WO1990014844A3 - Sucres utilises en tant qu'elements de liaison clivables pour l'apport et la liberation d'agents sous forme naturelle - Google Patents

Sucres utilises en tant qu'elements de liaison clivables pour l'apport et la liberation d'agents sous forme naturelle Download PDF

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Publication number
WO1990014844A3
WO1990014844A3 PCT/US1990/003008 US9003008W WO9014844A3 WO 1990014844 A3 WO1990014844 A3 WO 1990014844A3 US 9003008 W US9003008 W US 9003008W WO 9014844 A3 WO9014844 A3 WO 9014844A3
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WO
WIPO (PCT)
Prior art keywords
linker
provides
compound
release
native form
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Application number
PCT/US1990/003008
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English (en)
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WO1990014844A2 (fr
Inventor
Ananthachari Srinivasan
Vivekananda M Vrudhula
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Neorx Corp
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Publication date
Application filed by Neorx Corp filed Critical Neorx Corp
Publication of WO1990014844A2 publication Critical patent/WO1990014844A2/fr
Publication of WO1990014844A3 publication Critical patent/WO1990014844A3/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/0491—Sugars, nucleosides, nucleotides, oligonucleotides, nucleic acids, e.g. DNA, RNA, nucleic acid aptamers
    • 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
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • 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
    • A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6889—Conjugates 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/10—Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody
    • A61K51/1093—Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody conjugates with carriers being antibodies
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/02—Acyclic radicals, not substituted by cyclic structures
    • C07H15/04—Acyclic radicals, not substituted by cyclic structures attached to an oxygen atom of the saccharide radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/02—Acyclic radicals, not substituted by cyclic structures
    • C07H15/12—Acyclic radicals, not substituted by cyclic structures attached to a nitrogen atom of the saccharide radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/18—Acyclic radicals, substituted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20—Carbocyclic rings
    • C07H15/24—Condensed ring systems having three or more rings
    • C07H15/252—Naphthacene radicals, e.g. daunomycins, adriamycins
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2121/00—Preparations for use in therapy
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2123/00—Preparations for testing in vivo

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Analytical Chemistry (AREA)
  • Biophysics (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

L'invention concerne un conjugué clivable dont l'élément de liaison contient une liaison labile qui est clivable dans une variété de conditions douces, y compris des conditions faiblement acides. Etant donné que l'agent peut être lié directement à l'élément de liaison, le clivage peut produire la libération de l'agent naturel. La molécule de ciblage utilisée dans l'invention peut être une molécule intacte, un fragment de celle-ci ou un équivalent fonctionnel de celle-ci. Dans un mode particulièrement préféré de réalisation, la molécule de ciblage est un anticorps monoclonal dirigé vers un antigène associé à une tumeur chez l'homme. Un autre aspect de l'invention concerne un procédé permettant d'isoler un composé. Le composé se lie de manière covalente à une phase solide qui a été dérivée avec l'élément de liaison décrit ci-dessus et est libérée sous forme naturelle par une variété de conditions douces. Un aspect supplémentaire de l'invention concerne un procédé permettant d'introduire dans un composé un groupe sulfhydryle, amino ou hydroxyle libre en utilisant un réactif dont la structure s'apparente à l'élément de liaison décrit ci-dessus.
PCT/US1990/003008 1989-06-06 1990-05-30 Sucres utilises en tant qu'elements de liaison clivables pour l'apport et la liberation d'agents sous forme naturelle WO1990014844A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US36235589A 1989-06-06 1989-06-06
US362,355 1989-06-06

Publications (2)

Publication Number Publication Date
WO1990014844A2 WO1990014844A2 (fr) 1990-12-13
WO1990014844A3 true WO1990014844A3 (fr) 1991-03-07

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ID=23425768

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Application Number Title Priority Date Filing Date
PCT/US1990/003008 WO1990014844A2 (fr) 1989-06-06 1990-05-30 Sucres utilises en tant qu'elements de liaison clivables pour l'apport et la liberation d'agents sous forme naturelle

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WO (1) WO1990014844A2 (fr)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5505931A (en) * 1993-03-04 1996-04-09 The Dow Chemical Company Acid cleavable compounds, their preparation and use as bifunctional acid-labile crosslinking agents
US10233212B2 (en) 2015-11-03 2019-03-19 Industrial Technology Research Institute Compounds, linker-drugs and ligand-drug conjugates
WO2018009916A1 (fr) 2016-07-07 2018-01-11 The Board Of Trustees Of The Leland Stanford Junior University Conjugués d'adjuvant d'anticorps
AU2020241686A1 (en) 2019-03-15 2021-11-04 Bolt Biotherapeutics, Inc. Immunoconjugates targeting HER2

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0149760A2 (fr) * 1983-12-07 1985-07-31 Bayer Ag O-Acyl glycosylamides substitués, leurs méthodes de préparation et leur application
US4542225A (en) * 1984-08-29 1985-09-17 Dana-Farber Cancer Institute, Inc. Acid-cleavable compound
WO1987003286A1 (fr) * 1985-11-29 1987-06-04 The University Of Melbourne Composes conjugues a des anticorps de ricine
EP0251304A2 (fr) * 1986-07-03 1988-01-07 Takeda Chemical Industries, Ltd. Dérivés de glycosyle et leur utilisation
US4758421A (en) * 1985-03-15 1988-07-19 The Board Of Trustees Of The Leland Stanford Junior University Bleomycin conjugates and method
EP0318948A2 (fr) * 1987-12-02 1989-06-07 Neorx Corporation Immunoconjugués clivables pour la délivrance et libération d'agents sous forme naturelle
EP0336364A2 (fr) * 1988-04-06 1989-10-11 Neorx Corporation Substrats cellulaires modifiés utilisés comme linkers pour une rétention supérieure d'agents diagnostiques et thérapeutiques dans les cellules

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0149760A2 (fr) * 1983-12-07 1985-07-31 Bayer Ag O-Acyl glycosylamides substitués, leurs méthodes de préparation et leur application
US4542225A (en) * 1984-08-29 1985-09-17 Dana-Farber Cancer Institute, Inc. Acid-cleavable compound
US4758421A (en) * 1985-03-15 1988-07-19 The Board Of Trustees Of The Leland Stanford Junior University Bleomycin conjugates and method
WO1987003286A1 (fr) * 1985-11-29 1987-06-04 The University Of Melbourne Composes conjugues a des anticorps de ricine
EP0251304A2 (fr) * 1986-07-03 1988-01-07 Takeda Chemical Industries, Ltd. Dérivés de glycosyle et leur utilisation
EP0318948A2 (fr) * 1987-12-02 1989-06-07 Neorx Corporation Immunoconjugués clivables pour la délivrance et libération d'agents sous forme naturelle
EP0336364A2 (fr) * 1988-04-06 1989-10-11 Neorx Corporation Substrats cellulaires modifiés utilisés comme linkers pour une rétention supérieure d'agents diagnostiques et thérapeutiques dans les cellules

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Publication number Publication date
WO1990014844A2 (fr) 1990-12-13

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