Compounds for cancer imaging and therapy
AssigneeResearch Corporation Technologies, Inc.
InventorsChristy S. John, Jesse Baumgold, John G. McAfee, Terry Moody, Wayne Bowen
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Abstract
The present invention relates to a class of compounds having affinity for certain cancer cells, e.g. lung carcinomas, colon carcinomas, renal carcinomas, prostate carcinomas, breast carcinomas, malignant melanomas, gliomas, neuroblastomas and pheochromocytomas. The compounds of the present invention can also bind with high specificity to cell surface sigma receptors and can therefore be used for diagnostic imaging of any tissue having an abundance of cells with sigma receptors. The present invention provides such compounds as agents for diagnostic imaging and for detecting and treating tumors containing the cancer cells described above.
Claims36
A compound of the formula:
- wherein
- Q is a radionuclide;
- each R1, Ra and Rb are independently hydrogen, halide, lower alkyl or lower alkoxy;
- R3 is hydrogen or lower alkyl;
- R5 is a 6 to 7 membered monocyclic nitrogen containing heterocyclic ring, which R5 group is bonded to (NR3)(CH2)m by a carbon atom on said heterocyclic ring and which heterocyclic ring is unsubstituted or substituted with at least one C1-6 alkyl or substituted or unsubstituted arylalkyl, said arylalkyl being unsubstituted or substituted with a halogen, C1-6 alkoxy or C1-6 alkyl group and said nitrogen containing heterocyclic ring having up to seven ring atoms, including 2-6 carbon atoms and 1-3 ring heteroatoms, at least one of the ring atoms on the heterocyclic ring is nitrogen;
- q is an integer from 0 to 2;
- j is an integer from 0 to 6;
- and
- m is an integer from 0 to 6.
The compound according to claim wherein R1 is alkoxy.
A compound of the formula:
- wherein
- Q is a radionuclide,
- each R1, Ra and Rb are independently hydrogen, halide, lower alkyl or lower alkoxy;
- R3 is hydrogen or lower alkyl;
- R5 is a 5 to 7 membered monocyclic nitrogen containing heterocyclic ring which R5 group is bonded to (NR3) (CH2)m by a carbon atom on said heterocyclic ring and which heterocyclic ring is substituted with an unsubstituted or substituted arylalkyl, wherein the substituent on the arylalkyl is halogen, alkoxy or C1-6 alkyl group and said nitrogen containing heterocyclic ring having up to seven ring atoms, including 2-6 carbon atoms and 1-3 ring heteroatoms, of at least one of which is nitrogen,
- q is an integer from 0 to 2;
- j is an integer from 0 to 6;
- and
- m is an integer from 0 to 6.
Dependencies are inferred from the claim text.