57 results about "Oxoquinolines" patented technology

The present invention relates to pharmaceutical compositions comprising a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention.

The present invention relates to pharmaceutical compositions comprising a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention.

The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.

The present invention relates to the use of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide and pharmaceutical compositions thereof for the treatment of cystic fibrosis, in patients, including kits and / or products thereof.

The present invention relates to pharmaceutical compositions containing a solid dispersion of N—[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide including formulations of the solid dispersions into powders, granules and mini-tablets, methods for manufacturing and processing the powders, granules and mini-tablets, and methods for treating cystic fibrosis employing the pharmaceutical composition.

The present invention relates to pharmaceutical compositions containing a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide including formulations of the solid dispersions into powders, granules and mini-tablets, methods for manufacturing and processing the powders and mini-tablets and methods for treating cystic fibrosis employing the pharmaceutical composition.

The present invention relates to pharmaceutical compositions comprising a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention.

The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.

The present invention relates to pharmaceutical compositions containing a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide including formulations of the solid dispersions into powders, granules and mini-tablets, methods for manufacturing and processing the powders, granules and mini-tablets, and methods for treating cystic fibrosis employing the pharmaceutical composition.

The invention relates to the field of pharmaceutical synthesis, and in particular relates to a preparation method for a medicament Ivacaftor for treating cystic fibrosis. The method is characterized by comprising the following steps of: protecting phenolic hydroxyl by using alkoxycarbonyl by using 2,4-ditertiary butyl phenol as an initial raw material; nitrifying and reducing phenolic hydroxyl; condensing the phenolic hydroxyl with 4-oxo-1,4-dihydroquinolines-3-formyl chloride to obtain carbonic acid (2,4-ditertiary butyl-5-(1,4-dihydro-4-oxoquinoline-3-formamide) phenylester ethyl ester; and finally removing alkoxycarbonyl under an alkali condition to obtain the Ivacaftor. The method can be used for overcoming multiple defects of the existing synthetic method, is simple and easily available in raw materials, convenient to experimentally operate and postprocess, high in yiled, good in product quality and suitable for scale production.

The invention relates to a sterilization compound containing ZJ0712. The effective components comprise ZJ0712 (A) and a quinoline bactericide (B), wherein the quinoline bactericide is proquinazid or benzoquinate, the weight ratio of A to B is 100:1 to 1:100, and the weight percentage of the active component in the compound is 10-80 percent. The compound can be prepared into suspending agent, wettable powder, water dispersible granules and the like. The sterilization compound is suitable for farmlands, orchards and the like and is used for preventing and treating multiple plant diseases especially powdery mildew of crops such as corns, vegetables, fruit trees, flowers and the like.

The present invention relates to crystalline solvate forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and methods for their preparation. The present invention further relates to pharmaceutical compositions comprising the crystalline solvate forms, as well as methods of treatment therewith.

Pharmaceutical compositions including N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and methods of using such compositions are described herein.

The invention discloses a synthetic method of norfloxacin. The method comprises the following steps: taking toluene as a solvent, causing methyl carbonate to react with 2,4-dichloroo-5-fluoroacetophenone in the presence of a catalyst at the temperature of 70-90 DEG C to obtain 2,4-dichloro-5-fluorobenzenepropionic acid methyl ester, reflux reacting with N,N-dimethylformamide dimethyl acetal in toluene solution for 2-3h to obtain 3-ethylamino-2-(2,4-dichloro-5-fluorobenzoyl) methyl acrylate, cyclizing to obtain 1-ethyl-7-chloro-6-fluo-1,4-dihydro-4-oxoquinoline-3-carboxylic acid methyl ester, reacting with a chelating agent at the temperature of 80-110 DEG C for 2-3h to obtain 1-ethyl-7-chloro-6-fluo-1,4-dihydro-4-oxoquinoline-3-carboxylic acid methyl ester trifluoracetic acid anhydride bononized chelate, reacting with piperazine at the temperature of 20-40 DEG C for 10-24h to obtain the norfloxacin. The method has the advantages of simple process and mild reaction condition, avoids production of reverse ring in the traditional process, provides high-purity product, and is applicable to industrialized production.

The subject invention provides deuterated N-ethyl-N-phenyl-1,2-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide, its salts and uses.

Disclosed are fungicidal mixtures, compositions and methods for controlling plant diseases relating to combinations comprising (a) at least one compound selected from phenylamidines of Formula I, N-oxides, and agriculturally suitable salts thereof (I) wherein A is C3alkylene, optionally substituted with one or two methyl; W is CR<5>R<6>R<7>or SiR<8>R<9>R<10>; and R<1>, R<2>, R<3>, R<4>, R<5>, R<6>, R<7>, R<8>, R<9> and R<10>are as defined in the disclosure; and (b) at least one compound selected from alkylenebis(dithiocarbamate) fungicides, compounds acting at the bc1complex of the fungal mitochondrial respiratory electron transfer site, cymoxanil, compounds acting at the demethylase enzyme of the sterol biosynthesis pathway, morpholine and piperidine compounds that act on the sterol biosynthesis pathway, phenylamide fungicides, pyrimidinone fungicides, chlorothalonil, carboxamides acting at complex II of the fungal mitochondrial respiratory electron transfer site, quinoxyfen, metrafenone, cyflufenamid, cyprodinil, copper compounds, phthalimide fungicides, fosetyl-aluminum, benzimidazole fungicides, cyazofamid, fluazinam, iprovalicarb, propamocarb, validamycin, dichlorophenyl dicarboximide fungicides, zoxamide and dimethomorph, and their agriculturally suitable salts.

