- DEUTERATED SGC STIMULATORS
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The present disclosure relates to stimulators of soluble guanylate cyclase (sGC), pharmaceutical formulations comprising them and their uses thereof, alone or in combination with one or more additional agents, for treating various diseases, wherein an increase in the concentration of nitric oxide (NO) or an increase in the concentration of cyclic Guanosine onophosphate (cGMP), or both, or an upregulation of the NO pathway is desirable. The compounds are of Formula I: or a pharmaceutically acceptable salt thereof, wherein each of Y1, Y2, Y3, Y4, Y5, Y6, Y7, Y8 and Y9 is independently selected from hydrogen and deuterium, as well as pharmaceutical compositions, methods and uses thereof.
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- H-D Exchange Deuteration of Arenes at Room Temperature
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Arene nuclei efficiently underwent the hydrogen (H)-deuterium (D) exchange reaction catalyzed by platinum group metals on carbon in a mixed solvent of 2-propanol and D2O at room temperature to produce deuterium-labeled arenes. Platinum on carbon (Pt/C) and iridium on carbon (Ir/C) were applicable catalysts, and the various arenes bearing a carbonyl group, fluorine, phenolic hydroxy group, amino group, or phosphonic acid on the aromatic nucleus were effectively deuterated. Nonheating conditions are valuable for the scalable industrial preparation.
- Sawama, Yoshinari,Nakano, Akihiro,Matsuda, Takumi,Kawajiri, Takahiro,Yamada, Tsuyoshi,Sajiki, Hironao
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supporting information
p. 648 - 653
(2019/02/14)
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- HYDROGEN ISOTOPE-ENRICHED ANALOGUES OF 1,2,4-OXANDIAZOLE BENZOIC ACID COMPOUNDS, COMPOSITIONS AND USES THEREOF
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Novel hydrogen isotope-enriched 1,2,4-oxadiazole benzoic acid compounds, methods of their use and pharmaceutical compositions thereof are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature tra
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Paragraph 00157
(2017/07/14)
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- Synthesis of substituted indoles and carbazoles from 2-fluorophenyl imines
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The synthesis of a series of indole and carbazole derivatives from 2-fluorophenyl imines is reported. 2-Fluoroaniline-d4 (13) is prepared and used to investigate the mechanism of this indolization. 2-Fluorophenyl enaminone 17 gives the synthetically useful carbazole 20 via a similar indolization and in situ alkylation.
- Kudzma, Linas V.
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p. 1661 - 1666
(2007/10/03)
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