WO1997010853A3 - Bifunktionelle nicotinamid-chelatbildner vom typ n2s2 für radioaktive isotope - Google Patents

Bifunktionelle nicotinamid-chelatbildner vom typ n2s2 für radioaktive isotope Download PDF

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Publication number
WO1997010853A3
WO1997010853A3 PCT/DE1996/001824 DE9601824W WO9710853A3 WO 1997010853 A3 WO1997010853 A3 WO 1997010853A3 DE 9601824 W DE9601824 W DE 9601824W WO 9710853 A3 WO9710853 A3 WO 9710853A3
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WO
WIPO (PCT)
Prior art keywords
type
chelating agents
radioactive isotopes
nicotinamide
functional
Prior art date
Application number
PCT/DE1996/001824
Other languages
English (en)
French (fr)
Other versions
WO1997010853A2 (de
Inventor
Ludger Dinkelborg
Christoph Stephan Hilger
Wolfgang Kramp
Johannes Platzek
Bernd Raduechel
Original Assignee
Diagnostikforschung Inst
Ludger Dinkelborg
Christoph Stephan Hilger
Wolfgang Kramp
Johannes Platzek
Bernd Raduechel
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 Diagnostikforschung Inst, Ludger Dinkelborg, Christoph Stephan Hilger, Wolfgang Kramp, Johannes Platzek, Bernd Raduechel filed Critical Diagnostikforschung Inst
Priority to AU13005/97A priority Critical patent/AU1300597A/en
Priority to EP96944563A priority patent/EP0851771A2/de
Publication of WO1997010853A2 publication Critical patent/WO1997010853A2/de
Publication of WO1997010853A3 publication Critical patent/WO1997010853A3/de

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575—Hormones
    • C07K14/57536—Endothelin, vasoactive intestinal contractor [VIC]
    • 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
    • A61K51/0497—Organic compounds conjugates with a carrier being an organic compounds
    • 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
    • A61K51/088—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins conjugates with carriers being peptides, polyamino acids or proteins
    • 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
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • 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 System
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/081—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/1013—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/14—Angiotensins: Related peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Physics & Mathematics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Veterinary Medicine (AREA)
  • Biochemistry (AREA)
  • Optics & Photonics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Public Health (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Toxicology (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

Die Erfindung betrifft neue Verbindungen der allgemeinen Formel (I) M - L, worin M für ein Radioisotop von Tc oder Re und L für einen Liganden der allgemeinen Formel (II) steht, worin R?1, R2, R3, R4, R5 und R6¿ unterschiedliche Bedeutung haben können und für Gruppen stehen, die einerseits für die koordinative Bindung von Metallionen, andererseits für die Kopplung an sich selektiv anreichernde Verbindungen geeignet sind. Die neuen Verbindung dienen zur Komplexierung von Technetium und Rhenium und werden in der medizinischen Diagnostik und Therapie eingesetzt.
PCT/DE1996/001824 1995-09-21 1996-09-19 Bifunktionelle nicotinamid-chelatbildner vom typ n2s2 für radioaktive isotope WO1997010853A2 (de)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU13005/97A AU1300597A (en) 1995-09-21 1996-09-19 N2s2-type bi-functional nicotinamide chelating agents for radioactive isotopes
EP96944563A EP0851771A2 (de) 1995-09-21 1996-09-19 Bifunktionelle nicotinamid-chelatbildner vom typ n2s2 für radioaktive isotope

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE1995136783 DE19536783A1 (de) 1995-09-21 1995-09-21 Bifunktionelle Nicotinamid-Chelatbildner vom Typ N¶2¶S¶2¶ für radioaktive Isotope
DE19536783.9 1995-09-21

Publications (2)

Publication Number Publication Date
WO1997010853A2 WO1997010853A2 (de) 1997-03-27
WO1997010853A3 true WO1997010853A3 (de) 1997-08-28

Family

ID=7773890

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/DE1996/001824 WO1997010853A2 (de) 1995-09-21 1996-09-19 Bifunktionelle nicotinamid-chelatbildner vom typ n2s2 für radioaktive isotope

Country Status (5)

Country Link
EP (1) EP0851771A2 (de)
AU (1) AU1300597A (de)
CA (1) CA2232340A1 (de)
DE (1) DE19536783A1 (de)
WO (1) WO1997010853A2 (de)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19652374A1 (de) * 1996-12-04 1998-06-10 Schering Ag Verwendung von Endothelin-Konjugaten in der Therapie, neue Endothelin-Konjugate, diese enthaltende Mittel, sowie Verfahren zu deren Herstellung
US7060251B1 (en) 1997-09-08 2006-06-13 The General Hospital Corporation Imaging agents for early detection and monitoring of cardiovascular plaque
AU9307498A (en) * 1997-09-08 1999-03-29 General Hospital Corporation, The Imaging agents for early detection and monitoring of cardiovascular plaque
US6388062B1 (en) 1998-05-08 2002-05-14 The Wistar Institute Of Anatomy And Biology Modified p53 tetramerization domains having hydrophobic amino acid substitutions
AU3875400A (en) * 1999-03-12 2000-09-28 Government of The United States of America, as represented by The Secretary Department of Health & Human Services, The National Institutes of Health, The Hydrazide inhibitors of hiv-1 integrase
WO2003000657A1 (fr) 2001-06-20 2003-01-03 Daiichi Pharmaceutical Co., Ltd. Derives de diamine
WO2003016302A1 (fr) 2001-08-09 2003-02-27 Daiichi Pharmaceutical Co., Ltd. Derives de diamine
WO2003000680A1 (fr) * 2001-06-20 2003-01-03 Daiichi Pharmaceutical Co., Ltd. Derives de diamine
JP4630267B2 (ja) * 2002-12-25 2011-02-09 第一三共株式会社 ジアミン誘導体
CA2511493A1 (en) * 2002-12-25 2004-07-15 Daiichi Pharmaceutical Co., Ltd. Diamine derivatives
CN1751025B (zh) * 2002-12-25 2010-05-12 第一制药株式会社 二胺衍生物
JP2007510643A (ja) * 2003-11-06 2007-04-26 ジーイー・ヘルスケア・アクスイェ・セルスカプ 医薬化合物

