US4810486A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Bone-seeking complexes of technetium-99m
Assignee: GE Healthcare Ltd
•
Filing: 1987-06-29
•
Granted: 1989-03-07
•
Expires: 2007-06-29
Abstract
Abstract A composition for use in the preparation of a bone-scanning agent comprises a mixture of a bis-phosphonic acid of formula (I), wherein R 1 and R 3 may be the same or different group selected from H, --SO 3 H and a lower aliphatic group which may optionally contain one or more hetero atoms and which contains at least one --SO 3 H group; R 2 is a group selected from H, --OH, --NH 2 , --NHMe, --NMe 2 and lower alkyl optionally substituted by one or more polar groups; R 4 is a group selected from H, --OH, --NH 2 --NHMe, --NMe 2 , --SO 3 H and a lower alkyl optionally substituted by one or more polar groups; and n is 0 or 1; with the proviso that when n is 0, R 1 is not H and that when n is 1, R 1 and R 3 cannot both be H; or a non-toxic salt thereof, together with a reducing agent for pertechnetate ions. Technetium-99m, as an aqueous solution of pertechnetate ions, is added to the composition to form a complex of Tc-99m, and the bisphosphonate. The complex is useful as a bone-scanning agent and is rapidly taken up in bone to give scans of high definition.
Inventors
- 👤 James D. Kelly
- 👤 David V. Griffiths
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 21:43
CPC Classifications
C; C07; C07F; C07F9/00; C07F9/02; C07F9/28; C07F9/38; C07F9/3804; C07F9/3839; C07F9/3865; A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/0489; A61K2123/00
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
171 words
A composition for use in the preparation of a bone-scanning agent which comprises a mixture of bis-phosphonic acid having the general formula (I): ##STR5## wherein R 1 and R 3 may be the same or different group selected from H, --SO 3 H and a lower aliphatic group which may optionally contain one or more hetero atoms and which contains at least one --SO 3 H group; R 2 is a group selected from H, --OH, --NH 2 , --NHMe, --NMe 2 and lower alkyl optionally substituted by one or more polar groups; R 4 is a group selected from H, --OH, --NH 2 , --NHMe, --NMe 2 , --SO 3 H and a lower alkyl optionally substituted by one or more polar groups; and n is 0 or 1; with the proviso that when n is 0, R 1 is not H and that when n is 1, R 1 and R 3 cannot both be H; or a non-toxic salt thereof, together with a reducing agent for pertechnetate ions.
Claim 2
Dependent Claim
171 words
A composition for use in the preparation of a bone-scanning agent which comprises a mixture of bis-phosphonic acid having the general formula (I): ##STR5## wherein R 1 and R 3 may be the same or different group selected from H, --SO 3 H and a lower aliphatic group which may optionally contain one or more hetero atoms and which contains at least one --SO 3 H group; R 2 is a group selected from H, --OH, --NH 2 , --NHMe, --NMe 2 and lower alkyl optionally substituted by one or more polar groups; R 4 is a group selected from H, --OH, --NH 2 , --NHMe, --NMe 2 , --SO 3 H and a lower alkyl optionally substituted by one or more polar groups; and n is 0 or 1; with the proviso that when n is 0, R 1 is not H and that when n is 1, R 1 and R 3 cannot both be H; or a non-toxic salt thereof, together with a reducing agent for pertechnetate ions.
Claim 3
Dependent Claim
72 words
A composition as claimed in claim 1 which comprises a mixture of a bis-phosphonic acid having the general formula II: ##STR6## wherein R 1 is --SO 3 H or a lower aliphatic group containing from 1 to 6 carbon atoms and which contains one or two --SO 3 H groups, and R 2 is as defined in claim 1; or a non-toxic salt thereof; together with a reducing agent for pertechnetate ions.
Claim 4
Dependent Claim
43 words
A composition as claimed in claim 2 wherein the group R 1 in the bis-phosphonic acid II is --CH 2 N(CH 2 SO 3 H) 2 or (CH 2 ) m SO 3 H, where m is an integer from 1 to 6.
Claim 5
Dependent Claim
14 words
A composition as claimed in claim 3 wherein the bis-phosphonic acid is 2,2-diphosphonoethanesulphonic acid.
Claim 6
Dependent Claim
75 words
A composition as claimed in claim 1 which comprises a mixture of a bis-phosphonic acid having the general formula III: ##STR7## wherein R 1 is --SO 3 H or --CH 2 SO 3 H and R 4 is H, --OH, --NH 2 , --NHMe, --NMe 2 , --SO 3 H, or a lower alkyl optionally substituted by one or more polar groups; or a non-toxic salt thereof, together with a reducing agent for pertechnetate ions.
Claim 7
Dependent Claim
30 words
A composition as claimed in claim 1, wherein the reducing agent for pertechnetate ions is a non-toxic salt of tin (2+), iron (2+) or chromium (2+) or is metallic tin.
Claim 8
Dependent Claim
19 words
A composition as claimed in claim 6, wherein the reducing agent is selected from stannous chloride and stannous fluoride.
Claim 9
Independent Claim
33 words
A method of preparing a technetium-99m labelled bone scanning agent comprising adding technetium-99m, as an aqueous solution of pertechnetate ions, to a composition as claimed in any one of claims 1 to 7.
Claim 10
Dependent Claim
19 words
A method as claimed in claim 8, wherein the pertechnetate ions are added as a solution in isotonic saline.
Claim 11
Dependent Claim
161 words
A bone-seeking composition comprising an aqueous solution of a complex of technetium-99m and a bis-phosphonic acid having the general formula I: ##STR8## wherein R 1 and R 3 may be the same or different group selected from H, --SO 3 H and a lower aliphatic group which may optionally contain one or more hetero atoms and which contains at least one --SO 3 H group; R 2 is a group selected from H, --OH, --NH 2 , --NHMe, --NMe 2 and lower alkyl optionally substituted by one or more polar groups; R 4 is a group selected from H, --OH, --NH 2 , --NHMe, --NMe 2 , --SO 3 H and a lower alkyl optionally substituted by one or more polar groups; and n is 0 or 1; with the proviso that when n is 0, R 1 is not H and that when n is 1, R 1 and R 3 cannot both be H; or a non-toxic salt thereof.
Claim 12
Dependent Claim
161 words
A bone-seeking composition comprising an aqueous solution of a complex of technetium-99m and a bis-phosphonic acid having the general formula I: ##STR8## wherein R 1 and R 3 may be the same or different group selected from H, --SO 3 H and a lower aliphatic group which may optionally contain one or more hetero atoms and which contains at least one --SO 3 H group; R 2 is a group selected from H, --OH, --NH 2 , --NHMe, --NMe 2 and lower alkyl optionally substituted by one or more polar groups; R 4 is a group selected from H, --OH, --NH 2 , --NHMe, --NMe 2 , --SO 3 H and a lower alkyl optionally substituted by one or more polar groups; and n is 0 or 1; with the proviso that when n is 0, R 1 is not H and that when n is 1, R 1 and R 3 cannot both be H; or a non-toxic salt thereof.
Claim 13
Dependent Claim
21 words
A bone-seeking composition as claimed in claim 10 which comprises an aqueous solution of a complex of technetium-99m and 2,2-diphosphonoethanesulphonic acid.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-03-06 | 1992-09-05 | 1993-03-07 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-03-06 | 1996-09-05 | 1997-03-07 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-03-06 | 2000-09-05 | 2001-03-07 | $7700.00 | Window Closed / Lapsed |