公开(公告)号：US20190023722A9

公开(公告)日：2019-01-24

申请号：US15557854

申请日：2016-03-14

申请人： THE JOHNS HOPKINS UNIVERSITY

发明人： MARTIN G. POMPER ,  RONNIE C. MEASE ,  SANGEETA RAY

IPC分类号： C07F5/00 ,  A61K51/04

摘要： PSMA-targeted PET/SPECT agents for imaging PSMA-positive cancer and or tumor neovasculature and PSMA-targeted radiotherapeutic agent for the treatment of PSMA-positive cancer or tumor neovasculature are disclosed. Methods of imaging PSMA expressing tumors, or cells and kits also are disclosed.

公开(公告)号：US20190225589A1

公开(公告)日：2019-07-25

申请号：US15752340

申请日：2016-08-15

申请人： THE JOHNS HOPKINS UNIVERSITY

发明人： MARTIN G. POMPER ,  YING CHEN ,  XING YANG ,  RONNIE C. MEASE ,  SANGEETA RAY

IPC分类号： C07D249/04 ,  C07B59/00

摘要： 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：US20180222922A1

公开(公告)日：2018-08-09

申请号：US15580779

申请日：2016-06-08

申请人： THE JOHNS HOPKINS UNIVERSITY

发明人： MARTIN G. POMPER ,  RONNIE C. MEASE ,  XING YANG ,  CATHERINE FOSS

IPC分类号： C07D513/04 ,  A61K51/04

CPC分类号： C07D513/04 ,  A61K51/0459

摘要： Radiofluorinated 7-Amino-5-thio-thiazolo[4,5-d]pyrimidines targeting Fractalkine Receptor (CX3CR1) are disclosed. Methods of imaging CX3CR1-expressing tumors or cells also are disclosed.

公开(公告)号：US20160008493A1

公开(公告)日：2016-01-14

申请号：US14777117

申请日：2014-03-17

申请人： THE JOHNS HOPKINS UNIVERSITY

发明人： MARTIN C. POMPER ,  HAOFAN WANG ,  IL MINN ,  RONNIE C. MEASE

IPC分类号： A61K51/04 ,  C07C235/42 ,  G01N33/60

CPC分类号： A61K51/04 ,  C07B59/001 ,  C07C233/76 ,  C07C235/42 ,  G01N33/60 ,  G01N2333/90203

摘要： A detectable substrate for aldehyde dehydrogenase (ALDH) can include a radiolabel. When acted upon by ALDH in an ALDH-expressing cell, e.g., cancer cells, the radiolabeled substrate accumulates in the ALDH-expressing cell. ALDH-expressing cells can be distinguished by the accumulated radioactivity. When combined with suitable imaging technique, the detectable substrate can be used for in vivo imaging of cancer cells.

摘要翻译： 用于醛脱氢酶（ALDH）的可检测底物可以包括放射性标记。 当ALDH在ALDH表达细胞（例如癌细胞）中作用时，放射性标记的底物积聚在ALDH表达细胞中。 ALDH表达细胞可以通过累积的放射性来区分。 当与合适的成像技术组合时，可检测的底物可用于癌细胞的体内成像。

公开(公告)号：US20180236112A1

公开(公告)日：2018-08-23

申请号：US15888634

申请日：2018-02-05

申请人： THE JOHNS HOPKINS UNIVERSITY

发明人： MARTIN G. POMPER ,  SANGEETA RAY ,  RONNIE C. MEASE ,  HASSAN SHALLAL

IPC分类号： A61K51/08 ,  C07D249/04 ,  C07K5/02 ,  C07K5/097

CPC分类号： A61K51/088 ,  A61K38/00 ,  A61K38/06 ,  A61K45/06 ,  A61K51/0482 ,  C07D249/04 ,  C07K5/0217 ,  C07K5/06086 ,  C07K5/0815 ,  C07K5/0821

摘要： The present invention provides bivalent and multivalent ligands with a view to improving the affinity and pharmacokinetic properties of a urea class of PSMA inhibitors. The compounds and their synthesis can be generalized to multivalent compounds of other target antigens. Because they present multiple copies of the pharmacophore, multivalent ligands can bind to receptors with high avidity and affinity, thereby serving as powerful inhibitors. The modular multivalent scaffolds of the present invention, in one or more embodiments, contains a lysine-based (α-, ε-) dialkyne residue for incorporating two or more antigen binding moieties, such as PSMA binding Lys-Glu urea moieties, exploiting click chemistry and one or more additional lysine residues for subsequent modification with an imaging and/or therapeutic nuclides or a cytotoxic ligands for tumor cell killing.

