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EP0451824A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Chelating compounds and their use

Assignee: Nihon Medi Physics Co Ltd
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Filing: 1991-04-10
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Granted: —
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Expires: 2011-04-10
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Abstract

Abstract A chelating compound of the formula: (R-NHOC-CH2)n-A-(CH2COOH)m (I) wherein R is an aromatic ring-containing organic group, A is a residue of an aminopolyacetic acid excluding acetic acid groups (-CH2COOH) therefrom, m is an integer of at least two and n is an integer of 1 or 2, or its salt, which has a specificity to a hepatobiliary system so that a chelate compound formed between said chelating compound and a metallic element through a chelate bond is useful as a diagnostic or therapeutic agent for hepatobiliary organs and tissues. <IMAGE>

Inventors

  • 👤 Shigemi Seri
  • 👤 Hirohiko Yamauchi
  • 👤 Makoto Azuma
  • 👤 Yoji Arata

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-28 08:28
CPC Classifications
C; C07; C07C; C07C311/00; C07C311/30; C07C311/37; C07C311/38; C07C311/39; C07C311/41; A; A61; A61K; A61K49/00; A61K49/06; A61K51/00; A61K51/02; A61K51/04; A61K51/0474; A61K51/0478; A61K51/048; A61K51/0497; A61P; A61P1/00; A61P1/16; A61P43/00; C07C237/00; C07C237/02; C07C237/04; C07C237/06; C07C237/10; A61K2123/00

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 106 words
A process for the preparation of a chelating compound of the formula: (R-NHOC-CH₂) n -A-(CH₂COOH) m (I) wherein R is an aromatic ring-containing organic group, A is a residue of an aminopolyacetic acid excluding acetic acid groups (-CH₂COOH) therefrom, m is an integer of at least two and n is an integer of 1 or 2, or its salt, which comprises reacting an aromatic ring-containing organic amine of the formula R-NH₂, wherein R is as defined above with an aminopolyacetic acid of the formula (HOOCCH₂) n -A-(CH₂COOH) m wherein A, m and n are each as defined above in any reactive form in an inert solvent.
Claim 2
Dependent Claim 39 words
The process according to claim 1, wherein the aromatic ring-containing organic group is aryl, ar(lower)-alkyl, arylsulfonyl, ar(lower)alkylsulfonyl, arylamino-(lower) alkyl, ar(lower)alkylamino(lower)alkyl, arylsulfonylamino(lower)alkyl or ar(lower)alkylsulfonylamino(lower)alkyl, the aryl moiety being phenyl or naphthyl optionally substituted with lower alkyl, lower alkylamino or di(lower)-alkylamino.
Claim 3
Dependent Claim 14 words
The process according to claim 1, wherein the aromatic ring-containing organic group is dansyl.
Claim 4
Dependent Claim 14 words
The process according to claim 1, wherein the aromatic ring-containing organic group is dansylamino(lower)alkyl.
Claim 5
Dependent Claim 54 words
The process according to claim 1, wherein the aminopolyacetic acid comprises a hydrocarbon chain in a straight, branched or cyclic form, at least two amino groups present in the hydrocarbon chain and/or at the terminal position and at least three acetic acid (-CH₂COOH) groups each attached to a nitrogen atom in said amino groups.
Claim 6
Dependent Claim 24 words
The process according to claim 1, wherein the aminopolyacetic acid is ethylenediamine-tetraacetic acid (EDTA), diethylenetriamine-pentaacetic acid (DTPA), trans-1,2-cyclohexadiamine-tetraacetic acid (CyDTA) or 1,4,7,10-tetraazacyclododecane-tetraacetic acid (DOTA).
Claim 7
Dependent Claim 31 words
A process for the preparation of a chelate compound, which comprises binding a compound prepared according to any of claims 1 to 6 and a metallic element through a chelate bond.
Claim 8
Dependent Claim 14 words
The process according to claim 7, wherein the metallic element is a radioactive element.
Claim 9
Dependent Claim 17 words
The process according to claim 8, wherein the radioactive element is technetium-99m, indium-111, rhenium-186, rhenium-188 or yttrium-90.
Claim 10
Dependent Claim 14 words
The process according to claim 7, wherein the metallic element is a paramagnetic element.
Claim 11
Dependent Claim 12 words
The process according to claim 10, wherein the paramagnetic element is gadolinium.

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