Citations (8)

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Publication number Priority date Publication date Assignee Title
EP0403243A1 (de) * 1989-06-16 1990-12-19 Merck Frosst Canada Inc. Chelat-Derivate von atrialnatriurethischem Faktor (ANF)
WO1993015771A1 (en) * 1992-02-06 1993-08-19 Mallinckrodt Medical, Inc. Ligands for improving metal chelate formation kinetics
WO1994000489A2 (en) * 1992-06-23 1994-01-06 Diatech, Inc. Radioactively-labeled somatostantin-derived peptides for imaging and therapeutic uses
WO1994009128A1 (en) * 1992-10-22 1994-04-28 Mallinckrodt Medical, Inc. Therapeutic treatment for inhibiting vascular restenosis
DE4301871A1 (de) * 1993-01-13 1994-07-14 Diagnostikforschung Inst Neue Mittel zur Diagnose von Gefäßerkrankungen
WO1995006633A1 (en) * 1993-09-03 1995-03-09 Resolution Pharmaceuticals Inc. Hydrazino-type n2s2 chelators
WO1995019791A1 (en) * 1994-01-24 1995-07-27 Neorx Corporation Radiolabeled annexins
WO1995032192A1 (en) * 1994-05-19 1995-11-30 Neorx Corporation Aromatic amine substituted bridged nitrogen and sulfur donor atom ligands for imaging

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0403243A1 (de) * 1989-06-16 1990-12-19 Merck Frosst Canada Inc. Chelat-Derivate von atrialnatriurethischem Faktor (ANF)
WO1993015771A1 (en) * 1992-02-06 1993-08-19 Mallinckrodt Medical, Inc. Ligands for improving metal chelate formation kinetics
WO1994000489A2 (en) * 1992-06-23 1994-01-06 Diatech, Inc. Radioactively-labeled somatostantin-derived peptides for imaging and therapeutic uses
WO1994009128A1 (en) * 1992-10-22 1994-04-28 Mallinckrodt Medical, Inc. Therapeutic treatment for inhibiting vascular restenosis
DE4301871A1 (de) * 1993-01-13 1994-07-14 Diagnostikforschung Inst Neue Mittel zur Diagnose von Gefäßerkrankungen
WO1995006633A1 (en) * 1993-09-03 1995-03-09 Resolution Pharmaceuticals Inc. Hydrazino-type n2s2 chelators
WO1995019791A1 (en) * 1994-01-24 1995-07-27 Neorx Corporation Radiolabeled annexins
WO1995032192A1 (en) * 1994-05-19 1995-11-30 Neorx Corporation Aromatic amine substituted bridged nitrogen and sulfur donor atom ligands for imaging

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
CHI DY ET AL: "Homodimeric and heterodimeric bis(amino thiol) oxometal complexes with rhenium(V) and technetium (V). Control of heterodimeric complex formation and an approach to metal complexes that mimic steroid hormones.", J MED CHEM, APR 1 1994, VOL. 37, NO. 7, PAGES 928-37, XP002034420 *
COULAIS Y ET AL: "SYNTHESIS, CHARACTERIZATION AND BIODISTRIBUTION OF NEW 99MTC OXO AND NITRIDO COMPLEXES WITH BI- AND TETRADENDATE UNSATURATED NS AND N2S2 SCHIFF BASES DERIVED FROM 2-AMINOCYCLOPENTENE-1- DITHIOCARBOXYLIC ACID AS POTENTIAL HEART IMAGING AGENTS", NUCLEAR MEDICINE AND BIOLOGY, vol. 21, no. 2, 1 February 1994 (1994-02-01), pages 263 - 268, XP000434379 *
O'NEIL J P ET AL: "PROGESTIN RADIOPHARMACEUTICALS LABELED WITH TECHNETIUM AND RHENIUM: SYNTHESIS, BINDING AFFINITY, AND IN VIVO DISTRIBUTION OF A NEW PROGESTIN N2S2-METAL CONJUGATE", BIOCONJUGATE CHEMISTRY, vol. 5, no. 3, 1 May 1994 (1994-05-01), pages 182 - 193, XP000446095 *
YAMAMURA T. ET AL: "Ni(II) complexes of N,N'-ethylenebis(o-mercaptobenzamide): A quadridentate thiolato amide {S2N2} ligand", BULL. CHEM. SOC. JPN., 1990, VOL. 63, NO. 4, SEITEN 999-1004, XP002034477 *

Also Published As

Publication number Publication date
EP0851771A2 (de) 1998-07-08
WO1997010853A2 (de) 1997-03-27
CA2232340A1 (en) 1997-03-27
AU1300597A (en) 1997-04-09
DE19536783A1 (de) 1997-03-27

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