Title:
PET PROBES OF RADIOFLUORINATED CARBOXIMIDAMIDES FOR IDO-TARGETED IMAGING
Document Type and Number:
WIPO Patent Application WO/2016/040458
Kind Code:
A3
Abstract:
18F labeled ID01 imaging constructs are constructed for positron emission tomography (PET). Synthetic methodology involves the coupling of a l-fluoro-2-halo-4- aminobenzene and a 4-amino-N-hydroxy-l,2,5-oxadiazole-3-carboximidoyl chloride wherein at least one of the coupled compounds comprises an 18F. The 18F labeled IDO1 imaging constructs are useful for imaging cancer cells in a patient.
Inventors:
TIAN HAIBIN (US)
GILLIES ROBERT J (US)
GILLIES ROBERT J (US)
Application Number:
PCT/US2015/049152
Publication Date:
May 19, 2016
Filing Date:
September 09, 2015
Export Citation:
Assignee:
H LEE MOFFITT CANCER CT & RES (US)
International Classes:
C07D273/02; A61K49/00; A61K51/04
Domestic Patent References:
| WO2006122150A1 | 2006-11-16 |
Other References:
LAZAROVA, N. ET AL.: "Integration of a microwave reactor with Synthia to provide a fully automated radiofluorination module.", JOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, vol. 50, no. 5-6, 2007, pages 463 - 465
SUGAE, S. ET AL.: "Fluorine-18-labeled 5-fluorouracil is a useful radiotracer for differentiation of malignant tumors from inflammatory lesions.", ANNALS OF NUCLEAR MEDICINE, vol. 22, no. 1, 2008, pages 65 - 72
YUE, E. W. ET AL.: "Discovery of potent competitive inhibitors of indoleamine 2, 3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model.", JOURNAL OF MEDICINAL CHEMISTRY, vol. 52, no. 2, 2009, pages 7364 - 7367
HUANG, X. ET AL.: "Synthesis of [18F] 4-amino-N-(3-chloro-4-fluorophenyl) -N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide (ID05L): a novel potential PET probe for imaging of IDO1 expression.", JOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, vol. 58, no. 4, pages 156 - 162
SUGAE, S. ET AL.: "Fluorine-18-labeled 5-fluorouracil is a useful radiotracer for differentiation of malignant tumors from inflammatory lesions.", ANNALS OF NUCLEAR MEDICINE, vol. 22, no. 1, 2008, pages 65 - 72
YUE, E. W. ET AL.: "Discovery of potent competitive inhibitors of indoleamine 2, 3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model.", JOURNAL OF MEDICINAL CHEMISTRY, vol. 52, no. 2, 2009, pages 7364 - 7367
HUANG, X. ET AL.: "Synthesis of [18F] 4-amino-N-(3-chloro-4-fluorophenyl) -N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide (ID05L): a novel potential PET probe for imaging of IDO1 expression.", JOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, vol. 58, no. 4, pages 156 - 162
Attorney, Agent or Firm:
EISENSCHENK, Frank, C. et al. (Lloyd & EisenschenkPo Box 14295, Gainesville FL, US)
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