Nitro-imidazole hypoxia imaging agent

US7977361B2 · kind B2 · utility

Assignee

• Siemens Medical Solutions USA, Inc. · US

Inventors

• Thomas Lee Collier · Perkasie, US
• Brian A. Duclos · Kalamazoo, US
• Umesh B. Gangadharmath · Los Angeles, US
• Zhiyong Gao · Los Angeles, US
• Farhad Karimi · Mansfield, US
• Dhanalakshmi Kasi · Los Angeles, US
• Hartmuth C. Kolb · El Segundo, US
• Qianwa Liang · La Puente, US
• Henry Clifton Padgett · Hermosa Beach, US
• Joseph C. Walsh · Santa Monica, US
• Tieming Zhao · Los Angeles, US

Key dates

• Filing date: Jul 15, 2010
• Grant date: Jul 12, 2011
• Expiry date: Jul 15, 2030

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D403/12
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

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.