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

Applicant: OSAKA UNIVERSITY

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

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

Abstract: 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：EP4483905A1

公开(公告)日：2025-01-01

申请号：EP23759947.7

申请日：2023-02-21

Applicant: OSAKA UNIVERSITY

Inventor： SHIRAKAMI, Yoshifumi ,  KADONAGA, Yuichiro ,  KANEDA, Kazuko ,  WATABE, Tadashi ,  FUKASE, Koichi ,  SHIMOYAMA, Atsushi ,  ASO, Ayaka ,  YOSHIYA, Taku

IPC: A61K47/54 ,  A61K51/04 ,  A61P35/00 ,  C07D401/12 ,  C07H15/26 ,  C07K5/02

Abstract: It is an object of the present invention to provide drugs that bind specifically to FAPα, are effective in the treatment and diagnosis of tumors or cancers expressing FAPα, for example, in the treatment and diagnosis of solid cancers such as pancreatic cancer, sarcoma, esophageal cancer, lung cancer, breast cancer, prostate cancer, head and neck cancer, ovarian cancer, colon cancer, neuroendocrine tumor, thyroid cancer, uterine cancer, liver cancer and the like (particularly, pancreatic cancer), and have a lower risk of prolonged side effects.
The present invention provides a conjugate comprising a radioactive moiety comprising an aryl group substituted with a radionuclide selected from 211 At, 210 At, 131 I, 125 I, 124 I, 123 I, 77 Br and 76 Br, and a bioactive moiety having an affinity for fibroblast activation protein α (FAPα).

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

Applicant: OSAKA UNIVERSITY

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

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

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

Abstract: 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.