- PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND METHODS OF USE THEREOF
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Provided herein are compounds, compositions, and methods useful for inhibiting protein tyrosine phosphatase, e.g., protein tyrosine phosphatase non-receptor type 2 (PTPN2) and/or protein tyrosine phosphatase non-receptor type 1 (PTPN1), and for treating related diseases, disorders and conditions favorably responsive to PTPN 1 or PTPN2 inhibitor treatment, e.g., a cancer or a metabolic disease.
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Paragraph 00533
(2020/09/27)
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- 2-(pyrazol-4-yl)-1,3-oxaselenolanes from pyrazole carbaldehydes and 2-selanyl-1-ethanol
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Pyrazole carbaldehydes react with 2-selanyl-1-ethanol at room temperature in the presence of trimethylchlorosilane followed by treatment C with triethyl amine to afford the corresponding 2-(pyrazol-4-yl)-1,3-oxaselenolanes. The structure of the novel compounds was confirmed by IR, 13 C, 1 H, 15N, and 77 Se NMR spectroscopy.this article online at wileyonlinelibrary.com.
- Papernaya, Lyubov K.,Shatrova, Alexandra A.,Levanova, Ekaterina P.,Albanov, Alexandr I.,Klyba, Lyudmila V.,Rudyakova, Elena V.,Levkovskaya, Galina G.
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- Synthesis of heterocyclic compounds from 4-formylpyrazoles
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Formylation of pyrazole and 2,5-dimethylpyrazole gave a number of pyrazole-containing aldehydes, which can be used to obtain chromenes, tetrahydrochromenes, 1,4-dihydropyrano[2,3-c]pyrazoles, pyrano[3,2-c]chromenes, thiochromeno[4,3-b]pyrans, pyrano[3,2-c
- Mortikov,Rodinovskaya,Fedorov,Shestopalov,Belyakov
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p. 443 - 456
(2015/02/02)
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- Selenoacetalyzation of 4-formylpyrazoles in the presence of trimethylchlorosilane
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The reaction of 3,5-dimethyl-4-formylpyrazoles, bearing various substituents at N-1 atom, with propane-1,3-diselenol and 2-hydroxypropane-1,3- diselenol in the presence of Cyrillic capital letter teCyrillic capital letter emSCl proceeds without heating to
- Papernaya, Lyubov K.,Shatrova, Alexandra A.,Levanova, Ekaterina P.,Albanov, Alexandr I.,Klyba, Lyudmila V.,Rudyakova, Elena V.,Levkovskaya, Galina G.
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p. 466 - 475
(2013/12/04)
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- Fragmentation of pyrazolecarbaldehyde thio- and dithioacetals under electron impact and chemical ionization
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The mass spectra of 1-substituted 3,5-dimethyl-1H-pyrazole-4-carbaldehyde bis(2-hydroxyethyl) dithioacetals and thioacetals were studied for the first time. The main fragmentation pathways of their molecular ions generated under electron impact and chemic
- Klyba,Papernaya,Sanzheeva,Shatrova,Rudyakova,Levkovskaya
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p. 1851 - 1858
(2012/03/11)
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- Vilsmeier-Haak formylation of 3,5-dimethylpyrazoles
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Formylation of N-alkyl-3,5-dimethyl-1H-pyrazoles according to Vilsmeier-Haak led to the formation of the corresponding 4-formyl derivatives. 3,5-Dimethyl-1H-pyrazole having no substituent on the nitrogen atom failed to undergo formylation at the 4 position under analogous conditions. 3,5-Dimethyl-1H-pyrazole-4-carbaldehyde was synthesized by alkaline hydrolysis of methyl β-(4-formyl-3,5-dimethyl-1H-pyrazol-1-yl)propionate and subsequent heating of the acid thus formed.
- Attaryan,Antanosyan,Panosyan,Asratyan,Matsoyan
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p. 1817 - 1819
(2008/02/08)
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- Formation of Indoles, Isoquinolines, and Other Fused Pyridines from Azidoacrylates
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Mild thermal decomposition in boiling toluene or xylene of the azidocinnamates (1) - (6), readily prepared from the corresponding aldehyde and ethyl azidoacetate, gives indoles in good yield when there is an unsubstituted ortho position, and dihydroisoquinolines, and hence isoquinolines, when there is an o-methyl or methylene group.In the presence of iodine, which seems to favour a radical type process, the yield of isoquinoline is increased, and isoquinoline formation can compete with the indole-forming cyclisation to a free ortho-position.Iodine also catalyses primary enamine formation by a hydrogen abstraction process.The thiophene (7) and pyrazole (8) are formed and decomposed similarly to give the corresponding c-fused pyridines (28) and (29).The 2,6-dichloro compound (9) thermolyses to the stable 2H-azirine (32) which isomerises to the nitrile (33) on stronger heating.Yields in these azide decompositions are sometimes high, though they can be variable and the reactions, though easily carried out, can be complex
- Henn, Lothar,Hickey, Deirde M. B.,Moody, Christopher J.,Rees, Charles W.
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p. 2189 - 2197
(2007/10/02)
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