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Conformationally strained trans-cycloalkenes for radiolabeling

A technology of objects and compounds, applied in the directions of in vivo radioactive preparations, radioactive carriers, preparations for in vivo experiments, etc., can solve problems such as short half-life fluorides

Inactive Publication Date: 2019-04-16
UNIVERSITY OF DELAWARE +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, 18 The short half-life of F, the moderate nucleophilicity of fluoride, and the inherently low concentrations for both biology and radiochemistry make it possible to 18 F introduction into complex biomolecules is challenging

Method used

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  • Conformationally strained trans-cycloalkenes for radiolabeling
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  • Conformationally strained trans-cycloalkenes for radiolabeling

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Embodiment

[0058] Materials and methods

[0059]All commercially available analytical grade chemicals were purchased from Aldrich (St. Louis, MO) and used without further purification. Analytical reversed-phase HPLC using a Gemini 5 μC18 column (250 x 4.6 mm) was performed on a SPD-M30A photodiode array detector (Shimadzu) and a model 105S single channel radiation detector (Carroll & Ramsey Associates). Radioactive HPLC analysis was performed at 1 mL / min with a water / acetonitrile eluent mixture. For other HPLC analyses, the solvent was modified with 0.1% trifluoroacetic acid.

[0060] Stopped Flow Kinetic Analysis

[0061] Using an excess of the appropriate sTCO diastereomer (4 or 5) under pseudo-first-order conditions, and by following the 11 attributable to 11 measured at 298 nm using a SX 18MV-R stopped-flow spectrophotometer (Applied Photophysics Ltd.) The exponential decay of the absorbance of the tetrazine chromophore is used to measure the second order rate constant. For each ...

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Abstract

Conformationally strained irans-cycloalkenes and derivatives thereof suitable for radiolabeling in a subject in need thereof.

Description

[0001] This application claims priority to US Application No. 62 / 267,441 filed December 15, 2015, the entire contents of which are hereby incorporated by reference for all purposes. Background of the invention [0002] Positron emission tomography (PET) is a non-invasive imaging modality capable of tracking radiolabeled biomolecules in vivo. This imaging technique uses radionuclides that emit positrons that collide with electrons and produce two detectable gamma rays. Among the common radionuclides used in PET, 18 F is the most widely used due to high positron efficiency, high specific radioactivity, and clinically attractive half-life (-110 minutes). These properties minimize toxic effects and radiation exposure to the patient. However, 18 The short half-life of F, the moderate nucleophilicity of fluoride, and the inherently low concentrations for both biology and radiochemistry make it possible to 18 The introduction of F into complex biomolecules is challenging. Theref...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/04C07D257/08
CPCA61K51/082A61K51/088C07B59/001C07B59/002C07B2200/05C07C43/172C07C309/72C07D225/02C07D257/02C07D311/44C07D313/18C07D403/12C07D405/12C07F7/0812C07C2602/24C07C2602/26C07D225/00C07D317/44C07F1/08C07F5/00C07F7/0807C07F7/0816
Inventor 约瑟夫·福克斯李子博刘雨迈克尔·汤普森·泰勒丹尼斯·斯瓦图内克卡塔琳娜·罗尔芬王梦哲吴战宏拉古·万纳马史蒂芬·华莱士贾森·W·秦
Owner UNIVERSITY OF DELAWARE