.Type: ApplicationFiled: March 28, 2013Publication date: October 17, 2013Inventors: Mary Erickson, David C. Litzinger, Soumitra S. Ghosh, Zijian Guo, Jonathan David Roth
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Patent number: 8557765Abstract: Novel spatially-defined macrocyclic compounds incorporating peptide bond surrogates are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle species that exhibit a specific interaction with a particular biological target. In particular, compounds according to the invention are disclosed as agonists or antagonists of a mammalian motilin receptor and a mammalian ghrelin receptor.Type: GrantFiled: May 26, 2009Date of Patent: October 15, 2013Assignee: Tranzyme Pharma Inc.Inventors: Pierre Deslongchamps, Yves Dory, Luc Ouellet, Gérald Villeneuve, Mahesh Ramaseshan, Daniel Fortin, Mark L. Peterson, Hamid R. Hoveyda, Sylvie Beaubien, Éric Marsault, Graeme L. Fraser
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Publication number: 20130261051Abstract: The present invention relates to methods for treatment of a condition or disease where administration of insulin will be of benefit, comprising administering, to a patient in need thereof, effective dosages of an insulin, insulin analogue or derivative thereof, which exhibits a prolonged profile of action, wherein said dosages are administered at intervals of varying length.Type: ApplicationFiled: October 27, 2011Publication date: October 3, 2013Inventor: Thue Johansen
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Patent number: 8541368Abstract: 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: GrantFiled: September 21, 2012Date of Patent: September 24, 2013Assignee: Novo Nordisk A/SInventors: Jesper F. Lau, Thomas Kruse, Henning Thoegersen, Ulrich Sensfuss, Peter Kresten Nielsen
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Patent number: 8536120Abstract: The present invention provides novel compounds that have been demonstrated to be modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, iso forms and variants thereof). These compounds are useful as antagonists of the ghrelin receptor as well as inverse agonist, partial agonist or a combination of these activities as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, diabetes, central nervous system disorders, genetic disorders, and hyperproliferative disorders.Type: GrantFiled: April 30, 2007Date of Patent: September 17, 2013Assignee: The Administrators of The Tulane Educational FundInventors: Cyril Y. Bowers, Gloria S. Tannenbaum, David H. Coy, Simon J. Hocart
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Publication number: 20130231279Abstract: The disclosure provides a method for enhancing memory of a subject, lowering blood glucose levels in a subject, and treating schizophrenia, the methods comprise intranasally administering to the subject an amount of a oxytocin peptide or analogue thereof having a beneficial effect.Type: ApplicationFiled: July 30, 2011Publication date: September 5, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventor: David Feifel
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Publication number: 20130225487Abstract: Compounds of Formula (A) and (B) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by sodium-glucose transporter inhibitors (in particular, SGLT2 inhibitors).Type: ApplicationFiled: March 12, 2013Publication date: August 29, 2013Applicant: Pfizer Inc.Inventor: Pfizer Inc.
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Publication number: 20130225485Abstract: Compositions and methods for preventing, treating or controlling conditions or disorders associated with obesity, diet and nutrition are provided. The methods provided generally involve the administration of an Amylin or an Amylin agonist to a subject in order to prevent, treat or control conditions or disorders associated with obesity, diet and nutrition.Type: ApplicationFiled: September 28, 2012Publication date: August 29, 2013Applicant: Amylin Pharmaceuticals, LLCInventor: Amylin Pharmaceuticals, LLC
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Patent number: 8507428Abstract: 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: GrantFiled: December 20, 2011Date of Patent: August 13, 2013Assignee: Indiana University Research and Technology CorporationInventors: Richard D. DiMarchi, Brian P. Ward
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Publication number: 20130203651Abstract: The invention is directed to a pharmaceutical composition containing at least one FGF-21 (fibroblast growth factor 21) compound, at least one GLP-1R (glucagon-like peptide-1 receptor) agonist and optionally at least one anti-diabetic drug and/or at least one DPP-4 (dipeptidyl peptidase-4) inhibitor for the treatment of at least one metabolic syndrome and/or atherosclerosis, in particular diabetes, dyslipidemia, obesity and/or adipositas.Type: ApplicationFiled: January 21, 2011Publication date: August 8, 2013Applicant: SANOFIInventors: Mark Sommerfeld, Hans-Ludwig Schaefer, Oliver Boscheinen, Paul Habermann, Ercole Rao, Matthias Dreyer
