Siemens Medical Solutions Usa, Inc.

Threshold Pharmaceuticals, Inc.

Thomas Lee Collier

Joseph C Walsh

Hartmuth C Kolb

Umesh B Gangadharmath

Dhanalakshmi Kasi

Farhad Karimi

Qianwa Liang

Tieming Zhao

Henry Clifton Padgett

Brian A Duclos

Zhiyong Gao

Kai Chen

Bing Wang

Gang Chen

Vani P Mocharla

Peter J H Scott

Chunfang Xia

Steven Zigler

Johanna Santiago

The present application discloses methods for identifying inhibitors with high binding-affinity for the carbonic anhydrase-IX (CA-IX) enzyme using click chemistry and uses the candidates thereof as positron emission tomography (PET) imaging agents.

Development of molecular imaging probes for carbonic anhydrase-IX using click chemistry

A vented filter is placed at the HPLC (High Performance Liquid Chromatography) loop entry port of an HPLC injector valve. The vented filter prevents the push gas used to deliver the crude radiolabeled product from over-pushing the liquid to waste. Push gas is vented off when the entire crude liquid product has passed through the vented filter and been loaded onto the HPLC loop.

Vented filter for automatic HPLC loop loading

The present invention relates to novel radioactively labeled bioreducible tracers of Formula I useful for detecting hypoxic tumors or ischemic tissue in vivo. In one embodiment, the tracers consist of a 2-nitroimidazole moiety, a triazole, metabolically stable linker with pharmacokinetics enhancing substituents, and a radioisotope. The preferred in vivo imaging modality is positron emission tomography. 

Nitro-imidazole hypoxia imaging agent

Nitro-imidazole hypoxia imaging agents

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Perkasie, PA, United States of America

Thomas Lee Collier