WO1989011877A3 - Conjugates for bone imaging and bone cancer therapy - Google Patents

Conjugates for bone imaging and bone cancer therapy Download PDF

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Publication number
WO1989011877A3
WO1989011877A3 PCT/US1989/002510 US8902510W WO8911877A3 WO 1989011877 A3 WO1989011877 A3 WO 1989011877A3 US 8902510 W US8902510 W US 8902510W WO 8911877 A3 WO8911877 A3 WO 8911877A3
Authority
WO
WIPO (PCT)
Prior art keywords
bone
conjugates
atoms
cancer therapy
imaging
Prior art date
Application number
PCT/US1989/002510
Other languages
French (fr)
Other versions
WO1989011877A2 (en
Inventor
Alan R Fritzberg
Jean-Luc E Vanderheyden
Sudhakar Kasina
Jeffrey N Fitzner
Original Assignee
Neorx Corp
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 Neorx Corp filed Critical Neorx Corp
Priority to EP89907544A priority Critical patent/EP0444038B1/en
Priority to DE68925034T priority patent/DE68925034T2/en
Publication of WO1989011877A2 publication Critical patent/WO1989011877A2/en
Publication of WO1989011877A3 publication Critical patent/WO1989011877A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F13/00—Compounds containing elements of Groups 7 or 17 of the Periodic Table
    • C07F13/005—Compounds without a metal-carbon linkage
    • 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
    • A61K51/0497—Organic compounds conjugates with a carrier being an organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/3804—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
    • C07F9/3839—Polyphosphonic acids
    • C07F9/3873—Polyphosphonic acids containing nitrogen substituent, e.g. N.....H or N-hydrocarbon group which can be substituted by halogen or nitro(so), N.....O, N.....S, N.....C(=X)- (X =O, S), N.....N, N...C(=X)...N (X =O, S)
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The present invention provides conjugates formed from calcified tissues targeting agents and radiolabeled compounds. One such conjugate comprises a chelate and a targeting agent that is capable of associating with calcified tissue, wherein the chelate contains at least four atoms selected from nitrogen atoms or sulfur atoms or combinations thereof as the donor atoms. Another aspect of the invention provides conjugates for diagnostic and therapeutic purposes, including those related to bone cancer.
PCT/US1989/002510 1988-06-10 1989-06-08 Conjugates for bone imaging and bone cancer therapy WO1989011877A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP89907544A EP0444038B1 (en) 1988-06-10 1989-06-08 Conjugates for bone imaging and bone cancer therapy
DE68925034T DE68925034T2 (en) 1988-06-10 1989-06-08 CONJUGATES FOR BONE IMAGING AND THERAPY OF BONE CANCER.

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US20515688A 1988-06-10 1988-06-10
US205,156 1988-06-10
US207,686 1988-06-16
US07/207,686 US5089249A (en) 1988-06-10 1988-06-16 Conjugates for bone imaging and bone cancer therapy

Publications (2)

Publication Number Publication Date
WO1989011877A2 WO1989011877A2 (en) 1989-12-14
WO1989011877A3 true WO1989011877A3 (en) 1990-03-08

Family

ID=26900166

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1989/002510 WO1989011877A2 (en) 1988-06-10 1989-06-08 Conjugates for bone imaging and bone cancer therapy

Country Status (8)

Country Link
US (1) US5089249A (en)
EP (1) EP0444038B1 (en)
JP (1) JPH03504976A (en)
AT (1) ATE131073T1 (en)
AU (1) AU3842989A (en)
CA (1) CA1338072C (en)
DE (1) DE68925034T2 (en)
WO (1) WO1989011877A2 (en)

Families Citing this family (23)