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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
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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
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Publication number: 20130203661Abstract: The disclosure provides chimeric polypeptides and nucleic acid molecules encoding chimeric polypeptides. Also provided are pharmaceutical compositions and methods of treatment for diseases and disorders including lipodystrophy, dyslipidemia, hyperlipidemia, overweight, obesity, hypothalamic amenorrhea, Alzheimer's disease, leptin deficiency, fatty liver disease or diabetes (including type I and type II). Additional diseases and disorders which can be treated by the compounds and methods described herein include nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD), metabolic syndrome X and Huntington's Disease.Type: ApplicationFiled: March 28, 2013Publication date: August 8, 2013Applicants: ASTRAZENECA PHARMACEUTICALS LP, Amylin Pharmaceuticals, LLCInventors: Amylin Pharmaceuticals, LLC, ASTRAZENECA PHARMACEUTICALS LP
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Publication number: 20130196898Abstract: The present invention relates to methods for preventing or treating of metabolic disorders and related conditions, such as in certain patient groups.Type: ApplicationFiled: November 26, 2010Publication date: August 1, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Klaus Dugi, Eva Ulrike Graefe-Mody, Michael Mark, Hans-Juergen Woerle, Heike Zimdahl-Gelling
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Publication number: 20130183385Abstract: A peptide having a sequence selected from SEQ ID NO:11, SEQ ID NO:12, SEQ ID NO:13, SEQ ID NO:14, SEQ ID NO:15, SEQ ID NO:16, SEQ ID NO:17 and SEQ ID NO:18. Said peptide used for the treatment of type I diabetes, Type II diabetes, metabolic syndrome, or obesity, or of apetite suppression, or for mitigating insulin resistance, or for reducing an undesirably high fasting serum glucose level, or for reducing an undesirably high peak serum glucose level, or for reducing an undesirably high peak serum insulin level, or for reducing an undesirably large response to a glucose tolerance test.Type: ApplicationFiled: November 2, 2012Publication date: July 18, 2013Applicant: NU-CO DEVELOPMENT GMBHInventor: NU-CO DEVELOPMENT GMBH
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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
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Publication number: 20130184199Abstract: Compositions and methods for modulating the deposition of elastin by administering compositions including insulin receptor agonists are described herein.Type: ApplicationFiled: January 7, 2013Publication date: July 18, 2013Applicants: HUMAN MATRIX SCIENCES, LLCInventors: HUMAN MATRIX SCIENCES, LLC, THE HOSPITAL FOR SICK CHILDREN
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Publication number: 20130172243Abstract: Methods for reducing body weight, altering body composition, treating diabetes, reducing HbA1c and reducing average daily blood glucose by the use of exendins, exendin agonists or exendin analog agonists are provided.Type: ApplicationFiled: December 7, 2012Publication date: July 4, 2013Applicant: Amylin Pharmaceuticals, LLCInventor: Amylin Pharmaceuticals, LLC
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Publication number: 20130172244Abstract: The present invention relates to methods for treating and/or preventing metabolic diseases comprising the subcutaneous or transdermal administration of a therapeutically effective amount of a certain DPP-4 inhibitor. The invention further relates to a subcutaneous combination of a certain DPP-4 inhibitor and GLP-1 having a short half life, particularly for reducing weight.Type: ApplicationFiled: December 27, 2012Publication date: July 4, 2013Inventors: Thomas KLEIN, Michael MARK
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Publication number: 20130157936Abstract: A method and a composition for decreasing ghrelin levels and/or decreasing ghrelin/unacylated ghrelin ratio in a subject, the method comprising administering an effective amount of unacylated ghrelin, a fragment thereof, an analog thereof and/or pharmaceutically acceptable salts thereof to the subject wherein a reduction in ghrelin levels and/or a reduction in ghrelin/unacylated ghrelin ratio is beneficial to the subject. Also, use of ghrelin level and/or ghrelin/unacylated ghrelin ratio as biomarkers for determining a subject's likelihood of responding to and/or benefiting from administration of unacylated ghrelin.Type: ApplicationFiled: December 14, 2012Publication date: June 20, 2013Applicant: ALIZÉ PHARMA SASInventor: Alizé Pharma Sas
