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Title: Radio-methyl vorozole and methods for making and using the same

Patent ·
OSTI ID:1150009
; ;

Radiotracer vorozole compounds for in vivo and in vitro assaying, studying and imaging cytochrome P450 aromatase enzymes in humans, animals, and tissues and methods for making and using the same are provided. [N-radio-methyl] vorozole substantially separated from an N-3 radio-methyl isomer of vorozole is provided. Separation is accomplished through use of chromatography resins providing multiple mechanisms of selectivity.

Research Organization:
Brookhaven National Laboratory (BNL), Upton, NY (United States)
Sponsoring Organization:
USDOE
DOE Contract Number:
AC02-98CH10886
Assignee:
Brookhaven Science Associates, LLC (Upton, NY)
Patent Number(s):
8,795,629
Application Number:
12/704,114
OSTI ID:
1150009
Country of Publication:
United States
Language:
English

References (16)

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Preparation and comparison of a pentafluorophenyl stationary phase for reversed-phase liquid chromatography journal January 1990
Chromatographic classification and comparison of commercially available reversed-phase liquid chromatographic columns containing phenyl moieties using principal component analysis journal June 2007
Distribution of Aromatase Cytochrome P450 Messenger Ribonucleic Acid in Adult Rhesus Monkey Brains1 journal October 1997
Unique distribution of aromatase in the human brain: In vivo studies with PET and [N-methyl-11C]vorozole journal April 2010
Development Summary towards a Manufacturable Process for R 83842 [( S )-6-[(4-chlorophenyl) (1H-1,2,4-triazol-1-yl)methyl]-1-methyl-1H-benzotriazole] † journal May 2000
Comparative evaluation of positron emission tomography radiotracers for imaging the norepinephrine transporter: (S,S) and (R,R) enantiomers of reboxetine analogs ([11C]methylreboxetine, 3-Cl-[11C]methylreboxetine and [18F]fluororeboxetine), (R)-[11C]nisox: Norepinephrine transporter radiotracers for PET journal June 2005
Synthesis and PET studies of [11C-cyano]letrozole (Femara), an aromatase inhibitor drug journal February 2009
Synthesis and activity of 1H-benzimidazole and 1H-benzotriazole derivatives as inhibitors of Acanthamoeba castellanii journal May 2004
Controversies of aromatase localization in human breast cancer—Stromal versus parenchymal cells journal August 2007
Aromatase inhibition by R 76713: Experimental and clinical pharmacology journal January 1989
R 76713, a new specific non-steroidal aromatase inhibitor journal June 1989
Comparative effects of the aromatase inhibitor R76713 and of its enantiomers R83839 and R83842 on steroid biosynthesis in vitro and in vivo journal December 1990
1H,6H-Triazolo[4,5-e]benzotriazole-3-oxides and 5,5’-(Z)-Diazene-1,2-diylbis(2-methyl-2H-1,2,3-benzotriazole) Derived from Chloronitrobenzotriazoles and Hydrazine journal August 2005
Reinvestigation of the synthesis and evaluation of [N-methyl-11C]vorozole, a radiotracer targeting cytochrome P450 aromatase journal April 2009

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Related Subjects

37 INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY