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Claims for Patent: 4,233,285

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Claims for Patent: 4,233,285

Title: Mercaptocarboxylic acid radiopharmaceuticals
Abstract:Mercaptocarboxylic acid chelated heavy metal radioisotope pharmaceuticals and methods for making them.
Inventor(s): Winchell; Harry S. (Lafayette, CA), Lin; Tz-Hong (Berkeley, CA)
Assignee: Medi-Physics, Inc. (Emeryville, CA)
Application Number:05/359,719
Patent Claims: 1. A radiopharmaceutical comprising a complex of a mercaptocarboxylic acid chelating agent having at least one carboxylic acid group and at least one mercapto group with a radioactive heavy metal ion produced by reduction with stannous chloride in the presence of the chelating agent wherein said complex is formed at a pH of from about 2 to 4 and the mole ratio of said metal chelating agent to stannous chloride present to reduce such metal ion is about three to one.

2. The radiopharmaceutical of claim 1 wherein said chelating agent is selected from the group consisting of mercaptoacetic acid, 2-mercaptopropionic acid, 3-mercaptopropionic acid, mercaptosuccinic acid and 2,3-dimercaptosuccinic acid.

3. The radiopharmaceutical of claim 2 wherein said agent is 2,3-dimercaptosuccinic acid and said heavy metal ion is technetium 99m.

4. A reagent for producing a radiopharmaceutical comprising an aqueous solution containing mercaptocarboxylic acid chelating agent having at least one carboxylic acid group and at least mercapto group, 99-m-technetium pertechnetate and stannous chloride, where the mole ratio of said chelating agent to stannous chloride is about 3 to 1 and the pH of said solution being from about 2 to about 4.

5. The composition of claim 4 wherein said chelating agent is selected from the group consisting of mercaptoacetic acid, 2-mercaptopropionic acid, 3-mercaptopropionic acid, mercaptosuccinic acid and 2,3-dimercaptosuccinic acid.

6. The composition of claim 4 wherein said agent is 2,3-dimercaptosuccinic acid.

7. A method of imaging the renal cortex, brain abnormalities, tumors and myocardial infarcts of a patient comprising intravenously injecting said patient with a radiopharmaceutical comprising a complex of a mercaptocarboxylic acid metal chelating agent with a radioactive heavy metal ion produced by reduction with stannous chloride, wherein said complex is formed at a pH of from 2 to 4 and the mol ratio of said metal chelating agent to stannous chloride present to produce metal ion is about three to one, and scanning with a suitable apparatus.

8. The method of claim 7 wherein said chelating agent is selected from the group consisting of mercaptoacetic acid, 2-mercaptopropionic acid, 3-mercaptopropionic acid, mercaptosuccinic acid and 2,3-dimercaptosuccinic acid.

9. The method of claim 8 wherein said metal ion is technetium-99m and said chelating agent is 2,3-dimercaptosuccinic acid.
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