公开(公告)号：EP4317165A1

公开(公告)日：2024-02-07

申请号：EP22775737.4

申请日：2022-03-24

申请人： OSAKA UNIVERSITY

发明人： SHIRAKAMI, Yoshifumi ,  KANEDA, Kazuko ,  KADONAGA, Yuichiro ,  WATABE, Tadashi ,  TOYOSHIMA, Atsushi ,  FUKASE, Koichi ,  SHINOHARA, Atsushi ,  YAMANAKA, Toshio ,  KONDOH, Yutaka

IPC分类号： C07F5/02 ,  A61P35/00 ,  C07B59/00 ,  C07C227/16 ,  C07C229/36 ,  A61K31/198

摘要： The present invention provides a method for producing radiolabeled tyrosine derivatives with good purity and stability, by a safe method suitable for industrial production of pharmaceuticals.
The present invention relates to a method for producing Compound (5) and Radiolabeled Compound (6).

wherein each symbol is as defined in the description.

公开(公告)号：EP4438608A2

公开(公告)日：2024-10-02

申请号：EP24193023.9

申请日：2018-08-03

申请人： Osaka University

发明人： SHIRAKAMI, Yoshifumi ,  IKEDA, Hayato ,  KANAI, Yasukazu ,  SHIMOSEGAWA, Eku ,  HATAZAWA, Jun ,  WATABE, Tadashi ,  KANEDA, Kazuko

IPC分类号： C07F5/02

CPC分类号： C07F5/025 ,  C07B2200/0520130101 ,  C07F13/005 ,  C07B59/004

摘要： The present invention aims to produce a radiolabeled aryl compound by a method that enables an easy labelling with a high radiochemical yield in a short time, and that enables formulation immediately after the labelling.
The present invention relates to a method of producing the radiolabeled aryl compound (I), which comprises reacting the aryl boronic acid compound (II) with a radionuclide selected from 123I, 124I, 125I and 131I, in the presence of an oxidizing agent selected from N-bromosuccinimide and N-chlorosuccinimide, in water.

         Ar-X     (I)

         Ar-Y     (II)

wherein each symbol is as defined in the description.

公开(公告)号：EP4438608A3

公开(公告)日：2024-10-30

申请号：EP24193023.9

申请日：2018-08-03

申请人： Osaka University

发明人： SHIRAKAMI, Yoshifumi ,  IKEDA, Hayato ,  KANAI, Yasukazu ,  SHIMOSEGAWA, Eku ,  HATAZAWA, Jun ,  WATABE, Tadashi ,  KANEDA, Kazuko

IPC分类号： C07F13/00 ,  C07B59/00 ,  C07F5/02

摘要： The present invention aims to produce a radiolabeled aryl compound by a method that enables an easy labelling with a high radiochemical yield in a short time, and that enables formulation immediately after the labelling.
The present invention relates to a method of producing the radiolabeled aryl compound (I), which comprises reacting the aryl boronic acid compound (II) with a radionuclide selected from 123 I, 124 I, 125 I and 131 I, in the presence of an oxidizing agent selected from N-bromosuccinimide and N-chlorosuccinimide, in water.

         Ar-X     (I)

         Ar-Y     (II)

wherein each symbol is as defined in the description.

公开(公告)号：EP3733216A1

公开(公告)日：2020-11-04

申请号：EP18894698.2

申请日：2018-12-28

申请人： Osaka University

发明人： SHIRAKAMI, Yoshifumi ,  WATABE, Tadashi ,  KANEDA, Kazuko ,  SHIMOSEGAWA, Eku ,  SHINOHARA, Atsushi ,  HATAZAWA, Jun

IPC分类号： A61K51/00 ,  A61K9/08 ,  A61K47/22 ,  A61P5/14 ,  A61P35/00

摘要： The present invention aims to provide an astatine solution that can be used in RI internal radiotherapy and the like for the treatment of thyroid gland disease and the like, and a production method thereof.
The present invention provides a method for producing a solution containing 211 At - (astatide ion) at a high radiochemical purity by using 211 At obtained by a nuclear reaction as a starting material, including a step of adding a reducing agent to a solution containing an impurity derived from 211 At; and a solution containing 211 At - (astatide ion) at a radiochemical purity of not less than 30%.

公开(公告)号：EP4378948A1

公开(公告)日：2024-06-05

申请号：EP22849616.2

申请日：2022-07-29

申请人： OSAKA UNIVERSITY

发明人： SHIRAKAMI, Yoshifumi ,  KANEDA, Kazuko ,  KADONAGA, Yuichiro ,  WATABE, Tadashi ,  TOYOSHIMA, Atsushi ,  FUKASE, Koichi ,  YOSHIYA, Taku

IPC分类号： C07K4/00 ,  A61K38/08 ,  A61K51/08 ,  A61P13/08 ,  A61P35/00 ,  C07B59/00 ,  C07C273/18 ,  C07C275/16 ,  C07F5/02 ,  G01T1/161

CPC分类号： A61K38/08 ,  A61K51/08 ,  A61P13/08 ,  A61P35/00 ,  C07B59/00 ,  C07C273/18 ,  C07C275/16 ,  C07F5/02 ,  C07K4/00 ,  G01T1/161

摘要： The aims of the present invention are to provide an agent that binds specifically to PSMA, is effective in the treatment and diagnosis of tumors or cancers expressing PSMA, for example, the treatment and diagnosis of prostate cancer, especially castration-resistant prostate cancer (CRPC), further especially metastatic castration-resistant prostate cancer (mCRPC), and does not exhibit side effects due to accumulation in the kidney or salivary glands.
The present invention provides a radiolabeled compound represented by Formula (I) or a pharmaceutically acceptable salt thereof:

wherein each symbol is as defined in the description.

公开(公告)号：EP3766521A1

公开(公告)日：2021-01-20

申请号：EP19767854.3

申请日：2019-02-22

申请人： Osaka University

发明人： FUKASE, Koichi ,  SHINOHARA, Atsushi ,  KANAI, Yoshikatsu ,  KABAYAMA, Kazuya ,  KANEDA, Kazuko ,  ZHANG, Zijian ,  HATAZAWA, Jun ,  SHIRAKAMI, Yoshifumi ,  SHIMOYAMA, Atsushi ,  MANABE, Yoshiyuki

IPC分类号： A61K51/00 ,  A61K31/198 ,  A61K31/28 ,  A61P35/00

摘要： To develop a compound which is highly accumulated in cancer cells and capable of emitting an α-ray and provide a pharmaceutical composition for cancer treatment including the compound.
A pharmaceutical composition for cancer treatment including a compound having a structure in which 211 At is introduced as a substituent into an amino acid derivative having an affinity with an amino acid transporter LAT1 or a pharmaceutically acceptable salt of the compound.