公开(公告)号：US20180085478A1

公开(公告)日：2018-03-29

申请号：US15639445

申请日：2017-06-30

申请人： THE JOHNS HOPKINS UNIVERSITY

发明人： MARTIN G. POMPER ,  SANGEETA RAY ,  RONNIE C. MEASE ,  CATHERINE ANNE FOSS

IPC分类号： A61K51/04 ,  G01N33/60 ,  A61K31/145 ,  C07F13/00 ,  C07D257/02 ,  C12Q1/37 ,  A61K31/195 ,  G01N33/574 ,  C07D257/00 ,  C07D215/12 ,  C07D213/38 ,  A61K38/06 ,  A61K31/4402 ,  A61K31/395

CPC分类号： A61K51/0472 ,  A61K31/145 ,  A61K31/195 ,  A61K31/395 ,  A61K31/4402 ,  A61K38/06 ,  A61K51/0402 ,  C07D213/38 ,  C07D215/12 ,  C07D257/00 ,  C07D257/02 ,  C07F13/00 ,  C12Q1/37 ,  G01N33/57434 ,  G01N33/60 ,  G01N2500/04 ,  A61K2300/00

摘要： The prostate-specific membrane antigen (PSMA) is increasingly recognized as a viable target for imaging and therapy of cancer. Various 99mTc/Re-labeled compounds were prepared by attaching known Tc/Re chelating agents to an amino-functionalized PSMA inhibitor with or without a variable length linker moiety. Ex vivo biodistribution and in vivo imaging demonstrated the degree of specific binding to engineered PSMA+ PC3 PIP tumors.

公开(公告)号：US20180051039A1

公开(公告)日：2018-02-22

申请号：US15557854

申请日：2016-03-14

申请人： THE JOHNS HOPKINS UNIVERSITY

发明人： MARTIN G. POMPER ,  RONNIE C. MEASE ,  SANGEETA RAY

IPC分类号： C07F5/00 ,  A61K51/04

摘要： PSMA-targeted PET/SPECT agents for imaging PSMA-positive cancer and or tumor neovasculature and PSMA-targeted radiotherapeutic agent for the treatment of PSMA-positive cancer or tumor neovasculature are disclosed. Methods of imaging PSMA expressing tumors, or cells and kits also are disclosed.

公开(公告)号：US20150104387A1

公开(公告)日：2015-04-16

申请号：US14243535

申请日：2014-04-02

申请人： THE JOHNS HOPKINS UNIVERSITY

发明人： MARTIN G. POMPER ,  RONNIE C. MEASE ,  YING CHEN ,  Sangeeta Ray

IPC分类号： C07F5/02 ,  A61K49/00 ,  A61K51/04 ,  G01N33/50 ,  C07D311/82 ,  C07F13/00 ,  C07D209/12 ,  C07D311/20 ,  C07D249/04 ,  C07D257/02

CPC分类号： C07D257/02 ,  A61K49/0052 ,  A61K51/0421 ,  A61K51/044 ,  A61K51/0446 ,  A61K51/0453 ,  A61K51/0472 ,  C07D209/12 ,  C07D209/14 ,  C07D213/04 ,  C07D249/04 ,  C07D255/02 ,  C07D311/14 ,  C07D311/20 ,  C07D311/82 ,  C07F5/027 ,  C07F13/005 ,  G01N33/5091

摘要： Prostate-specific membrane antigen (PSMA) targeting compounds are described. Uses of the compounds for imaging, therapy, cell sorting, and tumor mapping are also described.

摘要翻译： 描述了前列腺特异性膜抗原（PSMA）靶向化合物。 还描述了用于成像，治疗，细胞分选和肿瘤作图的化合物的用途。

公开(公告)号：US20180133348A1

公开(公告)日：2018-05-17

申请号：US15578473

申请日：2016-06-01

申请人： THE JOHNS HOPKINS UNIVERSITY

发明人： XING YANG ,  IL MINN ,  STEVEN ROWE ,  SANGEETA RAY ,  RONNIE C. MEASE ,  MICHAEL GORIN ,  MOHAMAD ALLAF ,  MARTIN G. POMPER

IPC分类号： A61K51/04 ,  A61P35/00

CPC分类号： A61K51/0497 ,  A61P35/00 ,  C07D417/12 ,  C07D417/14

摘要： 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：US20170283384A1

公开(公告)日：2017-10-05

申请号：US15618788

申请日：2017-06-09

申请人： THE JOHNS HOPKINS UNIVERSITY ,  INTUITIVE SURGICAL OPERATIONS, INC.

发明人： MARTIN G. POMPER ,  RONNIE C. MEASE ,  YING CHEN ,  SANGEETA RAY ,  JONATHAN SORGER

IPC分类号： C07D257/02 ,  A61K51/04 ,  C07D311/82 ,  C07D213/04 ,  C07D209/14 ,  C07D249/04 ,  C07F5/02 ,  C07D209/12 ,  C07D255/02 ,  A61K49/00 ,  G01N33/50 ,  C07D311/14 ,  C07D311/20 ,  C07F13/00

CPC分类号： C07D257/02 ,  A61K49/0032 ,  A61K49/0052 ,  A61K51/0421 ,  A61K51/044 ,  A61K51/0446 ,  A61K51/0453 ,  A61K51/0472 ,  C07D209/12 ,  C07D209/14 ,  C07D209/24 ,  C07D213/04 ,  C07D249/04 ,  C07D255/02 ,  C07D311/14 ,  C07D311/20 ,  C07D311/82 ,  C07F5/027 ,  C07F13/005 ,  G01N33/5091 ,  G01N2800/342

摘要： Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.