5118-04-7Relevant academic research and scientific papers
NOVEL HETEROCYCLIC COMPOUNDS AS BET INHIBITORS
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Page/Page column 53-54; 70-72, (2022/01/24)
Provided are heterocyclic compounds of formula (I) as bromodomain and extraterminal (BET) inhibitors, pharmaceutical compositions comprising the compounds, their synthesis and their use for treating diseases and conditions wherein inhibition of one or more BET bromodomains provides a benefit.
Isoxazole compounds and pharmaceutical compositions containing them for treatment and prophylaxis of retroviruses diseases
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, (2008/06/13)
Substituted isoxazole derivatives of the formula STR1 in which R1 denotes lower alkyl, n denotes the integer 6, 7 or 8, A denotes a group of the formula STR2 and R2 denotes hydrogen, methyl, chlorine or bromine. The novel compounds have a pronounced antiviral action and can be employed for the treatment and prophylaxis of virus diseases.
Nitrogen-arylmethoxy-thiophene derivatives and acid addition salts thereof, and pharmaceutical preparations containing these compounds
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, (2008/06/13)
The invention relates to new nitrogen-arylmethoxy-thiophene derivatives of the formula I STR1 wherein the R--CH2 --O-group is in position 4 or 5 of the thiophene ring, R denotes a 2-pyridinyl- or 2-quinolinyl group and R1 denotes a --COO-lower alkyl-, --CO--(CH2)n--CH3 or --CH(OH)--(CH2)n --CH3 group, wherein n represents an integer from 2 to 6, and their hydrates and/or their pharmaceutically acceptable acid addition salts, a process for their preparation and pharmaceutical products containing these compounds. The new compounds and their salts have useful pharmacological properties. They can be used as active compounds for medicaments for the treatment and prevention of diseases, caused by a disturbance in arachidonic acid metabolism.
Fries Rearrangement of some 3-Acetoxy- and 3-Propionyloxy-thiophenes
Banks, Malcolm R.
, p. 507 - 514 (2007/10/02)
The Fries rearrangement of ten 3-alkanoyloxythiophenes has been studied in dichloromethane using aluminium chloride as catalyst.An intermolecular component of the mechanism has been demonstrated by the observation of all possible mixed products in approximately equal proportions in a crossover experiment. 3-Alkanoyloxythiophenes were prepared from the corresponding 3-hydroxythiophenes and the rearrangement proceeded generally at ambient temperature to give 3-hydroxy-2-alkanoylthiophenes in good yields.This synthetic route provides a useful alternative to the Friedel-Crafts alkanoylation.The structures of both the acyl and 3-thiophenoxy moieties were found to exert an influence on the rearrangement.Acetyl esters rearranged at a faster rate than propionyl esters.An ester or cyano group in the 4-position did not interfere with the rearrangement whereas an acetyl group prevented it; two ester groups in the tiophene ring also prevent rearrangement occuring yielding 3-hydroxythiophenes in almost quantitative yield.
