956 results about "Quinolone" patented technology

This invention relates to novel antimicrobial compounds of formula;wherein X, R1, R3, R5, R6, and R8 are defined in the claims, and to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically-acceptable salts, hydrates, and biohydrolyzable esters, amides and imides thereof, and to compositions and uses of such compounds. The invention also relates to compounds derived from these compounds having antimicrobial uses.

Substituted quinolone compounds and compositions are provided along with methods for the use of those compounds in the treatment of diseases and disorders such as cancer.

The invention discloses a C3 / C3 fluoroquinolone dimmer derivative using oxadiazole as a connection chain as well as a preparation method and an application thereof. The C3 / C3 fluoroquinolone dimmer derivative using oxadiazole as a connection chain is a compound which has the following structural general formula (I), wherein R1 and R1' are independently selected from H, (C1-C10) alkyl, (C3)-(C10) cycloalkyl, (C1)-(C10) haloalkyl and substituted aryl group or substituted heterocyclic aryl group; R2 and R2' are independently selected from H, (C1-C7)alkyl, (C3)-(C7) cycloalkyl, substituted aryl group, substituted heterocyclic aryl group and hydrocarbon acyl or sulfonyl; R3 and R3' are independently selected from H, (C1-C5) alkyl, (C3)-(C5) cycloalkyl, substituted aryl radical or substitutionalheterocyclic aryl radical; and X and Y are independently selected from CH, N or carbon atoms connected with halogen, alkyl, oxyl, sulfenyl, amino, substituted amino, substituted aryl radical or substituted heterocyclic aryl radical. The C3 / C3 fluoroquinolone dimmer derivative using oxadiazole as a connection chain can be used for preparing medicaments for treating tumors and preventing microbialinfection diseases.

The pharmaceutical composition of the present invention comprises a carbostyril derivative which is a dopamine-sero-tonin system stabilizer and a mood stabilizer in a pharmaceutically acceptable carrier. The carbostyril derivative may be aripiprazole or a metabolite thereof. The mood stabilizer may include but is not limited to lithium, valproic acid, divalproex sodium, carbamaza-pine, oxcarbamazapine, zonisamide, lamotragine, topiramate, gabapentin, levetiracetam or clonazepam. These compositions are used to treat patients with mood disorders, particularly bipolar disorder with or without psychotic features, mania or mixed episodes. Methods are provided for separate administration of a carbostyril derivative and a mood stabilizer to a patient with a mood disorder.

The invention belongs to the technical field of food detection methods, and particularly relates to a method for determining multiresidue of veterinary drugs in animal-derived foods. The method comprises the following steps of weighing a sample, adding an acetic acid-acetonitrile solution, carrying out vibrating extraction, centrifuging to obtain acetonitrile extracting solution, loading the extracting solution obtained by centrifuging into a centrifuge tube with a mixed filler, carrying out vibrating centrifugation, sucking purified liquid, concentrating by blowing nitrogen, diluting to constant volume and detecting by UPLC / MS / MS (ultra performance liquid chromatography-tandem mass spectrometry). The method disclosed by the invention is firstly applied in detecting animal-derived foods and 107 kinds of veterinary drugs such as sulfonamides, quinolones, beta agonists in animal products are subjected to fast qualitative and quantitative detection, the detection limit is completely capable of meeting the detection requirements and the detection efficiency is greatly promoted.

An antimicrobial composition comprising (a) a cationic surfactant derived from the condensation of fatty acids and esterified dibasic amino acids, such as lauric arginate and (b) an antibiotic, such as of β-lactam antibiotics, polypeptides, quinolones. The composition may be used as a stand alone antimicrobial formulation, or in combination with medical articles or medical devices.

The present invention relates to a method of treating a patient suffering from a disorder of the central nervous system associated with 5-HT1A receptor subtype, comprising as an active ingredient a carbostyril derivative or a salt thereof represented by the formula (1): wherein the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or a double bond.

This invention relates to new generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically acceptable salts, hydrates, prodrugs, polymorphs and pseudopolymorphs thereof, to their preparation, to their compositions and to their use.

