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US4925650A
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Technetium -99m complex for examining the renal function
Assignee: Mallinckrodt Inc
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Filing: 1988-11-16
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Granted: 1990-05-15
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Expires: 2008-11-16
Abstract
Abstract The invention relates to a technetium-99m complex of the general formula ##STR1## wherein Z is a sulphur atom or an amino group of the general formula R 17 --N--(R 18 ) k , in which k is 0 or 1 and R 17 and R 18 have the same meanings as the symbols R 1 -R 16 ; each of the symbols R 1 -R 16 is individually selected from the group consisting of hydrogen, straight or branched, unsubstituted or substituted alkyl having 1-4 carbon atoms, and ACOOH, wherein A is a straight or branched, unsubstituted or substituted alkly group having 0-4 carbon atoms; and R 5 together with R 6 or R 9 together with R 10 additionally may form an oxygen atom; Tc represents technetium-99m; t is 0 or 1; and n is 0 or 1; with the provisos that (a) if R 15 , R 16 , R 17 and/or R 18 are/is ACOOH, A is a straight or branched, unsubstituted or substituted alkyl group having 1-4 carbon atoms; (b) at least one of the symbols R 1 -R 18 is ACOOH; and (c) if t is 1, at least two of the symbols R 1 -R 18 are ACOOH; or a pharmaceutically acceptable salt of this compound. The invention further relates to a radiopharmaceutical composition comprising said complex, to the use of this composition for examining the renal function, and to a kit for preparing such a composition.
Inventors
- 👤 Dennis L. Nosco
- 👤 Alfons M. Verbruggen
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 06:25
CPC Classifications
C; C07; C07F; C07F13/00; C07F13/005; A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/0474; A61K51/0478; A61K2123/00
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
197 words
Technetium-99m complex of the general formula ##STR6## wherein Z is an amino group of the general formula R 17 --N--(R 18 ) k , in which k is 0 or 1 and R 17 and R 18 have the same meanings as the symbols R 1 -R 16 is individually selected from the group consisting of hydrogen, straight or branched, unsubstituted or substituted alkyl having 1-4 carbon atoms, and ACOOH, wherein A is a straight or branched, unsubstituted or substituted alkyl group having 0-4 carbon atoms; and R 5 together with R 6 or R 9 together with R 10 additionally may form an oxygen atom; Tc represents technetium-99m; t is 0 or 1; and n is 0 or 1; with the provisos that (a) if at least one of R 15 , R 16 , R 17 and R 18 is ACOOH, A is a straight or branched, unsubstituted or substituted alkyl group having 1-4 carbon atoms; (b) at least one of the symbols R 1 -R 18 is ACOOH; and (c) if t is 1, at least two of the symbols R 1 -R 18 are ACOOH; or a pharmaceutically acceptable salt of this compound.
Claim 2
Dependent Claim
197 words
Technetium-99m complex of the general formula ##STR6## wherein Z is an amino group of the general formula R 17 --N--(R 18 ) k , in which k is 0 or 1 and R 17 and R 18 have the same meanings as the symbols R 1 -R 16 is individually selected from the group consisting of hydrogen, straight or branched, unsubstituted or substituted alkyl having 1-4 carbon atoms, and ACOOH, wherein A is a straight or branched, unsubstituted or substituted alkyl group having 0-4 carbon atoms; and R 5 together with R 6 or R 9 together with R 10 additionally may form an oxygen atom; Tc represents technetium-99m; t is 0 or 1; and n is 0 or 1; with the provisos that (a) if at least one of R 15 , R 16 , R 17 and R 18 is ACOOH, A is a straight or branched, unsubstituted or substituted alkyl group having 1-4 carbon atoms; (b) at least one of the symbols R 1 -R 18 is ACOOH; and (c) if t is 1, at least two of the symbols R 1 -R 18 are ACOOH; or a pharmaceutically acceptable salt of this compound.
