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WO2011038900A3 - Peptide analogues of glucagon for diabetes therapy - Google Patents

Peptide analogues of glucagon for diabetes therapy Download PDF

Info

Publication number
WO2011038900A3
WO2011038900A3 PCT/EP2010/005943 EP2010005943W WO2011038900A3 WO 2011038900 A3 WO2011038900 A3 WO 2011038900A3 EP 2010005943 W EP2010005943 W EP 2010005943W WO 2011038900 A3 WO2011038900 A3 WO 2011038900A3
Authority
WO
WIPO (PCT)
Prior art keywords
amino acid
glucagon
optionally
terminal
peptide analogues
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/EP2010/005943
Other languages
French (fr)
Other versions
WO2011038900A2 (en
Inventor
Finbarr Paul Mary O'harte
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Ulster University
Original Assignee
Ulster University
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ulster University filed Critical Ulster University
Publication of WO2011038900A2 publication Critical patent/WO2011038900A2/en
Publication of WO2011038900A3 publication Critical patent/WO2011038900A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575—Hormones
    • C07K14/605—Glucagons
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biophysics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Biochemistry (AREA)
  • Toxicology (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Endocrinology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

The present invention concerns a peptide analogue of glucagon that is further modified by one or more of the following modifications: (i) deletion of at least one amino acid, optionally selected from His1 and Phe6; (ii) at least one substitution of an L- or D- amino acid for the corresponding wild-type amino acid, optionally at one or more of positions 3, 4, 5, 6 and 9; (iii) a C-terminal modification selected from amidation of the C- terminal Thr29; (iv) PEGylation of the C-terminal Thr29; and (v) addition of an L- or D- amino acid, optionally Lys, to the C-terminal Thr29, as well as pharmaceutical compositions containing them and their use in methods of treating diabetes.
PCT/EP2010/005943 2009-09-29 2010-09-29 Peptide analogues of glucagon for diabetes therapy Ceased WO2011038900A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0917072A GB0917072D0 (en) 2009-09-29 2009-09-29 Peptide analogues of glucagon for diabetes therapy
GB0917072.1 2009-09-29

Publications (2)

Publication Number Publication Date
WO2011038900A2 WO2011038900A2 (en) 2011-04-07
WO2011038900A3 true WO2011038900A3 (en) 2011-06-23

Family

ID=41350545

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2010/005943 Ceased WO2011038900A2 (en) 2009-09-29 2010-09-29 Peptide analogues of glucagon for diabetes therapy

Country Status (2)

Country Link
GB (1) GB0917072D0 (en)
WO (1) WO2011038900A2 (en)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013041678A1 (en) * 2011-09-23 2013-03-28 Novo Nordisk A/S Novel glucagon analogues
GB201214493D0 (en) * 2012-08-14 2012-09-26 Univ Ulster Therapies
RU2683039C2 (en) 2013-04-18 2019-03-26 Ново Нордиск А/С Stable protracted glp-1/glucagon receptor co-antagonists for medical use
JP2017525656A (en) 2014-06-04 2017-09-07 ノヴォ ノルディスク アー／エス GLP-1 / glucagon receptor co-agonist for medical use
US10046058B2 (en) 2014-12-02 2018-08-14 Rezolute, Inc. Use of hydrophobic organic acids to increase hydrophobicity of proteins and protein conjugates
AR103322A1 (en) 2014-12-30 2017-05-03 Hanmi Pharm Ind Co Ltd GLUCAGON DERIVATIVES WITH IMPROVED STABILITY
JOP20200119A1 (en) * 2015-01-09 2017-06-16 Lilly Co Eli Gip and glp-1 co-agonist compounds
AU2016270302B2 (en) 2015-06-04 2020-09-17 Rezolute, Inc. Amine pegylation methods for the preparation of site-specific protein conjugates
CR20180034A (en) 2015-06-30 2018-04-16 Hanmi Pharm Ind Co Ltd GLUCAGON DERIVATIVES AND A COMPOSITION THAT INCLUDES A CONJUGATE OF PROLONGED ACTION OF THE SAME.
AU2016382394B2 (en) 2015-12-31 2019-07-04 Hanmi Pharm. Co., Ltd. Long-acting conjugate of triple glucagon/GLP-1/GIP receptor agonist
PE20190355A1 (en) 2016-06-29 2019-03-07 Hanmi Pharm Ind Co Ltd DERIVATIVE OF GLUCAGON, CONJUGATE OF THE SAME, COMPOSITION INCLUDING THE SAME AND THERAPEUTIC USE OF THE SAME

