EP0054920A1
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EP
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3-Aminomethylene-2,4-pentanedione bis(thiosemicarbazone) derivatives, and their production and use
Assignee: Nihon Medi Physics Co Ltd
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Filing: 1981-12-17
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Granted: —
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Expires: 2001-12-17
Abstract
Abstract A radioactive diagnostic agent which comprises a physiologically active substance and a radioactive metallic element combined with a compound of the formula: wherein R I and R 2 are each hydrogen, C 1 -C 3 alkyl or phenyl. The agent is characteristic in having a high stability even after being administered into a human body and showing the substantially the same behavior as the physiologically active substance itself in a human body.
Inventors
- 👤 Nobuo Ueda
- 👤 Susumu Kondo
- 👤 Masaaki Hazue
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-26 00:46
CPC Classifications
A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/08; A61K51/081; A61K51/088; A61K2123/00
Claims Analysis
Total Claims: 26
Claim 1
Independent Claim
21 words
A compound of the formula: wherein R 1 and R 2 are each hydrogen, C 1 -C 3 alkyl or phenyl.
Claim 2
Dependent Claim
21 words
A compound of the formula: wherein R 1 and R 2 are each hydrogen, C 1 -C 3 alkyl or phenyl.
Claim 3
Dependent Claim
14 words
The compound according to claim 1, wherein R and R 2 are each methyl.
Claim 4
Dependent Claim
14 words
The compound according to claim 1, wherein R and R 2 are each ethyl.
Claim 5
Dependent Claim
23 words
A physiologically active substance-combined compound comprising the compound according to claim 1 and a physiologically active substance bound therewith by a chemical bond.
Claim 6
Dependent Claim
17 words
The physiologically active substance-combined compound according to claim 4, wherein the chemical bond is a carbonamide linkage.
Claim 7
Dependent Claim
17 words
The physiologically active substance-combined compound according to claim 4, wherein the chemical bond is a pentamethylene linkage.
Claim 8
Dependent Claim
18 words
The physiologically active substance-combined compound according to claim 4, wherein the physiologically active substance is human serum albumin.
Claim 9
Dependent Claim
16 words
The physiologically active substance-combined compound according to claim 4, wherein the physiologically active substance is urokinase.
Claim 10
Dependent Claim
38 words
A radioactive metallic element-labeled, physiologically active substance-combined compound comprising the compound according to claim 1, a physiologically active substance bound therewith by a chemical bond and a radioactive metallic element bound with said compound through a chelating bond.
Claim 11
Dependent Claim
21 words
The radioactive metallic element-labeled, physiologically active substance-combined compound according to claim 9, wherein the radioactive metallic element is 9 9m Tc.
Claim 12
Dependent Claim
20 words
The radioactive metallic element-labeled, physiologically active substance-combined compound according to claim 9, wherein the radioactive metallic element is 67 Ga.
Claim 13
Dependent Claim
20 words
The radioactive metallic element-labeled, physiologically active substance-combined compound according to claim 9, wherein the radioactive metallic element is 111 In.
Claim 14
Dependent Claim
24 words
A process for preparing the compound according to claim 1, which comprises condensing 3-aminomethylene-2,4-pentanedione with 4-R-thiosemicarbazide wherein R is R or R 2 .
Claim 15
Dependent Claim
16 words
The process according to claim 13, wherein the condensation is carried out in a single step.
Claim 16
Dependent Claim
15 words
The process according to claim 13, wherein the condensation is carried out in two steps.
Claim 17
Dependent Claim
27 words
A process for preparing the physiologically active substance-combined compound according to claim 4, which comprises reacting the compound according to claim 1 with a physiologically active substance.
Claim 18
Dependent Claim
44 words
The process according to claim 16, wherein the physiologically active substance has a carboxyl group, and the reaction proceeds between the amino group in the compound according to claim 1 and the carboxyl group in the physiologically active substance to form a carbonamide linkage.
Claim 19
Dependent Claim
57 words
The process according to claim 16, wherein the physiologically active substance has an amino group, and the reaction proceeds between the amino group in the compound according to claim 1 and the amino group in the physiologically active substance in the presence of glutaraldehyde, followed by reduction to form a pentamethylene linkage between the said amino groups.
Claim 20
Dependent Claim
40 words
A process for preparing the radioactive metallic element-labeled, physiologically active substance-combined compound according to claim 9, which comprises contacting the physiologically active substance-combined compound according to claim 4 with a radioactive metallic element to combine them through a chelating bond.
Claim 21
Dependent Claim
16 words
The process according to claim 19, wherein the contact is carried out in an aqueous medium.
Claim 22
Dependent Claim
19 words
The process according to claim 19, wherein the contact is carried out in the presence of a reducing agent.
Claim 23
Dependent Claim
13 words
A non-radioactive carrier comprising the physiologically active substance-combined compound according to claim 4.
Claim 24
Dependent Claim
14 words
The non-radioactive carrier according to claim 22, which is in the form of solution.
Claim 25
Dependent Claim
15 words
The non-radioactive carrier according to claim 22, which is in the form of lyophilized powder.
Claim 26
Dependent Claim
17 words
A radioactive diagnostic agent comprising the radioactive metallic element-labeled, physiologically active substance-combined compound according to claim 9.
References Cited (Backward Citations)
EP0024464A1
Cited
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