147972-27-8Relevant articles and documents
Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives
Gillespie, Roger J.,Adams, David R.,Bebbington, David,Benwell, Karen,Cliffe, Ian A.,Dawson, Claire E.,Dourish, Colin T.,Fletcher, Allan,Gaur, Suneel,Giles, Paul R.,Jordan, Allan M.,Knight, Antony R.,Knutsen, Lars J.S.,Lawrence, Anthony,Lerpiniere, Joanne,Misra, Anil,Porter, Richard H.P.,Pratt, Robert M.,Shepherd, Robin,Upton, Rebecca,Ward, Simon E.,Weiss, Scott M.,Williamson, Douglas S.
, p. 2916 - 2919 (2008/12/22)
The (-)-(11R,2′S)-enantiomer of the antimalarial drug mefloquine has been found to be a reasonably potent and moderately selective adenosine A2A receptor antagonist. Further investigation of this compound has led to the discovery of a series of keto-aryl thieno[3,2-d]pyrimidine derivatives, which are potent and selective antagonists of the adenosine A2A receptor. These derivatives show selectivity against the A1 receptor. Furthermore, some of these compounds have been shown to have in vivo activity in a commonly used model, suggesting the potential for the treatment of Parkinson's disease.
Substituted quinazolines as angiotensin II antagonists
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, (2008/06/13)
There are disclosed compounds of the general formula I: STR1 wherein A is --CR7 =CR8 --; Z is --CR7 =CR8 --; X is H, NR 9 R10, OR11, CN, F, Cl, I, Br, perfluoroalkyl, alkyl,alkoxy, alkyl-OH, alkoxyalkyl, --(CH2)n CO2 R11,--(CH2)n CONR9 R10 ; Y is NR13,NR13 CR12 R14, CR12 R14 NR13 ; R1 is 5-tetrazolyl, CO2 R11,SO3 H, NHSO2 CH3, NHSO2 CF3 ; R2,R3,R4,R7 R8 is H, alkyl, alkoxy, alkoxyalkyl, alkyl-OH, perfluoroalkyl, aralkyl, CN, NO2, SO2 R13, --(CH2)n CO2 R11,--(CH2)n CONR9 R10, OR11,F,Cl,Br,I,NR9 R10 ; R5 is alkyl, alkoxy, alkoxyalkyl, alkyl-OH, perfluoroalkyl, aralkyl, H, --CN, NO2, SO2 R13,--(CH2)n CO2 R11, --(CH2)n CONR9 R10, --OH,OR11,F,Cl,Br,I,NR9 R10 ; R9,R10 is H, alkyl, alkoxyalkyl,alkyl-OH, perfluoroalkyl, aralkyl; R11 is H, alkyl, aralkyl, alkoxyalkyl; R12,R14 is H, alkyl, alkoxy, alkoxyalkyl, alkyl-OH, perfluoroalkyl, aralkyl, CN, NO2, SO2 R13, --(CH2)n CO2 R11, --(CH2)n CONR9 R10 ; R13 is H, OR11, alkyl, perfluoroalkyl, aralkyl, --(CH2)n CO2 R11,--(CH2)n CONR9 R10 ; wherein alkyl is defined as 1-8 carbons, branched or straight chain; perfluoroalkyl is defined as 1-6 carbons; aralkyl is defined as 7-12 carbons or 7-12 carbons substituted with fluorine, bromine or chlorine and the phamaceutically acceptable salts, solvates and hydrates thereof, which by virtue of their ability to antagonize angiotensin II are useful for the treatment of hypertension and congestive heart-failure. The compounds are also useful for reducing lipid levels in the blood plasma and are thus useful for treating hyperlipidemia and hypercholesterolemia. Also disclosed are processes for the production of said compounds and pharmaceutical compositions containing said compounds.