公开(公告)号：US11078166B2

公开(公告)日：2021-08-03

申请号：US15752340

申请日：2016-08-15

Applicant: THE JOHNS HOPKINS UNIVERSITY

Inventor： Martin G. Pomper ,  Ying Chen ,  Xing Yang ,  Ronnie C. Mease ,  Sangeeta Ray

IPC: C07D249/04 ,  A61K51/04 ,  C07B59/00

Abstract: Triazole conjugated urea-based and thiourea-based scaffolds that have high binding affinity to PSMA are disclosed. These scaffolds can be radiolabeled and used to image cells and tumors that express PSMA. Methods of synthesizing radiofluorinated triazole conjugated urea-based and thiourea-based scaffolds also are disclosed.

公开(公告)号：US10857246B2

公开(公告)日：2020-12-08

申请号：US15578473

申请日：2016-06-01

Applicant: THE JOHNS HOPKINS UNIVERSITY

Inventor： Xing Yang ,  Il Minn ,  Steven Rowe ,  Sangeeta Ray ,  Ronnie C. Mease ,  Michael Gorin ,  Mohamad Allaf ,  Martin G. Pomper

IPC: A61K51/04 ,  C07D417/14 ,  C07D417/12 ,  A61P35/00

Abstract: Highly potent and selective radionuclide-based imaging and therapy agents targeting carbonic anhydrase IX with minimum non-specific organ uptake are disclosed. Methods of imaging and/or treating carbonic anhydrase IX-expressing cells or tumors also are disclosed.

公开(公告)号：US20200330613A1

公开(公告)日：2020-10-22

申请号：US16908218

申请日：2020-06-22

Applicant: The Johns Hopkins University

Inventor： Sangeeta Ray ,  Xing Yang ,  Xiaolei Song ,  Michael T. McMahon ,  Martin G. Pomper

IPC: A61K49/00 ,  C07F19/00 ,  C07F1/04 ,  C08F222/38 ,  A61K49/08 ,  A61K49/12 ,  C07F5/00 ,  C07F5/02 ,  A61K51/06 ,  A61K49/14

Abstract: Salicylic acid-based polymeric CEST contrast agents targeting prostate-specific membrane antigen, pharmaceutical composition comprising the same and methods of use thereof are disclosed.

公开(公告)号：US11911488B2

公开(公告)日：2024-02-27

申请号：US16984415

申请日：2020-08-04

Applicant: The Johns Hopkins University

Inventor： Martin G. Pomper ,  Ronnie C. Mease ,  Sangeeta Ray ,  Ying Chen ,  Xing Yang

IPC: A61K51/04 ,  A61K41/00 ,  A61K49/00 ,  C07D213/82 ,  C07D209/12 ,  C07C271/22 ,  C07C275/16 ,  C07C323/62

CPC classification number: A61K51/0402 ,  A61K41/0057 ,  A61K49/0002 ,  A61K49/0021 ,  A61K49/0032 ,  A61K49/0041 ,  A61K49/0052 ,  A61K51/0455 ,  C07C271/22 ,  C07C275/16 ,  C07C323/62 ,  C07D209/12 ,  C07D213/82 ,  A61K49/0017 ,  A61K49/0019

Abstract: Carbamate and beta-amino acid urea-based scaffolds that have high binding affinity to PSMA are disclosed. These scaffolds can be radiolabeled and used for imaging cells and tumors that express PSMA or for cancer radiotherapy. These compounds also can comprise a fluorescent dye and be used for imaging cells and tumors that express PSMA or for photodynamic therapy.

公开(公告)号：US20230364274A1

公开(公告)日：2023-11-16

申请号：US18354282

申请日：2023-07-18

Applicant: The Johns Hopkins University

Inventor： Xing Yang ,  Sridhar Nimmagadda ,  Steven Rowe ,  Stephanie Slania ,  Martin G. Pomper

IPC: A61K51/04 ,  A61K47/54

CPC classification number: A61K51/0485 ,  A61K47/545 ,  A61K51/0478 ,  A61K51/0482

Abstract: Imaging and radiotherapeutics agents targeting fibroblast-activation protein-α (FAP-α) and their use in imaging and treating FAP-α related diseases and disorders are disclosed.

