公开(公告)号：US11071794B2

公开(公告)日：2021-07-27

申请号：US16824139

申请日：2020-03-19

Applicant: Five Eleven Pharma Inc.

Inventor： Zehui Wu ,  Zhihao Zha ,  Futao Liu ,  Karl Ploessl ,  Seok Rye Choi ,  Hank F. Kung

IPC: A61K51/00 ,  A61M36/14 ,  A61K51/04 ,  A61B6/03 ,  C07B59/00 ,  C07D221/06 ,  C07D213/64 ,  C07D405/04 ,  C07C217/80 ,  C07D471/04 ,  C07C323/37 ,  C07D277/66

Abstract: The present invention relates to deuterated compounds according to Formula I-A, Formula II-A, Formula II-D, and Formula III-A. These compounds can be used as PET imaging agents for evaluating Parkinson's Disease, Alzheimer Disease, and for determining specific serotonin reuptake inhibitor (SSRIi) activity for treatment of depression. The present invention also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I-A, Formulae II-A, Formula II-D, or Formula III-A, or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20200230263A1

公开(公告)日：2020-07-23

申请号：US16824139

申请日：2020-03-19

Applicant: Five Eleven Pharma Inc.

Inventor： Zehui WU ,  Zhihao ZHA ,  Futao LIU ,  Karl PLOESSL ,  Seok Rye CHOI ,  Hank F. KUNG

IPC: A61K51/04 ,  A61B6/03 ,  C07B59/00 ,  C07D221/06 ,  C07D213/64 ,  C07D405/04 ,  C07C217/80 ,  C07D471/04 ,  C07C323/37

Abstract: The present invention relates to deuterated compounds according to Formula I-A, Formula II-A, Formula II-D, and Formula III-A. These compounds can be used as PET imaging agents for evaluating Parkinson's Disease, Alzheimer Disease, and for determining specific serotonin reuptake inhibitor (SSRIi) activity for treatment of depression. The present invention also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I-A, Formulae II-A, Formula II-D, or Formula III-A, or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20240158420A1

公开(公告)日：2024-05-16

申请号：US18547609

申请日：2021-03-17

Applicant: FIVE ELEVEN PHARMA, INC ,  BIOMOLECULAR PROBES BIOTECHNOLOGY (BEIJING) CO., LTD

Inventor： Hank F KUNG ,  Zhihao ZHA ,  Karl PLOESSL ,  Seok Rye CHOI ,  David ALEXOFF

IPC: C07F5/06 ,  G01N33/574 ,  G01N33/68

CPC classification number: C07F5/069 ,  G01N33/57434 ,  G01N33/68

Abstract: A radiopharmaceuticals in clinical popularization is facilitated. By means of the biological characteristic of specifically targeting PSMA of the [18F]AlF-P16-093, the labeled product has important potential clinical values in the aspects of early diagnosis, preoperative staging, treatment guidance, recurrence and metastasis focus detection of prostate cancer.

公开(公告)号：US20240139350A1

公开(公告)日：2024-05-02

申请号：US18263722

申请日：2021-02-01

Applicant: FIVE ELEVEN PHARMA, INC ,  BIOMOLECULAR PROBES BIOTECHNOLOGY (BEIJING) CO., LTD

Inventor： Hank F KUNG ,  Zhihao ZHA ,  Karl PLOESSL ,  Seok Rye CHOI ,  David ALEXOFF

IPC: A61K51/04

CPC classification number: A61K51/0455 ,  A61K2123/00

Abstract: A radioactively labeled ligand for a fibroblast activation protein-alpha imaging agent and a preparation method therefor are provided. The radioactively labeled ligand for the fibroblast activation protein-alpha imaging agent has structural formal (I). The compound has a good 68Ga labeling property, a high stability and a good affinity for FAP tumors. The radioactively labeled ligand for 68Ga-labeled FAPi can be used as a tumor positron imaging agent.

公开(公告)号：US10688200B2

公开(公告)日：2020-06-23

申请号：US15385490

申请日：2016-12-20

Applicant: Five Eleven Pharma Inc.

