65 results about "Pyrazolone derivatives" patented technology

Pyrazolone derivatives of Formula I or a pharmaceutically acceptable salt thereof are MCP-1 antagonists and are thus useful in the treatment of inflammatory diseases or conditions, atherosclerosis, restenosis, and immune disorders such as arthritis and transplant rejection ##STR1## where: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 can be independently H, C.sub.1-20 alkyl, C.sub.5-7 cycloalkyl, --(CH.sub.2).sub.n NR.sub.6 R.sub.7 --(CH.sub.2).sub.0-6 CONR.sub.6 R.sub.7, --(CH.sub.2).sub.n OH or --(CH.sub.2).sub.0-6 CO.sub.2 R.sub.11, biphenyl, aryl of from 6 to 10 carbon atoms, or aryl of from 6 to 10 carbon atoms substituted up to 3 times by halogen, --CN, lower alkyl of from 1-4 carbon atoms, --OH, nitro, --SO.sub.2 H, SO.sub.2 lower alkyl, --SO.sub.2 NR.sub.6 R.sub.7 lower alkoxy --C0.sub.2 R.sub.11, --CONR.sub.6 R.sub.7, --NR.sub.6 R.sub.7 or CH.sub.2 OH.

The invention belongs to the field of monosaccharide component analysis, and in particular relates to a method for detecting monosaccharide components in rainbow conk glycopeptide. The method comprises the following steps of: carrying out a test on HPLC (High Performance Liquid Chromatography) chromatographic condition and systematic compatibility; subsequently respectively absorbing a mixed reference solution and a test solution to be injected into the HPLC chromatographic instrument so as to obtain a chromatogram, wherein the reference solution is a 1phenyl-3-methyl-5-pyrazolone derivative solution of D-glucose, D-mannose, D-xylose, L-xylose, D-galactose, D-arabinose, D-hydrochloric acid glucosamine and L-rhamnose reference solutions; and the test solution is a 1-phenyl-3-methyl-5-pyrazolone derivative solution of a rainbow conk glycopeptide acid hydrolysis product. Polysaccharide peptide products such as rainbow conk glycopeptide, rainbow conk intracellular glycopeptide, rainbow conk extracellular glycopeptides and coriolus versicolor polysaccharide are distinguished by detecting the mole ratio of eight monosaccharide ingredients in a test sample, so that the quality and the curative effect of the rainbow conk glycopeptide are ensured.

There is provided a medicament for treating amyotrophic lateral sclerosis (ALS) or symptoms caused by ALS and / or suppressing the progression thereof, which is characterized in the usage, dosage and administration period of the pyrazolone derivative represented by the following formula (wherein each symbol indicates the same meaning as that defined in the specification):

The invention discloses a chiral 1, 4-dihydropyran (2, 3-c) pyrazole derivative as well as a synthesis method and application of the chiral 1, 4-dihydropyran (2, 3-c) pyrazole derivative. The synthesis method comprises the steps of with methylbenzene as a solvent, enabling a substituted or unsubstituted imidazolone derivative and propanedinitrile to react under the analysis of a Takemoto catalyst, and carrying out after-treatment on a reaction product to obtain the chiral 1, 4-dihydropyran (2, 3-c) pyrazole derivative. The method has the advantages of flexible reaction time, relatively high yield, simplicity and convenience in operation and the like, and is wide in application range. The chiral 1, 4-dihydropyran (2, 3-c) pyrazole derivative has an inhibiting effect on gram positive bacteria and gram negative bacteria.

The invention provides a substituted phenyl pyrazolone derivative and specifically relates to a 2-phenyl-pyrazoline-3-one compound as well as a pharmaceutically-acceptable salt and solvate thereof. Atarget compound is prepared by carrying out a reflux reaction on substituted ethyl acetoacetate and benzyloxyphenylhydrazine in a sodium hydroxide aqueous solution, then, carrying out hydrogenolysis on a benzyl group under the actions of palladium / carbon and hydrogen to obtain phenylpyrazolone phenol, then, making phenylpyrazolone phenol react with bromochloroalkane to obtain a chloride, and finally, carrying out condensation on the chloride and secondary amine. The substituted phenyl pyrazolone derivative provided by the invention shows good free radial scavenging capability in vitro, has relatively strong H3 receptor inhibiting activity, shows good blood brain barrier penetration capability and has unique double activities so as to have a unique clinic effect on treating neurodegenerative diseases such as cerebral apoplexy, presenile dementia, parkinsonism and amyotrophic lateral sclerosis. The compound provided by the invention is applied to preparation of drugs for treating centralsystem related diseases and inflammatory diseases. A structure of a general formula is shown as the specification.

