CA2420768C - Conjugates of defined stoichiometry - Google Patents

Conjugates of defined stoichiometry Download PDF

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Publication number
CA2420768C
CA2420768C CA2420768A CA2420768A CA2420768C CA 2420768 C CA2420768 C CA 2420768C CA 2420768 A CA2420768 A CA 2420768A CA 2420768 A CA2420768 A CA 2420768A CA 2420768 C CA2420768 C CA 2420768C
Authority
CA
Canada
Prior art keywords
linker
biomolecule
conjugate
molecular weight
conjugates
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.)
Expired - Fee Related
Application number
CA2420768A
Other languages
English (en)
French (fr)
Other versions
CA2420768A1 (en
Inventor
Eva Hoess
Herbert Andres
Frederic Donie
Rudolf Vogel
Hans-Peter Josel
Rupert Herrmann
Herbert von der Eltz
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.)
Individual
Original Assignee
F Hoffmann La Roche AG
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 DE10048417A external-priority patent/DE10048417A1/de
Priority claimed from EP01107491A external-priority patent/EP1245956A1/en
Application filed by F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of CA2420768A1 publication Critical patent/CA2420768A1/en
Application granted granted Critical
Publication of CA2420768C publication Critical patent/CA2420768C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K1/00General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107General 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
    • C07K1/1072General 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
    • C07K1/1077General 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/62Medicinal 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
    • A61K47/64Drug-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
    • A61K47/643Albumins, e.g. HSA, BSA, ovalbumin or a Keyhole Limpet Hemocyanin [KHL]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6889Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/5306Improving reaction conditions, e.g. reduction of non-specific binding, promotion of specific binding
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/531Production of immunochemical test materials
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/68Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/68Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • G01N33/6803General methods of protein analysis not limited to specific proteins or families of proteins
    • G01N33/6845Methods of identifying protein-protein interactions in protein mixtures
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10STECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S435/00Chemistry: molecular biology and microbiology
    • Y10S435/961Chemistry: molecular biology and microbiology including a step of forming, releasing, or exposing the antigen or forming the hapten-immunogenic carrier complex or the antigen per se
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10STECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S435/00Chemistry: molecular biology and microbiology
    • Y10S435/962Prevention or removal of interfering materials or reactants or other treatment to enhance results, e.g. determining or preventing nonspecific binding

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Analytical Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physics & Mathematics (AREA)
  • Biotechnology (AREA)
  • Food Science & Technology (AREA)
  • Cell Biology (AREA)
  • Pathology (AREA)
  • Microbiology (AREA)
  • General Physics & Mathematics (AREA)
  • Veterinary Medicine (AREA)
  • Biophysics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Genetics & Genomics (AREA)
  • Bioinformatics & Computational Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Peptides Or Proteins (AREA)
  • Solid-Sorbent Or Filter-Aiding Compositions (AREA)
  • Catalysts (AREA)
  • Production Of Liquid Hydrocarbon Mixture For Refining Petroleum (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Steroid Compounds (AREA)
CA2420768A 2000-09-29 2001-09-26 Conjugates of defined stoichiometry Expired - Fee Related CA2420768C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
DE10048417A DE10048417A1 (de) 2000-09-29 2000-09-29 Verbindungen mit verzweigtem Linker
DE10048417.4 2000-09-29
EP01107491A EP1245956A1 (en) 2001-03-29 2001-03-29 Conjugates of defined stoichiometry
EP01107491.1 2001-03-29
PCT/EP2001/011101 WO2002027317A2 (en) 2000-09-29 2001-09-26 Conjugates of defined stoichiometry

Publications (2)

Publication Number Publication Date
CA2420768A1 CA2420768A1 (en) 2002-04-04
CA2420768C true CA2420768C (en) 2012-09-25

Family

ID=26007222

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2420768A Expired - Fee Related CA2420768C (en) 2000-09-29 2001-09-26 Conjugates of defined stoichiometry

Country Status (9)

