331 results about "Quinolizidines" patented technology

The invention discloses a new gene purE1 which has high degradability on quinoline. Experiment shows that by using the purE1 gene to transform a microbe, the microbe can obtain degradation activity on quinoline, and the maximal degradation concentration of the degradation activity of the microbe provided by the purE1 gene and its coded protein is up to 850 mg / L. The invention has very important practical application value for the treatment of quinoline contaminants.

The invention relates to a compound as shown in a formula I or a pharmaceutically acceptable salt, a solvate, a prodrug, a stereoisomer, a tautomer, a polymorphic substance or metabolite, a pharmaceutical composition and medicinal usage of the compound. The compound as shown in the formula I or the pharmaceutically acceptable salt, the solvate, the prodrug, the stereoisomer, the tautomer, the polymorphic substance or metabolite and the pharmaceutical composition of the compound can be used as protein kinase inhibitors and particularly used for treating or preventing tumors.

Certain quinolizidine and octahydropyridopyrazine compounds, pharmaceutical compositions, and methods of their use, inter alia, as opioid receptor antagonists are disclosed.

The invention discloses a quinoline compound, and a preparation method, an intermediate, a medicinal composition and an application thereof / The invention provides a quinoline compound represented by formula 1 shown in the specification, and its pharmaceutically acceptable salts, solvates, metabolites, metabolism precursors or medicinal precursors. The quinoline compound has a good inhibition effect on tyrosine kinases C-Met, and can be used for preparing medicines for prevention, treatment or adjuvant treatment of many C-Met expression or activity related diseases, especially tumor diseases.

The invention discloses a quinolinic compound showed in the formula A and pharmacy acceptable solvate, optical isomers or polymorphic substance and a reaction intermediate compound showed in the formula D; wherein, R1, R2 and R3 are respective and independent H, halogen or group showed in the formula H; wherein, the R is H, the halogen, alkyl of C1-C4 or alkoxide of C1-C4. The invention further discloses a preparation method thereof and application for preparing medicines for inhibiting HMG CoA reductase and treating hyperlipemia related diseases. Compared with the existing fuvastatin, rosuvastatin and pitavastatin in the prior art, the quinolinic compound of the invention can better inhibiting the activity of the HMG CoA reductase and can be used for treating hyperlipemia related diseases.

The present invention provides a 4-oxoquinolizine antibacterial agent having a 2-pyridone skeleton as a partial structure and also having a strong antibacterial effect on gram-positive bacteria, gram-negative bacteria or anaerobic bacteria. The compound having the following formula (I) or a pharmaceutically acceptable salt thereof:wherein:R1 represents hydrogen atom or a carboxyl-protecting group,R2 represents hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxyl group or hydroxyl group,R3 represents phenyl group or an aromatic substituent selected from the group consisting of 5-membered and 6-membered heterocyclic groups and R3 has a substituent selected from the group consisting of a hydrogen atom, a lower alkyl group, a lower alkoxyl group, a nitro group, a cyano group, an amino group, an acyl group, a carbamoyl group and a ureido group, andR4 represents a hydrogen atom or a halogen atom.

The invention relates to a quinoline multi-target kinase inhibitor with antitumor activity and a preparation method thereof. A general structural formula of the compound is shown in a formula (I) described in the specification. In vitro cell experiments verify that the compound provided by the invention has strong in vitro inhibitory activity on five common tumor cell lines, namely human thyroid carcinoma SW579, human hepatic carcinoma HepG2, human lung adenocarcinoma A549, human colorectal adenocarcinoma HCT116 and human gastric carcinoma MKN45, antitumor activities of most of target compounds are better than or equivalent to that of a positive control drug Cabozantinib, and the in vitro cell experiments verify that the compound provided by the invention has strong inhibitory activity on two kinases KDR and MET, so that the compound provided by the invention has a broad application prospect in preparation of a new antitumor drug.

