34750-23-7Relevant academic research and scientific papers
Microwave-assisted synthesis and antibacterial evaluation of new derivatives of 1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one
Ebrahimpour, Zahra,Shiri, Ali,Bakavoli, Mehdi,Seyedi, Seyed Mohammad,Bahreini, Masoumeh,Oroojalian, Fatemeh
, p. 49 - 53 (2016/02/19)
Synthesis of new 1,2-dihydro-3H-pyrazolo[3,4-d] pyrimidin-3-ones 4-6 starting with ethyl 4-hydroxy-2-methylthio-pyrimidine-5-carboxylate (1) under classical heating and microwave-induced conditions is reported. The antibacterial activities of the synthesized compounds were evaluated using chloramphenicol and streptomycin as reference drugs.
NITROGEN CONTAINING HETEROCYCLIC COMPOUNDS AS PIK3 -DELTA INHIBITORS
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, (2012/01/15)
Substituted bicyclic heteroaryls of the following formulae and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory o
Optimisation of pharmacokinetic properties in a neutral series of 11β-HSD1 inhibitors
Scott, James S.,Gill, Adrian L.,Godfrey, Linda,Groombridge, Sam D.,Rees, Amanda,Revill, John,Schofield, Paul,S?rme, Pernilla,Stocker, Andrew,Swales, John G.,Whittamore, Paul R.O.
, p. 6756 - 6761 (2013/01/14)
11β-HSD1 is increasingly seen as an attractive target for the treatment of type II diabetes and other elements of the metabolic syndrome. In this program of work we describe how a series of neutral 2-thioalkyl-pyridine 11β-HSD1 inhibitors were optimized in terms of their pharmacokinetic properties to give compounds with excellent bioavailability in both rat and dog through a core change to pyrimidine. A potential reactive metabolite issue with 4-thioalkyl-pyrimidines was circumvented by a switch from sulfur to carbon substitution.
SUBSTITUTED PYRIMIDIN-5-CARBOXAMIDES 281
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Page/Page column 41, (2009/10/30)
A compound of formula (I): and pharmaceutically-acceptable salts thereof wherein the variable groups are defined within; their use in the inhibition of 11betaHSD1, processes for making them and pharmaceutical compositions comprising them are also described.
PYRIMIDINES AS INHIBITORS OF PHOSPHOINOSITIDE -3-KINASES (PI3K)
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Page/Page column 41, (2008/06/13)
The present invention provides pyrimidines of Formula (I): wherein R4, R6, and Y have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment
2,4,5,6-Tetrasubstituted pyrimidines and salts thereof
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, (2008/06/13)
Compounds of the formula SPC1 Wherein R1 is alkoxy of 1 to 3 carbon atoms, morpholino, thiomorpholino, 1-oxido-thiomorpholino, 1,1-dioxido-thiomorpholino, or EQU1 where A is hydrogen, alkanoyl of 1 to 4 carbon atoms, alkenoyl of 2 to 4 carbon atoms, methoxy-(alkanoyl of 1 to 4 carbon atoms), carboxyl-(alkanoyl of 1 to 4 carbon atoms), acetyl-(alkanoyl of 1 to 4 carbon atoms), methoxy-(alkenoyl of 2 to 4 carbon atoms), carboxyl-(alkenoyl of 2 to 4 carbon atoms), acetyl-(alkenoyl of 2 to 4 carbon atoms), aminocarbonyl, mono(alkyl of 1 to 4 carbon atoms)-aminocarbonyl, di-(alkyl of 1 to 4 carbon atoms)-aminocarbonyl, methoxymethylaminocarbonyl, pyridinoyl, salicyloyl, furanoyl, or (alkyl of 1 to 3 carbon atoms)-sulfonyl, R2 is morpholino, thiomorpholino, 1-oxido-thiomorpholino, 1,1-dioxido-thiomorpholino, piperazino or N'-[acetyl-(alkanoyl of 1 to 3 arbon atoms)]-piperazino, R3 is hydrogen, chlorine, bromine, nitro, cyano, formyl, acetyl or carbalkoxy of 2 to 4 carbon atoms, and R4 is hydrogen, chlorine, bromine, cyano, carbalkoxy of 2 to 4 carbon atoms, alkyl of 1 to 6 carbon atoms, mono(carbalkoxy of 2 to 4 carbon atoms)-alkyl of 1 to 6 carbon atoms, di(carbalkoxy of 2 to 4 carbon atoms)-alkyl of 1 to 6 carbon atoms, hydroxyl, allyloxy, alkoxy of 1 to 6 carbon atoms, mercapto, allylmercapto, (alkyl of 1 to 6 carbon atoms)-mercapto, 1-oxidothiomorpholino, or where B is hydrogen, alkyl of 1 to 3 carbon atoms, cyclohexyl, phenyl, chloro-phenyl, carboxy-phenyl, carbomethoxy-phenyl or pyridyl, And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as the salts are useful as antithrombotics.
