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公开(公告)号：EP2813513B1
公开(公告)日：2019-07-03
申请号：EP13746354.3
申请日：2013-02-07
Inventor： KIRIHATA,Mitsunori , UEHARA,Kohki
IPC: C07K11/02 , C07C229/08 , C07C235/12 , C07K1/06 , C07K11/00
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公开(公告)号：EP2602261B1
公开(公告)日：2016-10-12
申请号：EP11814640.6
申请日：2011-08-02
Applicant: Stella Pharma Corporation
Inventor： KIRIHATA,Mitsunori , HATTORI,Yoshihide , UEHARA,Kohki , TAKENAKA,Hiroshi
IPC: C07F5/02
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公开(公告)号：EP4501906A1
公开(公告)日：2025-02-05
申请号：EP23780886.0
申请日：2023-03-30
Applicant: Atransen Pharma Ltd. , Stella Pharma Corporation , OSAKA UNIVERSITY
Inventor： KANAI,Yoshikatsu , UEHARA,Kohki , OHTA,Yoichiro , TAKENAKA,Hiroshi , MASUI,Shin
IPC: C07C229/50 , A61K31/136 , A61K31/343 , A61K31/4418 , A61K31/47 , A61K51/00 , A61P35/00 , C07D213/24 , C07D215/20 , C07D307/83 , A61K101/02
Abstract: Provided is a tetrahydronaphthalene derivative that can be used as an LAT1-selective inhibitor and an LAT1-selective substrate. The present invention relates to a compound represented by formula (I) or a pharmaceutically acceptable salt thereof. In formula (I), M represents S, O, NH or the like; R 1C represents any one structure selected from the group consisting of a 5- to 7-membered aromatic heterocyclic group having a substituent, a C5- to 7-membered aromatic cyclic group having a substituent and a substituted or unsubstituted 8- to 16-membered polycyclic group, or the like; and n represents an integer of 0 to 5. The present invention also relates to a composition for treating cancer, a medicine for BNCT, a diagnostic drug for cancer, an LAT1-selective inhibitor, or a composition for enhancing a BNCT effect, each containing the compound or the pharmaceutically acceptable salt thereof.
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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
Applicant: Stella Pharma Corporation
Inventor： MURATA,Yusuke , TAKENAKA,Hiroshi , OHTA,Yoichiro , SUDANI,Aya , ISHIMURA,Miki , SUZUKI,Kensuke , KAI,Hiroyuki
CPC classification number: A61K31/69 , A61K41/00 , A61K51/00 , A61K51/04 , A61P35/00 , C07F5/02 , C07F5/025
Abstract: 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.
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35.发明公开
公开(公告)号：EP4029506A1
公开(公告)日：2022-07-20
申请号：EP20864172.0
申请日：2020-09-09
Applicant: Stella Pharma Corporation
Inventor： IGUCHI,Yoshiya , KATAKUSE,Yoshimitsu , NAKASHIMA,Hideki
Abstract: An object of the present invention is to provide a method for preventing precipitation by storing an injection solution for boron neutron capture therapy. The present invention provides a method for preventing precipitation of an injection solution for boron neutron capture therapy, the injection solution containing p-boronophenylalanine or a pharmaceutically acceptable salt thereof; a sugar alcohol; and a pH adjusting agent, having a pH of 6.5 to 8.0 and an osmotic pressure ratio of 1.0 to 1.8, and being to be administered by intravenous drip injection.
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Patent Agency Ranking
公开(公告)号：EP4029505A1
公开(公告)日：2022-07-20
申请号：EP20863900.5
申请日：2020-09-09
Applicant: Stella Pharma Corporation
Inventor： IGUCHI,Yoshiya , KATAKUSE,Yoshimitsu , NAKASHIMA,Hideki
Abstract: An object of the present invention is to provide an injection solution for boron neutron capture therapy. Provided is an injection solution for boron neutron capture therapy, containing p-boronophenylalanine or a pharmaceutically acceptable salt thereof, with a ratio of boron 10 of boron atoms in a compound of 75 % or more; a sugar alcohol; an antioxidant; and water, the injection solution having a pH of 6.5 to 7.8 and an osmotic pressure ratio of 1.0 to 1.8, the injection solution being to be administered by intravenous drip injection.
