- Phenacylation of 6-methyl-beta-nitropyridin-2-ones and further heterocyclization of products
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Reaction between the derivatives of 6-methyl-beta-nitropyridin-2-one and phenacyl bromides was studied, and the yields observed were extremely low. The pyridones were converted via chloropyridines to methoxyderivatives, which were N-phenacylated. N-Phenacyl derivatives of 4,6-dimethyl-5-nitropyridin-2-one under the action of base gave 5-hydroxy-8-nitroindolizine and under acidic conditions gave 5-methyl-6-nitrooxazole[3,2-a]pyridinium salt, which underwent recycization with MeONa to 5-methoxy-8-nitroindolizine.
- Babaev, Eugene V.,Rybakov, Victor B.
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- OGA INHIBITOR COMPOUNDS
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The present invention relates to O-GIcNAc hydrolase (OGA) inhibitors of formula (I). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C90RF72 mutations.
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Page/Page column 65
(2020/01/11)
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- CRYSTAL FORMS OF AN IMIDAZOLE DERIVATIVE
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The invention relates to the essentially pure Λ/-[({2-[4-(2-Ethyl-4,6-dimethyl-1 H- imidazo[4,5-c]pyridin-1 -yl)phenyl]ethyl}amino)carbonyl]-4- methylbenzenesulfonamide Polymorph Forms A and B and to processes for the preparation of, compositions containi
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Page/Page column 28
(2008/06/13)
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- COMBINATIONS COMPRISING ALPHA-2-DELTA LIGANDS
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The instant invention relates to a combination of an EP4-receptor antagonist and an alpha-2-delta ligand, and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof and their use in the treatment of pain, particularly inflammatory,
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Page/Page column 95
(2008/06/13)
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- Use of EP4 receptor ligands in the treatment of IL-6 involved diseases
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Methods of treating IL-6 involved diseases with EP4 receptor ligands, including EP4 receptor antagonists. Assays to determine the effect of test compounds on PGE2-induced whole blood cells activation.
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- EP4 RECEPTOR INHIBITORS TO TREAT RHEUMATOID ARTHRITIS
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The invention features a method of treating rheumatoid arthritis in a mammal comprising administering an agent that inhibits prostaglandin EP4 receptor (EP4) activity. Also featured is a method of identifying agents that selectively inhibit EP4 activity in vivo.
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- Synthesis of 3-nitropyrid-2(1H)-ones from C-nitroacetamide and 1,3-dicarbonyl compounds
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The reaction of nitroacetamide with 1,3-dicarbonyl compounds afforded 3-nitropyrid-2(1H)-ones. The chemical reactivities of nitroacetamide and nitroacetohydrazide were compared.
- Kislyi,Shestopalov,Kagramanov,Semenov
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p. 539 - 542
(2007/10/03)
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- Synthesis and Evaluation of 2-Pyridinone Derivatives as HIV-1-Specific Reverse Transcriptase Inhibitors. 2. Analogues of 3-Aminopyridin-2(1H)-one
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A series of nonnulceoside 3-aminopyridin-2(1H)-one derivatives was synthesized and evaluated for HIV-1 RT inhibitory properties.Several analogs proved to be potent and highly selective antagonists with in vitro IC50 values as low as 19 nM in the enzyme assay using rC*dG as template*primer.Two compounds from this series, 3-amino>-5-ethyl-6-methylpyridin-2(1H)-one (34, L-697,639) and the corresponding 4,7-dichloro analogue (37, L-697,661) inhibited the spread of HIV-1 IIIb infection by 95percent in MT4 cell culture at concentrations of 25-50 nM and were selected for clinical trials as antiviral agents.
- Saari, Walfred S.,Wai, John S.,Fisher, Thorsten E.,Thomas, Craig M.,Hoffman, Jacob M.,et al.
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p. 3792 - 3802
(2007/10/02)
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- Studies on Diazepines. XXVIII. Syntheses of 5H-1,3-Diazepines and 2H-1,4-Diazepines from 3-Azidopyridines
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Photolysis of 2-unsubstituted (5a-f) and 2,4-disubstituted (5k, l) 3-azidopyridines in the presence of sodium methoxide resulted in ring expansion to give the 4-methoxy-5H-1,3-diazepines (8 and 18), presumably via the azirine intermediates 6 and 17 derived from the initially formed singlet 3-pyridylnitrenes by cyclization at the 2-position of the pyridine ring.On the other hand, in the photolysis of 2-substituted 3-azidopyridines (5g-j), the cyclization of the nitrenes occurred predominantly at the vacant 4-position giving rise to the 3-methoxy-2H-1,4-diazepines (13).Keywords--3-azidopyridine; photolysis; pyridylnitrene; ring expansion; 5H-1,3-diazepine; 2H-1,4-diazepine; azirine intermediate
- Sawanishi, Hiroyuki,Tajima, Kayoko,Tsuchiya, Takashi
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p. 4101 - 4109
(2007/10/02)
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