| 摘要 |
PCT No. PCT/CA95/00249 Sec. 371 Date Mar. 20, 1996 Sec. 102(e) Date Mar. 20, 1996 PCT Filed Apr. 28, 1995 PCT Pub. No. WO96/03427 PCT Pub. Date Feb. 8, 1996For use in imaging sites of diagnostic interest within the body, the present invention provides radionuclide chelators of formula (I), wherein X is a linear or branched, saturated or unsaturated C1-4alkyl chain that is optionally interrupted by one or two heteroatoms selected from N, O and S; and is optionally substituted by at least one group selected from halogen, hydroxyl, amino, carboxyl C1-4alkyl, aryl and C(O)Z; Y is H or a substituent defined by X; X and Y may together form a 5- to 8-membered saturated or unsaturated heterocyclic ring optionally substituted by at least one group selected from halogen, hydroxyl, amino, carboxyl oxo, C1-4alkyl, aryl and C(O)Z; R1 through R4 are selected independently from H; carboxyl; C1-4alkyl; C1-4alkyl substituted with a group selected from hydroxyl, amino, sulfhydryl, halogen, carboxyl, C1-4alkoxycarbonyl and aminocarbonyl; an alpha carbon side chain of a D- or L-amino acid other than proline; and C(O)Z; R5 and R6 are selected independently from H; carboxyl; amino; C1-4alkyl; C1-4alkyl substituted by hydroxyl, carboxyl or amino; and C(O)Z; R7 is selected from H and a sulfur protecting group; and Z is selected from hydroxyl, C1-4alkoxy and a targeting molecule.
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