| 主权项 |
1. A radiolabeled glutaminylcyclase (QC) inhibitor suitable for use as an imaging agent, wherein:
a) the radiolabel is selected from the group consisting of 2H (D or deuterium), 3H (T or tritium), 11C, 14C, 13N, 15N, 15O, 17O, 18O, 35S, 36Cl, 82Br, 75Br, 76Br, 77Br, 123I, 124I, 125I, and 131I; or b) the radiolabeled inhibitor is a compound of formula (II):or a pharmaceutically acceptable salt thereof, including all tautomers and stereoisomers thereof wherein:
R1 represents —C1-6alkyl, -aryl, —C1-6alkylaryl, -cycloalkyl, —C1-6alkylcycloalkyl, -heteroaryl, —C1-6alkylheteroaryl, -heterocyclyl, —C1-6alkylheterocyclyl, -cycloalkyl substituted by phenyl, -cycloalkyl substituted by phenoxy, -phenyl substituted by cycloalkyl, -phenyl substituted by phenoxy, -phenyl substituted by phenyl, heterocycyl substituted by phenyl, heteroaryl substituted by phenyl, phenyl substituted by heterocyclyl, phenyl substituted by heteroaryl, phenyl substituted by —O-cycloalkyl, or phenyl substituted by -cycloalkyl-heterocyclyl;
in which any of aforesaid aryl, cycloalkyl, heterocyclyl, heteroaryl, phenyl, or phenoxy groups may optionally be substituted by one or more groups selected from C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, —C1-6thioalkyl, —SOC1-4alkyl, —SO2C1-4alkyl, C1-6alkoxy, —O—C3-8cycloalkyl, C3-8cycloalkyl, —SO2C3-8cycloalkyl, —SOC3-6cycloalkyl, C3-6alkenyloxy-, C3-6alkynyloxy-, —C(O)C3-6alkyl, —C(O)OC1-6alkyl, C1-6alkoxy-C1-6alkyl-, nitro, halogen, cyano, hydroxyl, —C(O)OH, —NH2, —NHC1-4alkyl, —N(C1-4alkyl)(C1-4alkyl), —C(O)N(C1-4alkyl)(C1-4alkyl), —C(O)NH2, —C(O)NH(C1-4alkyl), and —C(O)NH(C3-10cycloalkyl); R2 represents —C1-6alkyl, C1-6haloalkyl, -aryl, —C1-6alkylaryl, -cycloalkyl, —C1-6alkylcycloalkyl, -heteroaryl, —C1-6alkylheteroaryl, -heterocyclyl, or —C1-6alkylheterocyclyl;
in which any of aforesaid aryl, heteroaryl or heterocyclyl groups may optionally be substituted by one or more groups selected from C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, —C1-6thioalkyl, —SOC1-4alkyl, —SOC1-4alkyl, C1-6alkoxy-, —O—C3-8cycloalkyl, C3-8cycloalkyl, —SO2C3-8cycloalkyl, —SOC3-8cycloalkyl, C3-6alkenyloxy-, C3-6alkynyloxy-, —C(O)C1-6alkyl, —C(O)OC1-6alkyl, C1-6alkoxy-C1-6 alkyl-, nitro, halogen, cyano, hydroxyl, —C(O)OH, —NH2, —NHC1-4alkyl, —N(C1-6alkyl)(C1-4alkyl), —C(O)N(C1-4alkyl)(C1-4alkyl), —C(O)NH2, —C(O)NH(C1-4alkyl), and —C(O)NH(C3-10cycloalkyl); R3 represents C1-6alkyl or C1-6haloalkyl; n represents an integer selected from 0 to 3; and Ra represents C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, —C1-6thioalkyl, —SOC1-4alkyl, —SO2C1-4alkyl, C1-6alkoxy-, —O—C3-8cycloalkyl, C3-8cycloalkyl, —SO2C3-8cycloalkyl, —SO3-6cycloalkyl, C3-6alkenyloxy-, C3-6alkynyloxy-, —C(O)C1-6alkyl, —C(O)OC1-6alkyl, C1-6alkoxy-C1-6alkyl-, nitro, halogen, cyano, hydroxyl, —C(O)OH, —NH2, —NHC1-4alkyl, —N(C1-4alkyl)(C1-4alkyl), —C(O)N(C1-4alkyl)(C1-4alkyl), —C(O)NH2, —C(O)NH(C1-4alkyl), or —C(O)NH(C3-10cycloalkyl); and the radiolabel is selected from the group consisting of 2H (D or deuterium), 3H (T or tritium), 11C, 14C, 13N, 15N, 15O, 17O, 18O, 35S, 38Cl, 82Br, 75Br, 75Br, 77Br, 123I, 124I, 125I, and 131I. |
