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US 4,994,258 AGranted
Gamma emitting, CCK-A antagonists for pancreatic imaging
AssigneeMerck & Co., Inc.
InventorsH. Donald Burns, Nancy J. Brenner, Raymond E. Gibson, Howard F. Solomon
Life of this patent
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Abstract
Novel radiolabeled cholecystokinin-A (CCK-A) antagonists have been developed which, after intravenous injection, localize in the pancreas as a result of specific binding to CCK-A receptors. These tracers, when labeled with appropriate radiohalogens, are useful as commercial diagnostic imaging radiopharmaceuticals and radiotherapeutic drugs.
Claims14
A compound of Formula I:
- ##STR6## wherein:
- A is ##STR7## R.sup.1 is H, C.sub.1 -C.sub.6 linear or branched alkyl, (CH.sub.2).sub.n COOR.sup.8, (CH.sub.2).sub.n OH, (CH.sub.2).sub.n CN, (CH.sub.2).sub.n NR.sup.9 R.sup.10, ##STR8## R.sup.2 is H, --OH, --NO.sub.2, F, Cl, SO.sub.3 H, loweralkyl, loweralkoxy, (CH.sub.2).sub.p COOR.sup.8 or (CH.sub.2).sub.p NR.sup.9 R.sup.10 ;
- R.sup.3 is H, --OH, --NO.sub.2, CF.sub.3, F, Cl, loweralkyl, or loweralkoxy;
- R.sup.4 is H, --OH, --NO.sub.2, CF.sub.3, CN, F, Cl, loweralkyl, loweralkoxy, (CH.sub.2).sub.p COOR.sup.8 or (CH.sub.2).sub.p NR.sup.9 R.sup.10 ;
- R.sup.5, R.sup.6 and R.sup.7 are, independently, H or a radionuclide selected from the group consisting of .sup.122 I, .sup.123 I, .sup.125 I, .sup.131 I, .sup.75 Br, .sup.77 Br, .sup.82 Br, .sup.211 At, with the proviso that at least one of R.sup.5, R.sup.6 and R.sup.7 is not H;
- R.sup.8 is H or loweralkyl;
- R.sup.9 and R.sup.10 are, independently, H or loweralkyl;
- n is 1-4;
- m is 1-2;
- p is 0-4;
- or pharmaceutically acceptable salt thereof.
8 more elements
Dependencies are inferred from the claim text.