WO2008022015A3 - Retro-inverso incretin analogues, and methods of use thereof - Google Patents

Retro-inverso incretin analogues, and methods of use thereof Download PDF

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Publication number
WO2008022015A3
WO2008022015A3 PCT/US2007/075676 US2007075676W WO2008022015A3 WO 2008022015 A3 WO2008022015 A3 WO 2008022015A3 US 2007075676 W US2007075676 W US 2007075676W WO 2008022015 A3 WO2008022015 A3 WO 2008022015A3
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WO
WIPO (PCT)
Prior art keywords
retro
inverso
incretin
methods
relates
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/US2007/075676
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French (fr)
Other versions
WO2008022015A2 (en
Inventor
William W Bachovchin
Hung-Sen Lai
David George Sanford
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.)
Tufts University
Original Assignee
Tufts University
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Filing date
Publication date
Application filed by Tufts University filed Critical Tufts University
Publication of WO2008022015A2 publication Critical patent/WO2008022015A2/en
Publication of WO2008022015A3 publication Critical patent/WO2008022015A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • A61K38/30Insulin-like growth factors, i.e. somatomedins, e.g. IGF-1, IGF-2

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Endocrinology (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

One aspect of the present invention relates to synthetic analogues of a native peptide incretin hormone, e.g., glucagon-like peptide 1 (GLP-I), which in certain embodiments are rationally designed retro-inverso sequences with corrections for side-chain stereochemistry and terminus modifications for end-group effects. Another aspect of the invention relates to a method of treating a mammal suffering from diabetes, atherosclerosis, microangiopathy, kidney disorders, kidney failure, cardiac disease, diabetic retinopathy, ocular disorders, or blindness, comprising the step of administering a therapeutically effective amount of an incretin analogue of the present invention.
PCT/US2007/075676 2006-08-11 2007-08-10 Retro-inverso incretin analogues, and methods of use thereof Ceased WO2008022015A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US83710506P 2006-08-11 2006-08-11
US60/837,105 2006-08-11

Publications (2)

Publication Number Publication Date
WO2008022015A2 WO2008022015A2 (en) 2008-02-21
WO2008022015A3 true WO2008022015A3 (en) 2008-10-23

Family

ID=39082991

Family Applications (1)

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PCT/US2007/075676 Ceased WO2008022015A2 (en) 2006-08-11 2007-08-10 Retro-inverso incretin analogues, and methods of use thereof

Country Status (1)

Country Link
WO (1) WO2008022015A2 (en)

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8859491B2 (en) 2011-11-17 2014-10-14 Indiana University Research And Technology Corporation Glucagon superfamily peptides exhibiting glucocorticoid receptor activity
US8900593B2 (en) 2007-02-15 2014-12-02 Indiana University Research And Technology Corporation Glucagon/GLP-1 receptor co-agonists
US8969288B2 (en) 2008-12-19 2015-03-03 Indiana University Research And Technology Corporation Amide based glucagon and superfamily peptide prodrugs
US9018164B2 (en) 2005-11-07 2015-04-28 Indiana University Research And Technology Corporation Glucagon analogs exhibiting physiological solubility and stability
US9156902B2 (en) 2011-06-22 2015-10-13 Indiana University Research And Technology Corporation Glucagon/GLP-1 receptor co-agonists
US9249206B2 (en) 2010-12-22 2016-02-02 Indiana University Research And Technology Corporation Glucagon analogs exhibiting GIP receptor activity
US9309301B2 (en) 2011-06-22 2016-04-12 Indiana University Research And Technology Corporation Glucagon/GLP-1 receptor co-agonists
US9340600B2 (en) 2012-06-21 2016-05-17 Indiana University Research And Technology Corporation Glucagon analogs exhibiting GIP receptor activity
US9487571B2 (en) 2010-01-27 2016-11-08 Indiana University Research And Technology Corporation Glucagon antagonist-GIP agonist conjugates and compositions for the treatment of metabolic disorders and obesity

