WO2005099768A3 - Polymeric prodrug with a self-immolative linker - Google Patents

Polymeric prodrug with a self-immolative linker Download PDF

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Publication number
WO2005099768A3
WO2005099768A3 PCT/EP2005/003061 EP2005003061W WO2005099768A3 WO 2005099768 A3 WO2005099768 A3 WO 2005099768A3 EP 2005003061 W EP2005003061 W EP 2005003061W WO 2005099768 A3 WO2005099768 A3 WO 2005099768A3
Authority
WO
WIPO (PCT)
Prior art keywords
self
immolative linker
polymeric prodrug
prodrug
carrier
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/EP2005/003061
Other languages
French (fr)
Other versions
WO2005099768A2 (en
Inventor
Ulrich Hersel
Harald Rau
Robert Schnepf
Dirk Vetter
Thomas Wegge
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.)
Ascendis Pharma GmbH
Original Assignee
Complex Biosystems GmbH
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
Priority claimed from EP04075892A external-priority patent/EP1579873A1/en
Priority claimed from GB0415043A external-priority patent/GB0415043D0/en
Priority claimed from EP04019293A external-priority patent/EP1625855A1/en
Priority to BR122019000248A priority Critical patent/BR122019000248B8/en
Priority to CA2602705A priority patent/CA2602705C/en
Priority to EP09161152.5A priority patent/EP2087910B1/en
Priority to JP2007504348A priority patent/JP4950022B2/en
Priority to EP05716306.5A priority patent/EP1732607B1/en
Priority to AU2005232371A priority patent/AU2005232371B2/en
Priority to MXPA06010782A priority patent/MXPA06010782A/en
Application filed by Complex Biosystems GmbH filed Critical Complex Biosystems GmbH
Priority to BRPI0507875A priority patent/BRPI0507875B8/en
Priority to DK05716306.5T priority patent/DK1732607T3/en
Priority to ES05716306T priority patent/ES2741524T3/en
Priority to US10/594,097 priority patent/US8377917B2/en
Publication of WO2005099768A2 publication Critical patent/WO2005099768A2/en
Publication of WO2005099768A3 publication Critical patent/WO2005099768A3/en
Anticipated expiration legal-status Critical
Priority to AU2010212335A priority patent/AU2010212335B2/en
Priority to US13/759,440 priority patent/US9238686B2/en
Priority to US14/964,764 priority patent/US20160089448A1/en
Priority to US17/142,698 priority patent/US20210283264A1/en
Ceased legal-status Critical Current

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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
    • 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
    • A61K47/58—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 by reactions only involving carbon-to-carbon unsaturated bonds, e.g. poly[meth]acrylate, polyacrylamide, polystyrene, polyvinylpyrrolidone, polyvinylalcohol or polystyrene sulfonic acid resin
    • 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
    • A61K47/56—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
    • A61K47/61—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 the organic macromolecular compound being a polysaccharide or a derivative thereof
    • 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
    • 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
    • A61K47/643—Albumins, e.g. HSA, BSA, ovalbumin or a Keyhole Limpet Hemocyanin [KHL]
    • 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
    • A61K47/6903—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 the form being semi-solid, e.g. an ointment, a gel, a hydrogel or a solidifying gel
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/46—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • 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
    • C07K14/61—Growth hormone [GH], i.e. somatotropin
    • 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
    • C07K14/62—Insulins
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/96—Esters of carbonic or haloformic acids

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Toxicology (AREA)
  • Zoology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

A cascade carrier linked prodrug is described which comprises a biologically active moiety and - a masking group having at least one nucleophile and being distinct from the carrier. In one preferred embodiment of the invention, the prodrug has the structure represented by formula (I).
PCT/EP2005/003061 2004-03-23 2005-03-22 Polymeric prodrug with a self-immolative linker Ceased WO2005099768A2 (en)

Priority Applications (15)

