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    NEUROTENSIN RECEPTOR LIGANDS
    11.
    发明公开
    NEUROTENSIN RECEPTOR LIGANDS 审中-公开
    神经降压素，REZEPTORLIGANDEN

    公开(公告)号：EP2928870A1

    公开(公告)日：2015-10-14

    申请号：EP13814827.5

    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 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.

    摘要翻译： 本发明涉及式（I）的神经降压素受体拮抗剂：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; R 2选自（C 1 -C 6）烷基，（C 3 -C 8）环烷基，（C 3 -C 8）环烷基甲基，卤素，硝基和三氟甲基; ALK是（C 2 -C 5）亚烷基; R 3，R 4和R 5各自独立地选自氢和（C 1 -C 4）烷基，条件是R 3，R 4和R 5之一为下式（II） 其中ALK'是（C 2 -C 5）亚烷基; R 6选自氢和（C 1 -C 4）烷基; 并且R 7选自H，受体， - [受体 - 效应物]， - [接头 - 受体]和 - [接头 - 受体 - 效应物]，其中受体是介导效应物与 式（II）的N原子或其介导效应物与连接子的连接，效应子选自包含诊断活性剂和治疗活性剂的组，连接子是将受体与N（式 II）， - [受体效应剂]是效应物与受体复合或共价结合的部分， - [接头 - 受体]是连接子与受体结合的部分，和 - [接头 - 受体 - 效应物 ]是连接子与受体结合的部分，其中效应物与受体复合或共价结合; 或其药理学上可接受的盐，溶剂合物或水合物。