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 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.

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 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 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 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 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.