WO2006087354A3 - Insulinotropic agents conjugated with structurally well defined branched polymers - Google Patents

Insulinotropic agents conjugated with structurally well defined branched polymers Download PDF

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Publication number
WO2006087354A3
WO2006087354A3 PCT/EP2006/060007 EP2006060007W WO2006087354A3 WO 2006087354 A3 WO2006087354 A3 WO 2006087354A3 EP 2006060007 W EP2006060007 W EP 2006060007W WO 2006087354 A3 WO2006087354 A3 WO 2006087354A3
Authority
WO
WIPO (PCT)
Prior art keywords
well defined
branched polymers
structurally well
agents conjugated
insulinotropic agents
Prior art date
Application number
PCT/EP2006/060007
Other languages
French (fr)
Other versions
WO2006087354A2 (en
Inventor
Carsten Behrens
Jesper Lau
Janos Tibor Kodra
Mikael Kofod-Hansen
Thomas Kruse Hansen
Original Assignee
Novo Nordisk As
Carsten Behrens
Jesper Lau
Janos Tibor Kodra
Mikael Kofod-Hansen
Thomas Kruse Hansen
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 Novo Nordisk As, Carsten Behrens, Jesper Lau, Janos Tibor Kodra, Mikael Kofod-Hansen, Thomas Kruse Hansen filed Critical Novo Nordisk As
Priority to BRPI0607775A priority Critical patent/BRPI0607775A2/en
Priority to CA002601745A priority patent/CA2601745A1/en
Priority to AU2006215566A priority patent/AU2006215566A1/en
Priority to MX2007009906A priority patent/MX2007009906A/en
Priority to EP06708301A priority patent/EP1853321A2/en
Priority to JP2007555611A priority patent/JP2008530178A/en
Publication of WO2006087354A2 publication Critical patent/WO2006087354A2/en
Publication of WO2006087354A3 publication Critical patent/WO2006087354A3/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B82—NANOTECHNOLOGY
    • B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/595—Polyamides, e.g. nylon
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A61K47/641—Branched, dendritic or hypercomb peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/69—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
    • A61K47/6949—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Nanotechnology (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychiatry (AREA)
  • Biophysics (AREA)
  • Biotechnology (AREA)
  • General Engineering & Computer Science (AREA)
  • Medical Informatics (AREA)
  • Hospice & Palliative Care (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Novel GLP-1 conjugated with structurally well defined polymers and their therapeutically use.
PCT/EP2006/060007 2005-02-16 2006-02-16 Insulinotropic agents conjugated with structurally well defined branched polymers WO2006087354A2 (en)

Priority Applications (6)

Application Number Priority Date Filing Date Title
BRPI0607775A BRPI0607775A2 (en) 2005-02-16 2006-02-16 conjugate, pharmaceutical composition, use of a compound, and method for treating or preventing disease
CA002601745A CA2601745A1 (en) 2005-02-16 2006-02-16 Insulinotropic agents conjugated with structurally well defined branched polymers
AU2006215566A AU2006215566A1 (en) 2005-02-16 2006-02-16 Insulinotropic agents conjugated with structurally well defined branched polymers
MX2007009906A MX2007009906A (en) 2005-02-16 2006-02-16 Insulinotropic agents conjugated with structurally well defined branched polymers.
EP06708301A EP1853321A2 (en) 2005-02-16 2006-02-16 Insulinotropic agents conjugated with structurally well defined branched polymers
JP2007555611A JP2008530178A (en) 2005-02-16 2006-02-16 Derivatives of insulinotropic drugs conjugated with structurally well-defined branched polymers

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DKPA200500232 2005-02-16
DKPA200500232 2005-02-16

Publications (2)

Publication Number Publication Date
WO2006087354A2 WO2006087354A2 (en) 2006-08-24
WO2006087354A3 true WO2006087354A3 (en) 2007-08-02

Family

ID=36609320

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2006/060007 WO2006087354A2 (en) 2005-02-16 2006-02-16 Insulinotropic agents conjugated with structurally well defined branched polymers

Country Status (10)

