Patent ID: 8945510
Filing Date: 2015-02-03
Classification: A61K,C07B

Abstract:
1. A radiolabeled glutaminyl cyclase (QC) inhibitor for use as an imaging agent, comprising: a radiolabel selected from the group consisting of 2 H (D or deuterium), 3 H (T or tritium), 11 C, 14 C, 13 N, 15 N, 15 O, 17 O, 18 O, 18 F, 35 S, 36 Cl, 82 Br, 75 Br, 76 Br, 77 Br, 123 I, 124 I, 125 I, and 131 I: and a QC inhibitor compound of formula (I), or a pharmaceutically acceptable salt, including all tautomers and stereoisomers thereof; wherein R in which any of aforesaid heteroaryl groups may optionally be substituted by one or more groups selected from C and in which any of aforesaid carbocyclyl groups may optionally be substituted by one or more groups selected from C R in which any of aforesaid aryl and heteroaryl groups may optionally be substituted by one or more groups selected from C and in which any of aforesaid carbocyclyl and heterocyclyl groups may optionally be substituted by one or more groups selected from C or R in which any of aforesaid phenyl, benzyloxy and heteroaryl groups may optionally be substituted by one or more groups selected from C R in which aforesaid aryl may optionally be substituted by one or more groups selected from C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, —C 1-6 thioalkyl, —SOC 1-4 alkyl, —SO 2 C 1-4 alkyl, C 1-6 alkoxy-, —O—C 3-8 cycloalkyl, C 3-8 cycloalkyl, —SO 2 C 3-8 cycloalkyl, —SOC 3-6 cycloalkyl, C 3-6 alkenyloxy-, C 3-6 alkynyloxy-, —C(O)C 1-6 alkyl, —C(O)OC 1-6 alkyl, C 1-6 alkoxy-C 1-6 alkyl-, nitro, halogen, cyano, hydroxyl, —C(O)OH, —NH 2 , —NHC 1-4 alkyl, —N(C 1-4 alkyl)(C 1-4 alkyl), —C(O)N(C 1-4 alkyl)(C 1-4 alkyl), —C(O)NH 2 , —C(O)NH(C 1-4 alkyl) and, —C(O)N H(C 3-10 cycloalkyl); or R or R or R X represents C═O, O, S, CR Y represents CHR Z represents —N—R or X and Z represent two adjacent carbon atoms of a phenyl ring which is fused in that position and which is optionally substituted by one or more halogen or C R R in which said aforesaid aryl may be optionally substituted by C R provided that the moiety —Y—Z—X— represents a moiety other than —C(═O)—N(—R