Claims for Patent: 4,360,511

Summary for Patent: 4,360,511

Title:	Amines useful as brain imaging agents
Abstract:	Certain radioiodine containing amines useful as brain imaging agents are disclosed. The compounds of the invention are represented by the formula ##STR1## wherein I is a radioisotope of iodine with I-123 being preferred, R is lower alkyl or halogen, R.sub.1 and R.sub.2 are the same or different and are selected from the group consisting of hydrogen and lower alkyl, R.sub.3 and R.sub.4 are the same or different and are selected from the group consisting of hydrogen, alkyl, aryl, substituted aryl, aralkyl, substituted aralkyl and substituted carbamoyl methyl or R.sub.3 and R.sub.4 taken together with the nitrogen to which they are attached form a 5- or 6-membered ring which may be substituted with one or more lower alkyl groups, x is 0 to 4, y is 0 to 3 and z is 0 or 1 and pharmaceutically acceptable acid addition salts thereof.
Inventor(s):	Baldwin; Ronald M. (San Francisco, CA), Lin; Tz-Hong (Fremont, CA), Winchell; Harry S. (Lafayette, CA)
Assignee:	Medi-Physics, Inc. (Emeryville, CA)
Application Number:	06/161,097
Patent Claims:	1. A radioiodinated amine of the formula: ##STR9## wherein I is a radioisotope of iodine, R is lower alkyl or halogen; R.sub.1 is hydrogen or lower alkyl; R.sub.2 is lower alkyl; R.sub.3 and R.sub.4 are the same or different and are selected from the group consisting of hydrogen, alkyl, aryl, substituted aryl, aralkyl, substituted aralkyl and carbamoylmethyl or R.sub.3 and R.sub.4 taken together with the nitrogen to which they are attached form a 5- or 6-membered ring which may be substituted with one or more lower alkyl groups, and x is 0 to 4 and y is 0 to 3. 2. The compound of claim 1 wherein said compound is I-123-p-iodo-alpha-methylbenzylamine. 3. The compound of claim 1 wherein said compound is I-123-N-isopropyl-p-iodo-alpha-methylbenzylamine. 4. The compound of claim 1 wherein said compound I-123-R-p-iodoamphetamine. 5. The compound of claim 1 wherein said compound is I-123-S-p-iodoamphetamine. 6. The compound of claim 1 wherein said compound is I-123-R-N-isopropyl-p-iodoamphetamine. 7. The compound of claim 1 wherein said compound is I-123-S-N-isopropyl-p-iodoamphetamine. 8. A method of imaging the brain comprising intraveneously injecting an effective amount of a composition comprising a compound of claim 1 in a carrier suitable for intravenous injection and scanning the brain with scintiscanning means. 9. A method in accordance with claim 8 wherein said compound is I-123-p-iodo-.alpha.-methylbenzylamine. 10. A method in accordance with claim 8 wherein said compound is I-123-N-isopropyl-p-iodo-.alpha.-methylbenzylamine. 11. A method in accordance with claim 8 wherein said compound is I-123-R-p-iodoamphetamine. 12. A method in accordance with claim 8 wherein said compound is I-123-S-p-iodoamphetamine. 13. A method in accordance with claim 8 wherein said compound is I-123-R-N-isopropyl-p-iodoamphetamine. 14. A method in accordance with claim 8 wherein said compound is I-123-S-N-isopropyl-p-iodoamphetamine.