EP0200492A1
Expired / Lapsed
EP
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Radiodiagnostic agents
Assignee: Boston Children's Hospital
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Filing: 1986-04-25
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Granted: —
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Expires: 2006-04-25
Abstract
Abstract A bisamide-bisthiol ligand containing fatty acid substituted thiol useful for producing Tc-labelled radiodiagnostic imaging agents is described. The ligand forms a complex with the radionuclide 99m Tc suitable for administration as a radiopharmaceutical to obtain images of the heart for diagnosis of myo- ' cardial disfunction. I
Inventors
- 👤 Alun G. Jones
- 👤 John Lister-James
- 👤 Alan Davison
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-27 08:32
CPC Classifications
C; C07; C07F; C07F13/00; C07F13/005; A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K2123/00
Claims Analysis
Total Claims: 39
Claim 1
Independent Claim
91 words
Compounds useful for forming technetium-99m radioimaging agents having the structural formulae: wherein each R is independently selected from hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, or COR 4 wherein R 4 is selected from substituted or unsubstituted lower alkoxy; or two R's can be taken together to form a lower alkylidene or hydrocarbon ring; one of R' or R 2 is selected from hydrogen or a thiol protecting group;the other of R' or R is a C 14 to C2 4 fatty acid group; and salts thereof.
Claim 2
Dependent Claim
91 words
Compounds useful for forming technetium-99m radioimaging agents having the structural formulae: wherein each R is independently selected from hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, or COR 4 wherein R 4 is selected from substituted or unsubstituted lower alkoxy; or two R's can be taken together to form a lower alkylidene or hydrocarbon ring; one of R' or R 2 is selected from hydrogen or a thiol protecting group;the other of R' or R is a C 14 to C2 4 fatty acid group; and salts thereof.
Claim 3
Dependent Claim
20 words
The compounds of claim 1, wherein R' or R 2 is a C 15 to C 20 fatty acid moiety.
Claim 4
Dependent Claim
19 words
The compounds of claim 1, wherein R' or R 2 is a C,6 to C 18 fatty acid moiety.
Claim 5
Dependent Claim
19 words
A complex formed by reacting a compound of claim 1 with technetium in the presence of a reducing agent.
Claim 6
Dependent Claim
22 words
The complex of claim 4, wherein said reducing agent is selected from a dithionite group, a stannous ion, or a ferrous ion.
Claim 7
Dependent Claim
12 words
A complex formed by labelling a compound of claim 1 with technetium-99m.
Claim 8
Dependent Claim
20 words
A complex formed by labelling a compound of claim 1 with technetium by ligand exchange with a prereduced technetium complex.
Claim 9
Dependent Claim
26 words
A compound of claim 2, wherein R' or R 2 is selected from acetamidomethyl, loweral- kylaminocarbonyl, loweralkanoylaminomethyl, ar- oylaminomethyl, t-butyl, arylmethyl, aroyl, aryloxycarbonyl, or loweralkoxy carbonyl.
Claim 10
Dependent Claim
12 words
A compound of claim 8, wherein R' or R 2 is acetamidomethyl.
Claim 11
Dependent Claim
7 words
A technetium complex having the structural formula:
Claim 12
Dependent Claim
7 words
A technetium complex having the structural formula:
Claim 13
Dependent Claim
66 words
or wherein each R is independently selected from hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, or COR 4 wherein R 4 is selected from substituted or unsubstituted lower alkoxy; or two R's can be taken together to form a lower alkylidene group or a hydrocarbon ring; and R 5 is a C 12 to C 24 fatty acid group; and salts thereof.
Claim 14
Dependent Claim
66 words
or wherein each R is independently selected from hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, or COR 4 wherein R 4 is selected from substituted or unsubstituted lower alkoxy; or two R's can be taken together to form a lower alkylidene group or a hydrocarbon ring; and R 5 is a C 12 to C 24 fatty acid group; and salts thereof.
Claim 15
Dependent Claim
36 words
A kit for preparing a radiopharmaceutical preparation, said kit comprising a sealed vial containing a predetermined quantity of a compound of claim 1 and a sufficient amount of reducing agent to label said compound with technetium.
Claim 16
Dependent Claim
21 words
The kit of claim 11, wherein R' or R 2 is selected from acetamidomethyl, benzoyl, diphenylmethyl, ethyl aminocarbonyl, t-butyl or trityl.
Claim 17
Dependent Claim
12 words
The kit of claim 12, wherein R' or R 2 is acetamidomethyl.
Claim 18
Dependent Claim
22 words
The kit of claim 11, wherein said reducing agent is selected from a dithionite group, a stannous ion, or a ferrous ion.
