ES2040743T3 - Compuestos conjugados comprendiendo un ligando macrociclico y un anticuerpo. - Google Patents

Compuestos conjugados comprendiendo un ligando macrociclico y un anticuerpo.

Info

Publication number
ES2040743T3
ES2040743T3 ES198787301251T ES87301251T ES2040743T3 ES 2040743 T3 ES2040743 T3 ES 2040743T3 ES 198787301251 T ES198787301251 T ES 198787301251T ES 87301251 T ES87301251 T ES 87301251T ES 2040743 T3 ES2040743 T3 ES 2040743T3
Authority
ES
Spain
Prior art keywords
alkyl
antibody
league
macrocyclic
understanding
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 - Lifetime
Application number
ES198787301251T
Other languages
English (en)
Inventor
David Parker
Thomas Andrew Millican
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.)
UCB Celltech Ltd
Original Assignee
Celltech R&D Ltd
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 Celltech R&D Ltd filed Critical Celltech R&D Ltd
Application granted granted Critical
Publication of ES2040743T3 publication Critical patent/ES2040743T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/10—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2123/00—Preparations for testing in vivo

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Optics & Photonics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Immunology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Physics & Mathematics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Saccharide Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)

Abstract

UN COMPUESTO CONJUGADO TIENE LA ESTRUCTURA (I) DONDE: R1 ES -(CH2)P-R6-(CH2)Q- SIENDO P Y Q IGUALES O DIFERENTES CON VALOR 0, 1 O 2, Y -R6- ES -(CH2)N- DONDE N ES 0 O 1, -NH-, -O-, -S- O, R1 ESTA OPCIONALMENTE SUSTITUIDO CON UN ALQUILO EN CASO DE QUE NI P NI Q SEA CERO O NO SIENDO R6 UN -CH2-, R2 SON -CH2CH2- O -CH2CH2CH2- OPCIONALMENTE SUSTITUIDOS CON UN ALQUILO, UN ALCOXIALQUILO O UN HIDROXIALQUILO. R3 SON IGUALES O DIFERENTES, Y SON -H, ALQUILO, HIDROXIALQUILO, ALCOXIALQUILO, CARBOXIALQUILO, ESTER DE CARBOXIALQUILO, FOSFATO, SULFONATO O FOSFONATO. R4 ES (II), O (III) OPCIONALMENTE SUSTITUIDOS CON ALQUILO, DONDE R7 ES -H, ALQUILO, HIDROXIALQUILO O ALCOXIALQUILO SIEMPRE QUE CUANDO R4 SEA -CH-CH-CH2-, R3 NO SEA CARBOXIALQUILO. R5 ES UN LIGANTE, AB ES UN ANTICUERPO. EL COMPUESTO CONJUGADO PROPORCIONA COMPLEJOS DE METALES TALES COMO TC, CO, RE, CU, AU Y AG QUE SON REACTIVOS UTILES PARA LA OBTENCION DE IMAGENES "IN VIVO" Y PARA TERAPIA.
ES198787301251T 1986-02-13 1987-02-13 Compuestos conjugados comprendiendo un ligando macrociclico y un anticuerpo. Expired - Lifetime ES2040743T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB868603537A GB8603537D0 (en) 1986-02-13 1986-02-13 Conjugate compound

Publications (1)

Publication Number Publication Date
ES2040743T3 true ES2040743T3 (es) 1993-11-01

Family

ID=10592982

Family Applications (1)

Application Number Title Priority Date Filing Date
ES198787301251T Expired - Lifetime ES2040743T3 (es) 1986-02-13 1987-02-13 Compuestos conjugados comprendiendo un ligando macrociclico y un anticuerpo.

Country Status (10)

Country Link
US (1) US5087696A (es)
EP (1) EP0238196B1 (es)
JP (1) JPS63502659A (es)
AT (1) ATE67679T1 (es)
AU (1) AU7027987A (es)
DE (1) DE3773237D1 (es)
ES (1) ES2040743T3 (es)
GB (1) GB8603537D0 (es)
GR (1) GR3002794T3 (es)
WO (1) WO1987005030A1 (es)

