公开(公告)号：US11027029B2

公开(公告)日：2021-06-08

申请号：US15774632

申请日：2016-11-09

Applicant: CELLBION CO., LTD

Inventor： Jae Min Jeong ,  Sung-Hyun Moon ,  Yun-Sang Lee

IPC: A61K51/04 ,  C07D257/02 ,  A61P35/00 ,  G01N33/60 ,  A61K31/41 ,  G01N33/574 ,  C07D255/02 ,  C07F5/00

Abstract: The present invention relates to a peptide thiourea derivative, a pharmaceutically acceptable salt thereof, a radioisotope labeled compound comprising the same, and a pharmaceutical composition for treating or diagnosing prostate cancer comprising the same as an active ingredient. The peptide thiourea derivative of the present invention is excellent in stability in human serum when it is administered in vivo and not only binds well to PSMA expressed in prostate cancer but also inhibits excellently PSMA at a low concentration. Besides, the derivative of the invention has a high water-solubility and can be excreted through the kidney not through the bile passage so that a clear image of the tumor region of prostate cancer can be obtained. Therefore, the derivative of the present invention can be effectively used as a pharmaceutical composition for treating and diagnosing prostate cancer.

公开(公告)号：US20180339071A1

公开(公告)日：2018-11-29

申请号：US15774632

申请日：2016-11-09

Applicant: CELLBION CO., LTD

Inventor： Jae Min Jeong ,  Sung-Hyun Moon ,  Yun-Sang Lee

IPC: A61K51/04 ,  C07D255/02 ,  C07F5/00 ,  C07D257/02 ,  A61P35/00

Abstract: The present invention relates to a peptide thiourea derivative, a pharmaceutically acceptable salt thereof, a radioisotope labeled compound comprising the same, and a pharmaceutical composition for treating or diagnosing prostate cancer comprising the same as an active ingredient. The peptide thiourea derivative of the present invention is excellent in stability in human serum when it is administered in vivo and not only binds well to PSMA expressed in prostate cancer but also inhibits excellently PSMA at a low concentration. Besides, the derivative of the invention has a high water-solubility and can be excreted through the kidney not through the bile passage so that a clear image of the tumor region of prostate cancer can be obtained. Therefore, the derivative of the present invention can be effectively used as a pharmaceutical composition for treating and diagnosing prostate cancer.