Patent ID: 6359111
Filing Date: 2002-03-19
Classification: A61K,C07D

Abstract:
A compound comprising a ligand portion (L) which has binding affinity for an opioid receptor, and a therapeutically or diagnostically effective group (X) selected from radionuclide chelating agents, fluorochromes, toxins, drugs, polyboron moieties, proteins, biological response modifiers, chemical moieties capable of binding to other molecules, and radioisotopes selected from therapeutically effective alpha and beta emitters, and diagnostically effective gamma emitters, wherein L has the formula where G is selected from is a monocyclic, five- or six-membered, carbocyclic or heterocyclic, aromatic ring; R1 is selected from (C1-C5)alkyl, (C3-C6cycloalkyl)C1-C5alkylene, (C5-C7cycloalkenyl)C1-C5alkylene, aryl, aralkyl, trans-(C4-C5)alkenyl, allyl and furan-2-ylC1-C5alkylene; R2 is selected from H, OH and (C1-C5)alkyl-C(&boxH;O)Oâ€”; R3 is selected from H, (C1-C5)alkyl and (C1-C5)alkyl-C(&boxH;O)â€”; and R4 and R5 are independently selected from a direct bond to E, H, F, Cl, Br, NO2, CN, COOR1, NH2, (C1-C5)alkyl, (C1-C5)alkoxy or together are a benzo ring fused to with the proviso that one, but only one, of R4 and R5 may be a direct bond to E; andE is an extender arm, where E provides a stable chain of 2-60 atoms selected from carbon, oxygen, nitrogen and sulfur which covalently links together and distances the groups L and X.