Country Link
EP (1) EP1853321A2 (en)
JP (1) JP2008530178A (en)
KR (1) KR20070108180A (en)
CN (1) CN101123992A (en)
AU (1) AU2006215566A1 (en)
BR (1) BRPI0607775A2 (en)
CA (1) CA2601745A1 (en)
MX (1) MX2007009906A (en)
RU (1) RU2007128983A (en)
WO (1) WO2006087354A2 (en)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CU23556A1 (en) * 2005-11-30 2010-07-20 Ct Ingenieria Genetica Biotech POLYMER STRUCTURE SIMILAR TO DENDRÍMERO FOR THE OBTAINING OF CONJUGATES OF PHARMACEUTICAL INTEREST
JP4991168B2 (en) * 2006-03-10 2012-08-01 大阪瓦斯株式会社 New dendrimer
WO2008098693A2 (en) * 2007-02-16 2008-08-21 Bayer Healthcare Ag Convergent synthesis of glp-1
ES2402172T3 (en) * 2007-04-23 2013-04-29 Intarcia Therapeutics, Inc Suspension formulation of insulinotropic peptides and uses thereof
WO2008148839A2 (en) 2007-06-08 2008-12-11 Ascendis Pharma As Long-acting polymeric prodrugs of exendin
US20130123460A1 (en) 2010-04-30 2013-05-16 Sanwa Kagaku Kenkyusho Co., Ltd. Peptide for improving biostability of bioactive substance, and bioactive substance having improved biostability
KR101702251B1 (en) * 2012-11-29 2017-02-02 에스티팜 주식회사 Bile acid oligomer conjugate for novel vesicular transport and use thereof
ES2784603T3 (en) 2015-06-02 2020-09-29 Novo Nordisk As Insulins with recombinant polar extensions
MA43348A (en) * 2015-10-01 2018-08-08 Novo Nordisk As PROTEIN CONJUGATES
EP3544724A4 (en) * 2016-11-22 2020-10-14 Elektrofi, Inc Particles comprising a therapeutic or diagnostic agent and suspensions and methods of use thereof
US11471537B2 (en) 2017-04-05 2022-10-18 Novo Nordisk A/S Oligomer extended insulin-Fc conjugates
JP2022523510A (en) 2019-01-31 2022-04-25 エレクトロフィ，インコーポレイテッド Particle formation and morphological structure
CN110128526B (en) * 2019-05-30 2021-07-23 江苏诺泰澳赛诺生物制药股份有限公司 Long-acting exenatide derivative and salt thereof, and preparation method and application thereof
EP4027978A1 (en) 2019-09-13 2022-07-20 Elektrofi, Inc. Compositions and methods for the delivery of therapeutic biologics for treatment of disease
CN113896656B (en) * 2021-10-28 2023-02-07 成都泰和伟业生物科技有限公司 Preparation method of [2- [2- (Fmoc-amino) ethoxy ] acetic acid

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001051071A2 (en) * 2000-01-11 2001-07-19 Novo Nordisk A/S Transepithelial delivery of glp-1 derivatives
WO2004073620A2 (en) * 2003-02-14 2004-09-02 Quanta Biodesign, Ltd The selective and specific preparation of discrete peg compounds
WO2004083234A2 (en) * 2003-03-14 2004-09-30 Nobex Corporation Insulin polypeptide-oligomer conjugates, proinsulin polypeptide-oligomer conjugates and methods of synthesizing same
WO2005014049A2 (en) * 2003-08-08 2005-02-17 Novo Nordisk A/S Synthesis and application of new structural well defined branched polymers as conjugating agents for peptides
WO2005058954A1 (en) * 2003-12-18 2005-06-30 Novo Nordisk A/S Novel glp-1 compounds
WO2006010143A2 (en) * 2004-07-13 2006-01-26 Neose Technologies, Inc. Branched peg remodeling and glycosylation of glucagon-like peptide-1 [glp-1]

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001051071A2 (en) * 2000-01-11 2001-07-19 Novo Nordisk A/S Transepithelial delivery of glp-1 derivatives
WO2004073620A2 (en) * 2003-02-14 2004-09-02 Quanta Biodesign, Ltd The selective and specific preparation of discrete peg compounds
WO2004083234A2 (en) * 2003-03-14 2004-09-30 Nobex Corporation Insulin polypeptide-oligomer conjugates, proinsulin polypeptide-oligomer conjugates and methods of synthesizing same
WO2005014049A2 (en) * 2003-08-08 2005-02-17 Novo Nordisk A/S Synthesis and application of new structural well defined branched polymers as conjugating agents for peptides
WO2005014035A2 (en) * 2003-08-08 2005-02-17 Novo Nordisk Health Care Ag Use of galactose oxidase for selective chemical conjugation of protractor molecules to proteins of therapeutic interest
WO2005058954A1 (en) * 2003-12-18 2005-06-30 Novo Nordisk A/S Novel glp-1 compounds
WO2006010143A2 (en) * 2004-07-13 2006-01-26 Neose Technologies, Inc. Branched peg remodeling and glycosylation of glucagon-like peptide-1 [glp-1]

Also Published As

Publication number Publication date
KR20070108180A (en) 2007-11-08
CN101123992A (en) 2008-02-13
EP1853321A2 (en) 2007-11-14
BRPI0607775A2 (en) 2018-06-26
RU2007128983A (en) 2009-03-27
JP2008530178A (en) 2008-08-07
MX2007009906A (en) 2007-09-25
AU2006215566A1 (en) 2006-08-24
WO2006087354A2 (en) 2006-08-24
CA2601745A1 (en) 2006-08-24

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