WO1993021963A3 - Carboxamide modified polyamine chelators and radioactive complexes and conjugation - Google Patents

Carboxamide modified polyamine chelators and radioactive complexes and conjugation Download PDF

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Publication number
WO1993021963A3
WO1993021963A3 PCT/US1993/003844 US9303844W WO9321963A3 WO 1993021963 A3 WO1993021963 A3 WO 1993021963A3 US 9303844 W US9303844 W US 9303844W WO 9321963 A3 WO9321963 A3 WO 9321963A3
Authority
WO
WIPO (PCT)
Prior art keywords
conjugation
modified polyamine
chelators
complexes
radioactive complexes
Prior art date
Application number
PCT/US1993/003844
Other languages
French (fr)
Other versions
WO1993021963A2 (en
Inventor
William J Kruper Jr
William A Fordyce
A Dean Sherry
Original Assignee
Dow Chemical Co
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 to DE69317771T priority Critical patent/DE69317771T2/en
Priority to CA002134092A priority patent/CA2134092C/en
Priority to JP51940593A priority patent/JP3850870B2/en
Priority to KR1019940703764A priority patent/KR100245941B1/en
Application filed by Dow Chemical Co filed Critical Dow Chemical Co
Priority to HU9403051A priority patent/HU222761B1/en
Priority to ES93912349T priority patent/ES2114051T3/en
Priority to DK93912349T priority patent/DK0637253T3/en
Priority to AU42926/93A priority patent/AU674853B2/en
Priority to EP93912349A priority patent/EP0637253B1/en
Publication of WO1993021963A2 publication Critical patent/WO1993021963A2/en
Publication of WO1993021963A3 publication Critical patent/WO1993021963A3/en
Priority to FI944973A priority patent/FI944973A/en
Priority to NO944019A priority patent/NO304552B1/en
Priority to GR980400717T priority patent/GR3026533T3/en
Priority to HK98105598A priority patent/HK1006632A1/en

Links

Classifications

    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • 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
    • A61K51/0474—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
    • A61K51/0478—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group complexes from non-cyclic ligands, e.g. EDTA, MAG3
    • 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
    • A61K51/0474—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
    • A61K51/0482—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group chelates from cyclic ligands, e.g. DOTA
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Macromolecular Compounds Obtained By Forming Nitrogen-Containing Linkages In General (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Polymers With Sulfur, Phosphorus Or Metals In The Main Chain (AREA)
  • Peptides Or Proteins (AREA)
  • Paper (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Polysaccharides And Polysaccharide Derivatives (AREA)

Abstract

A group of functionalized polyaminocarboxamide modified chelators, such as 1,4 7,10-tetraaza-1-N-(1-carboxy-3-(4-aminophenyl)propyl)-7-N-(1-carboxymethyl)bis-4,10-N,N-(carboxamidomethyl)cyclododecane and 1,4 7,10-tetraaza-1-N-(1-carboxy-3-(4-aminophenyl)propyl)bis-4,7-N,N-(1-carboxymethyl)-10-N-(carboxamidomethyl)cyclododecane are disclosed. These modified chelators are capable of forming complexes with rare earth-type metal ions. When the complexes are covalently attached to an antibody or antibody fragment, they can be used in therapeutic and diagnostic applications.
PCT/US1993/003844 1992-04-24 1993-04-23 Carboxamide modified polyamine chelators and radioactive complexes and conjugation WO1993021963A2 (en)

Priority Applications (13)