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US4965392A (en) * 1987-03-26 1990-10-23 Neorx Corporation Chelating compounds for metal-radionuclide labeled proteins
DE68927479T2 (en) * 1988-05-02 1997-04-03 Phanos Tech Inc CONNECTIONS, COMPOSITIONS AND METHOD FOR BINDING ORGANIC AFFECTION SUBSTANCES TO SURFACE MEMBRANES OF BIOPARTICLES
US5700444A (en) * 1992-02-20 1997-12-23 Rhomed Incorporated Chemotactic peptide pharmaceutical applications
US5645815A (en) 1991-02-08 1997-07-08 Diatide, Inc. Radiolabled compounds for thrombus imaging
WO1992019274A1 (en) * 1991-05-08 1992-11-12 Mallinckrodt Medical, Inc. Technetium chelates to be used for determining the renal function
US5808091A (en) 1991-10-29 1998-09-15 Bracco International B.V. Rhenium and technetium complexes containing a hypoxia localizing moiety
US5463080A (en) * 1992-08-27 1995-10-31 Bracco International B.V. 2,4,6-triiodo-1,3-benzenedicarboxylic acid compounds used as radiolabelling reagents
US5608110A (en) * 1993-06-15 1997-03-04 Bracco International B.V. Heteroatom-bearing ligands and metal complexes thereof
DE69408145T2 (en) * 1993-07-19 1998-09-03 Resolution Pharm Inc HYDRAZINE WITH A N3S CONFIGURATION AS RADIONUCLEID CHELATORS
US5858327A (en) * 1993-09-03 1999-01-12 Resolutions Pharmaceuticals, Inc. Hydrazino-type N2 S2 radionuclide chelating compounds
US5574140A (en) * 1993-09-03 1996-11-12 Resolution Pharmaceutical Inc. Hydrazino-type N2 S2 chelators
ATE334704T1 (en) * 1993-11-16 2006-08-15 Bracco Int Bv IMMOBILIZED MARKING METHOD
CA2190727C (en) * 1994-05-19 2006-07-18 Sudhakar Kasina Aromatic amine substituted bridged nitrogen and sulfur donor atom ligands for imaging
BR9408590A (en) * 1994-06-03 1997-08-26 Malinckrodt Medical Inc Bone imaging agents quickly eliminated from 99m technetium phosphonate
US6005083A (en) 1997-03-28 1999-12-21 Neorx Corporation Bridged aromatic substituted amine ligands with donor atoms
US6359111B1 (en) 1998-05-28 2002-03-19 Neorx Corporation Opioid receptor targeting
EP1191948A2 (en) * 1999-06-11 2002-04-03 Neorx Corporation High dose radionuclide complexes for bone marrow suppression
US7094885B2 (en) * 1999-07-11 2006-08-22 Neorx Corporation Skeletal-targeted radiation to treat bone-associated pathologies
JP2001114792A (en) 1999-10-12 2001-04-24 Nihon Medi Physics Co Ltd Bisphosphonic acid derivative and its radioactive isotope- labeled product
AU2002249935A1 (en) 2001-01-08 2002-08-19 Neorx Corporation Radioactively labelled conjugates of phosphonates
US7053188B2 (en) 2002-02-22 2006-05-30 Purdue Research Foundation Monoclonal antibodies specific for neoplasia-specific NADH:disulfide reductase
TW200505934A (en) * 2003-03-26 2005-02-16 Nihon Mediphysics Co Ltd Compound having affinity with calcified tissue
WO2008004000A1 (en) * 2006-07-03 2008-01-10 Generics [Uk] Limited Novel process for the preparation of bisphosphonic acids

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3974268A (en) * 1975-05-30 1976-08-10 Research Corporation Bone-seeking technetium-99m imidodiphosphonate complex
EP0135160A2 (en) * 1983-08-19 1985-03-27 Massachusetts Institute Of Technology Bisamide bisthiol compounds useful for making technetium radiodiagnostic renal agents
EP0188256A2 (en) * 1985-01-14 1986-07-23 NeoRx Metal radionuclide labeled proteins for diagnosis and therapy
WO1987001289A1 (en) * 1985-08-28 1987-03-12 Amersham International Plc BONE-SEEKING COMPLEXES OF TECHNETIUM-99m

Family Cites Families (26)

