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Details for Patent: 5,648,063

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Details for Patent: 5,648,063

Title: Sterile composition comprising a chelate complex for magnetic resonance imaging
Abstract:A diagnostic medium contains at least one physiologically well tolerated complex salt comprising an anion of a complexing acid and one or more central ion or ions of an element with an atomic number of 21 to 29, 42, 44 or 57 to 83 and, optionally, one or more physiologically biocompatible cation or cations of an inorganic and/or organic base or amino acid, optionally, with additives customary in galenic formulations, dissolved or suspended in an aqueous medium.
Inventor(s): Gries; Heinz (Berlin, DE), Rosenberg; Douwe (Berlin, DE), Weinmann; Hanns-Joachim (Berlin, DE), Speck; Ulrich (Berlin, DE), Mutzel; Wolfgang (Berlin, DE), Hoyer; Georg-Alexander (Berlin, DE), Pfeiffer, deceased; Heinrich (late of Berlin, DE), Renneke; Franz-Josef (Nordkirchen, DE)
Assignee: Schering Aktiengesellschaft (Berlin, DE)
Filing Date:Aug 04, 1993
Application Number:08/101,811
Claims:1. A method of performing an NMR diagnostic procedure comprising administering to a patient an effective amount of an NMR diagnostic medium and them exposing the patient to an NMR measurement step to which the diagnostic medium is responsive, thereby imaging at least a portion of the patient's body, wherein the diagnostic medium comprises a physiologically compatible chelate complex of (a) a complexing agent and (b) at least one central paramagnetic ion of an element with an atomic number of 21 to 29, 42, 44 or 58 to 70 chelated therewith, wherein the complexing agent is of the formula ##STR13## wherein X is --COOY;

Y is a hydrogen atom, a metal ion equivalent or a physiologically compatible cation of an inorganic or organic base or amino acid; and

w is a number 1, 2 or 3;

provided that at least two of the substituents Y are metal ion equivalents of an element with an atomic number of 21 to 29, 42, 44 or 58 to 83.

2. A method of claim 1 wherein the concentration of chelate complex in the medium is 1 .mu.mole to 1 mole.

3. A method of claim 1 wherein the concentration of chelate complex in the medium is 1 .mu.mole to 5 mmole.

4. A method of claim 1 wherein the concentration of chelate complex in the medium is 250 mmole to 1 mole.

5. A method of claim 1 wherein the chelate complex is derived from a chelating agent which is 1,4,7,10-tetraazacyclododecanetetraacetic acid.

6. A method of claim 1 wherein the chelate complex is derived from a chelating agent which is 1,4,8,11-tetraazacyclotetradecanetetraacetic acid.

7. A method of claim 1 wherein said paramagneticion is Gd(III).

8. A method of claim 5, wherein the ion is Gd(III).

9. A method of claim 8, wherein the remaining Y is lysine, arginine or ornithine.

10. A method of claim 9, wherein the chelate complex is the lysine salt of the Gd(III) complex of 1,4,7,10-tetraazacyclododecanetetraacetic acid.

11. A method according to claim 1, wherein one or two of said Y groups are each a physiologically compatible cation of an inorganic or organic base or amino acid.

12. A method according to claim 1, wherein said chelate complex is dissolved or suspended in an aqueous medium.

13. A method according to claim 1, wherein said chelate complex is administered intravascularly or orally.

14. A method of performing an NMR diagnostic procedure comprising administering to a patient an effective amount of an NMR diagnostic medium and then exposing the patient to an NMR measurement step to which the diagnostic medium is responsive, thereby imaging at least a portion of the patient's body, wherein the diagnostic medium comprises a physiologically compatible chelate complex of (a) a complexing agent and (b) at least one central paramagnetic ion of an element with an atomic number of 21 to 29, 42, 44 or 57-70 chelated therewith, wherein the complexing agent is of the formula ##STR14## wherein R.sup.9 is carboxymethyl;

A is a hydrocarbon radical;

X is N;

D is ##STR15## R is carboxymethyl; and s and t are, in each case, independently, 0-5; and wherein said complex is optionally a complex with an inorganic or organic acid.

15. A method according to claim 14, wherein

A is ethylene;

s is 0; and

t is 0.

16. A method according to claim 14, wherein said complexing agent is 1,4,8,11-tetraazacyclotetradecane-N,N',N", N'"-tetraacetic acid.

17. A method of performing an NMR diagnostic procedure comprising administering to a patient an effective amount of an NMR diagnostic medium and them exposing the patient to an NMR measurement step to which the diagnostic medium is responsive, thereby imaging at least a portion of the patient's body, wherein the diagnostic medium comprises a physiologically compatible chelate complex of (a) a complexing agent and (b) at least one central paramagnetic ion of an element with an atomic number of 21 to 29, 42, 44 or 58 to 70 chelated therewith, wherein the complexing agent is of the formula ##STR16## wherein X is --PO.sub.3 HY;

Y is a hydrogen atom, a metal ion equivalent or a physiologically compatible cation of an inorganic or organic base or amino acid; and

w is a number 1, 2 or 3;

provided that at least two of the substituents Y are metal ion equivalents of an element with an atomic number of 21 to 29, 42, 44 or 58 to 83.

18. A method according to claim 17, wherein the chelate complex further comprises at least one physiologically compatible cation of an inorganic or organic base or amino acid.

