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公开(公告)号：US09815855B2
公开(公告)日：2017-11-14
申请号：US15122118
申请日：2015-01-28
Inventor： Hiroshi Takenaka , Yoichiro Ohta , Yusuke Taguchi , Sayuri Ueda , Yuko Ishino , Tomohiro Yoshikawa , Hideki Nakashima , Kohki Uehara , Mitsunori Kirihata
CPC classification number: C07F5/025 , C07B59/00 , C07B59/004 , C07B2200/05 , C07C45/63 , C07C47/55
Abstract: 18F-labeled 4-boronophenylalanine (BPA) can be produced by preparing and further processing a precursor of 18F-labeled BPA represented by the following formula: in which 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).
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12.发明申请公开(公告)号：US20170283441A1
公开(公告)日：2017-10-05
申请号：US15625909
申请日：2017-06-16
Inventor： Hiroshi Takenaka , Yoichiro Ohta , Yusuke Taguchi , Sayuri Ueda , Yuko Ishino , Tomohiro Yoshikawa , Hideki Nakashima , Kohki Uehara , Mitsunori Kirihata
IPC: C07F5/02 , C07C251/24 , C07C271/22 , C07C229/36
CPC classification number: C07F5/027 , C07C229/36 , C07C251/24 , C07C271/22 , Y02P20/55
Abstract: The present invention involves preparing compounds represented by the following formula: from a compound of the following formula: In these formulae: R1 represents a Br group, an iodine group, a Cl group, an NO2 group, or an NH2 group; R2 represents a halogen group, an NO2 group, an NH2 group, Sn(R6)3, N═N—NR7R8, OSO2R9, N R10R11, phenyliodonium, a heterocyclic group iodine, boric acid, or a borate ester; R30 represents a protective group PG1; R40 or R50 represent hydrogen, a protective group PG2, or C6H5(C6H5)C═N, in which NR40R50 are together.
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公开(公告)号：US20230416280A1
公开(公告)日：2023-12-28
申请号：US18252305
申请日：2021-11-08
Applicant: STELLA PHARMA CORPORATION
Inventor： Yusuke MURATA , Yoichiro OHTA , Hiroshi TAKENAKA , Kensuke SUZUKI
IPC: C07F5/02
CPC classification number: C07F5/025
Abstract: A method for producing 4-borono-L-phenylalanine and its intermediates is provided. The method is for producing a substituted phenyl compound represented by formula (II) from a substituted phenyl compound represented by formula (I). The method comprises a first step in which the 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. The method also can comprise a step of deprotecting the compound of formula (II) obtained in the second step.
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14.发明申请公开(公告)号：US20220296715A1
公开(公告)日：2022-09-22
申请号：US17753654
申请日：2020-09-09
Applicant: Stella Pharma Corporation
Inventor： Yoshiya Iguchi , Yoshimitsu Katakuse , Hideki Nakashima
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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公开(公告)号：US20220280540A1
公开(公告)日：2022-09-08
申请号：US17753658
申请日：2020-09-09
Applicant: Stella Pharma Corporation
Inventor： Yoshiya Iguchi , Yoshimitsu Katakuse , Hideki Nakashima
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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Patent Agency Ranking
公开(公告)号：US20190177341A1
公开(公告)日：2019-06-13
申请号：US16320989
申请日：2017-07-20
Inventor： Yoshihide Hattori , Kohki Uehara , Mitsunori Kirihata
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; —R1 represents —(CH2)n-X1—R3 (n represents an integer of 0 to 6; X1 represents O, S, NH, S—S, O—CO, NHCO or SCO, or does not exist; R3 represents C6-C20 alkyl, hydroxy C6-C20 alkyl, amino C6-C20 alkyl, azido C6-C20 alkyl, hydroxycarbonyl C6-C20 alkyl, or the like), or a group having a repeating sequence of —(CH2)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 —R2 is —(CH2)m-X2—R4 (m represents an integer from 0 to 8; X2 represents O, S, NH, S—S, O—CO, NHCO or SCO, or does not exist; and R4 represents a tumor recognition moiety), or does not existare prepared and used.