Application Number Priority Date Filing Date Title
ES93912349T ES2114051T3 (en) 1992-04-24 1993-04-23 CHELANTS BASED ON POLYAMINE MODIFIED BY CARBOXAMIDE AND RADIOACTIVE COMPLEXES AND CONJUGATES.
JP51940593A JP3850870B2 (en) 1992-04-24 1993-04-23 Carboxamide-modified polyamine chelating agents and radioactive complexes and conjugates
KR1019940703764A KR100245941B1 (en) 1992-04-24 1993-04-23 Carboxamide modified polyamine chelators and radioactive complexes and conjugates
AU42926/93A AU674853B2 (en) 1992-04-24 1993-04-23 Carboxamide modified polyamine chelators and radioactive complexes and conjugates
HU9403051A HU222761B1 (en) 1992-04-24 1993-04-23 Carboxamide modifield polyamine celators and radioactive complexes and conjugates
CA002134092A CA2134092C (en) 1992-04-24 1993-04-23 Carboxamide modified polyamine chelators and radioactive complexes thereof for conjugation to antibodies
DK93912349T DK0637253T3 (en) 1992-04-24 1993-04-23 Carboxamide modified polyamine chelators as well as radioactive complexes and conjugates
DE69317771T DE69317771T2 (en) 1992-04-24 1993-04-23 CARBOXAMIDE-MODIFIED POLYAMINE CHELATORS, RADIOACTIVE COMPLEXES AND CONJUGATES
EP93912349A EP0637253B1 (en) 1992-04-24 1993-04-23 Carboxamide modified polyamine chelators and radioactive complexes and conjugates
FI944973A FI944973A (en) 1992-04-24 1994-10-21 Carboxamide modified polyaminkelate formers and radioactive complexes and conjugates
NO944019A NO304552B1 (en) 1992-04-24 1994-10-21 Complex compounds, conjugates, pharmaceutical preparations containing such and compounds
GR980400717T GR3026533T3 (en) 1992-04-24 1998-04-03 Carboxamide modified polyamine chelators and radioactive complexes and conjugation.
HK98105598A HK1006632A1 (en) 1992-04-24 1998-06-18 Carboxamide modified polyamine chelators and radioactive complexes and conjugates

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US07/874,244 1992-04-24
US07/874,244 US5310535A (en) 1992-04-24 1992-04-24 Carboxamide modified polyamine chelators and radioactive complexes thereof for conjugation to antibodies

Publications (2)

Publication Number Publication Date
WO1993021963A2 WO1993021963A2 (en) 1993-11-11
WO1993021963A3 true WO1993021963A3 (en) 1993-12-09

Family

ID=25363311

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1993/003844 WO1993021963A2 (en) 1992-04-24 1993-04-23 Carboxamide modified polyamine chelators and radioactive complexes and conjugation

Country Status (18)

Country Link
US (2) US5310535A (en)
EP (1) EP0637253B1 (en)
JP (1) JP3850870B2 (en)
KR (1) KR100245941B1 (en)
AT (1) ATE164522T1 (en)
AU (1) AU674853B2 (en)
CA (1) CA2134092C (en)
DE (1) DE69317771T2 (en)
DK (1) DK0637253T3 (en)
ES (1) ES2114051T3 (en)
FI (1) FI944973A (en)
GR (1) GR3026533T3 (en)
HK (1) HK1006632A1 (en)
HU (1) HU222761B1 (en)
NO (1) NO304552B1 (en)
NZ (1) NZ252867A (en)
SG (1) SG49756A1 (en)
WO (1) WO1993021963A2 (en)