The invention discloses an ethirimol-contained bactericide combination, which comprises A) a first active ingredient ethirimol and B) a second active ingredient quinoxyfen or brasilense cyclamine. The weight ratio of the first active ingredient and the second active ingredient is 1:100-100:1. The ingredient compounding is scientific and reasonable, the prevention and control effects can be obviously improved, the sterilization range can be enlarged, the occurrence of fastness can be stayed, and the safety to the crop is high. The ethirimol-contained bactericide combination has excellent prevention and control effects on various powdery mildew and rust disease.

The invention discloses a feed and a preparation process thereof. The feed is composed of the following components in parts by weight: 40-50 parts by weight of corn flour, 20-25 parts by weight of hawthorn powder, 20-25 parts by weight of sweet potato powder, and 30-25 parts by weight of fish meal 35 parts by weight, 2-5 parts by weight of vitamins, 5-8 parts by weight of amino acids, 1-4 parts by weight of trace elements, 1-2 parts by weight of ethoxyquin, 2-5 parts by weight of sodium propionate, 3-5 parts by weight of cinnamon powder Parts by weight, calcium formate 2-4 parts by weight, sodium glutamate 1-3 parts by weight. The various components of the present invention have a synergistic effect on each other, wherein the food-attracting effect of hawthorn powder, fish meal, sodium glutamate and amino acids can improve the mouthfeel of the feed, improve the appetite of pigs, and increase food intake , promote growth, and shorten the growth cycle; the present invention adds a certain amount of ethoxyquin, calcium formate, sodium propionate, and cinnamon powder to the additive, and the three act together to effectively prevent the feed from being oxidized and mildewed. It has the effect of sterilizing and attracting food.

The invention mainly discloses a chemical preparation method of sarafloxacin hydrochloride. The method comprises the steps of: performing heat-perservation refluxing on 7-chloro-6-fluoro-1-p-fluoro phenyl-1,4-oxoquinoline-3-carboxylic acid (as shown in formula I in the specification) and piperazine which are used as raw materials in a solvent for 10 hours, and recovering the solvent and the piperazine after reaction; adding water, then adding a sodium hydroxide solution to regulate a pH value to not less than 13, filtering, adding salt into filtrate, filtering, and adding acid in the filtrate to regulate the pH value to 7.0-7.3 to obtain a wet crystal product of sarafloxacin (as shown in a formula II in the specification); and then, adding the wet product of the sarafloxacin (as shown in the formula II in the specification) into 85% ethanol, heating for refluxing, adding hydrochloric acid as a reagent, regulating a pH value to 2-2.5, and cooling and crystallizing to obtain the sarafloxacin hydrochloride (as shown in a formula III in the specification). The chemical preparation method disclosed by the invention has the advantages of easiness for solvent recovery, environment friendliness, high yield 3-5% higher than that of other methods, low cost about 10% lower than that of other methods, high product purity and the like.

The present invention discloses a germicidal composition containing fluopyram and proquinazid, and applications thereof. Effective active ingredients consist of a first active ingredient fluopyram and a second active ingredient proquinazid. A weight ratio of the first active ingredient and the second active ingredient is from 1:50 to 50:1, preferably from 1:40 to 40:1. The composition can be formulated to agriculturally allowable dosage forms of missible oil, suspensions, wettable powders, water dispersible granules, water emulsions, micro emulsions, micro capsules, granules, and an aqueous agent. The composition disclosed by the present invention has reasonable components and a good germicidal effect. Moreover, the activity and germicidal effect of the composition are not a simple sum of each component activity. Compared with an existing single agent, in addition to having a significant germicidal effect, the composition of the present invention has a significant synergistic effect and high safety for crops. The composition of the present invention has a significant prevention and control effect on powdery mildew.

Process for the preparation of the facial isomer of tris(8-oxoquinoline) aluminum(III) (Alq3), comprising the step of heating α-Alq3 in solid phase at a temperature equal to or higher than 350° C. but lower than 420° C., to obtain a mixture of γ-Alq3 and δ-Alq3.

The invention discloses a preparation method for enrofloxacin-d5. The preparation method comprises the following steps: performing a Buchwald-Hartwig coupling reaction on 1-ethyl-piperazine-d5 and 1-cyclopropyl-7-chloro-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic ethyl ester, and preparing 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(4-ethyl-1-piperazinyl)-3-quinoline carboxylic ethyl ester-d5; and after alkaline hydrolysis, to obtain the enrofloxacin-d5. The preparation method is capable of, through performing the coupling reaction on an esterified carboxylic group and ethyl piperazine, enabling a synthetic reaction to be more easily performed, the difficulty of the reaction is reduced, and a yield of products is very high. In addition, the isotope abundance can be guaranteed in the high-temperature reaction conditions, a reaction process is more easily controlled, the repeatability and the stability are higher, and the conditions of large-scale production are satisfied.

The present invention relates to [7-[(7S)-7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-6-fluoro-1-[(1R,2S)-2-fluorocyclopropyl]-8-methoxy-1,4-dihydro-4-oxoquinoline-3-carboxylic acid hemihydrate. This hemihydrate is stable and easy to prepare, and has excellent properties for a pharmaceutical bulk powder.