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1. WO1996005167 - DIMER DTPA DERIVATIVES AND THEIR METAL COMPLEXES, PHARMACEUTICALS CONTAINING THE SAME, THEIR USE IN DIAGNOSIS AND THERAPY AND PROCESS FOR PREPARING SAID COMPLEXES AND PHARMACEUTICALS

Publication Number WO/1996/005167
Publication Date 22.02.1996
International Application No. PCT/EP1995/003142
International Filing Date 08.08.1995
Chapter 2 Demand Filed 19.01.1996
IPC
A61K 49/06 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
49Preparations for testing in vivo
06Nuclear magnetic resonance (NMR) contrast preparations; Magnetic resonance imaging (MRI) contrast preparations
A61K 51/04 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51Preparations containing radioactive substances for use in therapy or testing in vivo
02characterised by the carrier
04Organic compounds
C07C 229/16 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
229Compounds containing amino and carboxyl groups bound to the same carbon skeleton
02having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
04the carbon skeleton being acyclic and saturated
06having only one amino and one carboxyl group bound to the carbon skeleton
10the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
16to carbon atoms of hydrocarbon radicals substituted by amino or carboxyl groups, e.g. ethylenediamine-tetra-acetic acid, iminodiacetic acids
C07C 229/36 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
229Compounds containing amino and carboxyl groups bound to the same carbon skeleton
02having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
34the carbon skeleton containing six-membered aromatic rings
36with at least one amino group and one carboxyl group bound to the same carbon atom of the carbon skeleton
C07C 229/76 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
229Compounds containing amino and carboxyl groups bound to the same carbon skeleton
76Metal complexes of amino carboxylic acids
C07C 237/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
237Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
02having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
04the carbon skeleton being acyclic and saturated
06having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
CPC
A61K 49/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
49Preparations for testing in vivo
06Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
A61K 51/048
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51Preparations containing radioactive substances for use in therapy or testing in vivo
02characterised by the carrier ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04Organic compounds
0474complexes 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
0478complexes from non-cyclic ligands, e.g. EDTA, MAG3
048DTPA (diethylenetriamine tetraacetic acid)
C07C 229/16
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
229Compounds containing amino and carboxyl groups bound to the same carbon skeleton
02having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
04the carbon skeleton being acyclic and saturated
06having only one amino and one carboxyl group bound to the carbon skeleton
10the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
16to carbon atoms of hydrocarbon radicals substituted by amino or carboxyl groups, e.g. ethylenediamine-tetra-acetic acid, iminodiacetic acids
C07C 229/36
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
229Compounds containing amino and carboxyl groups bound to the same carbon skeleton
02having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
34the carbon skeleton containing six-membered aromatic rings
36with at least one amino group and one carboxyl group bound to the same carbon atom of the carbon skeleton
C07C 229/76
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
229Compounds containing amino and carboxyl groups bound to the same carbon skeleton
76Metal complexes of amino carboxylic acids
C07C 237/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
237Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
02having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
04the carbon skeleton being acyclic and saturated
06having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
Applicants
  • SCHERING AKTIENGESELLSCHAFT [DE/DE]; Gewerblicher Rechtsschutz D-13342 Berlin, DE (AllExceptUS)
  • KRAUSE, Werner [DE/DE]; DE (UsOnly)
