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    • 4. 发明申请
    • CONJUGATE COMPRISING A NEUROTENSIN RECEPTOR LIGAND AND USE THEREOF
    • 包含神经递质受体配体并与其一起使用
    • WO2015188934A8
    • 2016-11-24
    • PCT/EP2015001166
    • 2015-06-10
    • 3B PHARMACEUTICALS GMBH
    • OSTERKAMP FRANKHAASE CHRISTIANREINEKE ULRICHSMERLING CHRISTIANEPASCHKE MATTHIASUNGEWIΒ JAN
    • A61P35/00A61K47/48
    • A61K51/0482A61K31/337A61K47/48061A61K47/48146A61K47/48184A61K47/48369A61K47/545A61K47/555A61K47/557A61K47/585A61K47/68A61K49/0043A61K51/04A61K51/0497A61K51/088
    • 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 R1 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; R2 is selected from the group consisting of (C1-C6)alkyl, (C3-C8)cycloalkyl, (C3C8)cycloalkylmethyl, halogen, nitro and trifluoromethyl; ALK' is (C2-C5)alkylidene; R3, R4 and R5 are each and independently selected from the group consisting of hydrogen and (C1-C4)alkyl under the proviso that one of R3, R4 and R5 is of the following formula (3) wherein ALK' is (C2-C5)alkylidene; R6 is selected from the group consisting of hydrogen and (C1-C4)alkyl; and R7 is a bond; or a pharmacologically acceptable salt, solvate or hydrate thereof.
    • 本发明涉及包含通式(1)[TM1] - [AD1] - [LM] - [AD2] - [TM2](1)的结构的缀合物,其中TM1是第一靶向部分,其中 第一靶向部分能够结合第一靶标,AD1是第一接头部分或不存在,LM是接头部分或不存在,AD2是第二接头部分或不存在,而TM2是第二靶向部分,其中 第二靶向部分能够结合第二靶标; 其中所述第一靶向部分和/或所述第二靶向部分是式(2)的化合物:其中R 1选自氢,甲基和环丙基甲基; AA-COOH是选自2-氨基-2-金刚烷羧酸,环己基甘氨酸和9-氨基 - 双环[3.3.1]壬烷-9羧酸的氨基酸; R2选自(C1-C6)烷基,(C3-C8)环烷基,(C3C8)环烷基甲基,卤素,硝基和三氟甲基; ALK'为(C2-C5)亚烷基; R3,R4和R5各自独立地选自氢和(C1-C4)烷基,条件是R3,R4和R5之一具有下式(3),其中ALK'是(C2-C5 )亚烷基; R 6选自氢和(C 1 -C 4)烷基; 而R7是一个键; 或其药理学上可接受的盐,溶剂合物或水合物。