Families Citing this family (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4885363A (en) * 1987-04-24 1989-12-05 E. R. Squibb & Sons, Inc. 1-substituted-1,4,7-triscarboxymethyl-1,4,7,10-tetraazacyclododecane and analogs
MX174467B (es) * 1986-01-23 1994-05-17 Squibb & Sons Inc 1,4,7-triscarboximetil-1,4,7,10-tetraazaciclodo decano substituido en 1 y compuestos analogos
US5271927A (en) * 1986-02-13 1993-12-21 Celltech Limited Antibody conjugates with macrocyclic ligands
DE3625417C2 (de) * 1986-07-28 1998-10-08 Schering Ag Tetraazacyclododecan-Derivate
FR2614020B1 (fr) * 1987-04-14 1989-07-28 Guerbet Sa Nouveaux ligands cycliques azotes, complexes metalliques formes par ces ligands, compositions de diagnostic contenant ces complexes et procede de preparation des ligands.
DE3713842A1 (de) * 1987-04-22 1988-11-17 Schering Ag Substituierte cyclische komplexbildner, komplexe und komplexsalze, verfahren zu deren herstellung und diese enthaltende pharmazeutische mittel
US4994560A (en) * 1987-06-24 1991-02-19 The Dow Chemical Company Functionalized polyamine chelants and radioactive rhodium complexes thereof for conjugation to antibodies
US5489425A (en) * 1987-06-24 1996-02-06 The Dow Chemical Company Functionalized polyamine chelants
ES2033433T3 (es) * 1987-07-16 1993-03-16 Nycomed As Procedimiento para preparar acidos aminopolicarboxilicos y sus derivados.
GB8719042D0 (en) * 1987-08-12 1987-09-16 Parker D Conjugate compounds
GB8719041D0 (en) * 1987-08-12 1987-09-16 Parker D Conjugate compounds
JP2520262B2 (ja) * 1987-08-21 1996-07-31 春幸 川原 パツチテスト材料
DE3728600A1 (de) * 1987-08-27 1989-03-09 Hoechst Ag Verfahren zur markierung von substanzen mit technetium oder rhenium
US4952394A (en) * 1987-11-23 1990-08-28 Bristol-Myers Company Drug-monoclonal antibody conjugates
DE68925904T2 (de) * 1988-05-25 1996-10-31 The United States Of America, Represented By The Secretary, U.S. Department Of Commerce, Springfield, Va. Makrocyclische chelate und verwendungsverfahren
US4988496A (en) * 1988-05-31 1991-01-29 Neorx Corporation Metal radionuclide chelating compounds for improved chelation kinetics
CA1340527C (en) * 1988-05-31 1999-05-04 Lidia Vallarino Macrocyclic complexes of yttrium, the lanthanides and the actinides having peripheral coupling functionalities
US5218128A (en) * 1988-06-15 1993-06-08 Centocor, Inc. Bifunctional coupling agents and radionuclide labeled compositions prepared therefrom
CN1033030C (zh) * 1988-06-24 1996-10-16 唐化学原料公司 大环双官能螯合剂及其配合物和抗体共轭物的制备方法
DE353450T1 (de) * 1988-06-24 1990-09-06 The Dow Chemical Co., Midland, Mich. Macrocyclische bifunktionelle chelatbildner, komplexe davon und ihre konjugierten antikoerper.
US5756065A (en) * 1988-06-24 1998-05-26 The Dow Chemical Company Macrocyclic tetraazacyclododecane conjugates and their use as diagnostic and therapeutic agents
FR2636632B1 (fr) * 1988-09-16 1996-02-02 Oris Ind Produits radiopharmaceutiques constitues par des complexes de tc, re ou y comportant des ligands tetraphosphonates et leur preparation
GB8903021D0 (en) * 1989-02-10 1989-03-30 Celltech Ltd Chemical compounds
US5354554A (en) * 1989-02-10 1994-10-11 Celltech Limited Crosslinked antibodies and processes for their preparation
GB8903022D0 (en) * 1989-02-10 1989-03-30 Celltech Ltd Chemical compounds
US5714149A (en) * 1989-02-10 1998-02-03 Celltech Therapeutics Limited Crosslinked antibodies and processes for their preparation
DE3911816A1 (de) * 1989-04-11 1990-10-25 Hoechst Ag Substituierte 1,4,7,10-tetraazacyclotridecane, verfahren zu deren herstellung sowie verwendung derselben zur markierung von substanzen mit radionukliden
US5308604A (en) * 1989-04-19 1994-05-03 Deutsches Krebsforschungsinstitut Conjugates for tumor localization and/or tumor therapy
US5808003A (en) * 1989-05-26 1998-09-15 Perimmune Holdings, Inc. Polyaminocarboxylate chelators
US5292868A (en) * 1989-05-26 1994-03-08 Akzo N.V. Chelating agents for attaching metal ions to proteins
FR2654102B1 (fr) * 1989-11-09 1992-01-10 Air Liquide Procede de synthese de derives polyazotes cycliques.
DE3938992A1 (de) * 1989-11-21 1991-05-23 Schering Ag Kaskadenpolymer-gebundene komplexbildner, deren komplexe und konjugate, verfahren zu ihrer herstellung und diese enthaltende pharmazeutische mittel
US5183653A (en) * 1990-04-13 1993-02-02 E. R. Squibb & Sons, Inc. Boronic acid adducts of metal dioxime complexes useful in labelling proteins and other amine-containing compounds
NZ243697A (en) * 1991-07-26 1994-04-27 Hoechst Ag Producing molecules labelled with a complex of technetium and/or rhenium with a macrocyclic agent; tumour-test-kit containing reactants therefor
US5739294A (en) * 1991-12-10 1998-04-14 The Dow Chemical Company Bicyclopol yazamacrocyclophosphonic acid complexes for use as contrast agents
US5480990A (en) * 1991-12-10 1996-01-02 The Dow Chemical Company Bicyclopolyazamacrocyclocarboxylic acid complexes for use as contrast agents
US5428139A (en) * 1991-12-10 1995-06-27 The Dow Chemical Company Bicyclopolyazamacrocyclophosphonic acid complexes for use as radiopharmaceuticals
US5310535A (en) * 1992-04-24 1994-05-10 The Dow Chemical Company Carboxamide modified polyamine chelators and radioactive complexes thereof for conjugation to antibodies
EP0955066A3 (en) * 1992-07-31 2002-08-28 Australian Nuclear Science And Technology Organisation Metal complexes of hydroxyaryl containing aminocarboxylic acid chelating agents
US5807535A (en) * 1992-07-31 1998-09-15 Australian Nuclear Science & Technology Organisation Metal complexes of hydroxyaryl containing aminocarboxylic acid chelating agents
US5648218A (en) * 1993-02-12 1997-07-15 Sealite Sciences, Inc. Preparation of photoprotein conjugates and methods of use thereof
EP0683822B1 (en) * 1993-02-12 2002-05-02 Sealite Sciences, Inc. Preparation of photoprotein conjugates and methods of use thereof
US5428156A (en) * 1993-04-02 1995-06-27 Associated Universities, Inc. Synthesis of macrocyclic polyaminocarboxylates and their use for preparing stable radiometal antibody immunoconjugates for therapy, spect and pet imaging
US5358704A (en) * 1993-09-30 1994-10-25 Bristol-Myers Squibb Hepatobiliary tetraazamacrocyclic magnetic resonance contrast agents
US20030130185A1 (en) * 2000-09-29 2003-07-10 David Bar-Or Metal-binding compounds and uses therefor
US20030158111A1 (en) * 1999-10-01 2003-08-21 David Bar-Or Methods and products for oral care
US7592304B2 (en) 1999-10-01 2009-09-22 Dmi Life Sciences, Inc. Metal-binding compounds and uses therefor
WO2001025265A1 (en) 1999-10-01 2001-04-12 Dmi Biosciences, Inc. Metal-binding compounds and uses therefor
US7632803B2 (en) * 1999-10-01 2009-12-15 Dmi Life Sciences, Inc. Metal-binding compounds and uses therefor
US6565828B2 (en) 2000-04-07 2003-05-20 Bristol-Myers Squibb Company Macrocyclic chelants for metallopharmaceuticals
US6517814B2 (en) 2001-01-09 2003-02-11 Bristol-Myers Squibb Pharma Company Macrocyclic chelants useful for metallopharmaceuticals
HUP0400027A3 (en) 2001-02-23 2006-01-30 Bristol Myers Squibb Pharma Co Labeled macrophage scavenger receptor antagonosts for imaging atherosclerosis and vulnerable plaque
EP1689448B1 (en) 2003-12-01 2015-07-29 Immunomedics Inc. Method for preparing dota-antibody conjugates
WO2007128874A1 (en) * 2006-05-05 2007-11-15 Wallac Oy Biomolecule labeling reactants based on azacycloalkanes and conjugates derived thereof
GB201419108D0 (en) * 2014-10-27 2014-12-10 Glythera Ltd Materials and methods relating to linkers for use in antibody drug conjugates