Application Number Priority Date Filing Date Title
DK05716306.5T DK1732607T3 (en) 2004-03-23 2005-03-22 POLYMER PRODRUG WITH A SELF-RELATED LINKER
ES05716306T ES2741524T3 (en) 2004-03-23 2005-03-22 Polymeric prodrug with an auto-immolator linker
US10/594,097 US8377917B2 (en) 2004-03-23 2005-03-22 Polymeric prodrug with a self-immolative linker
CA2602705A CA2602705C (en) 2004-03-23 2005-03-22 Polymeric prodrug with a reversible aromatic linker
EP09161152.5A EP2087910B1 (en) 2004-03-23 2005-03-22 Polymeric prodrugs
JP2007504348A JP4950022B2 (en) 2004-03-23 2005-03-22 Polymeric prodrugs with self-destructing linkers
EP05716306.5A EP1732607B1 (en) 2004-03-23 2005-03-22 Polymeric prodrug with a self-immolative linker
AU2005232371A AU2005232371B2 (en) 2004-03-23 2005-03-22 Polymeric prodrug with a self-immolative linker
MXPA06010782A MXPA06010782A (en) 2004-03-23 2005-03-22 Prodrug linker.
BR122019000248A BR122019000248B8 (en) 2004-03-23 2005-03-22 polymeric cascade prodrug binder reagent
BRPI0507875A BRPI0507875B8 (en) 2004-03-23 2005-03-22 polymeric cascade prodrug
AU2010212335A AU2010212335B2 (en) 2004-03-23 2010-08-13 Polymeric prodrug with a self-immolative linker
US13/759,440 US9238686B2 (en) 2004-03-23 2013-02-05 Polymeric prodrug with self-immolative linker
US14/964,764 US20160089448A1 (en) 2004-03-23 2015-12-10 Polymeric prodrug with a self-immolative linker
US17/142,698 US20210283264A1 (en) 2004-03-23 2021-01-06 Polymeric Prodrugs with a Self-Immolative Linker

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
EP04075892A EP1579873A1 (en) 2004-03-23 2004-03-23 Polymeric prodrugs
EP04075892.2 2004-03-23
GB0415043.9 2004-07-05
GB0415043A GB0415043D0 (en) 2004-07-05 2004-07-05 Prodrug linker
EP04019293A EP1625855A1 (en) 2004-08-13 2004-08-13 Polymeric prodrug with a self-immolative linker
EP04019293.2 2004-08-13

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US10/594,097 A-371-Of-International US8377917B2 (en) 2004-03-23 2005-03-22 Polymeric prodrug with a self-immolative linker
US13/759,440 Continuation US9238686B2 (en) 2004-03-23 2013-02-05 Polymeric prodrug with self-immolative linker

Publications (2)

Publication Number Publication Date
WO2005099768A2 WO2005099768A2 (en) 2005-10-27
WO2005099768A3 true WO2005099768A3 (en) 2006-08-10

Family

ID=34961964

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2005/003061 Ceased WO2005099768A2 (en) 2004-03-23 2005-03-22 Polymeric prodrug with a self-immolative linker

Country Status (11)

Country Link
US (4) US8377917B2 (en)
EP (2) EP1732607B1 (en)
JP (2) JP4950022B2 (en)
AU (2) AU2005232371B2 (en)
BR (2) BRPI0507875B8 (en)
CA (4) CA2940803A1 (en)
DK (1) DK1732607T3 (en)
ES (1) ES2741524T3 (en)
HU (1) HUE045882T2 (en)
MX (1) MXPA06010782A (en)
WO (1) WO2005099768A2 (en)

Cited By (8)

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CN102924725B (en) * 2012-11-29 2014-11-26 中国科学院长春应用化学研究所 Polyamino acid/chitosan composite material and preparation method thereof
US9943610B2 (en) 2012-12-21 2018-04-17 Bioalliance C.V. Hydrophilic self-immolative linkers and conjugates thereof
US9950077B2 (en) 2014-06-20 2018-04-24 Bioalliance C.V. Anti-folate receptor alpha (FRA) antibody-drug conjugates and methods of using thereof
US10472422B2 (en) 2016-01-08 2019-11-12 Abgenomics International Inc. Tetravalent anti-PSGL-1 antibodies and uses thereof
US11103593B2 (en) 2013-10-15 2021-08-31 Seagen Inc. Pegylated drug-linkers for improved ligand-drug conjugate pharmacokinetics
US11116847B2 (en) 2013-12-19 2021-09-14 Seagen Inc. Methylene carbamate linkers for use with targeted-drug conjugates
US11730822B2 (en) 2017-03-24 2023-08-22 Seagen Inc. Process for the preparation of glucuronide drug-linkers and intermediates thereof
US11844839B2 (en) 2016-03-25 2023-12-19 Seagen Inc. Process for the preparation of pegylated drug-linkers and intermediates thereof

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EP2113256A1 (en) 2008-04-29 2009-11-04 Ascendis Pharma AS PEGylated rhGH compounds
WO2009156481A1 (en) * 2008-06-25 2009-12-30 Ascendis Pharma As Pegylated bnp
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CA2769162C (en) * 2009-07-31 2017-12-05 Ascendis Pharma As Biodegradable polyethylene glycol based water-insoluble hydrogels
US9138462B2 (en) 2009-07-31 2015-09-22 Sanofi-Aventis Deutschland Gmbh Prodrugs comprising an insulin linker conjugate
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US9561285B2 (en) 2010-01-22 2017-02-07 Ascendis Pharma As Carrier-linked carbamate prodrug linkers
US9062094B2 (en) 2010-01-22 2015-06-23 Ascendis Pharma As Dipeptide-based prodrug linkers for aliphatic amine-containing drugs
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