公开(公告)号：US20200290982A1

公开(公告)日：2020-09-17

申请号：US16887754

申请日：2020-05-29

Applicant: The Johns Hopkins University ,  Northwestern University

Inventor： Sangeeta Ray ,  Martin G. Pomper ,  Thomas J. Meade ,  Ronnie C. Mease ,  Ying Chen ,  Xing Yang ,  Matthew Rotz

IPC: C07D257/02 ,  A61K49/10 ,  A61K51/04 ,  C07D403/14 ,  A61K49/12 ,  A61K51/06 ,  A61K49/00

Abstract: Low-molecular weight gadolinium (Gd)-based MR contrast agents for PSMA-specific T1-weighted MR imaging are disclosed. The (Gd)-based MR contrast agents exhibit high binding affinity for PSMA and exhibit specific T1 contrast enhancement at PSMA+ cells. The PSMA-targeted Gd-based MR contrast agents can be used for PSMA-targeted imaging in vivo. 86Y-labeled PSMA-binding ureas also are provided, wherein the PSMA-binding ureas also are suitable for use with other radiotherapeutics.

公开(公告)号：US10188754B2

公开(公告)日：2019-01-29

申请号：US14891531

申请日：2014-05-16

Applicant: THE JOHNS HOPKINS UNIVERSITY

Inventor： Xing Yang ,  Xiaolei Song ,  Sangeeta Ray ,  Martin G. Pomper ,  Michael T. McMahon

IPC: A61K49/10 ,  G01R33/56 ,  A61B5/05 ,  A61B6/03 ,  A61B5/055 ,  A61B5/00 ,  A61B6/00

Abstract: Compositions and methods for chemical exchange saturation transfer (CEST) based magnetic resonance imaging (MRI) or frequency labeled exchange (FLEX) imaging are disclosed. Beta-hydroxycarboxylate and beta-aminocarboxylate derivatives including salicylic acid, salicylates, salicylic acid prodrugs, N-alkyl/aryl/acyl/sulfonyl-anthranilic acid analogs, and any aromatic compound with OH/NH group ortho to the carboxylic acid group are disclosed. Such compounds can be used as general MRI organic contrast agents and produce significantly improved contrast in MR images detectable through CEST or FLEX.

公开(公告)号：US20160075667A1

公开(公告)日：2016-03-17

申请号：US14890311

申请日：2014-05-01

Applicant: The Johns Hopkins University

Inventor： Xing Yang ,  Xiaolei Song ,  Sangeeta Ray ,  Martin G. Pomper ,  Michael T. McMahon

IPC: C07D249/04 ,  C07D231/14 ,  A61K49/10 ,  C07D233/90

CPC classification number: C07D249/04 ,  A61K49/10 ,  C07D231/14 ,  C07D233/90 ,  C07D257/04

Abstract: The invention features novel heterocyclic compounds that are useful as MRI contrast agents. Specifically, the invention relates to a novel class of MRI contrast agents that produce significantly improved contrast in MR images that is detectable through chemical exchange saturation transfer (CEST) or frequency labeled exchange (FLEX) imaging. The MRI contrast agents of the invention include those delineated in the formulae provided herein. The invention also relates to various methods in which the MRI contrast agents are employed. Kits and pharmaceutical compositions thereof are also provided.

Abstract translation: 本发明的特征在于可用作MRI造影剂的新型杂环化合物。 具体而言，本发明涉及一种新型的MRI造影剂，其可以通过化学交换饱和转移（CEST）或频率标记交换（FLEX）成像检测出MR图像中产生显着改善的对比度。 本发明的MRI造影剂包括本文提供的化学式中描述的那些。 本发明还涉及使用MRI造影剂的各种方法。 还提供了试剂盒及其药物组合物。

公开(公告)号：US12115233B2

公开(公告)日：2024-10-15

申请号：US18585905

申请日：2024-02-23

Applicant: The Johns Hopkins University

Inventor： Xing Yang ,  Sridhar Nimmagadda ,  Steven Rowe ,  Stephanie Slania ,  Martin G. Pomper

IPC: A61K51/00 ,  A61K47/54 ,  A61K51/04 ,  A61M36/14

CPC classification number: A61K51/0485 ,  A61K47/545 ,  A61K51/0478 ,  A61K51/0482

Abstract: Imaging and radiotherapeutics agents targeting fibroblast-activation protein-α (FAP-α) and their use in imaging and treating FAP-α related diseases and disorders are disclosed.

公开(公告)号：US20200330624A1

公开(公告)日：2020-10-22

申请号：US16758182

申请日：2018-10-23

Applicant: The Johns Hopkins University

Inventor： Xing Yang ,  Sridhar Nimmagadda ,  Steven Rowe ,  Stephanie Slania ,  Martin G. Pomper

IPC: A61K51/04 ,  A61K47/54

Abstract: Imaging and radiotherapeutics agents targeting fibroblast-activation protein-α (FAP-α) and their use in imaging and treating FAP-α related diseases and disorders are disclosed.