The present invention relates to a method of simultaneously detecting a plurality of agro-veterinary drug residues in bee products. The extracted liquid trichloroacetic acid or perchloric acid and the extracted liquid acetate, phosphate or borate solution are added into a sample; the pH value is controlled between 4.5 and 9.0; the mixed solution is centrifuged, the filtrate is added into a solid phase extraction column to be extracted, the extraction column is eluted and dried, the column is washed by oxalic acid-methanol solution, the volume of the eluent is defined by the aqueous solution of methanol, the eluent is added into liquid chromatography-tandem mass spectrometry to be analyzed and tested, the acquired chromatographic peak is contrasted with the known standard chromatographic peak of the drug, and according to the retention time and the abundance of the mass spectrum ions, the specific name of the detected drug is determined. The method only requires one pre-treatment of the sample, and thus can simultaneously extract 11 classes and more than 60 kinds of veterinary drug residues, such as sulfonamides, quinolones, macrolides, lincomycins, nitroimidazoles, beta-lactams, tetracyclines, chloromycetins, trinethoprims, chlordimeform, triadimenol and the like, the efficiency of analysis is high, and the detection cost is greatly reduced.

A platelet aggregation inhibitor comprising a quinolone derivative or a pharmaceutically acceptable salt thereof as an active ingredient, and a novel quinolone derivative or a pharmaceutically acceptable salt thereof useful as a platelet aggregation inhibitor.

Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation. The compounds are useful in treating PI 3-kinase-dependent conditions including cardiovascular diseases such as coronary artery occlusion, stroke, acute coronary syndrome, acute myocardial infarction, vascular restenosis, atherosclerosis, and unstable angina; respiratory diseases such as asthma, chronic obstructive pulmonary diseases (COPD), and bronchitis; inflammatory disorders; neoplasms including cancers such as glioma, prostate cancer, small cell lung cancer, and breast cancer, and diseases linked to disordered white blood cell function, such as autoimmune and inflammatory diseases.

The present invention relates to use alpha -arteether as a antibacterial agent, preferably for gyr mutant bacteria which are resistant to quinolone drugs and can be used as therapeutic agents for treating drug resistant bacterial infections, and also as a antifungal agent.

The present invention discloses new quinolone derivatives with 3-position substituted by imidazol radical, benzoxazole and benzothiazole and possessing antitumor activity. The preparation process ofthe compounds is also disclosed.

The present invention relates to 3,4-disubstituted coumarin and quinolone derivatives and processes for their preparation. The invention also related to methods for treating infection of Hepatitis C virus by administering a 3,4-disubstituted coumarin or quinolone derivative.

Compounds of the following formula: are effective antimicrobial agents.

The invention discloses a fluoroquinolone acetal isoniazone, of which the chemical structure general formula is disclosed as Formula I shown in the description, wherein R1 is hydrogen atom or methyl group; R2 is hydrogen atom or amino group; R3 is hydrogen atom, methyl group, ethyl group, formacyl group, acetyl group, aroyl group or sulfonyl group; R4 is hydrogen atom or methyl group; and X is oxygen atom or sulfur atom. The fluoroquinolone isoniazone disclosed by the invention implements complementarity between the two anti-tuberculosis medicines fluoroquinolone and the isoniazide, lowers the toxic and side effect of the fluoroquinolone and the isoniazide, reduces the generation probability of drug resistance of Mycobacterium tuberculosis for the double-effect antimicrobial agent, and can be used as an anti-Mycobacterium tuberculosis medicine for brand-new structure development of medicinal active substances.

