| 摘要 |
<p>The present invention is related to a conjugate comprising a structure of general formula (I)
€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ[TM1] - [AD1] - [LM] - [AD2] - [TM2]€ƒ€ƒ€ƒ€ƒ€ƒ(I),
wherein
TM1 is a first targeting moiety, wherein the first targeting moiety is capable of binding to a first target,
AD1 is a first adapter moiety or is absent,
LM is a linker moiety or is absent,
AD2 is a second adapter moiety or is absent, and
TM2 is a second targeting moiety, wherein the second targeting moiety is capable of binding to a second target;
wherein the first targeting moiety and/or the second targeting moiety is a compound of formula (II):
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 (III)
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
R7 is a bond;
or a pharmacologically acceptable salt, solvate or hydrate thereof.</p> |