The invention discloses a method for determining holothurin content, which is characterized in that the method comprises the following steps of: hydrolyzing a sample with a trifluoroacetic acid aqueous solution, neutralizing the hydrolysate, filtering, adding water to fixed volume, adding 1-pheny-3-methy-5-pyrazolone derivative agent to carry out derivation reaction, determining the content of quinose in the derivatives by high-performance liquid chromatographic analysis, and calculating the holothurin content in the sample by multiplying the content of quinose by a conversion coefficient. The invention has the advantages of simple operation, high sensitivity, less sample consumption and good stability, and is suitable for content determination of glycosides of various sea cucumbers.

A glycoprotein and / or a glycopeptide which are a test substance is heated in the presence of a pyrazolone derivative, an isoxazolone derivative, a hydantoin derivative, a rhodanine derivative, a maleimide derivative, or the like under a basic condition to cleave and label a post-translational modification group for analysis, thereby enabling analysis of a post-translational modification of a serine residue and / or a threonine residue.

The invention relates to a new pyrazolone derivative of 4-(1-nitro-1-sulfonic group)ethyl-3-methyl-1-phenyl-2-pyrazol-5-ketone. The invention further relates to a method for preparing the new pyrazolone derivative and application of the pyrazolone derivative in an edaravone and related preparation quality control method as an impurity reference substance.

The invention discloses a PET (polyethylene terephthalate) base material used for a filter membrane, a preparation method as well as the filter membrane and a plasma display screen comprising the PET base material. The PET base material comprises one or more of inorganic pigment, organic pigment and dye, wherein the inorganic pigment is one or more of metallic oxide, sulfide, sulfate, chromate and carbon black; the organic pigment is one or more of azo pigment, phthalocyanine pigment, heterocyclic pigment, lake pigment and fluorescent pigment; and the dye is one or more of pyrazolone derivative, quinophthalone, fluorescent polycyclic ring dye, naphthazarin, benzopyrone, azo, fluorescent reactive dye, anthraquinone reactive dye, picene ketone dye, anthraquinone reactive derivative, fluorescent polycyclic ring and polymethylene dye. A material with a toning function is added into the PET base material, thus the phenomenon that chemical substances in pressure-sensitive adhesive (PSA) react with the material with the toning function to generate the discoloration is avoided, and meanwhile, the plasma screen capable of improving color is obtained.

The invention discloses a filter film and a plasma display screen including the same. The filer film comprises one or more polyethylene terephthalate (PET) structural units. Each PET structural unit comprises a PET base material, a functional layer arranged on the upper surface of the PET base material and a pressure-sensitive adhesive layer arranged on the lower surface of the PET base material, wherein the pressure-sensitive adhesive layer contains a near infrared ray blocking function material and / or a neon yellow light blocking function material. The PET base material contains inorganic pigment, organic pigment or dyestuff, wherein the inorganic pigment is a metallic oxide, sulfide, sulfate, chromate or carbon black, the organic pigment is azo pigment, phthalocyanine pigment, heterocyclic pigment or fluorescent pigment, and the dyestuff is a pyrazolone derivative, fluorescent polycyclic dyestuff, azo fluorescent reduced dyestuff, an anthraquinone reduction derivative or fluorescent polycyclic dyestuff. A color modulation function material is added into the PET base material rather than the pressure-sensitive adhesive layer, so that a color change phenomenon caused by chemical reaction of chemical substance in the pressure-sensitive adhesive layer and the color modulation function material is avoided.

A drug for the treatment of and / or inhibiting the progress of amyotrophic lateral sclerosis (ALS) or diseases attributable to ALS, characterized by a method of using a pyrazolone derivative represented by the following formula (wherein the symbols are the same as defined in the description) and by the dose of the derivative and the period of administration thereof.

