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US 6,187,910 B1Granted
Bridged aromatic substituted amine ligands with donor atoms
AssigneeNeoRx Corporation
InventorSudhakar Kasina
Life of this patent
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Abstract
The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.
Claims18
A compound of the formula:
- wherein:
- n=0 or 1;
- R1 and R2 are independently selected from hydrogen, ═O, with the proviso that both are not ═O, —(CH2)m—Z where m is 0-10 and Z represents a conjugation group or targeting moiety, and —(CH2)m—W where m is 0-10 and W represents a hydrolyzable group, or R1 and R2 are taken together to form a cyclic anhydride or a benzene ring;
- R3 is hydrogen, lower alkyl, alkoxy, halogen, hydroxyl, nitro, —(CH2)m—Z or —(CH2)m—W;
- R4 and R5 are attached at one or more of the ring positions and are independently selected from hydrogen, lower alkyl, alkoxy, halogen, hydroxyl, nitro, —(CH2)m—Z and —(CH2)m—W;
- R6 and R7 are independently selected from hydrogen with the proviso that both are not hydrogen, lower alkyl, alkoxy, halogen, hydroxyl, nitro, —(CH2)m—Z, —(CH2)m—W— and
- where Q represents a multivalent acid functionality group able to coordinate with metal ions, and p=0 to 1;
- R12 and R13 are independently selected from hydrogen, hydroxyl, carboxyl, phosphoric, and hydrocarbon radicals having from 1-10 carbon atoms, and physiologically acceptable salts of the acid radicals;
- X, X′, Y and Y′ are independently selected from carbon and sulfur to independently form 5 or 6 member aromatic rings wherein the remaining ring atoms are carbon;
- A and A′ are nitrogen, where A bears R8 and R10 and A′ bears R9 and R11, wherein R8 and R10 are joined to form a cyclic anhydride or R9 and R11 are joined to form a cyclic anhydride or both, and any of R8, R9, R10 and R11 not joined to form a cyclic anhydride are independently selected from hydrogen, lower alkyl, alkoxy, halogen, hydroxyl, nitro, —(CH2)m—Z, —(CH2)m—W and
- the compound has at least one Z, W or Q.
8 more elements
Dependencies are inferred from the claim text.