Claim 3
Dependent Claim
288 words
A complex as claimed in claim 1 of the general formula ##STR7## wherein Z is an amino group of the general formula R 17 '--N--(R 18 ') k , in which k is 0 or 1 and R 17 ' and R 18 ' have the same meanings as the symbols R 1 ', R 3 ', R 5 ', R 9 ', R 11 ', R 13 ', R 15 ' and R 16 ', each of the symbols R 1 ', R 3 ', R 5 ', R 9 ', R 11 ', R 13 ', R 15 ' and R 16 ' is individually selected from the group consisting of hydrogen, methyl and (CH 2 ) q COOH, wherein q is 0 or 1, Tc represents technetium-99m, and t is 0 or 1, with the provisos that (a) if at least one of R 15 ' and R 16 ' is (CH 2 ) q COOH, q is 1 (b) at least one of the symbols R 1 ', R 3 ', R 5 ', R 9 ', R 11 ', R 13 ', R 15 and R 16 ' is (CH 2 ) q COOH, (c) at most four of the symbols R 1 ', R 3 ', R 5 ', R 9 ', R 11 ', R 13 ', R 15 ' and R 16 ' are (CH 2 ) q COOH, and (d) if t is 1, at least two of the symbols R 1 ', R 3 ', R 5 ', R 9 ', R 11 ', R 13 ', R 15 ' and R 16 ' are (CH 2 ) q COOH, or a pharmaceutically acceptable salt of this compound.
Claim 4
Dependent Claim
41 words
A radiopharmaceutical composition for examining the renal function which, in addition to a liquid, pharmaceutically acceptable carrier material, comprises a technetium-99m complex, characterized in that the composition comprises a complex as claimed in claim 1 or 2 as the technetium-99m complex.
Claim 5
Dependent Claim
51 words
A method of performing a renal function examination, characterized in that a composition as claimed in claim 3 is administered to a warm-blooded living being in a quantity of 0.1 to 30 mCi, per 70 kg of body weight, and the radioactive radiation emitted by the living being is then recorded.
Claim 6
Dependent Claim
24 words
A method according to claim 4, wherein the quantity of the composition administered is 0.5 to 10 mCi per 70 kg of body weight.
Claim 7
Dependent Claim
172 words
Technetium-99m complex of the general formula ##STR8## wherein Z is a sulphur atom or an amino group of the general formula R 17 --N--(R 18 ) k , in which K is 0 or 1 and R 17 and R 18 have the same meanings as the symbols R 1 -R 16 ; each of the symbols R 1 -R 16 is individually selected from the group consisting of hydrogen, straight or branched, unsubstituted or substituted alkyl having 1-4 carbon atoms, and ACOOH, wherein A is a straight or branched, unsubstituted or substituted alkyl group having 0-4 carbon atoms; and R 5 together with R 6 or R 9 together with R 10 additionally may form an oxygen atom; Tc represents technetium-99m; t is 0 or 1; n is 0 or 1; with the proviso that at least two of the symbols R 1 -R 18 are ACOOH, wherein A is a straight or branched unsubstituted or substituted alkyl group having 1-4 carbon atoms, or a pharmaceutically acceptable salt of this compound.
Claim 8
Dependent Claim
172 words
Technetium-99m complex of the general formula ##STR8## wherein Z is a sulphur atom or an amino group of the general formula R 17 --N--(R 18 ) k , in which K is 0 or 1 and R 17 and R 18 have the same meanings as the symbols R 1 -R 16 ; each of the symbols R 1 -R 16 is individually selected from the group consisting of hydrogen, straight or branched, unsubstituted or substituted alkyl having 1-4 carbon atoms, and ACOOH, wherein A is a straight or branched, unsubstituted or substituted alkyl group having 0-4 carbon atoms; and R 5 together with R 6 or R 9 together with R 10 additionally may form an oxygen atom; Tc represents technetium-99m; t is 0 or 1; n is 0 or 1; with the proviso that at least two of the symbols R 1 -R 18 are ACOOH, wherein A is a straight or branched unsubstituted or substituted alkyl group having 1-4 carbon atoms, or a pharmaceutically acceptable salt of this compound.
Claim 9
Dependent Claim
165 words
A complex as claimed in claim 6, of the general formula ##STR9## wherein each of the symbols R 1 ', R 3 ', R 5 ', R 9 ' R 11 ', R 13 ', R 15 ' and R 16 'is individually selected from the group consisting of hydrogen, methyl and (CH 2 ) q COOH, wherein q is 0 or 1, Tc represents technetium-99m, and t is 0 or 1, with the provisos that (a) at least two of the symbols R 1 ', R 3 ', R 5 ', R 9 ', R 11 , R 13 ', R 15 ' and R 16 ' are (CH 2 ) q COOH, wherein q is 1, and (b) at most four of the symbols R 1 ', R 3 ', R 5 ', R 9 ', R 11 ', R 13 ', R 15 ' and R 16 ' are (CH 2 ) q COOH, or a pharmaceutically acceptable salt of this compound.