Country Link
US (1) US7897404B2 (enExample)
EP (2) EP1625857A3 (enExample)
JP (1) JP3836429B2 (enExample)
AT (1) ATE313796T1 (enExample)
AU (1) AU2001289923A1 (enExample)
CA (1) CA2420768C (enExample)
DE (1) DE60116146T2 (enExample)
ES (1) ES2254489T3 (enExample)
WO (1) WO2002027317A2 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100361933B1 (ko) 1993-09-08 2003-02-14 라 졸라 파마슈티칼 컴파니 화학적으로정의된비중합성결합가플랫폼분자및그것의콘주게이트
WO2001093914A2 (en) 2000-06-08 2001-12-13 La Jolla Pharmaceutical Company Multivalent platform molecules comprising high molecular weight polyethylene oxide
BR112013007614B1 (pt) 2010-10-25 2020-12-29 F. Hoffmann-La Roche Ag método para medir um analito, composição reagente, mistura reagente, uso de uma composição reagente, uso de uma amida de ácido carbônico e kit
CA2891280C (en) 2012-11-24 2018-03-20 Hangzhou Dac Biotech Co., Ltd. Hydrophilic linkers and their uses for conjugation of drugs to cell binding molecules
WO2019175845A2 (en) * 2018-03-15 2019-09-19 Levim Biotech Llp Antibody-biomolecule conjugates linked through multifunctional macromolecule and uses thereof
WO2021055880A1 (en) * 2019-09-20 2021-03-25 University Of Florida Researchfoundation, Incorporated Detection of antibodies against ran proteins from serum and tissue lysates

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2493382A (en) * 1948-10-29 1950-01-03 American Cyanamid Co Automatic sample collector
GB2095818B (en) 1981-03-27 1985-10-02 Exxon Research Engineering Co Staged adsorption/resorption heat pump
US5047324A (en) * 1986-12-09 1991-09-10 Miles Inc. Substantially pure enzyme-antibody conjugate preparations
US5554748A (en) * 1989-04-07 1996-09-10 Nycomed Salutar, Inc. Adducts of macrocyclic chelants
AU657483B2 (en) * 1990-07-20 1995-03-16 Pharmacia Ab Heterobifunctional reagents and conjugates with oxaalkylene units for amphiphilic bridge structures
US6120768A (en) * 1993-05-17 2000-09-19 Immunomedics, Inc. Dota-biotin derivatives
CN1114106C (zh) 1994-07-25 2003-07-09 罗切诊断学有限公司 金属螯合物标记的肽及其制备方法
DE59511054D1 (de) 1994-07-25 2006-08-10 Roche Diagnostics Gmbh Bestimmung von spezifischem immunglobulin unter verwendung multipler antigene
DE59507438D1 (de) * 1994-07-25 2000-01-20 Roche Diagnostics Gmbh Hydrophile metallkomplexe
ATE214073T1 (de) 1994-07-25 2002-03-15 Roche Diagnostics Gmbh Hapten-markierte peptide
DE4430972A1 (de) * 1994-07-25 1996-02-01 Boehringer Mannheim Gmbh Bestimmung von spezifischem Immunglobulin unter Verwendung multipler Antigene
US5958783A (en) 1994-07-25 1999-09-28 Roche Diagnostics Gmbh Metal complexes with a charged linker
GB9415143D0 (en) 1994-07-27 1994-09-14 Edwards Raymond Glycated haemoglobin assay
CA2258744A1 (en) * 1996-06-27 1997-12-31 G.D. Searle And Co. Particles comprising amphiphilic copolymers, having a cross-linked shell domain and an interior core domain, useful for pharmaceutical and other applications

Also Published As

Publication number Publication date
EP1364208B1 (en) 2005-12-21
ES2254489T3 (es) 2006-06-16
US7897404B2 (en) 2011-03-01
WO2002027317A2 (en) 2002-04-04
DE60116146T2 (de) 2006-09-14
EP1625857A2 (en) 2006-02-15
AU2001289923A1 (en) 2002-04-08
EP1625857A3 (en) 2008-08-27
DE60116146D1 (de) 2006-01-26
ATE313796T1 (de) 2006-01-15
WO2002027317A3 (en) 2003-09-12
EP1364208A2 (en) 2003-11-26
US20040087501A1 (en) 2004-05-06
JP2004510162A (ja) 2004-04-02
JP3836429B2 (ja) 2006-10-25
CA2420768A1 (en) 2002-04-04

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Effective date: 20190926