90259-60-2Relevant academic research and scientific papers
Synthesis of Diverse 11C-Labeled PET Radiotracers via Direct Incorporation of [11C]CO2
Mossine, Andrew V.,Brooks, Allen F.,Jackson, Isaac M.,Quesada, Carole A.,Sherman, Phillip,Cole, Erin L.,Donnelly, David J.,Scott, Peter J. H.,Shao, Xia
, p. 1382 - 1389 (2016)
Three new positron emission tomography (PET) radiotracers of interest to our functional neuroimaging and translational oncology programs have been prepared through new developments in [11C]CO2 fixation chemistry. [11C]QZ (glutaminyl cyclase) was prepared via a tandem trapping of [11C]CO2/intramolecular cyclization; [11C]tideglusib (glycogen synthase kinase-3) was synthesized through a tandem trapping of [11C]CO2 followed by an intermolecular cycloaddition between a [11C]isocyanate and an isothiocyanate to form the 1,2,4-thiadiazolidine-3,5-dione core; [11C]ibrutinib (Brutons tyrosine kinase) was synthesized through a HATU peptide coupling of an amino precursor with [11C]acrylic acid (generated from [11C]CO2 fixation with vinylmagnesium bromide). All radiochemical syntheses are fully automated on commercial radiochemical synthesis modules and provide radiotracers in 1-5% radiochemical yield (noncorrected, based upon [11C]CO2). All three radiotracers have advanced to rodent imaging studies and preliminary PET imaging results are also reported.
3-heteroalkyl-2,4.quinzaoline-diones
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, (2008/06/13)
A compound is described which is selected from the group consisting of those of the formula: wherein A is a divalent moiety of the formula:, -CnH2n- -CH2CH=CHCH2- or and n is an integer from 2-10, inclusive;, R is hydrogen, oxygen or alkyl having from one to four carbon atoms;, Z is C or N; and when, Z is N, ---is when, Z is C and R is oxygen, ---is ―――; and when, Z is C and R is alkyl, ---is R6 is hydrogen or alkyl having from one to four carbon atoms;, R1 and R2 may be the same or different and may be selected from the group consisting of hydrogen, halogen, trifluoromethyl, alkoxy having from one to four carbon atoms, alkyl having from one to four carbon atoms, nitro and amino; wherein Heteroaryl is wherein R3 and R4 may be selected from hydrogen, alkyl having from one to four carbon atoms, or phenyl; and, X is CH or N, together with the pharmaceutically acceptable salts thereof as well as a process for producing the same and its use for pharmaceutical processes.
3-heteroalkyl-2,4-quinzaolinediones
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, (2008/06/13)
Compounds of the formula: STR1 wherein A is a divalent moiety of the formula: or STR2 wherein n is an integer from 2-10, inclusive; R is hydrogen or alkyl having from one to four carbon atoms; R1 and R2 may be the same or different and may be selected from the group consisting of hydrogen, halogen, trifluoromethyl, alkoxy having from one to four carbon atoms, alkyl having from one to four carbon atoms, nitro and amino; wherein Heteroaryl is STR3 wherein R3 and R4 may be selected from hydrogen, alkyl having from one to four carbon atoms, or phenyl; and X is CH or N, together with the pharmaceutically acceptable salts thereof, which act as thromboxane synthetase inhibitors and hypotensive agents; methods for their production and use.
Thromboxane synthetase inhibitors and antihypertensive agents. 4. N-[(1H-imidazol-1-yl)alkyl] derivatives of quinazoline-2,4(1H,3H)-diones, quinazolin-4(3H)-ones, and 1,2,3-benzotriazin-4(3H)-ones
Wright Jr.,Tomcufcik,Chan,Marisco,Press
, p. 2277 - 2283 (2007/10/02)
The quinazolinedione, quinazolinone, and 1,2,3-benzotriazinone title compounds were prepared as analogues of N-[(1H-imidazol-1-yl)alkyl]-1H-isoindole-1,3(2H)-diones which were the subject of a previous report from our laboratories. These compounds were ev
3-imidazolylalkyl-, triazolylalkyl-, pyridinylalkyl-1,2,3-benzotriazin-4(3H)-ones and derivatives thereof
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, (2008/06/13)
Novel 3-heteroarylalkyl-1,2,3-benzotriazin-4(3H)-ones, having the structural formula: STR1 wherein A is a divalent moiety of the formula: STR2 wherein n is an integer from 3 to 10, inclusive; R1 and R2 may be the same or different an
3-heteroarylalkyl-4-quinazolinones
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, (2008/06/13)
Novel 3-heteroarylalkyl-4-quinazolinones which are useful as inhibitors of thromboxane synthetase and/or as antihypertensive agents in the treatment of hypertension and myocardial ischemia.
N-[2-4-(1H-Imidazol-1-yl)alkyl]-arylamides and pharmaceutical compositions
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, (2008/06/13)
This disclosure describes novel N-[ω-(1H-imidazol-1-yl)alkyl]arylamides which possess the property of inhibiting the enzyme thromboxane synthetase and are also useful in the treatment of hypertension and myocardial ischemia.
Hypoglycaemic and hypolipidaemic benzamide substituted (1H-) imidazole derivatives and compositions
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, (2008/06/13)
Benzamide derivatives of the general formula: STR1 wherein A represents a divalent straight- or branched-chain alkylene group containing from 1 to 6 carbon atoms and R1 represents a halogen atom or a hydroxy, mercapto, amino, nitro, cyano, carb
