Claims
- 1. A chelate complex of a compound of formula I ##STR19## wherein X represents a group of formula NR.sup.3 ; each R.sup.1 which may be the same or different represents a hydrogen atom, a group of formula OR.sup.3 or NR.sup.3 R.sup.3 or a C.sub.1-8 alkyl or (C.sub.1-8 alkoxy)-C.sub.1-8 alkyl group optionally substituted by a hydroxyl group or by a group of formula NR.sup.3 R.sup.3 or CONR.sup.3 R.sup.3 ;
- each R.sup.2 which may be the same or different represents a hydrogen atom or a C.sub.1-8 alkyl or C.sub.1-8 alkoxy group optionally mono- or poly-substituted by hydroxyl or C.sub.1-8 alkoxy groups;
- each R.sup.3 which may be the same or different represents a hydrogen atom, an optionally mono- or poly-hydroxylated C.sub.1-8 alkyl group or a group of formula CH.sub.2 Y;
- Y represents a group of formula COZ, CON(OH)R.sup.4, POZ.sub.2 or SO.sub.2 Z;
- Z represents a group of formula OR.sup.4, NR.sup.4 R.sup.4, or ##STR20## where each R.sup.11 which may the same or different is a hydrogen atom, a hydroxyl group or an optionally hydroxylated C.sub.1-8 alkyl group,
- s is 0, 1 or 2, and
- W is a group CHR.sup.11 or a group NR.sup.11 ; and
- each R.sup.4 which may be the same or different represents a hydrogen atom or an optionally mono- or poly-hydroxylated C.sub.1-8 alkyl, (C.sub.1-8 alkoxy)-C.sub.1-8 alkyl or poly-(C.sub.1-8 alkoxy)-C.sub.1-8 alkyl group;
- with the proviso that where s is 0 then in the resultant 5 membered heterocyclic ring W is a CHR.sup.11 group.
- 2. A chelate complex as claimed in claim 1 wherein Z represents a group of formula OR.sup.4 or NR.sup.4 and each R.sup.4 which may be the same or different represents a hydrogen atom or an optionally hydroxylated alkyl group, or a salt thereof.
- 3. A chelate complex as claimed in claim 1 wherein at least one group Z is of formula ##STR21## or a salt thereof.
- 4. A chelate complex as claimed in claim 1 wherein R.sup.1 represents a hydrogen atom, a hydroxyl group or a hydroxylated alkyl group, R.sup.2 represents a hydrogen atom or a hydroxylated alkyl group, R.sup.3 represents a hydrogen atom or a group of formula CH.sub.2 Y, X group NR.sup.3, Y represents a group of formula COZ and Z represents a hydroxyl group or a group NHR.sup.4' where R.sup.4' represents a hydrogen atom or an optionally hydroxylated alkyl group, or a salt thereof.
- 5. A chelate complex as claimed in claim 1 having a formula: ##STR22## where R.sup.5 represents CH.sub.2 COOH, R.sup.6 represents CH.sub.2 COOH, CH.sub.2 CON(CH.sub.3)CH.sub.2 CHOHCH.sub.2 OH, or CH.sub.2 CONHR.sup.7 and R.sup.7 represents CH.sub.3, CH.sub.2 CHOHCH.sub.2 OH or CH(CH.sub.2 OH).sub.2, or NR.sup.5 R.sup.6 represents a group ##STR23## where W represents a group CH.sub.2 or CHOH, s is 0 or 1 and R.sup.11 is hydrogen, or a salt thereof.
- 6. A chelate complex as claimed in claim 1 wherein each Y group is a carboxyl group or a salt or amide thereof.
- 7. A method of generating an image of the human or non-human animal body, said method comprising administering to said body a chelate complex or salt thereof as claimed in claim 1 and generating an X-ray image of at least a part of said body.
- 8. A method of generating an image of the human or non-human animal body, said method comprising administering to said body a chelate complex or salt thereof as claimed in claim 1 and generating a MR-diagnostic image of at least a part of said body.
- 9. A method of generating an image of the human or non-human animal body, said method comprising administering to said body a chelate complex or salt thereof as claimed in claim 1 and generating an ultrasound image of at least a part of said body.
- 10. A method of generating an image of the human or non-human animal body, said method comprising administering to said body a chelate complex or salt thereof as claimed in claim 1 and generating a scintigraphic image of at least a part of said body.
- 11. A chelate complex as claimed in claim 1 wherein the number of ion-forming groups Y is such that the metal chelate is a neutral species.
- 12. A chelate complex as claimed in claim 1 wherein the chelated metal species is a paramagnetic metal ion having an atomic number of 21-29, 42, 44 or 57-71.
- 13. A chelate complex as claimed in claim 12 wherein said paramagnetic metal ion is selected from ions of Eu, Gd, Dy, Ho, Cr, Mn and Fe.
- 14. A chelate complex as claimed in claim 13 wherein said paramagnetic metal ion is selected from Gd.sup.3+, Mn.sup.2+ and Dy.sup.3+.
- 15. A chelate complex as claimed in claim 1 wherein the chelated metal species is a heavy metal ion having an atomic number greater than 37.
- 16. A chelate complex as claimed in claim 1 wherein the chelated metal species is a radioactive metal ion.
- 17. A diagnostic or therapeutic agent comprising a physiologically acceptable metal chelate as claimed in claim 1 or a physiologically acceptable salt thereof, together with at least one pharmaceutical or veterinary carrier or excipient.
- 18. A method of radiotherapy practiced on a human or non-human animal body, said method comprising administering to said body a chelate complex as claimed in claim 16.
- 19. A process for the preparation of metal chelates as claimed in claim 16, said process comprising admixing in a solvent a chelate complex of a compound of formula I or a salt thereof together with an at least sparingly soluble compound of said metal.
- 20. A metal chelate complex of 2,3,5,6-tetrakis-aminomethyl-decacarboxymethyl piperazine and a paramagnetic ion of Gd.sup.3+.
Priority Claims (1)
Number |
Date |
Country |
Kind |
8900719 |
Jan 1989 |
GBX |
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Parent Case Info
This application is a Division of application Ser. No. 08/235,882, filed May 2, 1994, now U.S. Pat. No. 5,439,668, which is a Division of application Ser. No. 07/690,975, filed Jul. 24, 1991, now U.S. Pat. No. 5,348,954, which is a 371 of PCT/EP90/00079 filed Jan. 15, 1990.
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
5348954 |
Almen et al. |
Sep 1994 |
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5349668 |
Almen et al. |
Aug 1995 |
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Foreign Referenced Citations (1)
Number |
Date |
Country |
0250358 |
Dec 1987 |
EPX |
Non-Patent Literature Citations (1)
Entry |
Fossheim et al., J. Med Chem. 34:819-826 (1991). |
Divisions (2)
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Number |
Date |
Country |
Parent |
235882 |
May 1994 |
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Parent |
690975 |
Jul 1991 |
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