公开(公告)号：US10398790B2

公开(公告)日：2019-09-03

申请号：US15572632

申请日：2016-05-10

申请人： The Trustees of The University of Pennsylvania

发明人： Mark Sellmyer ,  Robert H. Mach ,  David A. Mankoff ,  Iljung Lee

IPC分类号： A61K51/04 ,  A61K31/395 ,  A61K49/00 ,  A61K47/54 ,  A61K31/495 ,  A61K31/505 ,  C07D239/49 ,  C07D403/12

摘要： The present invention provides radiolabeled trimethoprim which are useful in imaging tests such as PET scans. The compounds show robust bacterial uptake in vitro and identify infections from inflammation or tumor when administered to a subject. The compounds show rapid and sensitive detection of Ec DHFR containing tumors from control tumors and background tissue. In one aspect, a compound having the structure of formula (I) is provided or a pharmaceutically acceptable salt or prodrug thereof, wherein R is defined herein. Also provided are compositions containing these compounds, positron emission tomography reporter probe comprising these compounds, and methods of imaging a bacterial infection, tracking or monitoring bacteria, distinguishing a bacterial infection from inflammation or tumor, monitoring genetically fused protein expression, and monitoring genetically engineered cells in clinical scenarios such as immunotherapy for cancer treatment.

公开(公告)号：US20210138093A1

公开(公告)日：2021-05-13

申请号：US17099511

申请日：2020-11-16

申请人： The Trustees of the University of Pennsylvania

发明人： Mark Sellmyer ,  Robert H. Mach ,  David A. Mankoff ,  Iljung Lee

IPC分类号： A61K51/04 ,  A61K31/395 ,  A61K31/495 ,  A61K49/00 ,  C07D239/49 ,  C07D403/12 ,  A61K47/54 ,  A61K31/505

摘要： The present invention provides radiolabeled trimethoprim which are useful in imaging tests such as PET scans. The compounds show robust bacterial uptake in vitro and identify infections from inflammation or tumor when administered to a subject. The compounds show rapid and sensitive detection of Ec DHFR containing tumors from control tumors and background tissue. In one aspect, a compound having the structure of formula (I) is provided or a pharmaceutically acceptable salt or prodrug thereof, wherein R is defined herein. Also provided are compositions containing these compounds, positron emission tomography reporter probe comprising these compounds, and methods of imaging a bacterial infection, tracking or monitoring bacteria, distinguishing a bacterial infection from inflammation or tumor, monitoring genetically fused protein expression, and monitoring genetically engineered cells in clinical scenarios such as immunotherapy for cancer treatment.

公开(公告)号：US20190381197A1

公开(公告)日：2019-12-19

申请号：US16511052

申请日：2019-07-15

申请人： The Trustees of the University of Pennsylvania

发明人： Mark Sellmyer ,  Robert H. Mach ,  David A. Mankoff ,  Iljung Lee

IPC分类号： A61K51/04 ,  A61K31/395 ,  A61K31/495 ,  A61K31/505 ,  A61K47/54 ,  A61K49/00 ,  C07D239/49 ,  C07D403/12

摘要： The present invention provides radiolabeled trimethoprim which are useful in imaging tests such as PET scans. The compounds show robust bacterial uptake in vitro and identify infections from inflammation or tumor when administered to a subject. The compounds show rapid and sensitive detection of Ec DHFR containing tumors from control tumors and background tissue. In one aspect, a compound having the structure of formula (I) is provided or a pharmaceutically acceptable salt or prodrug thereof, wherein R is defined herein. Also provided are compositions containing these compounds, positron emission tomography reporter probe comprising these compounds, and methods of imaging a bacterial infection, tracking or monitoring bacteria, distinguishing a bacterial infection from inflammation or tumor, monitoring genetically fused protein expression, and monitoring genetically engineered cells in clinical scenarios such as immunotherapy for cancer treatment.