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Publication number Priority date Publication date Assignee Title
US3989730A (en) * 1972-06-15 1976-11-02 Research Corporation Bone-seeking technetium-99m complex
US4082840A (en) * 1972-09-13 1978-04-04 New England Nuclear Corporation Bone seeking technetium 99m complex
US4016249A (en) * 1972-09-13 1977-04-05 New England Nuclear Corporation Bone seeking technetium 99m complex
US3852414A (en) * 1972-09-13 1974-12-03 New England Nuclear Corp Bone seeking technetium 99m stannous phosphate complex
CA1027135A (en) * 1973-06-11 1978-02-28 Research Corporation Bone-seeking technetium-99m complex
US4032625A (en) * 1973-06-11 1977-06-28 Research Corporation Bone-seeking technetium-99m complex
US3987157A (en) * 1974-08-29 1976-10-19 Union Carbide Corporation Technetium 99-m labeled radio-diagnostic agents employing stannous tartrate and method of preparation
US4017595A (en) * 1975-08-28 1977-04-12 Research Corporation Bone-seeking indium-113m or indium-111 organic phosphonate complexes
US4233284A (en) * 1978-03-31 1980-11-11 The Procter & Gamble Company Stabilized radiographic scanning agents
US4337240A (en) * 1978-04-20 1982-06-29 New England Nuclear Corporation Denatured albumin complexes for radioscintigraphic imaging and evaluation of reticuloendothelial systems
US4247534A (en) * 1978-07-31 1981-01-27 The Procter & Gamble Company Radiographic scanning agent
JPS5750928A (en) * 1980-09-13 1982-03-25 Nippon Mejifuijitsukusu Kk Diagnostic agent for scanning bone
US4444690A (en) * 1982-02-25 1984-04-24 University Patents, Inc. Technetium chelates
US4504462A (en) * 1982-06-10 1985-03-12 Mallinckrodt, Inc. Process for making a lyophilized product for use in skeletal imaging
US4510125A (en) * 1982-12-08 1985-04-09 Mallinckrodt, Inc. Process for making lyophilized radiographic imaging kit
GB8310438D0 (en) * 1983-04-18 1983-05-25 Amersham Int Plc Bone-seeking complexes of technetium-99m
DE3331159A1 (en) * 1983-08-30 1985-03-14 Hoechst Ag, 6230 Frankfurt N- (4-AMINOBENZOYL) AMINODICARBONIC ACIDS FOR THE STABILIZATION OF TECHNETIUM-99M PREPARATIONS, STABILIZED INJECTION PREPARATIONS AND METHOD FOR THEIR PRODUCTION
US4582700A (en) * 1983-09-01 1986-04-15 Mallinckrodt, Inc. Products and processes
US4560548A (en) * 1984-04-10 1985-12-24 The Dow Chemical Company Bone seeking Tc-99m complexes of phosphonate derivatives of bis(aminoalkyl)piperazine
US4638051A (en) * 1984-04-30 1987-01-20 The Johns Hopkins University Brain imaging radiopharmaceuticals
US4606907A (en) * 1984-07-02 1986-08-19 The Dow Chemical Company Bone seeking Tc-99m complexes of phosphonate derivatives of polyamidoamines
DE3577550D1 (en) * 1984-09-21 1990-06-13 Dow Chemical Co AMINOCARBONIC ACID COMPLEXES FOR TREATING BONE TUMORS.
US4617184A (en) * 1984-11-29 1986-10-14 Tsolis Alexandros K 99m Tc-1,2-dihydroxy-1,2-bis(dihydroxyphosphinyl)ethane complex for skeleton scanning
US4830847A (en) * 1985-06-28 1989-05-16 The Procter & Gamble Company Diphosphonate-derivatized macromolecules
GB8615916D0 (en) * 1986-06-30 1986-08-06 Amersham Int Plc Bone-seeking complexes of technetium-99m
ATE106898T1 (en) * 1987-03-26 1994-06-15 Neorx Corp METAL RADIONUCLIDE LABELED PROTEINS AND GLYCOPROTEINS FOR DIAGNOSIS AND THERAPY.

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3974268A (en) * 1975-05-30 1976-08-10 Research Corporation Bone-seeking technetium-99m imidodiphosphonate complex
EP0135160A2 (en) * 1983-08-19 1985-03-27 Massachusetts Institute Of Technology Bisamide bisthiol compounds useful for making technetium radiodiagnostic renal agents
EP0188256A2 (en) * 1985-01-14 1986-07-23 NeoRx Metal radionuclide labeled proteins for diagnosis and therapy
WO1987001289A1 (en) * 1985-08-28 1987-03-12 Amersham International Plc BONE-SEEKING COMPLEXES OF TECHNETIUM-99m

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
International Journal of Radiation Applications & Instrumentation, part B, Nucl. Med. Biol., Volume 14, No. 3, 1987, Pergamon Journals Ltd, (GB), A.R. KETRING: "153Sm-EDTMP and 186Re-HEDP as Bone Therapeutic Radiopharmaceuticals", pages 223-232 *
The Journal of Nuclear Medicine, Volume 29, No. 5, May 1988, (New York, US), E.H. CHEESMAN et al.: "Technetium-99m ECD: Ester-Derivatized Diaminedithiol Tc Complexes for Imaging Brain Perfusion", page 788, No. 197 *

Also Published As

Publication number Publication date
US5089249A (en) 1992-02-18
EP0444038A1 (en) 1991-09-04
AU3842989A (en) 1990-01-05
ATE131073T1 (en) 1995-12-15
WO1989011877A2 (en) 1989-12-14
EP0444038B1 (en) 1995-12-06
DE68925034T2 (en) 1996-04-25
DE68925034D1 (en) 1996-01-18
CA1338072C (en) 1996-02-20
JPH03504976A (en) 1991-10-31

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