The invention discloses a monoamine oxidase from Pseudomonas sp., a coding gene, a recombinant expression vector, a recombination expression transformant, and the synthesis application of the monoamine oxidase in tetrahydroquinoline chiral amine compounds. The coding gene of the monoamine oxidase MAO5-ZMU is from Pseudomonas sp. ZMU-T01. The amino acid sequence of monoamine oxidase protein is shown in SEQID No.1, and the corresponding coding gen nucleotide sequence is shown in SEQIDNo.2; the monoamine oxidase gene can be connected with an expression carrier to construct to obtain a recombination expression plasmid; the recombination expression plasmid is converted to escherichia coli to obtain genetically engineered bacteria with monoamine oxidase activity. The genetically engineered bacteria with monoamine oxidase activity can be used for effectively catalyzing 2-methyl-1,2,3,4-tetrahydroquinoline compounds for oxidation splitting, has the characteristics of high selectivity, moderatereaction condition, environment protection and the like and can be used for the biosynthesis of the chiral tetrahydroquinoline compounds.

The invention relates to new substituted quinoline derivatives presented in general formula (1a), or general formula (1b) or general formula (1c), a medical acid added salt, a stereochemical heterogeneous formula and a tautomeric form thereof. The compound can be used for curing mycobacterium diseases, in particular to diseases caused by pathogenic mycobacteria, such as mycobacterium tuberculosis, mycobacterium bovis, mycobacterium avium and mycobacterium marinum and is particularly defined as following: R1 is mutually independent bromines; p is equal to 1, R2 is an alkoxy, and R3 is a randomly substituted phenyl or naphthyl; q is equal to 1, R4 and R5 are mutually independent hydrogen and a methyl or an ethyl, and R6 is hydrogen; r is equal to 0 or 1 and R7 is hydrogen. The invention also relates to a composition of the compound, applications of the compound of the composition to medicines for curing the mycobacterium diseases, and a method for preparing the compound of the composition, which comprises a medical carrier and is used as activated ingredient of curable effective quantity.

The invention discloses a non-hydrodenitrogeneration method for catalytically cracked gasoline. The non-hydrodenitrogeneration method for the catalytically cracked gasoline comprises the following steps: first, mixing a liquid denitrifying agent with the catalytically cracked gasoline by using a static mixer, standing, depositing, and pre-removing alkali nitrides; and then, performing contact reaction with a solid denitrifying agent through a fixed bed for finely removing the alkali nitrides. Through matching of the liquid denitrifying agent and the solid denitrifying agent, the alkali nitrides such as aliphatic amines, pyridines, quinolines and anilines and the like can be removed by pre-removing and finely removing steps; after the treatment of the liquid denitrifying agent, 80-90 percent of the alkali nitrides can be removed, and after the catalytically cracked gasoline passes through the solid denitrifying agent filled in a form of the fixed bed, the alkali nitrides can be removedcompletely, so that the negative effect of the alkali nitrides on a subsequent hydrodesulfurization catalyst can be completely eliminated. Therefore, the deep hydrodesulfurization of the catalytically cracked gasoline can be realized.

The invention relates to quinoline compound, a synthesis method and the application for preparing medicines of camptothecin alkaloid. The syntheticroute is concise, high-efficient and economical, and can play a great role in promoting the later industrialized production of camptothecin alkaloid.

The invention discloses a novel organic salt-a berberine glycyrrhizic acid enantiomer salt which can be used for medicine, and a preparation method and usage thereof. The chemical name of the berberine glycyrrhizic acid enantiomer salt is 5,6-dihydro-9,10-dimethoxy-benzo (g)-1,3-benzo-dioxolane[5,6-a]quinolizidine.18a(beta),20beta-carboxy-11-oxo-30-norolean-12-alkene-3beta-yl-2-O-beta-D-glucopyranuronosyl-a-D-glucopyranosiduronic acid. The preparation method comprises the steps that berberine hydrochloride is dissolved with water according to the pharmaceutical co-crystal principle, anion exchange resin is added, then the mixture is stirred for one hour and filtered, the filtrate is put into a water solution of a glycyrrhizic acid enantiomer and stirred for 30 minutes for centrifugation, the precipitate is dissolved in ethanol, and decompression is carried out to remove the solvent to get the berberine glycyrrhizic acid enantiomer salt. The organic salt with double mother nucleuses has practical significance for human in resisting diabetes, hyperlipidemia, tumor and chronic inflammatory diseases of rheumatoid arthritis, hepatitis, Alzheimer and the like and developing the medical industry.