The invention discloses an analysis method for simultaneously measuring residues of 12 sulfonamide medicaments, 19 quinolone medicaments and 8 benzimidazole medicaments and metabolites thereof in chicken liver by quick, easy, cheap, effective, rugged and safe (QuEChERS) extraction and purification-ultrahigh performance liquid chromatography-tandem mass spectrometry (QuEChERS-UPLC-MS / MS). The method comprises the following steps of: extracting a sample by using 1 percent acetic acid-acetonitrile solution, purifying the sample by using NH2 adsorbent, and degreasing the sample by using n-hexane;and then performing separation by using a Kromasil Eternity C18 chromatographic column (100mm*2.1mm, 2.5mum), performing gradient elution by using 0.1 percent formic acid and methanol as mobile phases, performing ionization in an electron spray positive ion (ESI<+>) mode, performing detection in a multi-reaction monitoring (MRM) mode, and performing quantification by an internal standard method. The 39 medicaments have good linearity (r is more than 0.98) in a blank adding concentration range of 5 to 100mug / kg, the average recovery rate of the medicaments in the adding level range of 10 to 50mug / kg, the relative standard deviation (RSD) is 1.5 to 23.4 percent, the limit of detection (LOD) of the 39 medicaments is 5mug / kg, and the low limit of quantification (LOQ) is 10mug / kg. The method is simple, convenient, quick, sensitive, accurate and rugged, and is suitable for confirmation and quantitative determination of the residues of the residues of the sulfonamide, quinolone and benzimidazole medicaments in the chicken liver.

A disclosed method for simultaneously analyzing and detecting residual veterinary drug compositions in animal tissue comprises: performing homogenate on an animal tissue sample by 50% acetonitrile and ethanol, performing ultrasonic extraction and hexane purifying, and performing further precipitation by acetonitrile and ethanol, concentrating, utilizing UPLC-MS / MS to perform multi-reaction monitoring (MRM) determination under the negative ion mode, and quantifying according to a standard curve and an external standard method, detecting and calculating to obtain the content of 46 residual veterinary drug compositions in animal tissue. The method is applicable to present commonly-used veterinary drugs such as 18 kinds of quinolone drugs, 22 kinds of sulfanilamide drugs, dapsone, phenylethanolamine A, amoxicillin, adamantanamine, rimantadine, ethoxyquin and the like, and is capable of performing one-step simultaneous rapid accurate detection, and the application scope of the method is enlarged.

Compounds of the following formula: 1 are effective antimicrobial agents.

Substituted quinolone carboxylic acids and their derivatives are described. These compounds modulate the effect of γ-aminobutyric acid (GABA) via a novel site on the GABAA receptor complex in a therapeutically relevant fashion and may be used to ameliorate CNS disorders amenable to modulation of the GABAA receptor complex.

Compounds having the general structure: which are effective antimicrobial agents.

Substituted quinolone derivatives in which an oxazolidinone, isoxazolinone, or isoxazoline is covalently bonded to a quinolone, methods of using the quinolone derivatives, and pharmaceutical compositions containing the quinolone derivatives are disclosed. Methods of synthesizing these substituted quinolone derivatives are also disclosed, and in particular a method of manufacturing a 7-(2-oxo-1,3-oxazolidin-3-yl)aryl-3-quinolinecarboxylic acid by condensing a 4-(2-oxo-1,3-oxazolidin-5-yl)aryl boronic acid with a 7-halo-quinolone derivative. The quinolone derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.

This invention relates to novel antimicrobial compounds of formula; wherein X, R1, R3, R5, R6, and R8 are defined in the claims, and to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically-acceptable salts, hydrates, and biohydrolyzable esters, amides and imides thereof, and to compositions and uses of such compounds. The invention also relates to compounds derived from these compounds having antimicrobial uses.

The invention discloses a method and a special quantum dot fluorescent immunoassay kit for detecting quinolone compounds. The quantum dot fluorescent immunoassay kit for detecting the quinolone compounds provided by the invention comprises specific antibodies, coating antigens and standard solution of the quinolone compounds, wherein the coating antigens are conjugates of hapten and carrier proteins of the quinolone compounds. Experiments prove that the kit of the invention has the characteristics of simple sample pretreatment process, simple and convenient operation, low cost, high specificity, high sensitivity, high accuracy, on-site monitoring, suitability for screening of a large number of samples, and the like.

