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US 5,690,906 AGranted
Dopamine D-3 and serotonin (5-HT.sub.1A) receptor ligands and imaging agents
AssigneeThe Trustees of the University of Pennsylvania
InventorHank F. Kung
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Abstract
Tetralin derivatives, such as 7-hydroxy-2-(N-n-propyl-N-3 '-iodo-2'-propenyl)-amino!tetralin and 8-hydroxy-2-(N-n-propyl-N-3 '-iodo-2'-propenyl)amino-tetralin, are disclosed which have affinity and specificity for dopamine D-3 and/or serotonin 5-HT.sub.1A receptors.
Claims41
Compounds of the formula ##STR14## where A is selected from the group consisting of OH and OCH.sub.3 and is at the 7- or 8-ring position;
- X is selected from the group consisting of CH.sub.2, O and S;
- D is --N(CH.sub.2 CH.sub.2 CH.sub.3)(R);
- R is selected from the group consisting of H, C.sub.1 -C.sub.5 alkyl and (CH.sub.2).sub.n CH.dbd.CHR';
- n is 1 or 2;
- R' is selected from the group consisting of an iodine atom, a bromine atom, a methyl group and an ethyl group;
- E is selected from the group consisting of H, C.sub.1 -C.sub.5 alkyl and (CH.sub.2).sub.n CH.dbd.CHR' and is at the 1- or 3-ring position;
- provided that one of D and E contains the moiety (CH.sub.2).sub.n CH.dbd.CHR' wherein R' is selected from the group consisting of an iodine atom and a bromine atom;
- or D and E may be taken together to form a ring selected from the group consisting of ##STR15## where R" is (CH.sub.2).sub.n CH.dbd.CH--R', provided that R' is here selected from the group consisting of an iodine atom and a bromine atom;
- and
- Y is selected from the group consisting of CH.sub.2, O and S;
- provided that such compound is an R-isomer;
- and pharmaceutically acceptable salts thereof.
9 more elements
Compounds of the formula ##STR16## where A is selected from the group consisting of OH and OCH.sub.3 and is at the 7- or 8-ring position;
- X is selected from the group consisting of CH.sub.2, O and S;
- D is --N(CH.sub.2 CH.sub.2 CH.sub.3)(R.sub.1);
- R.sub.1 is selected from the group consisting of H, C.sub.1 -C.sub.5 alkyl and (CH.sub.2).sub.n CH.dbd.CHSnBu.sub.3 ;
- n is 1 or 2;
- E is selected from the group consisting of H, C.sub.1 -C.sub.5 alkyl and (CH.sub.2).sub.n CH.dbd.CHSnBu.sub.3 and is at the 1- or 3- ring position;
- provided that one of D and E contains the moiety (CH.sub.2).sub.n CH.dbd.CHSnBu.sub.3 ;
- or D and E may be taken together to form a ring selected from the group consisting of ##STR17## where R" is (CH.sub.2).sub.n CH.dbd.CH--SnBu.sub.3 ;
- and
- Y is selected from the group consisting of CH.sub.2, O and S;
- provided that such compound is an R-isomer.
7 more elements
Dependencies are inferred from the claim text.