The invention discloses novel organic berberine glycyrrhetinic acid enantiomeric salts used for medicines and a production method and application thereof. The chemical name of the organic berberine glycyrrhetinic acid enantiomeric salts is: 5,6-dihydrogen-9,10-dimethoxybenzo[g]-1,3-benzodioxolane[5,6-a]quinolizidine.18a(beta),3beta-hydroxyl-11-oxooleanane-12-olefine-30-formate. The production method comprises the following steps of: respectively dissolving berberine and a glycyrrhetinic acid enantiomer in 80 percent ethanol according to a medicament eutecticum principle, mixing the two liquids, stirring for 2 hours, removing the ethanol under reduced pressure, and treating by using ethyl acetate to prepare the berberine glycyrrhetinic acid enantiomeric salts. The organic salts with dual parent nuclei have positive practical significance for resisting diseases such as tumors, diabetes, chronic inflammatory diseases such as rheumatoid arthritis, hepatitis, Alzheimer disease and the like of human and developing medicines.

The invention discloses a red to near-infrared phosphorescent iridium complex light-emitting material and application thereof to an electroluminescent device, belongs to the technical field of organic electroluminescence, and particularly relates to a dark red to near-infrared phosphorescent iridium complex light-emitting material with a 1-phenyl quinoline derivative as a first ligand and an amidino-guanidyl derivative as an auxiliary ligand. The general formula of a compound of the material is shown as follows. The red to near-infrared phosphorescent iridium complex light-emitting material is doped in a main material as a phosphorescent object to form a light-emitting layer of the organic electroluminescent device. The compound has the advantages that the preparation process is simple, and the manufactured electroluminescent device is high in efficiency and long in service life. The device can be used in the application fields of panel display, illumination, light sources and the like. The formula is shown in the description.

A 4-substituted phenylmino-3-nitroquinoline compound has the suppression action to the reproduction of tumor cells rich in epidermal growth factor receptor. Its preparing process and usage are also disclosed.

The invention discloses a matrine derivative which comprises quinoline, benzene rings, benzdioxan, naphthalene nucleus and indole codonopsine derivatives. The invention further discloses application of the derivative to a preparation method and pharmacy.

The invention provides a tetrahydroquinoline alkaloid Malaysiensin with immunosuppression activity and a production method and application of the tetrahydroquinoline alkaloid Malaysiensin with the immunosuppression activity. The compound is obtained by conducting SFM solid medium fermentation on Streptomyces sp.DSM 4137 and separating and purifying a fermentation product. The compound can significantly inhibit ConA-induced proliferation of T cells, an immunosuppression effect of the compound is equivalent to that of an immunosuppressor cyclosporin A which is clinically and widely used, and action mechanism studies show that Malaysiensin exerts the immunosuppression activity for a targeted NFAT signal path, is an efficient immunosuppressor, and can be used for producing immunosuppressive medicines for organ transplantation and autoimmune diseases.

The invention relates to a pyridine-quinoline compound, a preparation method thereof and an organic light-emitting device made from the compound. The pyridine-quinoline derivative is obtained by connection with boronic acid derivatives with different substituting groups on the basis of difluoropyridine-[2,3-g]quinoline; the preparation process is simple, the reaction condition is mild, the pyridine-quinoline derivative can be taken as an electron transport material to be applied to organic light-emitting devices. According to the pyridine-quinoline derivative, the preparation method and the organic light-emitting device, the prepared pyridine-quinoline compound is high in efficiency, high in brightness, long in service life, better in charge transfer capacity and high in glass transition temperature and non-crystallizable when applied to organic light-emitting devices.