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17.发明申请METHOD FOR PRODUCING 4-BORONO-L-PHENYLALANINE HAVING 18F ATOM INTRODUCED THEREINTO, AND PRECURSOR OF 4-BORONO-L-PHENYLALANINE HAVING 18F ATOM INTRODUCED THEREINTO 有权生产具有18F原子的4-溴硼酸-L-苯乙胺的方法，以及具有18F原子的4-溴硼酸 - 苯甲酰胺的前体公开(公告)号：US20170015684A1
公开(公告)日：2017-01-19
申请号：US15122118
申请日：2015-01-28
Inventor： Hiroshi TAKENAKA , Yoichiro OHTA , Yusuke TAGUCHI , Sayuri UEDA , Yuko ISHINO , Tomohiro YOSHIKAWA , Hideki NAKASHIMA , Kohki UEHARA , Mitsunori KIRIHATA
CPC classification number: C07F5/025 , C07B59/00 , C07B59/004 , C07B2200/05 , C07C45/63 , C07C47/55
Abstract: 18F-labeled 4-boronophenylalanine (BPA) can be produced by preparing and further processing a precursor of 18F-labeled BPA represented by the following formula: in which 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：一种制备18 F-标记的4-硼苯丙氨酸（BPA）的新方法; 和18 F标记的BPA的前体。 可以通过制备由式（1）表示的化合物并使用该化合物来制备18 F-标记的BPA。 式中，R1表示溴基，碘基，氟原子，二氮杂硼烷衍生物，BX3-或BX3-M +（式中，X表示卤素原子，M +表示一价单原子阳离子，多原子阳离子或络合物 阳离子）。
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18.发明申请CHIRAL 4-BORONOPHENYLALANINE (BPA) DERIVATIVE AND METHOD FOR PRODUCING SAME, AND METHOD FOR PRODUCING 18F-LABELED BPA USING SAID DERIVATIVE 有权化学式4-BORONOPHENYLALANINE（BPA）衍生物及其生产方法，以及使用合适的衍生物生产18F标记的BPA的方法公开(公告)号：US20150329564A1
公开(公告)日：2015-11-19
申请号：US14435678
申请日：2013-10-08
Inventor： Hiroshi TAKENAKA , Yoichiro OHTA , Yusuke TAGUCHI , Sayuri UEDA , Yuko ISHINO , Hideki NAKASHIMA , Kohki UEHARA , Mitsunori KIRIHATA
IPC: C07F5/02 , C07C229/08
CPC classification number: C07F5/025 , C07B59/001 , C07C229/08 , C07C229/36 , C07C251/24 , C07C271/22 , C07F5/027 , C07F5/04 , Y02P20/55
Abstract: Provided are: a novel chiral 4-boronophenylalanine (BPA) derivative; a method for producing the derivative; and a method for producing 18F-2-fluoro-4-borono-L-phenylalanine (18F-labeled BPA; 18F-BPA) using the derivative. A compound represented by formula (1) is prepared. In the formula, R represents BR3R4, BX3− or BX3−M+ (wherein X represents a halogen atom, and M+ represents a monovalent monoatomic cation, a polyatomic cation or a complex cation); R1 represents a hydrogen atom or a protecting group PG1; R2 represents a hydrogen atom or a protecting group PG2; R3 and R4 independently represent OH, or R3, R4 and B together form a ring that serves as a protecting group; and Y represents a halogen atom, NO2, NH2, Sn(R6)3, N═N—NR7R8, OSO2R9, NR10R11, a substituted or unsubstituted phenyliodo group or a substituted or unsubstituted heterocyclic iodo group. The compound is reacted with a fluorination reagent to prepare 18F-labeled BPA.
Abstract translation: 提供：新型手性4-硼苯丙氨酸（BPA）衍生物; 一种制备衍生物的方法; 以及使用该衍生物制备18F-2-氟-4-硼羟-L-苯丙氨酸（18F标记的BPA; 18F-BPA）的方法。 制备由式（1）表示的化合物。 在该式中，R表示BR 3 R 4，BX 3 - 或BX 3 -M +（其中X表示卤原子，M +表示一价单原子阳离子，多原子阳离子或络合阳离子）。 R1表示氢原子或保护基PG1; R2表示氢原子或保护基PG2; R3和R4独立地表示OH，或R3，R4和B一起形成用作保护基的环; Y表示卤素原子，NO 2，NH 2，Sn（R 6）3，N = N-NR 7 R 8，OSO 2 R 9，NR 10 R 11，取代或未取代的苯基碘基或取代或未取代的杂环碘基。 使化合物与氟化试剂反应以制备18F标记的BPA。
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19.发明授权公开(公告)号：US08940862B2
公开(公告)日：2015-01-27
申请号：US13857752
申请日：2013-04-05
Applicant: Koji Kawakami , Stella Pharma Corporation
Inventor： Koji Kawakami , Masayuki Kohno , Tomohisa Horibe , Oumi Nakajima , Mari Haramoto , Liying Yang
IPC: A61K38/00 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , C12P21/06 , C12N1/20 , C12N15/00 , C12N5/00 , C12N5/02 , C12N15/74 , A61P35/00 , C07H21/04 , C07K7/08 , A61K47/48 , C07K14/475 , C07K14/485 , C07K14/54 , C07K7/06 , C07K14/00
CPC classification number: C07K7/08 , A61K47/6425 , C07K14/475 , C07K14/485 , C07K14/54 , C07K2319/33 , C07K2319/55
Abstract: It is an object of the present invention to provide a substance usable as an anticancer agent or DDS, which has intracellular stability, which is capable of evading side effects from functional disorder with respect to normal cells, or which has instantaneous effect. The inventors developed a novel chimeric peptide targeting cancer cells which overexpress EGFR or the like using a binding peptide such as a peptide sequence binding to EGFR, and a lytic peptide sequence, thereby solving such an object. Particularly, by using a chimeric peptide including an EGF receptor-binding peptide or the like and a cytotoxic peptide, this object was solved.
Abstract translation: 本发明的目的是提供一种可以作为抗癌剂或DDS的物质，其具有细胞内稳定性，其能够逃避相对于正常细胞的功能障碍的副作用或具有瞬时作用。 本发明人开发了使用结合肽如结合EGFR的肽序列和裂解肽序列过表达EGFR等的靶向癌细胞的新型嵌合肽，从而解决了这样的问题。 特别地，通过使用包含EGF受体结合肽等的嵌合肽和细胞毒素肽，解决了该目的。
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公开(公告)号：US20210040244A1
公开(公告)日：2021-02-11
申请号：US16963864
申请日：2019-02-19
Applicant: TOKYO INSTITUTE OF TECHNOLOGY , STELLA PHARMA CORPORATION
Inventor： Nobuhiro NISHIYAMA , Takahiro NOMOTO , Yukiya INOUE , Ying YAO , Kaito KANAMORI , Hiroyasu TAKEMOTO , Makoto MATSUI , Keishiro TOMODA
Abstract: The present invention pertains to: a p-boronophenylalanine derivative that comprises a polymer to which a group represented by formula (I) is linked directly or via a linker; a composition containing same; and a kit for producing said derivative and composition.
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