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EP2025674A1 (en) 2007-08-15 2009-02-18 sanofi-aventis Substituted tetra hydro naphthalines, method for their manufacture and their use as drugs
MX2010004298A (en) 2007-10-30 2010-05-03 Univ Indiana Res & Tech Corp Compounds exhibiting glucagon antagonist and glp-1 agonist activity.
ES2509883T3 (en) 2007-10-30 2014-10-20 Indiana University Research And Technology Corporation Glucagon antagonists
CN102105159B (en) 2008-06-17 2015-07-08 印第安纳大学研究及科技有限公司 GIP-based mixed agonists for the treatment of metabolic disorders and obesity
EP2443146B1 (en) 2009-06-16 2016-10-05 Indiana University Research And Technology Corporation Gip receptor-active glucagon compounds
WO2011107494A1 (en) 2010-03-03 2011-09-09 Sanofi Novel aromatic glycoside derivatives, medicaments containing said compounds, and the use thereof
DE102010015123A1 (en) 2010-04-16 2011-10-20 Sanofi-Aventis Deutschland Gmbh New benzylamidic diphenylazetidinone compounds, useful for treating lipid disorders, hyperlipidemia, atherosclerotic manifestations or insulin resistance, and for reducing serum cholesterol levels
MX2012013001A (en) 2010-05-13 2013-02-26 Univ Indiana Res & Tech Corp Glucagon superfamily peptides exhibiting nuclear hormone receptor activity.
JP6050746B2 (en) 2010-05-13 2016-12-21 インディアナ ユニバーシティー リサーチ アンド テクノロジー コーポレーションIndiana University Research And Technology Corporation Glucagon superfamily of peptides exhibiting G protein-coupled receptor activity
EP2582709B1 (en) 2010-06-18 2018-01-24 Sanofi Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
EP2567959B1 (en) 2011-09-12 2014-04-16 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013045413A1 (en) 2011-09-27 2013-04-04 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
US20150297573A1 (en) 2012-10-24 2015-10-22 INSERM (Institut National de la Santé et de la Recherche Médicale) TPL2 KINASE INHIBITORS FOR PREVENTING OR TREATING DIABETES AND FOR PROMOTING Beta-CELL SURVIVAL
US10426818B2 (en) 2015-03-24 2019-10-01 Inserm (Institut National De La Sante Et De La Recherche Medicale) Method and pharmaceutical composition for use in the treatment of diabetes
WO2018213151A1 (en) * 2017-05-18 2018-11-22 Merck Sharp & Dohme Corp. Pharmaceutical formulation comprising incretin-insulin conjugates

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6803357B1 (en) * 1998-02-02 2004-10-12 New England Medical Center Hospitals, Inc. Method of regulating glucose metabolism, and reagents related thereto
US6960648B2 (en) * 2000-10-13 2005-11-01 Universite De Lausanne Intracellular delivery of biological effectors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6803357B1 (en) * 1998-02-02 2004-10-12 New England Medical Center Hospitals, Inc. Method of regulating glucose metabolism, and reagents related thereto
US6960648B2 (en) * 2000-10-13 2005-11-01 Universite De Lausanne Intracellular delivery of biological effectors

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9018164B2 (en) 2005-11-07 2015-04-28 Indiana University Research And Technology Corporation Glucagon analogs exhibiting physiological solubility and stability
US8900593B2 (en) 2007-02-15 2014-12-02 Indiana University Research And Technology Corporation Glucagon/GLP-1 receptor co-agonists
US9447162B2 (en) 2007-02-15 2016-09-20 Indiana University Research And Technology Corporation Glucagon/GLP-1 receptor co-agonists
US8969288B2 (en) 2008-12-19 2015-03-03 Indiana University Research And Technology Corporation Amide based glucagon and superfamily peptide prodrugs
US9487571B2 (en) 2010-01-27 2016-11-08 Indiana University Research And Technology Corporation Glucagon antagonist-GIP agonist conjugates and compositions for the treatment of metabolic disorders and obesity
US9249206B2 (en) 2010-12-22 2016-02-02 Indiana University Research And Technology Corporation Glucagon analogs exhibiting GIP receptor activity
US9156902B2 (en) 2011-06-22 2015-10-13 Indiana University Research And Technology Corporation Glucagon/GLP-1 receptor co-agonists
US9309301B2 (en) 2011-06-22 2016-04-12 Indiana University Research And Technology Corporation Glucagon/GLP-1 receptor co-agonists
US8859491B2 (en) 2011-11-17 2014-10-14 Indiana University Research And Technology Corporation Glucagon superfamily peptides exhibiting glucocorticoid receptor activity
US9340600B2 (en) 2012-06-21 2016-05-17 Indiana University Research And Technology Corporation Glucagon analogs exhibiting GIP receptor activity

Also Published As

Publication number Publication date
WO2008022015A2 (en) 2008-02-21

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