The invention relates to a 6-nitroacetophenone compound of the formula I, a preparation method and application thereof in preparing a 3-substitute-4-hydroxyquinoline compound, a 3-substitute-4-chloroquinoline compound and an intermediate of the compound of the formula I. In the formula I, X is a cyano-group, trifluoromethyl, nitryl, -NHCOR3, -NHCOOR3, -CONER3R3', -N=CHR3 or -CO2R3, wherein R3 and R3' are hydrogen, C1-C10 alkyl, C1-C10 alkenyl, aryl or the C1-C10 alkyl substituted by the aryl and the same or different; Z is -NH- or -O- or the formula II; R1 and R1' are formyl radicals, the C1-C10 alkyl, the C1-C10 alkenyl, the aryl, the C1-C10 alkyl substituted by the aryl, C1-C10 lauroyl groups, aroyl groups, the C1-C10 lauroyl groups substituted by the aryl, C1-C10 alkoxy carbonyl or the C1-C10 alkoxy carbonyl substituted by the aryl the same or different; R2 is the C1-C10 alkyl, the C1-C10 alkenyl or the aryl; the alkyl does not need to be substituted by halogen, alkoxy, the aryl or a heterocyclic radical containing 1-2 O or N, wherein the heterocyclic radical does not need to be substituted by the C1-C10 alkyl or the C1-C10 alkoxy; and when Z is -O- and R1 is methyl, R2 is not the methyl.

The invention discloses 2,8-bis(trifluoromethyl)quinoline 4-modified derivatives, a preparation method thereof and an application of the derivatives in prevention and treatment of plant diseases. Thetest results show that the compounds have excellent control effect on sclerotiniasclerotiorum, rhizoctonia solani, wheat phytoalexin, pyriculariaoryzae, phyllostictazeae, botrytis cinerea, watermelongummy stem blight and cotton fusarium wilt. The derivatives of the invention are simple in preparation process, low in price and easy to obtain raw materials, high in product purity and wide in bactericidal spectrum, and are expected to be developed into a new bactericide.

The invention relates to a novel preparation method of 1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-2H-benzo[a] quinolizidine-2-ketone. The technological method is economic, simple, convenient and high in total yield, and is suitable for industrial production.

The invention relates to a 6,7-disubstituted-4-aromatic quinoline derivative shown as a general formula I as well as pharmaceutically-acceptable salt, a hydrate, a solvate and pro-drug thereof, wherein substituents R1, X and Y have meanings given in the description. The invention further relates to a compound with a strong effect on inhibiting c-Met kinase shown as the general formula I and further relates to application of the compound and pharmaceutically-acceptable salt, a hydrate, a solvate and pro-drug thereof to preparation of a drug for treating a disease caused by the abnormally-high expression of the c-Met kinase, in particular to application to preparation of a drug for treating and / or preventing a cancer.

The application belongs to the technical field of medicines, provides a quinoline compound for combined treatment on the carcinoma of the colon and rectum and particularly provides use of combinationof a compound I or pharmaceutically acceptable salts thereof and a second therapeutic agent in preparation of drugs for treating the carcinoma of the colon and rectum and a combined pharmaceutical composition for treating the carcinoma of the colon and rectum. The combined pharmaceutical composition comprises: (i) the compound I or pharmaceutically acceptable salts thereof; and (ii) at least one second therapeutic agent, wherein a chemical name of the compound I is 1-[[[4-(4-fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinol-7-yl]oxy]methyl]cyclopropylamine.