Pyrazolone derivative emulsion formulations are provided. The emulsion formulations include a pyrazolone derivative active agent, e.g., Edaravone, oil, water and an emulsifier. Also provided are methods of making and using the subject emulsion formulations.

The object of the present invention is to provide a medicament useful for preventing and / or treating inflammatory bowel disease. The present invention provides a medicament for preventing and / or treating inflammatory bowel disease which comprises as an active ingredient a pyrazolone derivative represented by the following formula (I) or a physiologically acceptable salt thereof, or a hydrate thereof or a solvate thereof: wherein R<1> represents a hydrogen atom, an aryl group, an alkyl group, or an alkoxycarbonylalkyl group; R<2> represents a hydrogen atom, an aryloxy group, an arylmercapto group, an alkyl group or a hydroxyalkyl group; or R<1> and R<2> are combined with each other to represent an alkylene group; and R<3> represents a hydrogen atom, an alkyl group, a cycloalkyl group, a hydroxyalkyl group, a benzyl group, a naphthyl group, a phenyl group, or a phenyl group substituted with 1 to 3 substituents selected from the group consisting of an alkyl group, an alkoxy group, a hydroxyalkyl group, an alkoxycarbonyl group, an alkylmercapto group, an alkylamino group, a dialkylamino group, a halogen atom, a trifluoromethyl group, a carboxyl group, a cyano group, a hydroxyl group, a nitro group, an amino group and an acetamide group.

The disclosed subject matter provides pyrazolone derivative compounds, pharmaceutical compositions comprising such compounds, kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating heart failure.

The invention belongs to an organic photochromic material, and relates to preparations and applications of a thienyl group-containing pyrazolone derivative and its polymer film. The thienyl group-containing pyrazolone derivative is anyone of 1-phenyl-3-substituted-phenyl / thienyl / pyrryl / furyl / pyridyl / naphthyl-4-thienylmethylene-5-hydroxypyrazolone phenylsemicarbazone / methylthiosemicarbazide / ethylthiosemicarbazide / thiosemicarbazide or 1-phenyl-3-thienyl-4-subsituted-phenylmethylene / thienylmethylene / pyrrylmethyl / furylmethylene / pyridylmethylene / naphthylmethylene-5-hydroxypyrazolone phenylsemicarbazone / methylthiosemicarbazide / ethylthiosemicarbazide / thiosemicarbazide, and the polymer is anyone of polystyrene, polymethylstyrene, polyethylene and polypropylene. The thienyl group-containing pyrazolone derivative and its polymer film can be used in the information storage field, the molecular switch field, the false proof field, the optical eyeglass field, the intelligent window field and the like.

Disclosed is a pyrazolone derivative having blood sugar lowering action represented by formula (I), wherein R1 is hydrogen or low level alkyl or low level alkoxy, R2, R3, R4, R5 are separate hydrogen atom, halogen, low level alkyl, low level alkoxy, hydroxy, cyano, methylmercapto or methylsulfuryl, L and M each represents a link formed by the combination of L and M.

It is an object of the present invention to provide a novel medicament for preventing and / or treating ophthalmologic diseases caused by ocular angiogenesis. According to the present invention, provided is a medicament for preventing and / or treating ophthalmologic diseases caused by ocular angiogenesis, which comprises, as an active ingredient, a pyrazolone derivative such as 3-methyl-1-phenyl-2-pyrazolin-5-one, or a physiologically acceptable salt thereof, or a hydrate thereof or a solvate thereof.

The object of the present invention is to provide a medicament useful for preventing and / or treating inflammatory bowel disease. The present invention provides a medicament for preventing and / or treating inflammatory bowel disease which comprises as an active ingredient a pyrazolone derivative represented by the following formula (I) or a physiologically acceptable salt thereof, or a hydrate thereof or a solvate thereof: wherein R1 represents a hydrogen atom, an aryl group, an alkyl group, or an alkoxycarbonylalkyl group; R2 represents a hydrogen atom, an aryloxy group, an arylmercapto group, an alkyl group or a hydroxyalkyl group; or R1 and R2 are combined with each other to represent an alkylene group; and R3 represents a hydrogen atom, an alkyl group, a cycloalkyl group, a hydroxyalkyl group, a benzyl group, a naphthyl group, a phenyl group, or a phenyl group substituted with 1 to 3 substituents selected from the group consisting of an alkyl group, an alkoxy group, a hydroxyalkyl group, an alkoxycarbonyl group, an alkylmercapto group, an alkylamino group, a dialkylamino group, a halogen atom, a trifluoromethyl group, a carboxyl group, a cyano group, a hydroxyl group, a nitro group, an amino group and an acetamide group.

