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US4489054A
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Cationic lipophilic complexes of 99m Tc and their use for myocardial and hepatobiliary imaging
Assignee: RESEARCH Corp TECHNOLOGIES Inc A NOT-FOR-PROFIT NON-STOCK CORP OF
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Filing: 1983-04-14
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Granted: 1984-12-18
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Expires: 2003-04-14
Abstract
Abstract A method of imaging organs with 99mTc radiopharmaceuticals, especially of hepatobiliary imaging and negative myocardial infarct imaging in a mammal which comprises administering to the mammal a hepatobiliary or myocardial imaging amount of a cationic lipophilic complex of Tc-99m and detecting the Tc-99m complex in the mammal. A method for the preparation of cationic lipophilic complexes of Tc-99m.
Inventors
- 👤 Edward A. Deutsch
- 👤 Kenneth A. Glavan
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 13:37
CPC Classifications
C; C07; C07F; C07F9/00; C07F9/02; C07F9/28; C07F9/50; C07F9/5045; A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K2123/00
Claims Analysis
Total Claims: 27
Claim 1
Independent Claim
15 words
A cationic lipophilic complex of Tc-99m having an n-octanol/saline partition coefficient greater than about 0.05.
Claim 2
Dependent Claim
15 words
A cationic lipophilic complex of Tc-99m having an n-octanol/saline partition coefficient greater than about 0.05.
Claim 3
Dependent Claim
13 words
The complex of claim 1, which is soluble in non-polar water immiscible solvents.
Claim 4
Dependent Claim
13 words
The complex of claim 2, which is also soluble in polar water-miscible solvents.
Claim 5
Dependent Claim
70 words
The complex of claim 1, which has the formula (L.sub.2.sup.99m TcX.sub.2).sup.+ X.sup.- wherein L is a polyvalent neutral lipophilic ligand which is strongly chelating towards a 99m Tc cation; X are the same or different monovalent anionic ligands; or, in the formula (L 2 99m TcX 2 ) + , both X's are part of the same bidentate ligand capable of coordinating the cis positions of a 99m Tc cation.
Claim 6
Dependent Claim
85 words
The complex of claim 4, wherein L has the formula ##STR5## wherein n-2-5; wherein A is selected from the group consisting of a substituted or unsubstituted alkylene radical, a homomonocyclic or homopolycyclic lipophilic organic radical, and a heteromonocyclic or heteropolycyclic organic radical containing in at least one ring thereof an atom selected from the group consisting of N, O, P, S, or B; Y: are the same or different neutral functional groups having a free electron pair capable of complexing with a 99m Tc cation.
Claim 7
Dependent Claim
9 words
The complex of claim 5, wherein n=2 or 3.
Claim 8
Dependent Claim
13 words
The complex of claim 5, wherein A is -CH 2 CH 2 .
Claim 9
Dependent Claim
109 words
The complex of claim 5, wherein Y: are the same or different functional groups selected from the group consisting of Y 1 R 2 and Y 2 R, wherein Y 1 is an atom selected from the group consisting of N, P, As, Sb, and Bi; Y 2 is an atom selected from the group consisting of O, S, Se, and Te; and R is selected from the group consisting of hydrogen, an unsubstituted C 1 -C 15 straight or branched chain alkyl group, and a C 1 -C 15 straight or branched chain alkyl group substituted along or on the hydrocarbon chain with oxygen, nitrogen, sulfur or phosphorous.
Claim 10
Dependent Claim
92 words
The complex of claim 5, wherein said ligand X's are the same or different ligands selected from the group consisting of F - , Cl - , Br - , I - , SCN - , N 3 - , CN - , and RS - , wherein R is selected from the group consisting of an unsubstituted C 1 -C 15 straight or branched alkyl group, and a C 1 -C 15 straight or branched chain alkyl group substituted along or on the hydrocarbon chain with oxygen, nitrogen, sulfur or phosphorous.
Claim 11
Dependent Claim
28 words
The complex of claim 1, which is selected from the group consisting of ( 99m Tc(diars) 2 Br 2 )Br and ( 99m Tc(diars) 2 Cl 2 )Cl.
Claim 12
Dependent Claim
28 words
The complex of claim 1, which is selected from the group consisting of ( 99m Tc(DMPE) 2 Br 2 )Br and ( 99m Tc(DMPE) 2 Cl 2 )Cl.