A preservative-free opthalmic composition for treating eye infections is disclosed. The composition contains a quinolone compound in an amount effective as an antibiotic when the composition is placed in the eye. The composition is rendered isoosmotic with polyhydric alcohol. The composition may be utilized to treat ophthalmic conditions by topically applying the composition to the affected tissues.

The invention discloses a 3,3'-methene-difluoroquinolone derivative of a chiral oxazine quinoline ring as well as a preparation method and application of the 3,3'-methene-difluoroquinolone derivative. The 3,3'-methene-difluoroquinolone derivative has a chemical general structural formula I shown in the specification, wherein R represents cyclopropyl or ethyl or fluoroethyl; R1 represents a hydrogen atom or methyl or ethyl; R2 represents a hydrogen atom or methyl; X represents a nitrogen atom or a hydrocarbon (CH) group or a fluoro-substituted carbon atom (F-C) or a methoxyl-substituted carbon atom (CH3O-C). The 3,3'-methene-difluoroquinolone derivative of the chiral oxazine quinoline ring, disclosed by the invention, can be used for realizing the superposition of a difluoroquinolone framework and alpha, beta-unsaturated ketone pharmacophores, so that the antitumor activity of a new compound is improved, the toxic and side effects on normal cells can be reduced, and the 3,3'-methene-difluoroquinolone derivative can be used as an antitumor active substance for developing an antitumor drug of a totally new structure.

Compounds having the general structure:which are effective antimicrobial agents.

The invention discloses a medicinal composite preparation containing quinolones, a preparation method thereof and an application thereof. The medicinal composite preparation containing quinolones comprises the following components, by mass, 0.5-95% of a quinolone medicine or a salt compound thereof, 1-97% of an organic acid or a salt compound thereof, 1-98.5% of a sweetener, 0-45% of a flavor enhancer, 0-10% of a flavoring agent, and the balance excipient. Finished products prepared from the medicinal composite preparation containing quinolones, which have the characteristics of stability, excellent dispersibility, good palatability and easy absorption, can be used as a broad-spectrum antiseptic, have the advantages of strong bactericidal activity, wide in vivo distribution and no cross drug resistance with other antibiotic medicines, and are effective to bacteria and mycoplasmas, can be used to treat various infectious diseases of the alimentary system, the respiratory system, the urinary system or the skin soft tissue of animals, wherein the diseases are caused by the sensitive bacterial or the mycoplasmas.

The invention belongs to the technical field of detection of enrichment of remained antibiotics in a water body environment, and particularly relates to a synchronous detection method of tetracyclines, fluoroquinolones and sulfonamide antibiotics remained in the water body. The detection method comprises the following steps: (1) performing water sample pretreatment; (2) performing small-column enrichment of target antibiotics by using solid-phase extraction; (3) detecting on a machine by using high performance liquid chromatography and tandem mass spectrum. According to the method, once the sample feeding is carried out at one time, multiple antibiotics in the water body can be detected at the same time, the time consumption of a detection process is reduced, the detection accuracy and sensitivity are increased, the detection limit is low, and the condition of the trace amount of remained antibiotics in the water body environment can be detected; meanwhile, the detection method is convenient to operate and low in environment toxicity and is low in using amount of organic reagents.

The invention discloses a mixed bacterial agent capable of degrading antibiotics in soil, belonging to the field of microbial technology. The mixed bacterial agent is prepared by mixing Bacillus subtilis J5P2 and Pseudomonas J2 according to a volume ratio of (0.1-3): 1. A preparation method for the mixed bacterial agent comprises the following steps: I, preparation of a suspension; II, colony culture: (1) preparation of a medium and (2) culture; III, separation of strains; IV, subculture and domestication: (1) domestication, (2) preparation of a LB medium, and (3) preservation; V, preparation of inoculum liquid; and VI, preparation of the mixed bacterial agent. The mixed bacterial agent provided by the invention has the characteristics of capacity of effectively degrading a plurality of residual antibiotics in soil and reducing environmental pollution, etc., and can be used for the remediation of land contaminated by antibiotics such as tetracycline, penicillin, sulfadiazines and quinolones.