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995018153A1 (en) * 1993-12-29 1995-07-06 The Rockefeller University Glucagon analogs with serine replacements at position 16 having antagonistic activity
WO2001083527A2 (en) * 2000-05-03 2001-11-08 Amgen Inc. Glucagon antagonists
WO2004111078A2 (en) * 2003-06-18 2004-12-23 Theratechnologies Inc. Compounds that modulate the glucagon response and uses thereof
WO2009058734A1 (en) * 2007-10-30 2009-05-07 Indiana University Research And Technology Corporation Compounds exhibiting glucagon antagonist and glp-1 agonist activity
WO2009058662A2 (en) * 2007-10-30 2009-05-07 Indiana University Research And Technology Corporation Glucagon antagonists

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR036711A1 (en) 2001-10-05 2004-09-29 Bayer Corp PEPTIDES THAT ACT AS GLON-RECEPTOR AGONISTS AND AS GLUCAGON RECEPTOR ANTAGONISTS AND THEIR PHARMACOLOGICAL USE METHODS
WO2004007524A2 (en) 2002-07-17 2004-01-22 Boehringer Ingelheim Pharma Gmbh & Co. Kg Bicyclic oligopeptides
MX2009003400A (en) 2006-10-03 2009-04-28 Cadila Healthcare Ltd Antidiabetic compounds.

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995018153A1 (en) * 1993-12-29 1995-07-06 The Rockefeller University Glucagon analogs with serine replacements at position 16 having antagonistic activity
WO2001083527A2 (en) * 2000-05-03 2001-11-08 Amgen Inc. Glucagon antagonists
WO2004111078A2 (en) * 2003-06-18 2004-12-23 Theratechnologies Inc. Compounds that modulate the glucagon response and uses thereof
WO2009058734A1 (en) * 2007-10-30 2009-05-07 Indiana University Research And Technology Corporation Compounds exhibiting glucagon antagonist and glp-1 agonist activity
WO2009058662A2 (en) * 2007-10-30 2009-05-07 Indiana University Research And Technology Corporation Glucagon antagonists

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
AHN J-M ET AL: "DEVELOPMENT OF POTENT GLUCAGON ANTAGONISTS: STRUCTURE-ACTIVITY RELATIONSHIP STUDY OF GLYCINE AT POSITION 4", JOURNAL OF PEPTIDE RESEARCH, BLACKWELL PUBLISHING LTD, OXFORD; GB, vol. 58, no. 2, 1 August 2001 (2001-08-01), pages 151 - 158, XP001039109, ISSN: 1397-002X, DOI: DOI:10.1034/J.1399-3011.2001.00880.X *
CHRISTOPHE J: "Glucagon receptors: From genetic structure and expression to effector coupling and biological responses", BIOCHIMICA ET BIOPHYSICA ACTA - REVIEWS ON BIOMEMBRANES 1995 NL LNKD- DOI:10.1016/0304-4157(94)00015-6, vol. 1241, no. 1, 1995, pages 45 - 57, XP002632309, ISSN: 0304-4157 *
RAMALINGA DHARANIPRAGADA: "SYNTHETIC LINEAR AND CYCLIC GLUCAGON ANTAGONISTS", INTERNATIONAL JOURNAL OF PEPTIDE AND PROTEIN RESEARCH, MUNKSGAARD, COPENHAGEN, DK, vol. 42, no. 1, 1 July 1993 (1993-07-01), pages 68 - 77, XP000372575, ISSN: 0367-8377 *

Also Published As

Publication number Publication date
WO2011038900A2 (en) 2011-04-07
GB0917072D0 (en) 2009-11-11

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