Claim 19
Dependent Claim
41 words
A kit for preparing a radiopharmaceutical preparation, said kit comprising a sterilized, sealed vial comprising a lyophilized admixture of a reducing agent for technetium, and a compound of claim 1, capable of forming a pentacoordinate oxotechnetium complex in an aqueous solution.
Claim 20
Dependent Claim
22 words
The kit of claim 15, wherein said reducing agent is selected from a dithionite group, a stannous ion, or a ferrous ion.
Claim 21
Dependent Claim
12 words
The kit of claim 16, wherein said reducing agent is stannous chloride.
Claim 22
Dependent Claim
39 words
A method for diagnosing myocardial disfunction in a mammal, said method comprising injecting into said mammal a technetium complex of claim 10, in a suitable pharmacological carrier; and scanning the myocardial system of said mammal using radioscintigraphic imaging apparatus.
Claim 23
Dependent Claim
96 words
Compounds useful for forming technetium-99m radioimaging agents having the structural formulae: , wherein each R is independently selected from hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, or COR 4 wherein R 4 is selected from substituted or unsubstituted lower alkoxy; or two R's can be taken together to form a lower alkylidene group or a hydrocarbon ring; one of R' or R 2 is selected from hydrogen or a thiol protecting group; the other of R' or R 2 is a G 14 to C 24 fatty acid group; and salts thereof.
Claim 24
Dependent Claim
96 words
Compounds useful for forming technetium-99m radioimaging agents having the structural formulae: , wherein each R is independently selected from hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, or COR 4 wherein R 4 is selected from substituted or unsubstituted lower alkoxy; or two R's can be taken together to form a lower alkylidene group or a hydrocarbon ring; one of R' or R 2 is selected from hydrogen or a thiol protecting group; the other of R' or R 2 is a G 14 to C 24 fatty acid group; and salts thereof.
Claim 25
Dependent Claim
19 words
A complex formed by reacting a compound of claim 19 with technetium in the presence of a reducing agent.
Claim 26
Dependent Claim
12 words
A complex formed by labelling a compound of claim 19 with technetium-99m.
Claim 27
Dependent Claim
20 words
A complex formed by labelling a compound of claim 19 with technetium by ligand exchange with a prereduced technetium complex.
Claim 28
Dependent Claim
19 words
A compound of claim 19, wherein R' or R is selected from acetamidomethyl, benzoyl, diphenylmethyl, ethylaminocarbonyl, t-butyl or trityl.
Claim 29
Dependent Claim
12 words
A compound of claim 23, wherein R' or R 2 is acetamidomethyl.
Claim 30
Dependent Claim
36 words
A kit for preparing a radiopharmaceutical preparation, said kit comprising a sealed vial containing a predetermined quantity of a compound of claim 19 and a sufficient amount of reducing agent to label said compound with technetium.
Claim 31
Dependent Claim
13 words
The kit of claim 25, wherein said reducing agent is a stannous ion.
Claim 32
Dependent Claim
33 words
The kit of claim 26, wherein said compound and said reducing agent are lyophilized in a sterile vial and said compound is capable of forming a pentacoordinate oxotechnetium complex in an aqueous solution.
Claim 33
Dependent Claim
39 words
A bisamids-bisthiol compound capable of complexing technetium with the N 2 S 2 core to form a pentacoordinate oxotechnetium complex, said compound having a thiol-fatty acid group wherein the fatty acid group has from 14 to 24 carbon atoms.
Claim 34
Dependent Claim
39 words
A bisamids-bisthiol compound capable of complexing technetium with the N 2 S 2 core to form a pentacoordinate oxotechnetium complex, said compound having a thiol-fatty acid group wherein the fatty acid group has from 14 to 24 carbon atoms.
Claim 35
Dependent Claim
19 words
A complex formed by reacting a compound of claim 28 with technetium in the presence of a reducing agent.
Claim 36
Dependent Claim
12 words
A complex formed by labelling a compound of claim 28 with technetium-99m.
Claim 37
Dependent Claim
20 words
A complex formed by labeling a compound of claim 28 with technetium by ligand exchange with a prereduced technetium complex.
Claim 38
Dependent Claim
38 words
A kit for preparing a radiopharmaceutical composition, said kit comprising a sealed, sterile, pyrogen-free vial containing a predetermined quantity of a compound of claim 28 and a sufficient amount of reducing agent to label said compound with technetium.
Claim 39
Dependent Claim
42 words
A method for diagnosing myocardial disfunction in a mammal, said method comprising injecting into said mammal a technetium complex of bisamide-bisthiol compound of claim 28 in a suitable pharmacological carrier; and scanning the myocardial system of said mammal using radioscintigraphic imaging apparatus.
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