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1. 发明申请

WO2014086499A1 NEUROTENSIN RECEPTOR LIGANDS 审中-公开
标题翻译：神经降压素受体配体
公开(公告)号：WO2014086499A1
公开(公告)日：2014-06-12
申请号：PCT/EP2013003700
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 , A61K31/415 , A61K51/04 , C07D403/12
CPC分类号： C07D231/14 , A61K51/0482 , C07D403/12
摘要： The present invention is related to a compound of formula (I) 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, (C3-C8)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 formula (II) wherein ALK' is (C2-C5)alkylidene; R6 is selected from the group consisting of hydrogen and (C1-C4)alkyl; and R7 is selected from the group consisting of H and an Effector moiety; or a pharmacologically acceptable salt, solvate or hydrate thereof.
摘要翻译：本发明涉及式（I）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中的一个是式（II），其中ALK'是（C2-C5）亚; R6选自氢和（C1-C4）烷基; 并且R 7选自H和效应器部分; 或其药理学可接受的盐，溶剂化物或水合物。

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