- Chemoselective photochemical surface reaction - Ketene versus carbene reactivity from the photolysis of saturated monolayers of pyridyl diazoesters on single-crystal Pt
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Irradiation of saturated monolayers of 3-and 4-substituted pyridyl diazoacetates on single-crystal Pt surfaces leads to either the corresponding reactive carbene or stable ketene intermediate with the chemoselectivity determined by the position of the photoreactive substituent on the pyridyl ring, which ultimately directs the available interactions with neighboring substrates.
- Pitters, Jason L.,Adkinson, Dana K.,Griffiths, Keith,Norton, Peter R.,Workentin, Mark S.
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- NOVEL UREA 6,7-DIHYDRO-4H-PYRAZOLO[1,5-A]PYRAZINES ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for making the compounds.
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Page/Page column 37
(2020/05/29)
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- NOVEL 6,7-DIHYDRO-4H-PYRAZOLO[1,5-A]PYRAZINE INDOLE-2-CARBOXAMIDES ACTIVE AGAINST THE HEPATITIS B VIRUS (HBV)
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The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for mating the compounds.
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Page/Page column 86; 87
(2020/05/29)
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- LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS
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Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
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Paragraph 1253; 1254
(2014/07/23)
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- 3-Substituted indolizine-1-carbonitrile derivatives as phosphatase inhibitors
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In the course of studies directed toward the discovery of novel scaffolds for medicinal application, we synthesized a series of 3-substituted indolizine-1-carbonitrile derivatives. Some of them displayed activity against MPtpA/MPtpB phosphatases which are involved in infectious diseases. We report here the solid-phase synthesis and antiphosphatase activity of a series of indolizines.
- Weide, Timo,Arve, Lars,Prinz, Heino,Waldmann, Herbert,Kessler, Horst
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- Hydration of pyridylketenes: Formation of acid enol and dihydropyridine (Eneaminone) transients
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2-, 3-, and 4-Pyridylketenes 4 formed in water by photochemical Wolff rearrangements using flash photolysis undergo rapid hydration forming transient intermediates observed by UV spectroscopy. 3-Pyridylketene (3-4) formed the acid enol intermediate 3-10 which was converted to the acid 3-11, and phenylketene gave similar behavior. 4-Pyridylketene (4-4) reacted with a similar initial rate constant of 5.0 × 104 s-1 for decay of an absorption at 275 nm, with concomitant formation of a strong absorption at 370 nm with the same rate constant. The intermediate absorbing at 370 nm decayed with a lifetime 2.4 × 103 fold longer than that of the ketene, and is identified as 4-(carboxymethylene)-1,4-dihydropyridine (4-13), resulting from conjugate 1,6-addition of H2O to 4-4. 2-Pyridylketene (2-4) underwent hydration with a similar rate constant of 1.1 × 104 s-1 forming a transient with a UV absorption with maxima at 310 and 380 nm that decayed with biexponetial kinetics, with rate constants slower than the rate of formation by factors of 5.2 and 110, respectively. These results are interpreted as indicating the presence of two species, namely Z- and E-2-(carboxymethylene)-1,2-dihydropyridines (2-13), resulting from conjugate 1,4-addition of H2O to 2-4. The identifications of the 1,2- and 1,4-(carboxymethylene)dihydropyridines 2- and 4-13 were confirmed by comparison of their UV spectra with those of the corresponding N-methyl derivatives. The amination of 2-pyridylketene in CH3CN was reinvestigated, and spectroscopic evidence, computational studies, and preparation of the N-methyl analogue demonstrated formation of the 1,2-dihydropyridine Z-2-8f as the long-lived intermediate.
- Allen, Annette D.,Fedorov, Andrei V.,Tidwell, Thomas T.,Vukovic, Sinisa
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p. 15777 - 15783
(2007/10/03)
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