Inventor： Hank F. Kung ,  Karl Ploessl ,  Seok Rye Choi ,  Zhihao Zha ,  Zehui Wu

IPC: A61K51/04 ,  C07K5/02

Abstract: The present invention relates to compounds according to Formula I and Formula IV. These compounds display very good binding affinities to the PSMA binding sites. They can be labeled with [68Ga]GaCl3 with high yields and excellent radiochemical purity. The present invention also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I or Formula IV, or a pharmaceutically acceptable salt thereof.

公开(公告)号：US10253052B2

公开(公告)日：2019-04-09

申请号：US15203602

申请日：2016-07-06

Applicant: Five Eleven Pharma Inc.

Inventor： Hank F. Kung ,  Zehui Wu ,  Seok Rye Choi ,  Karl Plössl ,  Zhihao Zha

IPC: A61K51/04 ,  A61K49/10 ,  C07F9/38 ,  C07F9/6515 ,  C07F9/6524

Abstract: The present invention relates to compounds according to Formula I or Formula II, which are potential bone imaging agents. Certain compounds labeled with 68Ga displayed excellent bone uptake and retention. The present invention also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I or Formula II or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20170189568A1

公开(公告)日：2017-07-06

申请号：US15385490

申请日：2016-12-20

Applicant: Five Eleven Pharma Inc.

Inventor： Hank F. KUNG ,  Karl PLOESSL ,  Seok Rye CHOI ,  Zhihao ZHA ,  Zehui WU

IPC: A61K51/04 ,  C07K5/02

Abstract: The present invention relates to compounds according to Formula I and Formula IV. These compounds display very good binding affinities to the PSMA binding sites. They can be labeled with [68Ga]GaCl3 with high yields and excellent radiochemical purity. The present invention also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I or Formula IV, or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20170022224A1

公开(公告)日：2017-01-26

申请号：US15203602

申请日：2016-07-06

Applicant: Five Eleven Pharma Inc.

Inventor： Hank F. KUNG ,  Zehui Wu ,  Seok Rye Choi ,  Karl PLÖSSL ,  Zhihao Zha

IPC: C07F9/38 ,  A61K49/10 ,  A61K51/04

CPC classification number: C07F9/3873 ,  A61K51/0489 ,  A61K51/0497 ,  C07F9/3817 ,  C07F9/6515 ,  C07F9/6524

Abstract: The present invention relates to compounds according to Formula I or Formula II, which are potential bone imaging agents. Certain compounds labeled with 68Ga displayed excellent bone uptake and retention. The present invention also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I or Formula II or a pharmaceutically acceptable salt thereof.

Abstract translation: 本发明涉及式（I）或式（II）的化合物，它们是用于治疗骨肿瘤和转移的潜在骨成像剂和治疗剂。 用68Ga标记的某些化合物显示出优异的骨吸收和保留性。 本发明还涉及包含药学上可接受的载体和式（I）或式（II）的化合物或其药学上可接受的盐的药物组合物。

公开(公告)号：US20180344882A1

公开(公告)日：2018-12-06

申请号：US15994474

申请日：2018-05-31

Applicant: Five Eleven Pharma Inc.

Inventor： Zehui WU ,  Zhihao ZHA ,  Futao LIU ,  Karl PLOESSL ,  Seok Rye CHOI ,  Hank F. KUNG

IPC: A61K51/04 ,  A61B6/03 ,  C07B59/00 ,  C07D221/06

Abstract: The present invention relates to deuterated compounds according to Formula I-A, Formula II-A, Formula II-D, and Formula III-A. These compounds can be used as PET imaging agents for evaluating Parkinson's Disease, Alzheimer Disease, and for determining specific serotonin reuptake inhibitor (SSRIi) activity for treatment of depression. The present invention also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I-A, Formulae II-A, Formula II-D, or Formula III-A, or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20220125959A1

公开(公告)日：2022-04-28

申请号：US17605609

申请日：2020-04-27

Applicant: FIVE ELEVEN PHARMA INC.

Inventor： Hank F. KUNG ,  Zhihao ZHA ,  Karl PLOESSL ,  Seok Rye CHOI

IPC: A61K51/04 ,  A61P35/00 ,  A61K47/54

Abstract: The present disclosure relates to compounds according to Formula I. These compounds display very good binding affinities to the PSMA binding sites. They comprise a radioactive isotope or a chelating moiety that can be labeled with a radioactive metal such as [68Ga]or [177Lu]. The present disclosure also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I or a complex thereof, or a pharmaceutically acceptable salt thereof.