公开(公告)号：EP4361159A1

公开(公告)日：2024-05-01

申请号：EP22828062.4

申请日：2022-04-20

申请人： Stella Pharma Corporation

发明人： MURATA,Yusuke ,  TAKENAKA,Hiroshi ,  OHTA,Yoichiro ,  SUDANI,Aya ,  ISHIMURA,Miki ,  SUZUKI,Kensuke ,  KAI,Hiroyuki

IPC分类号： C07F5/02 ,  A61K31/69 ,  A61K41/00 ,  A61K51/00 ,  A61K51/04 ,  A61P35/00

CPC分类号： A61K31/69 ,  A61K41/00 ,  A61K51/00 ,  A61K51/04 ,  A61P35/00 ,  C07F5/02 ,  C07F5/025

摘要： Provided are new compounds that can have the property of being specifically taken up into cancer cells. In the present invention, novel 4-borono-phenylalanine derivatives, borono-phenylalanine derivatives having a heterocyclic skeleton, borono-phenylalanine derivatives having a fused ring structure, or pharmaceutically acceptable salts thereof are prepared. These compounds have the property of being taken up specifically by LAT1 and thus easily taken up specifically by cancer cells in the evaluation of LAT1 and LAT2 selective uptake, and can be conveniently used for neutron capture therapy and the like. A typical example is a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof.

公开(公告)号：EP4223762A1

公开(公告)日：2023-08-09

申请号：EP21891811.8

申请日：2021-11-08

申请人： Stella Pharma Corporation

发明人： MURATA,Yusuke ,  OHTA,Yoichiro ,  TAKENAKA,Hiroshi ,  SUZUKI,Kensuke

IPC分类号： C07F5/02

摘要： A method for producing 4-borono-L-phenylalanine and its intermediates is provided.
The method is for producing a compound represented by formula (II) from a compound represented by formula (I),


wherein, in formulas (I) and (II),
X represents Cl, F, Br, or I, R 1 represents NR 11 R 12 , R 11 represents H or a protective group of an amino group, R 12 represents a protective group of an amino group, R 2 represents COOR 21 , R 21 represents H or a linear or branched C1 to C10 alkyl group or benzyl group, R 3 represents H or COOR 31 , and R 31 represents a linear or branched C1-C10 alkyl group or a benzyl group; R 4 represents either boronic acid (B(OH) 2 ), boronic acid ester or boronic acid amide;
Provided is a method of production comprising: a first step in which a compound represented by formula (I) reacts with a linear or branched C1-C10 alkylmagnesium halide in the presence of a metal halide; and a second step in which a boronic acid ester or boronic acid amide reacts with the compound obtained in said first step.