Claim 13
Dependent Claim
12 words
The complex of claim 1, which is ( 99m Tc(tetraphos)Br 2 )Br.
Claim 14
Dependent Claim
12 words
The complex of claim 1 in combination with a pharmacologically inert vehicle.
Claim 15
Dependent Claim
11 words
The complex of claim 13, wherein said vehicle is 50:50 ethanol/saline.
Claim 16
Dependent Claim
120 words
A process of preparing a cationic lipophilic complex of 99m Tc of the formula: (L.sub.2.sup.99m TcX.sub.2)X wherein L is a neutral lipophilic ligand which is strongly chelating towards a 99m Tc cation and which is capable of reducing Tc +7 to a lower valence state; X are the same or different monovalent anionic ligands, which comprises: reducing a 99m Tc +7 species to a lower valency state species with a ligand L, wherein the 99m Tc +7 is present in an aqueous phase, wherein the ligand L is present in a water immiscible phase in intimate contact with said aqueous phase, and wherein during the reduction, said lower valency state species of 99m Tc is transferred to said non-aqueous phase.
Claim 17
Dependent Claim
120 words
A process of preparing a cationic lipophilic complex of 99m Tc of the formula: (L.sub.2.sup.99m TcX.sub.2)X wherein L is a neutral lipophilic ligand which is strongly chelating towards a 99m Tc cation and which is capable of reducing Tc +7 to a lower valence state; X are the same or different monovalent anionic ligands, which comprises: reducing a 99m Tc +7 species to a lower valency state species with a ligand L, wherein the 99m Tc +7 is present in an aqueous phase, wherein the ligand L is present in a water immiscible phase in intimate contact with said aqueous phase, and wherein during the reduction, said lower valency state species of 99m Tc is transferred to said non-aqueous phase.
Claim 18
Dependent Claim
68 words
The process of claim 15, wherein, after said transfer of said lower valency state species of 99m Tc into said water-immiscible phase, the process further comprises: adsorbing said species in complexation with said ligand L, on a material having adsorbing capacity for cations, being capable of separating cationic complexes from neutral or anionic molecules and eluting substantially pure ( 99m TcL 2 X 2 ) + species therefrom.
Claim 19
Dependent Claim
73 words
A kit comprising a carrier being compartmented to receive a series of containers in close confinement which comprises: a first container containing a source of 99mTc; a second container containing a polyvalent neutral lipophilic ligand L which is strongly chelating towards a 99m Tc cation which provides a cationic lipophilic complex of Tc-99m having an n-octanol/saline partition coefficient greater than about 0.05; a third container containing chromatographic material having adsorbing capacity for cations.
Claim 20
Dependent Claim
73 words
A kit comprising a carrier being compartmented to receive a series of containers in close confinement which comprises: a first container containing a source of 99mTc; a second container containing a polyvalent neutral lipophilic ligand L which is strongly chelating towards a 99m Tc cation which provides a cationic lipophilic complex of Tc-99m having an n-octanol/saline partition coefficient greater than about 0.05; a third container containing chromatographic material having adsorbing capacity for cations.
Claim 21
Dependent Claim
30 words
The kit of claim 17, wherein said second container further contains a reducing agent capable of reducing 99m Tc from a valency state of +VII to a lower valency state.
Claim 22
Dependent Claim
18 words
The kit of claim 17, wherein said third container is in the form of a short chromatography tube.
Claim 23
Dependent Claim
34 words
The kit of claim 17, wherein said third container is in the form of a syringe adapter capable of maintaining chromatographic material between the barrel of said syringe and the needle of said syringe.
Claim 24
Dependent Claim
17 words
The kit of claim 20, wherein said kit also contains a syringe capable of fitting said adapter.
Claim 25
Dependent Claim
23 words
The kit of claim 17, wherein said chromatographic material is selected from the group consisting of alumina, silica and a cationic exchange resin.
Claim 26
Dependent Claim
15 words
The kit of claim 17 wherein said 99m Tc generator is a Mo-99 molybdenum generator.
Claim 27
Dependent Claim
28 words
A diagnostic product for hepatobiliary, myocardial, pancreas and brain imaging in a mammal comprising an imaging amount of a cationic lipophilic complex of Tc-99m according to claim 1.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-12-18 | 1988-06-18 | 1988-12-18 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-12-18 | 1992-06-18 | 1992-12-18 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-12-18 | 1996-06-18 | 1996-12-18 | $7700.00 | Window Closed / Lapsed |