  • MAIER, Franz-Karl [DE/DE]; DE (UsOnly)
  • BAUER, Michael [DE/DE]; DE (UsOnly)
  • PRESS, Wolf-Rüdiger [DE/DE]; DE (UsOnly)
  • SCHUHMANN-GIAMPIERI, Gabriele [DE/DE]; DE (UsOnly)
  • PLATZEK, Johannes [DE/DE]; DE (UsOnly)
  • SCHMITT-WILLICH, Heribert [DE/DE]; DE (UsOnly)
Inventors
  • KRAUSE, Werner; DE
  • MAIER, Franz-Karl; DE
  • BAUER, Michael; DE
  • PRESS, Wolf-Rüdiger; DE
  • SCHUHMANN-GIAMPIERI, Gabriele; DE
  • PLATZEK, Johannes; DE
  • SCHMITT-WILLICH, Heribert; DE
Priority Data
P 44 28 874.308.08.1994DE
Publication Language German (DE)
Filing Language German (DE)
Designated States
Title
(DE) DIMERE DTPA-DERIVATE UND DEREN METALLKOMPLEXE, DIESE KOMPLEXE ENTHALTENDE PHARMAZEUTISCHE MITTEL, DEREN VERWENDUNG IN DER DIAGNOSTIK UND THERAPIE SOWIE VERFAHREN ZUR HERSTELLUNG DER KOMPLEXE UND MITTEL
(EN) DIMER DTPA DERIVATIVES AND THEIR METAL COMPLEXES, PHARMACEUTICALS CONTAINING THE SAME, THEIR USE IN DIAGNOSIS AND THERAPY AND PROCESS FOR PREPARING SAID COMPLEXES AND PHARMACEUTICALS
(FR) DERIVES DIMERES DE DTPA ET LEURS COMPLEXES METALLIQUES, AGENTS PHARMACEUTIQUES CONTENANT CES COMPLEXES, LEUR UTILISATION EN DIAGNOSTIC ET EN THERAPIE ET PROCEDE DE PREPARATION DE CES COMPLEXES ET AGENTS PHARMACEUTIQUES
Abstract
(DE)
Die Erfindung betrifft neue dimere DTPA-Derivate der allgemeinen Formel (I), bestehend aus den Inkrementen (A) und (B), wobei die Inkremente (A) und (B) über eines der Substituentenpaare R1 und R1', R2 und R2', R15 und R15', R1 und R2', R1' und R2, R1- und R15, R1 und R15', R2 und R15', R2' und R15 miteinander verknüpft sind, worin das jeweils verknüpfende Substituentenpaar für Heterocyclus, einen Phenylenrest, eine C0-C30-Alkylen- oder eine C7-C30 Aralkylenkette stehen, die gegebenenfalls durch 1-4 Hydroxy-, C1-C6-Alkoxy-, Carboxy- oder Mercaptogruppen substituiert und/oder durch 1 bis 6 Sauerstoff-, Stickstoff-, Schwefelatome, Sulfinyl- und/oder Sulfonylgruppen unterbrochen ist, und Y jeweils für ein Wasserstoffatom und/oder ein Metallionenäquivalent eines Elements der Ordnungszahlen 21-32, 37-39, 42-51 und 57-83 steht, und X und X' für eine Gruppe -OY, oder -CONR5R6 stehen; und die Verwendung der Metallkomplexe in der NMR- und/oder Röntgendiagnostik, der Radiodiagnostik und der Radiotherapie, sowie Verfahren zu deren Herstellung.
(EN)
New dimer DTPA derivatives have the general formula (I) that consists of the increments (A) and (B) which are interconnected by one of the pairs of substituents R1 and R1', R2 and R2', R15 and R15', R1 and R2', R1' and R2, R1' and R15, R1 and R15', R2 and R15', R2' and R15. The interconnecting substituent pairs stand for heterocycle, a phenylene residue, a C0-C30-alkylene or C7-C30-aralkylene chain, which may be optionally substituted by 1-4 hydroxy, C1-C6-alkoxy, carboxy or mercapto groups and/or interrupted by 1 to 6 oxygen, nitrogen or sulphur atoms or sulfinyl and/or sulfonyl groups; Y stands for a hydrogen atom and/or a metal ion equivalent of an element having atomic numbers 21-32, 37-39, 42-51 and 57-83; and X and X' stand for a group -OY or -CONR5R6. Also disclosed is the use of said metal complexes in NMR and/or röntgen diagnosis, in radiodiagnosis and radiotherapy, as well as a process for preparing the same.
(FR)
De nouveaux dérivés dimères de DTPA ont la formule générale (I) constituée des incréments (A) et (B) qui sont reliés l'un à l'autre par une des paires de substituants R1 et R1', R2 et R2', R15 et R15', R1 et R2', R1' et R2, R1' et R15, R1 et R15', R2 et R15', R2' et R15. La paire de substituants de liaison désigne un hétérocycle, un résidu phénylène, une chaîne alcylène C0-C30 ou une chaîne aralcylène C7-C30 éventuellement substitués par des groupes hydroxy 1-4, alcoxy, carboxy ou mercapto C1-C6 et/ou interrompus par 1 à 6 atomes d'oxygène, d'azote ou de soufre ou par 1 à 6 groupes sulfinyle et/ou sulfonyle. Y désigne un atome d'hydrogène et/ou un ion métallique équivalent d'un élément ayant les nombres atomiques 21-32, 37-39, 42-51 et 57-83, et X et X' désignent un groupe -OY ou -CONR5R6. L'invention concerne également l'utilisation de ces complexes métalliques en diagnostic par résonance magnétique nucléaire et/ou par radiographie, en radiodiagnostic et en radiothérapie, ainsi que leur procédé de préparation.
Also published as
CZPV1997-405
FI970535
NO19970602
NZ291798
SK17397
SK199700173
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