19. A method according to claim 17, wherein said chelate complex is dissolved or suspended in an aqueous medium.

20. A method according to claim 17, wherein said chelate complex is administered intravascularly or orally.

21. A method of claim 17, wherein the concentration of chelate complex in the medium is 1 .mu.mole to 1 mole.

22. A method of claim 17, wherein the concentration of chelate complex in the medium is 1 .mu.mole to 5 mmole.

23. A method of claim 17, wherein the concentration of chelate complex in the medium is 250 mmole to 1 mole.

24. A method of claim 17, wherein said paramagneticion is Gd(III).

25. A method of performing an NMR diagnostic procedure comprising administering to a patient an effective amount of an NMR diagnostic medium and them exposing the patient to an NMR measurement step to which the diagnostic medium is responsive, thereby imaging at least a portion of the patient's body, wherein the diagnostic medium comprises a physiologically compatible chelate complex of (a) a complexing agent and (b) at least one central paramagnetic ion of an element with an atomic number of 21 to 29, 42, 44 or 58 to 70 chelated therewith, wherein the complexing agent is of the formula ##STR17## wherein X is --CONHOY;

Y is a hydrogen atom, a metal ion equivalent or a physiologically compatible cation of an inorganic or organic base or amino acid; and

w is a number 1, 2 or 3;

provided that at least two of the substituents Y are metal ion equivalents of an element with an atomic number of 21 to 29, 42, 44 or 58 to 83.

26. A method according to claim 25, wherein the chelate complex further comprises at least one physiologically compatible cation of an inorganic or organic base or amino acid.

27. A method according to claim 25, wherein said chelate complex is dissolved or suspended in an aqueous medium.

28. A method according to claim 25, wherein said chelate complex is administered intravascularly or orally.

29. A method of claim 25, wherein the concentration of chelate complex in the medium is 1 .mu.mole to 1 mole.

30. A method of claim 25, wherein the concentration of chelate complex in the medium is 1 .mu.mole to 5 mmole.

31. A method of claim 25, wherein the concentration of chelate complex in the medium is 250 mmole to 1 mole.

32. A method of claim 25, wherein said paramagnetic is Gd(III).

33. A method according to claim 1, wherein said paramagnetic ion is chromium(III), manganese(II), iron(III), iron(II), cobalt(II), nickel(II), copper(II), praseodymium(III), neodymium(III), samarium(III), ytterbium(III), gadolinium(III), terbium(III), dysprosium(III), holmium(III) or erbium(III).

34. A method according to claim 5, wherein said paramagnetic ion is chromium(III), manganese(II), iron(III) , iron(II) , cobalt (II) , nickel (II) , copper(II) , praseodymium(III) , neodymium(III), samarium(III) , ytterbium(III) , gadolinium(III) , terbium(III) , dysprosium(III), holmium(III) or erbium(III).

35. A method according to claim 33, wherein said paramagnetic ion is manganese(II), iron(III), dysprosium(III), or ytterbium(III).

36. A method according to claim 34, wherein said paramagnetic ion is manganese(II), iron(III), dysprosium(III), or ytterbium(III).

37. A method according to claim 11, wherein said physiologically compatible cations are in each case sodium or N-methylglucamine.

38. A method according to claim 33, wherein one or two of said Y groups are each a physiologically compatible cation of an inorganic or organic base or amino acid.

39. A method according to claim 34, wherein one or two of said Y groups are each a physiologically compatible cation of an inorganic or organic base or amino acid.

40. A method according to claim 35, wherein one or two of said Y groups are each a physiologically compatible cation of an inorganic or organic base or amino acid.

41. A method according to claim 36, wherein one or two of said Y groups are each a physiologically compatible cation of an inorganic or organic base or amino acid.

42. A method according to claim 37, wherein said physiologically compatible cations are in each case sodium or N-methylglucamine.

43. A method according to claim 41, wherein said physiologically compatible cations are sodium or N-methylglucamine.

44. A method according to claim 43, wherein said paramagnetic ion is dysprosium(III).

45. A method according to claim 43, wherein said paramagnetic ion is ytterbium(III).

46. A method according to claim 43, wherein said paramagnetic ion is manganese(II).

47. A method according to claim 36, wherein said paramagnetic ion is iron(III). .

48. A method according to claim 44, wherein the physiologically compatible cation is sodium.

49. A method according to claim 45, wherein the physiologically compatible cation is sodium.

50. A method according to claim 46, wherein the physiologically compatible cations are N-methylglucamine.

51. A NMR contrast enhancing composition comprising:

a chelate complex of Gd with DOTA; and

a physiologically acceptable carrier,

wherein said composition is in sterile form.

52. A NMR contrast enhancing composition comprising a physiologically compatible chelate complex of (a) a complexing agent and (b) Gd chelated therewith, wherein the complexing agent is of the formula ##STR18## wherein R.sup.9 is carboxymethyl;

A is, in each case, ethylene or propylene;

X is N;

D is ##STR19## R is carboxymethyl; and s and t are each 0; and a pharmaceutically acceptable carrier, wherein said composition is in sterile form.

53. A composition according to claim 52, wherein w is each case is 1.

54. A composition according to claim 52, wherein said complexing agent is 1,4,8,11-tetraazacyclotetra-decane-N,N',N",N"'-tetraacetic acid, said composition being in sterile form.
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