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US 6,143,274 AGranted
Method for imaging and radiopharmaceutical therapy using 1-substituted-4,7,10-tricarboxymethyl-1,4,7,10-tetraazacyclododecane and analogs
OwnerMichael F. Tweedle, Glen T. Gaughan +1inventors
InventorsMichael F. Tweedle, Glen T. Gaughan, James J. Hagan
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Abstract
A method for imaging mammalian tissue utilizing a non-ionic complex of a paramagnetic ion of lanthanide element and a macrocyclic chelating agent.
Claims186
A method for imaging brain tissue of a mammalian host comprising the steps of:
- administering an effective amount of a contrast agent to the host, the contrast agent comprising a complex of a metal atom and a tetraazacyclo compound, the complex being charge neutral in aqueous solution;
- and
- obtaining an image of the brain tissue in vivo with an x-ray, radionuclide, ultrasound, or magnetic resonance imaging apparatus.
A method for imaging heart tissue of a mammalian host comprising the steps of:
- administering an effective amount of a contrast agent to the host, the contrast agent comprising a complex of a metal atom and a tetraazacyclo compound, the complex being charge neutral in aqueous solution;
- and
- obtaining an image of the heart tissue in vivo with an x-ray, radionuclide, ultrasound, or magnetic resonance imaging apparatus.
A method for imaging kidney tissue of a mammalian host comprising the steps of:
- administering an effective amount of a contrast agent to the host, the contrast agent comprising a complex of a metal atom and a tetraazacyclo compound, the complex being charge neutral in aqueous solution;
- and
- obtaining an image of the kidney tissue in vivo with an x-ray, radionuclide, ultrasound, or magnetic resonance imaging apparatus.
A method for imaging prostate tissue of a mammalian host comprising the steps of:
- administering an effective amount of a contrast agent to the host, the contrast agent comprising a complex of a metal atom and a tetraazacyclo compound, the complex being charge neutral in aqueous solution;
- and
- obtaining an image of the prostate tissue in vivo with an x-ray, radionuclide, ultrasound, or magnetic resonance imaging apparatus.
A method for imaging breast tissue of a mammalian host comprising the steps of:
- administering an effective amount of a contrast agent to the host, the contrast agent comprising a complex of a metal atom and a tetraazacyclo compound, the complex being charge neutral in aqueous solution;
- and
- obtaining an image of the breast tissue in vivo with an x-ray, radionuclide, ultrasound, or magnetic resonance imaging apparatus.
A method for imaging bladder tissue of a mammalian host comprising the steps of:
- administering an effective amount of a contrast agent to the host, the contrast agent comprising a complex of a metal atom and a tetraazacyclo compound, the complex being charge neutral in aqueous solution;
- and
- obtaining an image of the bladder tissue in vivo with an x-ray, radionuclide, ultrasound, or magnetic resonance imaging apparatus.
A method for imaging spleen tissue of a mammalian host comprising the steps of:
- administering an effective amount of a contrast agent to the host, the contrast agent comprising a complex of a metal atom and a tetraazacyclo compound, the complex being charge neutral in aqueous solution;
- and
- obtaining an image of the spleen tissue in vivo with an x-ray, radionuclide, ultrasound, or magnetic resonance imaging apparatus.
A method for imaging tumor tissue of a mammalian host comprising the steps of:
- administering an effective amount of a contrast agent to the host, the contrast agent comprising a complex of a metal atom and a tetraazacyclo compound, the complex being charge neutral in aqueous solution;
- and
- obtaining an image of the tumor tissue in vivo with an x-ray, radionuclide, ultrasound, or magnetic resonance imaging apparatus.
A method for arthrography comprising the steps of:
- administering an effective amount of a contrast agent to a host, the contrast agent comprising a complex of a metal atom and a tetraazacyclo compound, the complex being charge neutral in aqueous solution;
- and
- obtaining an image in vivo with an x-ray, radionuclide, ultrasound, or magnetic resonance imaging apparatus.
A method for radiopharmaceutical therapy comprising:
- administering an effective amount of a complex comprising a radioactive metal ion and a tetraazacyclo compound, said complex bound to a disease specific entity and said complex being charge neutral in aqueous solution.
A method for radiopharmaceutical therapy comprising:
- administering an effective amount of a complex comprising a radioactive metal ion and a tetraazacyclo compound, said complex bound to a disease specific entity, wherein the tetraazacyclo compound has the formula represented below:
- ##STR70## or a pharmaceutically acceptable salt thereof, wherein Y is oxygen or ##STR71## R.sub.1 is hydrogen, alkyl having from one to five carbon atoms, arylalkyl wherein the aryl portion is phenyl or substituted phenyl, alkoxy having from one to five carbon atoms, hydroxyalkyl wherein the alkyl portion has from one to five carbon atoms and having one or more hydroxy groups, ##STR72## wherein G is NH.sub.2, ##STR73## N(R.sub.4).sub.2, CN, wherein R.sub.4 is an alkyl or hydroxyalkyl, ##STR74## wherein n and m are zero or an integer from one to five, R.sub.2 is a hydrogen or alkyl,
- R.sub.3 is a hydrogen, hydroxyalkyl having form one to five carbon atoms and having one or more hydroxy groups, alkoxy having from one to five carbon atoms, phenyl or substituted phenyl or phenylalkyl or substituted phenylalkyl and
- X is chloro, bromo or iodo,
- wherein the term substituted phenyl refers to phenyl groups substituted with one, two or three halogen, hydroxyl, alkyl, alkoxy carbamoyl or carboxyl groups.
2 more elements
A method for radiopharmaceutical therapy comprising:
- administering an effective amount of a complex comprising a radioactive metal ion and an unsymmetrically substituted tetraazacyclo compound, said complex bound to a disease specific entity.
A method for radiopharmaceutical therapy comprising:
- administering an effective amount of a complex comprising a radioactive metal ion and an unsymmetrically substituted tetraazacyclo compound, said complex bound to a disease specific entity, wherein the tetraazacyclo compound has the formula represented below:
- ##STR75## or a pharmaceutically acceptable salt thereof, wherein Y is oxygen or ##STR76## R.sub.1 is hydrogen, alkyl having from one to five carbon atoms, arylalkyl wherein the aryl portion is phenyl or substituted phenyl, alkoxy having from one to five carbon atoms, hydroxyalkyl wherein the alkyl portion has from one to five carbon atoms and having one or more hydroxy groups, ##STR77## wherein G is NH.sub.2, ##STR78## N(R.sub.4).sub.2, CN, wherein R.sub.4 is an alkyl or hydroxyalkyl, ##STR79## wherein n and m are zero or an integer from one to five, R.sub.2 is a hydrogen or alkyl,
- R.sub.3 is a hydrogen, hydroxyalkyl having form one to five carbon atoms and having one or more hydroxy groups, alkoxy having from one to five carbon atoms, phenyl or substituted phenyl or phenylalkyl or substituted phenylalkyl and
- X is chloro, bromo or iodo,
- with the proviso that if R.sub.1 is --(CH.sub.2).sub.n G, n is one and R.sub.2 is hydrogen, then G is not CO.sub.2 H, and
- wherein the term substituted phenyl refers to phenyl groups substituted with one, two or three halogen, hydroxyl, alkyl, alkoxy carbamoyl or carboxyl groups.
3 more elements
Dependencies are inferred from the claim text.