- SSAO INHIBITORS AND USE THEREOF
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Provided are a compound of formula (I') or (I), a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of SSAO, a pharmaceutical composition comprising a compound of formula (I') or (I), and a method of treating or preventing a disease in which SSAO plays a role.
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Paragraph 00260
(2021/05/07)
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- Studies on the synthesis, stability and conformation of 2-sulfonyl-oxetane fragments
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2-(Arylsulfonyl)oxetanes have been prepared as new structural motifs of interest for medicinal chemistry. These are designed to fit within fragment space and be suitable for screening in fragment based drug discovery, as well as being suitable for further elaboration or incorporation into drug-like compounds. The oxetane ring is constructed through an efficient C-C bond forming cyclisation which allows the incorporation of a wide range of aryl-sulfonyl groups. Furthermore, biaryl-containing compounds can be accessed through Suzuki-Miyaura coupling from halogenated derivatives. With a number of oxetane containing fragment compounds available, their pH stability was assessed, indicating good half-life values for mono-substituted aryl sulfonyl oxetanes across the pH range (1 to 10). Solubility and metabolic stability data is also reported. Finally, the conformation of the fragments is assessed computationally, providing an indication of possible binding orientations.
- Morgan,Hollingsworth,Bull
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supporting information
p. 5265 - 5272
(2015/05/13)
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- SYNTHESIS AND CONFIGURATIONAL STUDIES OF ARYL CYCLOPROPYL SULFONES
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The cycloaddition of arylthiocarbenes to styrene gave stereospecifically cis-1-(arylthio)-2-phenylcyclopropanes, which were subsequently oxidized to the corresponding sulfones.The cyclopropanation of α,β-unsaturated sulfones with dimethylsulfonium methylide yielded stereoselectively trans-1-(arylsulfonyl)-2-arylcyclopropanes.The configurational assignments of these compounds have been arrived at on the basis of IR and PMR spectral data.Chemical shifts for ring protons and other substituents reveal that all the substituents tend to cause protons cis to them to appear at higher fields than those trans to them.This has been used as a criterion to distinguish between cis and trans aryl cyclopropyl sulfones.
- Reddy, D. Bhaskar,Balaji, T.,Reddy, B. Venkataramana
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p. 297 - 306
(2007/10/02)
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- Novel Alumina-catalysed Reactions of Arylthioalkyl Halides and Related Compounds
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Arylthioalkyl halides of the type ArS(CH2)nCl (Ar = phenyl or substituted phenyl, n = 1-4) undergo rearrangement on heating with neutral alumina to 1,n-bis(arylthio)alkanes of type ArS(CH2)nSAr in high yield.Similar rearrangements occur with some closely related structural types.The bis(arylthio)alkanes undergo further reaction with alumina at higher temperatures in air giving diaryl disulphides.Bis(o-iodophenylthio)methane eliminates iodine on heating with alumina, producing dibenzodithiepin.Some observations concerning the mechanism are presented.
- Jigajinni, Veerappa B.,Wightman, Richard H.
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p. 1801 - 1812
(2007/10/02)
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