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公开(公告)号：EP3492477A1
公开(公告)日：2019-06-05
申请号：EP17834146.7
申请日：2017-07-20
Inventor： HATTORI, Yoshihide , UEHARA, Kohki , KIRIHATA, Mitsunori
Abstract: To provide a novel boron-containing compound. A compound represented by the following formula: wherein black circle represents B, white circles represent B-H; -R 1 represents -(CH 2 )n-X 1 -R 3 (n represents an integer of 0 to 6; X 1 represents O, S, NH, S-S, O-CO, NHCO or SCO, or does not exist; R 3 represents C 6 -C 20 alkyl, hydroxy C 6 -C 20 alkyl, amino C 6 -C 20 alkyl, azido C 6 -C 20 alkyl, hydroxycarbonyl C 6 -C 20 alkyl, or the like), or a group having a repeating sequence of -(CH 2 ) 2 -O- 3 times or more and 10 times or less and having a methyl group or an ethyl group at the end on the oxygen atom side; and -R 2 is - (CH 2 )m-X 2 -R 4 (m represents an integer from 0 to 8; X 2 represents O, S, NH, S-S, O-CO, NHCO or SCO, or does not exist; and R 4 represents a tumor recognition moiety), or does not exist are prepared and used.
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38.发明授权OPTICALLY ACTIVE alpha-AMINO ACID INTO WHICH BSH IS INTRODUCED AND METHOD FOR SYNTHESIZING THE SAME 有权与BSH OFFSET旋光性α-氨基酸与合成方法THEREFOR
公开(公告)号：EP2319850B1
公开(公告)日：2017-03-29
申请号：EP09800426.0
申请日：2009-07-23
Applicant: Stella Pharma Corporation
Inventor： KIRIHATA,Mitsunori , ASANO,Tomoyuki , UEHARA,Kohki , HATTORI,Yoshihide , KUSAKA,Shintaro
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39.发明公开METHOD FOR PRODUCING 4-BORONO-L-PHENYLALANINE HAVING 18F ATOM INTRODUCED THEREINTO, AND PRECURSOR OF 4-BORONO-L-PHENYLALANINE HAVING 18F ATOM INTRODUCED THEREINTO 审中-公开用于生产4硼-L-苯丙氨酸进口它18F原子和4硼-L-苯丙氨酸PRE进口它18F-ATOM
公开(公告)号：EP3112340A1
公开(公告)日：2017-01-04
申请号：EP15754420.6
申请日：2015-01-28
Inventor： TAKENAKA, Hiroshi , OHTA, Yoichiro , TAGUCHI, Yusuke , UEDA, Sayuri , ISHINO, Yuko , YOSHIKAWA, Tomohiro , NAKASHIMA, Hideki , UEHARA, Kohki , KIRIHATA, Mitsunori
Abstract: The purpose of the present invention is to provide: a novel method for producing 18 F-labeled 4-boronophenylalanine (BPA) ; and a precursor of 18 F-labeled BPA. 18 F-labeled BPA can be produced by preparing a compound represented by formula (1) and using the compound. In the formula, R1 represents a bromo group, an iodo group, a fluoro group, a diazaborinane derivative, BX3- or BX3-M+ (wherein X represents a halogen atom; and M+ represents a monovalent monoatomic cation, a polyatomic cation or a complex cation).
Abstract translation: 本发明的目的是提供：一种新的制造方法18 F-标记的4硼 - 苯丙氨酸（BPA）; 和18的前体F-标记的BPA。 18 F-标记的BPA可以通过制备由式（1）表示的化合物和使用该化合物来制备。 在该式中，R 1表示溴基于碘基，氟基，diazaborinane衍生物，BX3-或BX3-M +（worin X表示卤素原子;和M + darstellt一价单原子阳离子，多原子阳离子或复杂 阳离子）。
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40.发明公开OPTICALLY ACTIVE -AMINO ACID INTO WHICH BSH IS INTRODUCED AND METHOD FOR SYNTHESIZING THE SAME 有权麻省理工学院BSH VERSETZTE OPTISCH AKTIVE alpha-AMINOSÄUREUND SYNTHESEVERFAHRENDAFÜR
公开(公告)号：EP2319850A1
公开(公告)日：2011-05-11
申请号：EP09800426.0
申请日：2009-07-23
Applicant: Stella Pharma Corporation
Inventor： KIRIHATA,Mitsunori , ASANOI,Tomoyuki , UEHARA,Kohki , HATTORI,Yoshihide , KUSAKA,Shintaro
Abstract: Disclosed is the method for producing an optically active BSH amino acid, which comprises a step of reacting an optically active α-amino acid derivative having a halogen in a side chain with a cyanoethyl BSH compound represented by formula (1). An optically active BSH amino acid obtained by the method is also disclosed.
Abstract translation: 公开了光学活性BSH氨基酸的制造方法，其包括使侧链上具有卤素的光学活性±氨基酸衍生物与式（1）所示的氰乙基BSH化合物反应的工序。 还公开了通过该方法获得的光学活性BSH氨基酸。
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