| 摘要 |
The present invention is related to neurotensin receptor antagonists of formula (I):
wherein
R 1 is selected from the group consisting of hydrogen, methyl and cyclopropylmethyl;
AA-COOH is an amino acid selected from the group consisting of 2-amino-2-adamantane carboxylic acid, cyclohexylglycine and 9-amino-bicyclo[3.3.1]nonane-9-carboxylic acid;
R 2 is selected from the group consisting of (C 1 -C 6 )alkyl, (C 3 -C 8 )cycloalkyl, (C 3 -C 8 )cycloalkylmethyl, halogen, nitro and trifluoromethyl;
ALK is (C 2 -C 5 )alkylidene;
R 3 , R 4 and R 5 are each and independently selected from the group consisting of hydrogen and (C 1 -C 4 )alkyl under the proviso that one of R 3 , R 4 and R 5 is of the following formula (II)
wherein
ALK' is (C 2 -C 5 )alkylidene;
R 6 is selected from the group consisting of hydrogen and (C 1 -C 4 )alkyl; and
R 7 is selected from the group comprising H, Acceptor, -[Acceptor-Effector], -[Linker-Acceptor], and -[Linker-Acceptor-Effector], wherein Acceptor is a moiety which mediates linking of an Effector to the N atom of formula (II) or which mediates linking of the Effector to the Linker,
Effector is selected from the group comprising a diagnostically active agent and a therapeutically active agent,
Linker is a moiety which links the Acceptor to the N atom of formula (II),
-[Acceptor-Effector] is a moiety where the Effector is complexed or covalently bound to the Acceptor,
-[Linker-Acceptor] is a moiety where the Linker is conjugated to the Acceptor, and
-[Linker-Acceptor-Effector] is a moiety where the Linker is conjugated to the Acceptor, whereby the Effector is complexed or covalently bound to the Acceptor;
or a pharmacologically acceptable salt, solvate or hydrate thereof. |
