公开(公告)号：US20150336876A1

公开(公告)日：2015-11-26

申请号：US14761897

申请日：2014-01-21

Applicant: OSAKA UNIVERSITY ,  KNC LABORATORIES CO., LTD.

Inventor： Yoshikatsu KANAI ,  Shushi NAGAMORI ,  Yoshihiko KITAURA ,  Masahiro NEYA ,  Naohiro MATSUSHITA

IPC: C07C217/48 ,  C07D333/20 ,  C07D277/28 ,  C07C217/72 ,  C07D215/233 ,  C07D213/68 ,  C07C255/54 ,  C07C255/37 ,  C07D215/26 ,  C07D209/48 ,  C07D401/12 ,  C07D409/06 ,  C07D405/06 ,  C07D417/06 ,  C07D413/06 ,  C07C271/16

CPC classification number: C07C217/48 ,  C07C211/09 ,  C07C217/04 ,  C07C217/72 ,  C07C255/37 ,  C07C255/54 ,  C07C271/16 ,  C07C271/20 ,  C07C317/22 ,  C07C317/28 ,  C07C323/20 ,  C07C323/25 ,  C07D209/48 ,  C07D213/68 ,  C07D215/22 ,  C07D215/233 ,  C07D215/26 ,  C07D263/32 ,  C07D277/28 ,  C07D295/08 ,  C07D307/52 ,  C07D333/20 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D409/06 ,  C07D413/04 ,  C07D413/06 ,  C07D417/04 ,  C07D417/06

Abstract: The invention provides a compound having a selective inhibitory activity against highly-expressed LAT-1 in tumor cell. The compound is represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, and a LAT-1 inhibitor comprising the same.

Abstract translation: 本发明提供对肿瘤细胞中高表达LAT-1具有选择性抑制活性的化合物。 化合物由式（I）表示：其中每个符号如说明书中所定义，或其盐，和含有该化合物的LAT-1抑制剂。

公开(公告)号：US20160038620A1

公开(公告)日：2016-02-11

申请号：US14766826

申请日：2014-02-10

Applicant: OSAKA UNIVERSITY ,  NARD INSTITUTE, LTD.

Inventor： Shushi NAGAMORI ,  Yoshikatsu KANAI ,  Hidekazu NAKAO ,  Tokutaro OGATA

IPC: A61K51/04 ,  C07C309/73 ,  C07C229/36

CPC classification number: A61K51/0402 ,  C07B2200/05 ,  C07C229/36 ,  C07C309/73 ,  C07C323/63 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D295/096

Abstract: A compound having a structure represented by the general formula (I): (wherein n is 0 or 1; R1 represents a hydrogen atom (only if n=0), a halogen atom, a C1-C6 alkyl group, a C1-C6 haloalkyl group, an optionally substituted amino group, an optionally substituted phenyl group, a C1-C6 alkylthio group, a C1-C6 alkoxy group, a C1-C6 haloalkoxy group or a C7-C12 aralkyloxy group; R2 represents —(CH2)p—[O(CH2)q]r—X (wherein X is a halogen atom, p is an integer of 1 to 6, q is an integer of 1 to 4, and r is an integer of 0 to 4); R3 represents a hydrogen atom, a C1-C6 alkyl group, a C7-C16 aralkyl group or a C6-C14 aryl group; and R4 represents a hydrogen atom or a C1-C6 alkyl group), or a pharmaceutically acceptable salt thereof excels FAMT in terms of the tendency to accumulate intensively in cancer, the affinity for LAT1 and the selectivity for cancer, and can be labeled using an automated synthesizer in clinical settings, and therefore is useful as a highly versatile PET imaging agent.

Abstract translation: 具有由通式（I）表示的结构的化合物：其中n为0或1; R1表示氢原子（仅n = 0），卤素原子，C1-C6烷基，C1-C6 卤代烷基，任选取代的氨基，任选取代的苯基，C 1 -C 6烷硫基，C 1 -C 6烷氧基，C 1 -C 6卤代烷氧基或C 7 -C 12芳烷氧基; R 2表示 - （CH 2）p - [O（CH 2）q] r -X（其中X是卤素原子，p是1至6的整数，q是1至4的整数，r是0至4的整数）; R 3表示 氢原子，C1-C6烷基，C7-C16芳烷基或C6-C14芳基; R4表示氢原子或C1-C6烷基）或其药学上可接受的盐优于FAMT 在癌症中积聚的趋势，对LAT1的亲和力和对癌症的选择性，并且可以在临床环境中使用自动合成仪进行标记，因此可用作高度通用的PET成像 绅士