27646-80-6Relevant academic research and scientific papers
1,2,3,5-TETRAHYDROIMIDAZO[1,2-C]PYRIMIDINE DERIVATIVES USEFUL IN THE TREATMENT OF DISEASES AND DISORDERS MEDIATED BY LP-PLA2
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Page/Page column 29; 31, (2016/02/18)
The present invention relates to novel compounds that inhibit Lp‐PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases or disorders associated with the activity of Lp‐PLAs
2,3-DIHYDROIMIDAZOL[1,2-C]PYRIMIDIN-5(1H)-ONE BASED LIPOPROTEIN-ASSOCIATED PHOSPHOLIPASE A2 (LP-PLA2) INHIBITORS
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Page/Page column 27-28, (2014/08/07)
The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
HYDROXYMORPHOLINESS AND THEIR USE FOR THE TREATMENT OF INFLAMMATORY DISORDERS AND PAIN
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Page/Page column 10, (2010/10/03)
A compound useful for therapy of a pain or inflammatory condition, is of formula (I): wherein: R1 is aryl or heteroaryl and is optionally substituted with one or more groups selected from alkyl, CF3, OR6, OCOR6, CONH2, CN, Cl, Br, I, N(R6)2,NO2, NHCHO, NHCONH2, NHSO2R6, CON(R6)2, S(O)nR6, CH2OH and OCON(R6)2 wherein n is 0-2; R2 and R3 are each H, alkyl, cycloalkyl or CH2 OH, or CR2R3 forms a ring; R4 is H or alkyl; and R6 is H, alkyl or cycloalkyl; or a salt thereof.
Synthesis, conformation, crystal structures and DNA cleavage abilities of tetracyclic analogs of quinocarcin
Williams, Robert M.,Glinka, Tomasz,Gallegos, Renee,Ehrlich, Paul P.,Flanagan, Mark E.,Coffman, Hazel,Park, Gyoosoon
, p. 2629 - 2642 (2007/10/02)
Two totally synthetic, racemic analogs of quinocarcin have been designed and their crystal structures determined. Both substances effect the modest cleavage of plasmid DNA. Alteration of the conformation of the reactive oxazolidine fused to the piperazine
N-Alkyl-5,5-dimethyl-2-oxomorpholin-3-yl radicals. Characterization and reaction with molecular oxygen
Benson Jr., Okster,Demirdji, Samuel H.,Haltiwanger, R. Curtis,Koch, Tad H.
, p. 8879 - 8886 (2007/10/02)
The synthesis of bi(4,5,5-trimethyl-2-oxomorpholin-3-yl) (TM-3′ dimer), bi(5,5-dimethyl-4-cthyl-2-oxomorpholin-3-yl) (DEM-3 dimer), and bi(5,5-dimethyl-4-isopropyl-2-oxomorpholin-3-yl) (DIM-3 dimer) by one-electron oxidation of 4,5,5-trimethyl-2-oxomorpholine (8), 5,5-dimethyl-4-ethyl-2-oxomorpholine (9), and 5,5-dimethyl-4-isopropyl-2-oxomorpholine (10), respectively, with photochemically generated rert-butoxyl radical is described. dl-TM-3′ dimer, meso-DEM-3 dimer, and meso-DIM-3 dimer were characterized from spectra and by X-ray crystallography. In solution the radical dimers existed in equilibrium with the captodatively substituted radicals, 4,5,5-trimethyl-2-oxomorpholin-3-yl (TM-3′), 5,5-dimethyl-4-ethyl-2-oxomorpholin-3-yl (DEM-3), and 5,5-dimethyl-4-isopropyl-2-oxomorpholin-3-yl (DIM-3), respectively, as indicated by EPR spectroscopy. The activation parameters for bond homolysis in ethanol solvent were measured by oxidatively trapping the radicals with diphenylpicrylhydrazyl (DPPH). The half-lives for bond homolysis vary by S orders of magnitude at 25°C with a value of only 2.3 s for DIM-3 dimer. DIM-3 dimer reacted quantitatively with molecular oxygen to form a mixture of meso- and dl-bis(5,5-dimethyl-4-isopropyl-2-oxomorpholin-3-yl) peroxides (DIM-3 peroxides), which were isolated and characterized spectroscopically and analytically. At ambient temperature the peroxides fragmented by C-O bond homolysis to release the DIM-3 radical as indicated by EPR spectroscopy and were solvolyzed by protic solvent with release of hydrogen peroxide. The solvolysis was reversed by evaporation of the protic solvent, which restored most of the DIM-3 peroxides. The peroxides also slowly fragmented irreversibly to 5,5-dimethyl-3-hydroxy-4-isopropyl-2-oxomorpholine (21) and 5,5-dimethyl-2,3-dioxo-4-isopropylmorpholine (23) in polar aprotic solvent.