It is intended to provide drugs for treating and / or preventing ischemic diseases which are safe and have little side effects. Namely, drugs comprising a combination of an antithrombotic agent and a pyrazolone derivative defined in the description or its pharmaceutically acceptable salt.

The invention relates to the field of organic synthesis, and discloses a fused ring pyrazolone derivative and a preparation method thereof. The preparation method comprises the steps: (1) mixing [Cp *IrCl2] 2, AgOAc, pyrazolone compounds, azide compounds and a solvent for a reaction; and (2) carrying out TLC tracking reaction and column chromatography separation to obtain the fused ring pyrazolone derivative. The preparation method has the advantages of easily available raw materials, high stability, high yield, simple reaction conditions and the like.

The invention belongs to an organic photochromic material, and relates to preparations and applications of a thienyl group-containing pyrazolone derivative and its polymer film. The thienyl group-containing pyrazolone derivative is anyone of 1-phenyl-3-substituted-phenyl / thienyl / pyrryl / furyl / pyridyl / naphthyl-4-thienylmethylene-5-hydroxypyrazolone phenylsemicarbazone / methylthiosemicarbazide / ethylthiosemicarbazide / thiosemicarbazide or 1-phenyl-3-thienyl-4-subsituted-phenylmethylene / thienylmethylene / pyrrylmethyl / furylmethylene / pyridylmethylene / naphthylmethylene-5-hydroxypyrazolone phenylsemicarbazone / methylthiosemicarbazide / ethylthiosemicarbazide / thiosemicarbazide, and the polymer is anyone of polystyrene, polymethylstyrene, polyethylene and polypropylene. The thienyl group-containing pyrazolone derivative and its polymer film can be used in the information storage field, the molecular switch field, the false proof field, the optical eyeglass field, the intelligent window field and the like.

An electroluminescent material Tb(L1)3(L2)n is disclosed, where Tb is three-valence positive ion of Tb, Li is the organic chelating negative ion of pyrazolinone and L2 is neutral ligand. The device prepared from it is also disclosed. Their advantages are high brightness and high efficiency.

The present invention relates to a preparation method of a pyrazolone derivative. The method comprises the following steps: 1-substituted-3-trifluoromethyl-5-pyrazolone, substituted benzaldehyde and an appropriate amount of an additive reagent-grade crude silica gel are uniformly mixed, and then are stirred at room temperature to a obtain compound 4,4'-(arylmethylene)bis(1-aryl-3-trifluoromethyl-1H-pyrazole-5(4H)one), and the solid crude silica gel which is filtered out is washed with an appropriate amount of a solvent, and is dried for cycle use. The method of the invention has the advantagesof environment friendliness, easily available raw materials, mild reaction conditions, simplicity in experiment operation, strong universality, convenience in post-treatment of the product, cycle useof the additive crude silica gel after simple treatment, and high yield of the product.

The invention discloses a tetralin pyrazolone triazine compound as well as a preparation method and application thereof. The tetralin pyrazolone triazine compound is shown in the general formula (I). The preparation method comprises the following steps: the compounds shown in the general formulas (II) and (III) are mixed in a solvent to react under the catalysis of protonic acid or lewis acid so as to obtain the compound as shown in the general formula (I). According to the invention, a simple and practical novel method is provided for preparing a tetralin pyrazolone derivative. The prepared compound is not reported in documents and is a novel compound. The preparation method provided by the invention is an acid catalysis cycloaddition method, the reaction has molecular economy, the catalyst is protonic acid or lewis acid, application of transition metal is avoided, and the product is prevented from heavy metal pollution risk; an expensive phosphine catalyst is not required, and the cost is low.

