WO2008098693A3 - Convergent synthesis of glp-1 - Google Patents

Convergent synthesis of glp-1 Download PDF

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Publication number
WO2008098693A3
WO2008098693A3 PCT/EP2008/000846 EP2008000846W WO2008098693A3 WO 2008098693 A3 WO2008098693 A3 WO 2008098693A3 EP 2008000846 W EP2008000846 W EP 2008000846W WO 2008098693 A3 WO2008098693 A3 WO 2008098693A3
Authority
WO
WIPO (PCT)
Prior art keywords
glp
convergent synthesis
convergent
synthesis
bei
Prior art date
Application number
PCT/EP2008/000846
Other languages
French (fr)
Other versions
WO2008098693A2 (en
Inventor
Joachim Krueger
Hans-Christian Militzer
Konrad Siegel
Torsten Minuth
Original Assignee
Bayer Healthcare Ag
Joachim Krueger
Hans-Christian Militzer
Konrad Siegel
Torsten Minuth
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 Bayer Healthcare Ag, Joachim Krueger, Hans-Christian Militzer, Konrad Siegel, Torsten Minuth filed Critical Bayer Healthcare Ag
Publication of WO2008098693A2 publication Critical patent/WO2008098693A2/en
Publication of WO2008098693A3 publication Critical patent/WO2008098693A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/06—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using protecting groups or activating agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/10—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using coupling agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
    • C07K1/1072—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups
    • C07K1/1077—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups by covalent attachment of residues other than amino acids or peptide residues, e.g. sugars, polyols, fatty acids
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06086—Dipeptides with the first amino acid being basic
    • C07K5/06095—Arg-amino acid

Abstract

The present invention relates to a process for the manufacture of the polypeptide GLP-1 (SEQ ID NO 1) and its PEGylated derivative, bei fragment condensation (convergent synthesis).
PCT/EP2008/000846 2007-02-16 2008-02-02 Convergent synthesis of glp-1 WO2008098693A2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP07003302 2007-02-16
EP07003302.2 2007-02-16
EP07005646 2007-03-20
EP07005646.0 2007-03-20

Publications (2)

Publication Number Publication Date
WO2008098693A2 WO2008098693A2 (en) 2008-08-21
WO2008098693A3 true WO2008098693A3 (en) 2008-11-20

Family

ID=39690576

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2008/000846 WO2008098693A2 (en) 2007-02-16 2008-02-02 Convergent synthesis of glp-1

Country Status (1)

Country Link
WO (1) WO2008098693A2 (en)

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001004156A1 (en) * 1999-07-12 2001-01-18 Zealand Pharmaceuticals A/S Peptides that lower blood glucose levels
WO2003040309A2 (en) * 2001-10-05 2003-05-15 Bayer Pharmaceuticals Corporation Peptides acting as both glp-1 receptor agonists and glucagon receptor antagonists and their pharmacological methods of use
WO2006087354A2 (en) * 2005-02-16 2006-08-24 Novo Nordisk A/S Insulinotropic agents conjugated with structurally well defined branched polymers

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001004156A1 (en) * 1999-07-12 2001-01-18 Zealand Pharmaceuticals A/S Peptides that lower blood glucose levels
WO2003040309A2 (en) * 2001-10-05 2003-05-15 Bayer Pharmaceuticals Corporation Peptides acting as both glp-1 receptor agonists and glucagon receptor antagonists and their pharmacological methods of use
WO2006087354A2 (en) * 2005-02-16 2006-08-24 Novo Nordisk A/S Insulinotropic agents conjugated with structurally well defined branched polymers

Also Published As

Publication number Publication date
WO2008098693A2 (en) 2008-08-21

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