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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
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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
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Publication number: 20130157933Abstract: The present invention encompasses albumin fusion proteins. Nucleic acid molecules encoding the albumin fusion proteins of the invention are also encompassed by the invention, as are vectors containing these nucleic acids, host cells transformed with these nucleic acids vectors, and methods of making the albumin fusion proteins of the invention and using these nucleic acids, vectors, and/or host cells. Additionally the present invention encompasses pharmaceutical compositions comprising albumin fusion proteins and methods of treating or preventing diseases, disorders or conditions related to diabetes mellitus using albumin fusion proteins of the invention.Type: ApplicationFiled: April 1, 2011Publication date: June 20, 2013Inventors: Craig A. Rosen, William A. Haseltine, Steven M. Ruben
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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
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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
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Publication number: 20130137631Abstract: 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: ApplicationFiled: August 22, 2012Publication date: May 30, 2013Applicant: Amylin Pharmaceuticals, LLCInventors: Odile Esther LEVY, Alain D. Baron, Lawrence J. D'Souza, Mary Erickson, Soumitra G. 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
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Publication number: 20130137629Abstract: Various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis can be treated with a compound selected from an incretin mimetic and a dipeptidyl peptidase IV inhibitor in combination with a Compound of Formula I or a pharmaceutically acceptable salt thereof Three of R1, R2, R3, R4 and R5 are hydrogen and the remainder are independently selected from the group consisting of hydrogen, halo, hydroxy, methyl, ethyl, perfluoromethyl, methoxy, ethoxy, and perfluoromethoxy; and m is 0, 2 or 4. R6 is hydrogen, O or hydroxy, and X is —OR7, wherein R7 is hydrogen or alkyl having from 1 to 3 carbon atoms; or R6 is hydrogen, and X is —NR8R9, wherein R8 is hydrogen or hydroxy and R9 is hydrogen, methyl or ethyl. When X is —NR8R9, hydroxy none of R1, R2, R3, R4 and R5 is hydroxy.Type: ApplicationFiled: January 24, 2013Publication date: May 30, 2013Applicant: WELLSTAT THERAPEUTICS CORPORATIONInventor: WELLSTAT THERAPEUTICS CORPORATION
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Publication number: 20130133089Abstract: Leptin muteins, in particular leptin antagonists, with increased binding affinity to leptin receptor are provided. These compounds as well as pharmaceutical composition comprising them are useful for the treatment of any disorder in which a non-desirable or deleterious activity of endogenous leptin or an altered innate immune response is implicated.Type: ApplicationFiled: April 17, 2011Publication date: May 23, 2013Applicants: THE MEDICAL RESEARCH, INFRASTRUCTURE, AND HEALTH SERVICES FUND OF THE TEL-AVIV, YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEMInventors: Arieh Gertler, Eran Elinav, Zamir Halpern
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Patent number: 8445439Abstract: The present invention provides an itch suppressant containing cholecystokinin 2 receptor agonist such as a peptide having an amino acid sequence homologous with a partial amino acid sequence of at least seven C-terminal amino acids of the peptide having the amino acid sequence represented by SEQ:ID No. 1 as an active ingredient as a rapid-acting itch suppressant effective in treating skin illnesses associated with strong itch such as atopic dermatitis having few side effects. [SEQ:?ID?No.Type: GrantFiled: October 22, 2010Date of Patent: May 21, 2013Assignee: University of Occupational and Environmental Health, JapanInventors: Yoshiki Tokura, Shoko Fukamachi
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Publication number: 20130123170Abstract: Disclosed are peptide and peptidomimetic compounds generally according to formula (I) that are useful as GHRP analogs: R1-A1-A2-A3-A4-A5-R2??(I) wherein: A1 is Aib, Apc or Inp; A2 is D-Bal, D-Bip, D-Bpa, D-Dip, D-1Nal, D-2Nal, D-Ser(Bzl), or D-Trp; A3 is D-Bal, D-Bip, D-Bpa, D-Dip, D-1Nal, D-2Nal, D-Ser(Bzl), or D-Trp; A4 is 2Fua, Orn, 2Pal, 3Pal, 4Pal, Pff, Phe, Pim, Taz, 2Thi, 3Thi, Thr(Bzl); A5 is Apc, Dab, Dap, Lys, Orn, or deleted; R1 is hydrogen, (C1-6)alkyl, (C5-14)aryl, (C1-6)alkyl(C5-14)aryl, (C3-8)cycloakyl, or (C2-10)acyl; and R2 is OH or NH2; and pharmaceutical compositions and methods of use thereof.Type: ApplicationFiled: January 4, 2013Publication date: May 16, 2013Applicant: Ipsen Pharma, S.A.S.Inventor: Ipsen Pharma, S.A.S.