A method for purifying a pyrazolinone derivative comprising a step of mixing a solution containing a mixture containing the pyrazolinone derivative and a good solvent which can dissolve the pyrazolinone derivative with a poor solvent to crystallize the pyrazolinone derivative.

An object of the present invention is to provide a medicament and method which is useful for prevention and / or therapy of arterial wall injury. According to the present invention, there is provided a method for prevention and / or therapy of arterial wall injury which comprises a step of administering the pyrazolone derivative represented by the following formula (I) or the physiologically acceptable salt thereof, or the hydrate or solvate thereof in a preventively or therapeutically effective amount to mammals including humans:wherein R1 represents a hydrogen atom, an aryl group, an alkyl group, or an alkoxycarbonylalkyl group; R2 represents a hydrogen atom, an aryloxy group, an arylmercapto group, an alkyl group or a hydroxyalkyl group; or R1 and R2 are combined with each other to represent an alkylene group; and R3 represents a hydrogen atom, an alkyl group, a cycloalkyl group, a hydroxyalkyl group, a benzyl group, a naphthyl group, a phenyl group, or a phenyl group substituted with 1 to 3 substituents selected from the group consisting of an alkyl group, an alkoxy group, a hydroxyalkyl group, an alkoxycarbonyl group, an alkylmercapto group, an alkylamino group, a dialkylamino group, a halogen atom, a trifluoromethyl group, a carboxyl group, a cyano group, a hydroxyl group, a nitro group, an amino group and an acetamide group.

The invention discloses a pyranopyrazole acrylate derivative, a preparation method and application thereof. The preparation method of this type of derivative is as follows: the MBH carbonate containing quinoline heterocycle as shown in formula (II), the pyrazolone derivative shown in formula (III) are mixed with solvent, add chiral phosphine catalyst and The base is stirred and reacted to prepare the pyranopyrazole acrylate derivatives shown in the formula (I). The method of the present invention has the characteristics of easy-to-obtain raw materials, simple and convenient operation, high chemical selectivity and regioselectivity, and the target compound is effective against human colon cancer cell HT-29, human non-small cell lung cancer cell A549, and triple-negative breast cancer cell MDA-MB-231. It has better effect of inhibiting proliferation in vitro, therefore, the method of the present invention has great implementation value and application prospect.

The invention discloses a pyran-pyrazole acrylate derivative as well as a preparation method and application thereof. The preparation method of the derivative comprises the following steps: mixing MBH carbonate containing quinoline heterocycle as shown in a formula (II), a pyrazolone derivative as shown in a formula (III) and a solvent, adding a chiral phosphine catalyst and alkali, and carrying out stirring reaction for 36-240 hours at -20 to 80 DEG C to prepare the pyranopyrazole acrylate derivative, that is, the 1,4-dihydropyrazolo[4',3':5,6]pyrano[2,3-b]quinoline-4-acrylate derivative. The method has the advantages that raw materials are easy to obtain, operation is easy and convenient, and chemical selectivity and regioselectivity are high; the target compound has a good in-vitro proliferation inhibition effect on human colon cancer cells HT-29, human non-small cell lung cancer cells A549 and triple negative breast cancer cells MDA-MB-231. Thus, the method has high implementation value and application prospects.

The invention discloses a preparation method of a 4-thio-pyrazolone derivative. According to the method, a pyrazolone derivative is directly applied to react with sulfonyl chloride in the presence of potassium iodide and triphenylphosphine to synthesize the 4-thio-pyrazolone derivative, wherein the used solvent is 1,4-dioxane, the reaction temperature is 60-100 DEG C, and the reaction time is 8-24 hours; and gradient elution is carried out on dichloromethane and methanol as a mobile phase at the volume ratio of (40 to 1) to (20 to 1) to obtain a white or light yellow solid. A series of thio-pyrazolone compounds are synthesized by the novel method for the first time, and can be used as important medical intermediates of analgesic medicines, antipyretic medicines and antibacterial medicines.

The invention relates to meldrum's acid, barbituric acid and pyrazolone derivatives substituted with hydroxylamine as hno donors. The disclosed subject matter provides certain N-substituted hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and / or development of a disease or condition. In some embodiments, the diseaseor condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.