摘要:
Compounds of the formula are disclosed, wherein: Y is an alkylene bridge of 3-9 carbon atoms; Z is N or HC; R is hydrogen or lower-alkyl of 1-3 carbon atoms, with the proviso that when Z is N, R is lower-alkyl; R 1 and R 2 are each hydrogen, halogen, methyl, nitro, lower-alkoxycarbonyl or trifluoromethyl; and Het is a heterocyclic group, and pharmaceutically acceptable acid addition salts thereof, as well as methods for preparation and use thereof. The compounds exhibit valuable antiviral properties.
摘要:
A hydroquinoline compound of the formula (1): wherein R 1 , R 2 , R 3 , A, l, m and n are as defined or its pharmaceutically acceptable salt, composition containing the compound and processes for preparing same are disclosed. The compound is useful as an antiulcer agent.
摘要:
Nucleic acid hybridization probes are provided which comprise an N 4 -(substituted amino) cytosine moiety, wherein the substituted amino group comprises a tag moiety, whereby the probe is detected. Methods of preparing probes of the Invention, intermediates used in such methods, and methods of using the probes of the invention in hybridization assays are also provided. Typical tag moieties employed with the probes of the invention are biotinyl, aminothiadiazole and fluorescein derivatives, connected to N 4 -amino groups of modified cytosines of the probe through linker moieties.
摘要:
Organo-silicone compounds are of the formula: wherein R is hydrogen, halogen or alkyl, R R 2 and R 3 are each alkyl, alkoxy, phenyl, substituted phenyl, alkylcarbonyloxy or trialkylsilyloxy, R 4 is hydrogen, alkyl or alkenyl, and m and n are each an integer, (e.g. 2 or 3) but are not both 2 when R 1 , R 2 and R 3 are all methyl. The preferred halogen is F. Preparation is by equimolar condensation of a 3-R 6 5-R-substituted uracil with the side chain moiety terminating in -N = C = 0, -NHR 4 or -NR 4- CO-CI, in a solvent preferably at 0-10°C. Pharmaceutical compositions for oral use or as suppositar- ies or for injection contain one of the compounds and are useful as anti-cancer agents.
摘要:
An improved process for the preparation of 7-substituted amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids of formula is described where an alkyl ester of a 6,7,8-trifluoro precursor is converted to a trialkylsilyl ester which fluorine at C 7 is directly displaced to the desired product.
摘要:
The present invention comprises a liquid tea mix concentrate. The liquid tea mix concentrate is shelf-stable and substantially free of sulfur. It is characterized by a low pH, low water activity, high total solids, reduced levels of theaf- lavin and thearubigin, and a polyphenolic profile and molecular weight distribution distinct from other liquid tea mix concentrates. Tea beverage prepared from the concentrate is storage-stable in flavor and clarity. Acid-catalyzed degradation reactions that normally occur between tea mix components causing the development of off- flavor and malodorous sulfurous compounds and precipitates are accelerated during processing. By removing the resultant compounds, the development of off-flavors, off-aromas, and precipitates in the liquid tea concentrate is prevented without the use of preservatives.
摘要:
Compounds of formula (I): in which: R 1 represents a hydrogen atom, an alkyl group, a substituted alkyl group, a C 2 -C 6 alkenyl group, an aryl group, a substituted aryl group or a (C 1 -C 6 alkoxycarbonyl group; R 2 represents a hydrogen atom, a C 1 -C 6 alkyl group or a C 3 or C 4 alkenyl group; R 3 represents a hydrogen atom or a C 1 -C 6 alkyl group; R 4 represents a hydroxy group, a C 1 -C 21 aliphatic acyloxy group or an aromatic acyloxy group; R 5 represents a C 1 -C 12 alkyl group, a C 1 -C 6 alkoxy group, a hydroxy group, a C 1 -C 7 aliphatic acyloxy group or an aromatic acyloxy group; R 6 represents a hydrogen atom, a C 1 -C 6 alkyl group or a C 1 -C 6 alkoxy group; and n is 0, 1, or 2; and pharmaceutically acceptable salts thereof are valuable in the treatment of circulatory disorders and allergies.