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Publication number: 20130123169Abstract: The present invention provides peptidomimetic macrocycles capable of modulating growth hormone levels and methods of using such macrocycles for the treatment of disease.Type: ApplicationFiled: October 18, 2012Publication date: May 16, 2013Applicant: Aileron Therapeutics, Inc.Inventor: Aileron Therapeutics, Inc.
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Publication number: 20130118491Abstract: A method of introducing a physiologically-active agent into the circulatory system of a mammal is disclosed herein. The method utilizes a rapid drug delivery system which prevents deactivation or degradation of the active agent being administered to a patient in need of treatment. In particular, the drug delivery system is designed for pulmonary drug delivery such as by inhalation, for delivery of the active agents such as proteins and peptides to the pulmonary circulation in a therapeutically effective manner avoiding degradation of the active agents in peripheral and vascular tissue before reaching the target site.Type: ApplicationFiled: January 9, 2013Publication date: May 16, 2013Applicant: MannKind CorporationInventor: MannKind Corporation
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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
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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
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Publication number: 20130102528Abstract: The present invention relates to a compound which is an agonist of the oxytocin receptor o for use in the treatment of a feeding disorder with early-onset. In a particular embodiment, the agonist of the oxytocin receptor is the oxytocin or an active fragment thereof.Type: ApplicationFiled: May 25, 2011Publication date: April 25, 2013Applicants: CHU DE TOULOUSE, UNIVERSITE DE LA MEDITERRANEEInventors: Francoise Muscatelli, Maithe Tauber, Fabienne Schaller, Denise Thuilleaux
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Publication number: 20130096050Abstract: This invention relates to novel compositions comprising analogs of naturally occurring polypeptides, wherein the analog comprises an a-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. The compositions and methods of this invention are particularly useful to identify novel therapeutic modulators of in-vivo receptor activity with extended half-lives and relevant bioactivity as compared to the naturally translated polypeptides upon which the analogs are derived.Type: ApplicationFiled: April 22, 2011Publication date: April 18, 2013Applicant: Longevity Biotech, Inc.Inventor: Scott J Shandler
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Publication number: 20130089545Abstract: The invention provides a peptide comprising the amino acid sequence given below, together with uses of the peptide and methods associated therewith. The peptide finds particular use as an appetite suppressant and in the treatment of obesity.Type: ApplicationFiled: September 22, 2011Publication date: April 11, 2013Inventor: Stephen Robert Bloom
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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
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Publication number: 20130090285Abstract: The invention provides methods for treating diabetes or obesity, as well as methods for inducing weight loss, preventing weight gain, or controlling weight in a patient in need thereof. The methods comprise administering to the patient at least one effective dose of a GLP-1 receptor agonist, or a regimen of GLP-1 receptor agonist comprising a plurality of substantially evenly spaced doses. The effective dose or regimen does not induce substantial nausea or appetite suppression in the patient.Type: ApplicationFiled: June 27, 2012Publication date: April 11, 2013Applicant: PHASEBIO PHARMACEUTICALS, INC.Inventors: Lynne M. Georgopoulos, Susan Arnold
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Publication number: 20130090287Abstract: The present invention relates to osmotic delivery devices, formulations, and methods for delivery of two or more beneficial agents. In one aspect, the present invention provides osmotic delivery devices useful for substantially concurrent administration of two or more beneficial agents. In another aspect, the present invention provides beneficial agent formulations for use in the osmotic delivery devices. The formulations include formulations wherein beneficial agents are soluble in the vehicle, suspension formulations comprising particle formulations of one or more beneficial agent, and combinations thereof. Further, methods for treatment of a variety of diseases or conditions using two or more beneficial agents are disclosed, wherein the methods are preferably practiced using the osmotic delivery devices and/or formulations of the invention.Type: ApplicationFiled: November 29, 2012Publication date: April 11, 2013Applicant: INTARCIA THERAPEUTICS, INC.Inventors: Thomas R. Alessi, Karling Alice Leung, Ryan D. Mercer, Cristina G. Negulescu, Catherine M. Rohloff, Bing Yang