申请人:3B PHARMACEUTICALS GMBH
公开号:US20170119913A1
公开(公告)日:2017-05-04
The present invention is related to a conjugate comprising a structure of general formula (1) [TM1]-[AD1]-[LM]-[AD2]-[TM2] (1), 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 (2): 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 (3) wherein ALK′ is (C
2
-C
5
)alkylidene; R
6
is selected from the (2) group consisting of hydrogen and (C
1
-C
4
)alkyl; and R
7
is a bond; or a pharmacologically acceptable salt, solvate or hydrate thereof.