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2803528C2 (de) * 1977-03-09 1984-10-18 Tabushi, Iwao, Kyoto Schwermetallionen-Adsorbens und dessen Verwendung zum Adsorbieren von Schwermetallionen
FR2550449B1 (fr) * 1983-08-12 1986-01-31 Commissariat Energie Atomique Agents de relaxation specifiques d'organes ou de pathologies, utilisables pour modifier les contrastes en imagerie medicale par resonance magnetique nucleaire
CA1260827A (en) * 1984-08-31 1989-09-26 Richard C. Siegel Antibody-metal ion complexes
US4899755A (en) * 1985-05-08 1990-02-13 The General Hospital Corporation Hepatobiliary NMR contrast agents
US4678667A (en) * 1985-07-02 1987-07-07 501 Regents of the University of California Macrocyclic bifunctional chelating agents
US4885363A (en) * 1987-04-24 1989-12-05 E. R. Squibb & Sons, Inc. 1-substituted-1,4,7-triscarboxymethyl-1,4,7,10-tetraazacyclododecane and analogs

Also Published As

Publication number Publication date
DE3773237D1 (de) 1991-10-31
JPS63502659A (ja) 1988-10-06
ATE67679T1 (de) 1991-10-15
EP0238196A1 (en) 1987-09-23
GB8603537D0 (en) 1986-03-19
GR3002794T3 (en) 1993-01-25
EP0238196B1 (en) 1991-09-25
AU7027987A (en) 1987-09-09
US5087696A (en) 1992-02-11
WO1987005030A1 (en) 1987-08-27

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