| 主权项 |
1. An imaging agent which comprises an 18F-labelled compound of Formula I: where:X1, X2 and X3 are independently Br, Cl, 19F or 18F, with the proviso that at least one of X1, X2 and X3 is 18F;M is Al3+, Ga3+, In3+, Sc3+, Y3+, Ho3+, Er3+, Tm3+, Yb3+ or Lu3+;Z1 is a tridentate triamine chelating agent wherein all 3 amine donors are bound to M, wherein Z1 has at least one Y group, and optionally also a Q group covalently conjugated thereto;p is 1, 2 or 3;y is 0 or 1;Y is independently -(A1)x-Y1 or -(A1)x-Y1-Q where each A1 is independently —CH2— or —O—, provided that Y does not comprise any —O—O— bonds;
wherein x is an integer of value 1 to 6; and Y1 is —NHRa, —NH(CH2)2NHRa, —NH(CH2)3NHRa, —(C═O)NHRa, —NH(C═O)Ra, —NH(C═NH)NHRa, —ORa, a Y2 group or a Y3 group; Y2 is: Y3 is Arg, Lys, Asn, Gln, Ser, Thr or Tyr; wherein Ra is independently H, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C2-4 alkoxyalkyl or C1-4 hydroxyalkyl; and wherein each R1 is independently C1-4 alkyl, C2-4 alkoxyalkyl or C1-4 hydroxyalkyl; and R2 is independently H, C1-4 alkyl or Si(C1-4 alkyl)3;Q is -L-[BTM];L is a synthetic linker group of formula -(A)m- wherein each A is independently —CR2—, —CR═CR—, —C≡C—, —CR2CO2—, —CO2CR2—, —NRCO—, —CONR—, —CR═N—O—, —NR(C═O)NR—, —NR(C═S)NR—, —SO2NR—, —NRSO2—, —CR2OCR2—, —CR2SCR2—, —CR2NRCR2—, a C4-8 cycloheteroalkylene group, a C4-8 cycloalkylene group, —Ar—, —NR—Ar—, —O—Ar—, —Ar—(CO)—, an amino acid, a sugar or a monodisperse polyethyleneglycol (PEG) building block,
wherein each R is independently chosen from H, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C2-4 alkoxyalkyl or C1-4 hydroxyalkyl; m is an integer of value 1 to 20;each Ar is independently a C5-12 arylene group, or a C3-12 heteroarylene group;BTM is a biological targeting moiety. |