Claim 10
Dependent Claim
41 words
A radiopharmaceutical composition for examining the renal function which, in addition to a liquid, pharmaceutically acceptable carrier material, comprises a technetium-99m complex, characterized in that the composition comprises a complex as claimed in claim 6 or 7 as the technetium-99m complex.
Claim 11
Dependent Claim
51 words
A method of performing a renal function examination, characterized in that a composition as claimed in claim 8 is administered to a warm-blooded living being in a quantity of 0.1 to 30 mCi per 70 kg of body weight, and the radioactive radiation emitted by the living being is then recorded.
Claim 12
Dependent Claim
24 words
A method according to claim 9, wherein the quantity of the composition administered is 0.5 to 10 mCi per 70 kg of body weight.
Claim 13
Dependent Claim
160 words
Technetium-99m complex of the general formula ##STR10## wherein Z is a sulphur atom or an amino group of the general formula R 17 --N--(R 18 ) k , in which k is 0 or 1 and R 17 and R 18 have the same meanings as the symbols R 1 -R 16 ; each of the symbols R 1 -R 16 is individually selected from the group consisting of hydrogen, straight or branched, unsubstituted or substituted alkyl having 1-4 carbon atoms, and COOH; and R 5 together with R 6 or R 9 together with R 10 additionally may form an oxygen atom; Tc represents technetium-99m; t is 0 or 1; and n is 0 or 1; with the provisos that (a) at least one of the symbols R 1 -R 18 is COOH; and (b) if t is 1, at least two of the symbols R 1 -R 18 are COOH, or a pharmaceutically acceptable salt of this compound.
Claim 14
Dependent Claim
160 words
Technetium-99m complex of the general formula ##STR10## wherein Z is a sulphur atom or an amino group of the general formula R 17 --N--(R 18 ) k , in which k is 0 or 1 and R 17 and R 18 have the same meanings as the symbols R 1 -R 16 ; each of the symbols R 1 -R 16 is individually selected from the group consisting of hydrogen, straight or branched, unsubstituted or substituted alkyl having 1-4 carbon atoms, and COOH; and R 5 together with R 6 or R 9 together with R 10 additionally may form an oxygen atom; Tc represents technetium-99m; t is 0 or 1; and n is 0 or 1; with the provisos that (a) at least one of the symbols R 1 -R 18 is COOH; and (b) if t is 1, at least two of the symbols R 1 -R 18 are COOH, or a pharmaceutically acceptable salt of this compound.
Claim 15
Dependent Claim
168 words
A complex as claimed in claim 11 of the general formula ##STR11## wherein each of the symbols R 1 ', R 3 ', R 5 ', R 9 ', R 11 , R 13 ', R 15 ' and R 16 ' is individually selected from the group consisting of hydrogen, methyl and COOH, Tc represents technetium-99m; t is 0 or 1; and n is 0 or 1; with the provisos that (a) at least one of the symbols R 1 ', R 3 ', R 5 ', R 9 ', R 11 ', R 13 ', R 15 ' and R 16 ' is COOH, (b) at most four of the symbols R 1 ', R 3 ', R 5 ' R 9 ', R 11 ', R 13 , R 15 ' and R 16 ' are COOH, and (c) if t is 1, at least two of the symbols R 1 ', R 3 ', are COOH, or a pharmaceutically acceptable salt of this compound.
Claim 16
Dependent Claim
41 words
A radiopharmaceutical composition for examining the renal function which, in addition to a liquid, pharmaceutically acceptable carrier material, comprises a technetium-99m complex, characterized in that the composition comprises a complex as claimed in claim 11 or 12 as the technetium-99m complex.
Claim 17
Dependent Claim
51 words
A method of performing a renal function examination, characterized in that a composition as claimed in claim 13 is administered to a warm-blooded living being in a quantity of 0.1 to 30 mCi per 70 kg of body weight, and the radioactive radiation emitted by the living being is then recorded.
Claim 18
Dependent Claim
24 words
A method according to claim 14, wherein the quantity of the composition administered is 0.5 to 10 mCi per 70 kg of body weight.
References Cited (Backward Citations)
US2810753A
Cited
EP0188256A2
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1993-05-14 | 1993-11-13 | 1994-05-15 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-05-14 | 1997-11-13 | 1998-05-15 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-05-14 | 2001-11-13 | 2002-05-15 | $7700.00 | Window Closed / Lapsed |