Dopamine receptor ligands and imaging agents
First Claim
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1. A compound selected from the group consisting of compounds of the formula ##STR14## where Y and Y'"'"' are independently selected from the group consisting of hydrogen C1 -C5 alkyl, C1 -C5 alkenyl and C1 -C5 alkynyl groups;
- Z is selected from the group consisting of H, Halogen (Hal), C═
CH--Hal;
C1 -C10 alkylene-Hal;
C1 -C10 alkylene--C═
CH--Hal;
C1 -C10 alkylene-phenyl-Hal;
or C1-C10 alkylene-heteroaryl-hal;
Hal is selected from the group consisting of I, 123 I, 125 I and 131 I; and
A is an alkylene moiety of from two to eight carbon atoms.
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Abstract
Novel CNS dopamine D-2 receptors, such as the compound 5-iodo-7-N-[(1-ethyl-2-pyrrolidinyl)methyl]carboxamide-2,3-dihydrobenzofuran, are disclosed. These compounds are useful as imaging agents for D-2 receptors in the human brain and exhibit good brain retention and in vivo stability.
30 Citations
8 Claims
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1. A compound selected from the group consisting of compounds of the formula ##STR14## where Y and Y'"'"' are independently selected from the group consisting of hydrogen C1 -C5 alkyl, C1 -C5 alkenyl and C1 -C5 alkynyl groups;
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Z is selected from the group consisting of H, Halogen (Hal), C═
CH--Hal;
C1 -C10 alkylene-Hal;
C1 -C10 alkylene--C═
CH--Hal;
C1 -C10 alkylene-phenyl-Hal;
or C1-C10 alkylene-heteroaryl-hal;Hal is selected from the group consisting of I, 123 I, 125 I and 131 I; and A is an alkylene moiety of from two to eight carbon atoms. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8)
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Specification
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Current AssigneeTrustees Of The University Of Pennsylvania (University of Pennsylvania)
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Original AssigneeTrustees Of The University Of Pennsylvania (University of Pennsylvania)
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InventorsKung, Hank F., Murphy, Raymond
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Primary Examiner(s)Stoll, Robert L.
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Assistant Examiner(s)COVERT, JOHN
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Application NumberUS07/339,006Time in Patent Office1,156 DaysField of Search424/1.1, 514/422, 548/400, 548/525, 549/354, 549/414, 549/456, 546/126, 564/161, 564/163, 564/180, 564/181, 564/189US Class Current546/126CPC Class CodesA61K 2123/00 Preparations for testing in...A61K 51/0446 having five-membered rings ...C07D 207/09 Radicals substituted by nit...C07D 405/12 linked by a chain containin...
