公开(公告)号：US20170015684A1

公开(公告)日：2017-01-19

申请号：US15122118

申请日：2015-01-28

Applicant: STELLA PHARMA CORPORATION ,  OSAKA PREFECTURE UNIVERSITY PUBLIC CORPORATION

Inventor： Hiroshi TAKENAKA ,  Yoichiro OHTA ,  Yusuke TAGUCHI ,  Sayuri UEDA ,  Yuko ISHINO ,  Tomohiro YOSHIKAWA ,  Hideki NAKASHIMA ,  Kohki UEHARA ,  Mitsunori KIRIHATA

IPC: C07F5/02 ,  C07B59/00 ,  C07C47/55 ,  C07C45/63

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）。

公开(公告)号：US20150329564A1

公开(公告)日：2015-11-19

申请号：US14435678

申请日：2013-10-08

Applicant: Stella Pharma Corporation ,  Osaka Prefecture University Public Corporation

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。

公开(公告)号：US20220354875A1

公开(公告)日：2022-11-10

申请号：US17636246

申请日：2020-09-11

Applicant: STELLA PHARMA CORPORATION

Inventor： Yoshiya IGUCHI ,  Yoshimitsu KATAKUSE ,  Hideki NAKASHIMA

IPC: A61K31/69 ,  A61K41/10 ,  A61J1/10 ,  A61J1/14

Abstract: The present invention relates to a pharmaceutical composition comprising a liquid composition containing p-boronophenylalanine, in which the liquid composition is accommodated in a packaging material and satisfies the following Condition I or Condition II: Condition I: the liquid composition comprises substantially no antioxidant and a concentration of dissolved oxygen in the liquid composition is 3.5 ppm or less; Condition II: the liquid composition comprises an antioxidant and a concentration of dissolved oxygen in the liquid composition is 3.0 ppm or less.