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    NEUROTENSIN RECEPTOR LIGANDS
    6.
    发明公开
    NEUROTENSIN RECEPTOR LIGANDS 审中-公开

    公开(公告)号：EP3712131A1

    公开(公告)日：2020-09-23

    申请号：EP20166422.4

    申请日：2013-12-06

    申请人： 3B Pharmaceuticals GmbH

    发明人： OSTERKAMP, Frank ,  SMERLING, Christiane ,  REINEKE, Ulrich ,  HAASE, Christian ,  UNGEWIß, Jan

    IPC分类号： C07D231/14 ,  C07D403/12 ,  A61K31/415 ,  A61K51/04

    摘要： The present invention is related to a compound 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 (Ci-C4)alkyl under the proviso that one of R 3 , R 4 and R 5 is of the 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 consisting of H and an Effector moiety; or a pharmacologically acceptable salt, solvate or hydrate thereof.

    CONJUGATE COMPRISING A NEUROTENSIN RECEPTOR LIGAND AND USE THEREOF
    10.
    发明公开
    CONJUGATE COMPRISING A NEUROTENSIN RECEPTOR LIGAND AND USE THEREOF 审中-公开
    包含神经降压素受体配体的共轭物及其用途

    公开(公告)号：EP3154638A1

    公开(公告)日：2017-04-19

    申请号：EP15730392.6

    申请日：2015-06-10

    申请人： 3B Pharmaceuticals GmbH

    发明人： OSTERKAMP, Frank ,  HAASE, Christian ,  REINEKE, Ulrich ,  SMERLING, Christiane ,  PASCHKE, Matthias ,  UNGEWIß , Jan

    IPC分类号： A61P35/00 ,  A61K47/50

    CPC分类号： A61K51/0482 ,  A61K31/337 ,  A61K47/545 ,  A61K47/555 ,  A61K47/557 ,  A61K47/585 ,  A61K47/68 ,  A61K49/0043 ,  A61K51/04 ,  A61K51/0497 ,  A61K51/088

    摘要： 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.

    摘要翻译： 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是第一衔接头部分或不存在，LM是接头部分或不存在，AD2是第二衔接头部分或不存在，并且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 - 二环[3.3.1]壬烷-9羧酸的氨基酸; R2选自（C1-C6）烷基，（C3-C8）环烷基，（C3-C8）环烷基甲基，卤素，硝基和三氟甲基; ALK'是（C 2 -C 5）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中的一个具有下式（3），其中ALK'是（C2-C5 ）亚烷基; R6选自氢和（C1-C4）烷基; R7是一个键; 或其药理学可接受的盐，溶剂化物或水合物。