The invention discloses a synthesis method of 11H-indolo [3,2-c] quinoline compounds, belonging to the technical field of synthesis of indolo quinoline compounds. The technical scheme of the invention is mainly characterized by taking 2-(2-bromo-aryl)-1H-indolo, ammonia water and aldehyde compounds as raw materials, taking dimethyl sulfoxide or N,N-dimethyl formamide as a solvent, taking transition metal salt as a catalyst, taking potassium carbonate as alkali, and taking L-proline as a ligand to carry out one-pot, two-step and three-component tandem reaction to synthesize 11H-indolo [3,2-c] quinoline compounds with multiple substitute modes. The synthesis method disclosed by the invention has the advantages that starting materials are simple and easy to prepare, and substrates are wide in range of application, high in regioselectivity and simple in operation.

The present invention relates to a quinoline compound, as well as a preparation method and medical use therefor. Specifically, the present invention relates to a novel quinolone compound represented by the general formula (I) and a method for preparing the same, as well as a use therefor as an inhibitor for a plurality of protein kinases, and a use in the prevention and / or treatment of cancer in particular; the definition of each group in the general formula (I) is the same as the definition in the description.

The invention relates to a 5-substituted sulfur etherified / selenium etherified / tellurium etherified quinoline compound and a preparation method therefor. The preparation method is characterized by comprising: carrying out a reaction at a certain temperature for a certain time to obtain the 5-substituted sulfur etherified / selenium etherified / tellurium etherified quinoline compound with a high yield and high selectivity by taking quinoline, diaryl(alkyl) disulfide (R2SSR2) or diaryl(alkyl) diselenide (R2SeSeR2) or diaryl(alkyl) ditelluride (R2TeTeR2) as raw materials, copper salt that is low in price and is easily available as a catalyst and a common oxidant as an oxidant and a common organic solvent as a reaction solvent. The method has the advantages of being relatively low in cost, high in yield, simple to operate, less in pollution and the like, and has certain feasibility for realizing industrial production.

The present invention relates to a diarylo[a,g]quinolizidine compound of formula (I), enantiomer, diastereoisomer, racemate, mixture, pharmaceutically acceptable salt, crystalline hydrate or solvate thereof; the preparation method thereof, and uses thereof in preparing an experimental model drugs related to dopamine receptors and 5-HT receptors or a medicament for treating or preventing a disease related to dopamine receptors and 5-HT receptors.

The invention discloses a method for preparing an N-(5-chloro-8-quinolyl)benzamide compound by adopting an electrochemical micro-channel reaction device, which comprises the following steps: dissolving an 8-(benzoylamino)quinoline compound in a first organic solvent to prepare a reaction solution A; dissolving dichloromethane and copper acetate in a second organic solvent, and preparing a reactionsolution B; respectively pumping the reaction solution A and the reaction solution B into a micro mixer of an electrochemical micro-channel reaction device at the same time for mixing, and then enabling the mixture to flow into a micro-reactor for reaction, thereby obtaining the product. Compared with the prior art, the method has the advantages that a traditional oxidizing agent is not needed, and a new method for electrocatalytically and selectively preparing the chloroquinoline compound by taking dichloromethane as a chlorination reagent through a micro-flow field is creatively developed;meanwhile, a micro-channel reaction device is utilized, so that the reaction time is greatly shortened, the reaction conversion rate is increased, and the yield is remarkably increased and reaches 85%.

The invention discloses a quinolines derivative. The structural formula of the quinolines derivative is shown as the formula (I) or the formula (II) in the description, wherein R represents hydroxyl, phenyl, substituted phenyl, naphthenic base, amino, substituted amino, pentabasic or hexabasic heterocyclic group, C1 to C8 alkyl or substituted C1 to C8 alkyl, halogeno or glycosyl; X is N, O or S; Y is C1 to C3 alkyl or hydrogen and n is an integer from 0 to 6. The invention further discloses a preparation method and application of the quinolines derivative. The quinolines derivative provided by the invention has a very strong inhibition effect on transcription expression of a cancer gene c-myc and has a remarkable inhibition effect on a plurality of cancer cell plants and particularly has a relatively strong inhibition effect on lymphoma cells; the quinolines derivative has small toxicity on normal cells and has a wide application space in the preparation of an anti-tumor medicine.