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US6099856A (en) 1992-06-15 2000-08-08 Emisphere Technologies, Inc. Active agent transport systems
US5629020A (en) * 1994-04-22 1997-05-13 Emisphere Technologies, Inc. Modified amino acids for drug delivery
US5578323A (en) 1992-06-15 1996-11-26 Emisphere Technologies, Inc. Proteinoid carriers and methods for preparation and use thereof
US5811127A (en) 1992-06-15 1998-09-22 Emisphere Technologies, Inc. Desferrioxamine oral delivery system
US5792451A (en) 1994-03-02 1998-08-11 Emisphere Technologies, Inc. Oral drug delivery compositions and methods
US5643957A (en) 1993-04-22 1997-07-01 Emisphere Technologies, Inc. Compounds and compositions for delivering active agents
US6461643B2 (en) * 1993-04-22 2002-10-08 Emisphere Technologies, Inc. Oral drug delivery compositions and methods
US5709861A (en) 1993-04-22 1998-01-20 Emisphere Technologies, Inc. Compositions for the delivery of antigens
EP1025840B1 (en) 1993-04-22 2005-06-29 Emisphere Technologies, Inc. Oral drug compositions
US5989539A (en) 1995-03-31 1999-11-23 Emisphere Technologies, Inc. Compounds and compositions for delivering active agents
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US6001347A (en) 1995-03-31 1999-12-14 Emisphere Technologies, Inc. Compounds and compositions for delivering active agents
US5866536A (en) 1995-03-31 1999-02-02 Emisphere Technologies, Inc. Compounds and compositions for delivering active agents
US5965121A (en) 1995-03-31 1999-10-12 Emisphere Technologies, Inc. Compounds and compositions for delivering active agents
US5750147A (en) 1995-06-07 1998-05-12 Emisphere Technologies, Inc. Method of solubilizing and encapsulating itraconazole
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EP1018877A4 (en) * 1995-10-17 2000-08-09 Dovetail Technologies Inc Low molecular weight cell, bone marrow and immune stimulants
EP0904065A4 (en) 1996-06-14 2000-06-14 Emisphere Tech Inc Microencapsulated fragrances and method for preparation
US6358504B1 (en) * 1997-02-07 2002-03-19 Emisphere Technologies, Inc. Compounds and compositions for delivering active agents
US5879681A (en) 1997-02-07 1999-03-09 Emisphere Technolgies Inc. Compounds and compositions for delivering active agents
US5990166A (en) 1997-02-07 1999-11-23 Emisphere Technologies, Inc. Compounds and compositions for delivering active agents
US6060513A (en) 1997-02-07 2000-05-09 Emisphere Technologies, Inc. Compounds and compositions for delivering active agents
US6313088B1 (en) 1997-02-07 2001-11-06 Emisphere Technologies, Inc. 8-[(2-hydroxy-4-methoxy benzoyl) amino]-octanoic acid compositions for delivering active agents
US5939381A (en) 1997-02-07 1999-08-17 Emisphere Technologies, Inc. Compounds and compositions for delivering active agents
US5876710A (en) 1997-02-07 1999-03-02 Emisphere Technologies Inc. Compounds and compositions for delivering active agents
US5804688A (en) 1997-02-07 1998-09-08 Emisphere Technologies, Inc. Compounds and compositions for delivering active agents
US5863944A (en) 1997-04-30 1999-01-26 Emisphere Technologies, Inc. Compounds and compositions for delivering active agents
US5962710A (en) 1997-05-09 1999-10-05 Emisphere Technologies, Inc. Method of preparing salicyloylamino acids
ATE309197T1 (en) 1999-02-05 2005-11-15 Emisphere Tech Inc METHOD FOR PRODUCING ALKYLATED SALICYLAMIDES
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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
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EP0353450A1 (en) * 1988-06-24 1990-02-07 The Dow Chemical Company Macrocyclic bifunctional chelants, complexes thereof and their antibody conjugates
EP0374947A1 (en) * 1988-12-23 1990-06-27 The Dow Chemical Company Process for preparing isothiocyanato functionalized metal complexes
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Also Published As

Publication number Publication date
EP0637253B1 (en) 1998-04-01
SG49756A1 (en) 1998-06-15
NO944019L (en) 1994-12-12
JPH07506365A (en) 1995-07-13
DK0637253T3 (en) 1999-02-01
JP3850870B2 (en) 2006-11-29
EP0637253A1 (en) 1995-02-08
ES2114051T3 (en) 1998-05-16
HU222761B1 (en) 2003-10-28
US5310535A (en) 1994-05-10
HUT70429A (en) 1995-10-30
HK1006632A1 (en) 1999-03-05
DE69317771D1 (en) 1998-05-07
KR950701231A (en) 1995-03-23
NO304552B1 (en) 1999-01-11
DE69317771T2 (en) 1998-07-30
CA2134092C (en) 2003-07-29
AU674853B2 (en) 1997-01-16
WO1993021963A2 (en) 1993-11-11
FI944973A (en) 1994-12-02
NO944019D0 (en) 1994-10-21
ATE164522T1 (en) 1998-04-15
NZ252867A (en) 1997-03-24
GR3026533T3 (en) 1998-07-31
US5739323A (en) 1998-04-14
KR100245941B1 (en) 2000-04-01
CA2134092A1 (en) 1993-11-11
AU4292693A (en) 1993-11-29
FI944973A0 (en) 1994-10-21

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