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

公开(公告)号：US20140187814A1

公开(公告)日：2014-07-03

申请号：US14141721

申请日：2013-12-27

Applicant: NARD Institute, Ltd.

Inventor： Hidekazu NAKAO ,  Junichi HOSHINO ,  Tokutaro OGATA ,  Naoki MIYASHITA ,  Yoshikazu YAMAMOTO

IPC: C07C229/36 ,  C07C227/16

CPC classification number: C07C229/36 ,  C07C227/16 ,  C07C271/22 ,  Y02P20/55

Abstract: The objective of the present invention is to provide a tyrosine derivative which is useful as a melatonin MT1 receptor antagonist, and a method for producing a specific tyrosine derivative with high yield by efficiently introducing an iodine atom at the para position of the phenolic hydroxy group in the benzene ring of tyrosine with good regioselectivity. The tyrosine derivative of the present invention is characterized in being represented by the following formula (I): wherein R1 is a protective group of the amino group and the like; R2 is a protective group of the carboxy group and the like; R3 is a hydrogen atom and the like; R4 is a halogen atom and the like; A is —(CH2)l—[Z(CH2)m]n—; X is a leaving group.

Abstract translation: 本发明的目的是提供可用作褪黑激素MT1受体拮抗剂的酪氨酸衍生物，以及通过在酚羟基的对位有效引入碘原子而以高产率制备特异性酪氨酸衍生物的方法 酪氨酸苯环具有良好的区域选择性。 本发明的酪氨酸衍生物的特征在于由下式（I）表示：其中R1是氨基的保护基等; R2是羧基等的保护基; R3是氢原子等; R4是卤素原子等; A是 - （CH 2）1 - [Z（CH 2）m] n - X是离职小组。