Claims
- 1. A pharmaceutical composition comprising:
a) from about 0.01% to about 99.99% by weight, of a 1,4,8,11-tetraaza-bicyclo [6.6.2] hexadecane manganese (II) complex magnetic resonance imaging agent selected from the group: 28iv) and mixtures thereof; wherein each R is independently selected from the group consisting of:
i) C1—C18 hydrocarbyl; ii) —(CH2)nCO2—; iii) CH3(CH2)nCO—; iv) —(CH2)nR1; v) —(CH2)nOPO3—; vi) —[(CH2)nOPO3R2(phenyl)2]—; R1 is hydroxyl, 2-hydroxyphenyl, 2-pyridyl, 2-furfuryl, and mixtures thereof; R2 is C1—C12 linear, branched, or cyclic alkylene; R3 is selected from the group consisting of:
i) hydrogen; ii) C1—C18 hydrocarbyl; iii) —OH; iv) —(CH2)mCO2—; v) —O(CH2)mCO2—; vi) and mixtures thereof; the indices m and n have the value from 0 to about 10; X is an pharmaceutically compatible anion in sufficient amount q to provide electronic neutrality; and b) the balance carriers and other adjunct ingredients.
- 2. A composition according to claim 1 comprising from about 1 % to about 50%, of said imaging agent.
- 3. A composition according to claim 1 comprising from about 10% to about 75% by weight, of said imaging agent.
- 4. A composition according to claim 1 wherein said carrier is an inert solid.
- 5. A composition according to claim 1 wherein R is selected from the group consisting of methyl, ethyl, isopropyl, butyl, and mixtures thereof.
- 6. A composition according to claim 1 wherein at least one R unit comprises —(CH2)nCO2 —, n is from 1 to 4.
- 7. A composition according to claim 6 wherein n is 1.
- 8. A composition according to claim 1 wherein each R unit comprises —(CH2)nCO2—, n is from 1 to 4.
- 9. A composition according to claim 1 wherein said complex has the formula:
- 10. A composition according to claim 1 wherein said complex has the formula:
- 11. A pharmaceutical composition comprising an MRI agent having the formula selected from the group consisting of:
- 12. A composition according to claim 11 wherein at least one R unit comprises —(CH2)nCO2—, n is from 1 to 4.
- 13. A composition according to claim 12 wherein n is 1.
- 14. A composition according to claim 11 wherein each R unit comprises —(CH2)nCO2—, n is from 1 to 4.
- 15. A method for providing an enhanced magnetic resonance image contrast in human or animal tissue, said method comprising the step of administering to a human an effective amount, of a composition comprising:
a) from about 0.01% to about 99.99% by weight, of a 1,4,8,11 -tetraaza-bicyclo[6.6.2] hexadecane manganese (II) complex magnetic resonance imaging agent selected from the group: 32iv) and mixtures thereof; wherein each R is independently selected from the group consisting of:
i) C1—C18 hydrocarbyl; ii) —(CH2)nCO2—; iii) CH3(CH2)nCO—; iv) —(CH2)nR1; v) —(CH2)nOPO3—; vi) —[(CH2)nOPO3R2(phenyl)2]—; R1 is hydroxyl, 2-hydroxyphenyl, 2-pyridyl, 2-furfuryl, and mixtures thereof; R2 is C1—C12 linear, branched, or cyclic alkylene; R3is selected from the group consisting of:
i) hydrogen; ii) C1—C18 hydrocarbyl; iii) —OH; iv) —(CH2)mCO2—; v) —O(CH2)mCO2—; vi) and mixtures thereof; the indices m and n have the value from 0 to about 10; X is an pharmaceutically compatible anion in sufficient amount q to provide electronic neutrality; and
b) the balance carriers and other adjunct ingredients.
- 16. A method according to claim 15 wherein the serum blood levels of said agent is from about 0.001 moles to about 2 moles per liter.
- 17. A method for providing an enhanced magnetic resonance image contrast in human or animal tissue, said method comprising the step of:
A) administering to a human an effective amount of a composition comprising:
a) from about 0.01% to about 99.99% by weight, of a 1,4,8,11-tetraaza-bicyclo[6.6.2] hexadecane manganese (II) complex magnetic resonance imaging agent selected from the group: 33iv) and mixtures thereof; wherein each R is independently selected from the group consisting of:
i) C1—C18 hydrocarbyl; ii) —(CH2)nCO2—; iii) CH3(CH2)nCO—; iv) —(CH2)nR1; v) —(CH2)nOPO3—; vi) —[(CH2)nOPO3R2(phenyl)2]—; R1 is hydroxyl, 2-hydroxyphenyl, 2-pyridyl, 2-furfuryl, and mixtures thereof; R2 is C1—C12 linear, branched, or cyclic alkylene;
R3 is selected from the group consisting of:
i) hydrogen; ii) C2—C18 hydrocarbyl; iii) —OH; iv) —(CH2)mCO2—; v) —O(CH2)mCO2—; vi) and mixtures thereof; the indices m and n have the value from 0 to about 10; X is an pharmaceutically compatible anion in sufficient amount q to provide electronic neutrality; and
b) the balance carriers and other adjunct ingredients; and B) sustaining said effective amount of MRI agent for a period of time exceeding one hour.
- 18. A method according to claim 17 wherein at least one R unit comprises —(CH2)nCO2—, n is from 1 to 4.
- 19. A method according to claim 18 wherein n is 1.
- 20. A method according to claim 17 wherein each R unit comprises —(CH2)nCO2—, n is from 1 to 4.
Parent Case Info
[0001] This Application claims priority to U.S. Provisional Pat. App. Ser. No. 60/235,011 filed Sep. 25, 2000.
Provisional Applications (1)
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Number |
Date |
Country |
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60235011 |
Sep 2000 |
US |