79 results about "Benzoxazinones" patented technology

Q is —N=or CR2 X is S, O or NOR3 Y is —O—, —S—, —SO— or —SO2—R and R1 are each, independently, H, a substituted or unsubstituted aliphatic, aromatic, heteroaromatic or aralkyl groupR2 is H or a substituentR3 is H, or —C(O)R4 R4 is a substituted or unsubstituted aliphatic or aromatic groupn is an integer from 0 to 1Chemical compounds having structural formula I and physiologically acceptable salts thereof, are inhibitors of serine / threonine and tyrosine kinase activity. Several of the tyrosine kinases, whose activity is inhibited by these chemical compounds, are involved in angiogenic processes. Thus, these chemical compounds can ameliorate disease states where angiogenesis or endothelial cell hyperproliferation is a factor. These compounds can be used to treat cancer and hyperproliferative disorders.

Ultraviolet light absorbing polymer film, coating, or molded article UV filter elements are described which comprise a polymer phase having molecularly dispersed therein a) a first ultraviolet absorbing dibenzoylmethane compound of formula (I) where R1 through R5 are each independently hydrogen, halogen, nitro, or hydroyxl, or further substituted or unsubstituted alkyl, alkenyl, aryl, alkoxy, acyloxy, ester, carboxyl, alkyl thio, aryl thio, alkyl amine, aryl amine, alkyl nitrile, aryl nitrile, arylsulfonyl, or 5-6 member heterocylce ring groups, and b) a second ultraviolet light absorbing compound which absorbs ultraviolet light at a wavelength for which the first compound is deficient at absorbing. In particular embodiments, the second ultraviolet light absorbing compound may comprise a hydroxyphenyl-s-triazine, hydroxyphenylbenzotriazole, formamidine, benzoxazinone, or benzophenone compound. In a specific embodiment of the invention, the above UV absorbing compounds are employed in cellulose acetate film for the fabrication of a protective film for polarizers for use in display applications.

Substituted benzoxazin-4(3H)-ones are provided which are useful for treating thrombosis and for reducing the likelihood and / or severity of a secondary ischemic event in a patient.

[PROBLEMS]To provide a compound useful as an agent for the treatment of circulatory diseases, nervous system diseases, metabolic diseases, reproductive system diseases, and digestive tract diseases.[MEANS FOR SOLVING PROBLEMS]The compound, which is for use as an active ingredient, is represented by the formula (I):[wherein R1 represents optionally halogenated C1-6 alkyl, etc.; R2 represents, e.g., a group represented by the formula (II-1) or (II-4)(wherein W represents C1-6 alkylene, etc. and R represents C1-6 alkyl, etc.); R3 represents hydrogen, C1-6 alkyl, etc.; X represents —O—, —NH—, etc.; and Y1, Y2, Y3, and Y4 each independently represents —CH—, —N—, etc.].

The present invention refers to a method for controlling undesired vegetation at a plant cultivation site, the method comprising the steps of providing, at said site, a plant that comprises at least one nucleic acid comprising a nucleotide sequence encoding a wild-type or a mutated protoporphyrinogen oxidase (PPO) which is resistant or tolerant to a benzoxazinone-derivative herbicide by applying to said site an effective amount of said herbicide. The invention further refers to plants comprising wild-type or mutated PPO enzymes, and methods of obtaining such plants.

Benzoxazinone and quinazolinone compounds useful in organic light emitting devices (OLEDS) are described.

The present invention refers to a method for controlling undesired vegetation at a plant cultivation site, the method comprising the steps of providing, at said site, a plant that comprises at least one nucleic acid comprising a nucleotide sequence encoding a wild-type or a mutated protoporphyrinogen oxidase (PPO) which is resistant or tolerant to a benzoxazinone-derivative herbicide by applying to said site an effective amount of said herbicide. The invention further refers to plants comprising wild-type or mutated PPO enzymes, and methods of obtaining such plants.

The present invention relates generally to pharmaceutical agents containing a heterocyclic moiety, and in particular, to heterocyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterocyclic MMP-13 inhibiting compounds with a benzoxazinone moiety, that exhibit an increased potency and selectivity in relation to currently known MMP-13 inhibitors.

The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one of formula (VI-i) which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.

The invention provides a novel synthetic method of a bis-benzoxazine ketone ultraviolet absorbent, and belongs to the technical field of fine chemical engineering. The method comprises the following steps: A, stirring, anhydrides, used as raw materials, of o-aminobenzoic acid and (o-, m-, p-) phthaloyl dichloride or (o-, m-, p-)phthalic acid for a certain time in a non-polar solvent; B, adding chemical dehydrating agent or physical dehydrating agent in a reaction system without separating, slowly heating and refluxing for a certain time to obtain (o-, m-, p-)substituted bis-benzoxazine ketone ultraviolet absorbent; wherein the stirring time in the step A is not less than 1 hour, the refluxing time is 5-10 hours in the step B, the chemical dehydrating agent used in the step B is various dehydrating agents reacted with the water, including but not limited to alkaline calcium oxide, soda lime, acidic concentrated sulfuric acid, concentrated phosphoric acid, polyphosphoric acid, phosphorus pentoxide, thionyl chloride, acetic anhydride and the like, neutral molecular sieve, water-absorbent, anhydrous cupric sulfate and the like; the physical dehydrating agent comprises but not limited to non-protonic solvent such as benzene, methylbenzene, xylene and the like. The method provided by the invention has the advantages of being simple in operation flow, low in cost, simple in equipment, and suitable for the scale industrial production.

The invention belongs to the field of pharmaceutical chemistry and particularly relates to a benzoxazinone derivative, a preparation method thereof and application thereof in related diseases. The benzoxazinone derivative provided herein has a specific structure shown in formula I or II that is shown in the description. The invention also provides a synthetic method shown in formula I or II and application thereof in related diseases, mainly relating to tumors, cardiovascular diseases, neurodegenerative diseases, metabolic diseases, inflammatory diseases and the like.

The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one of formula (VI-i) which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor. In an embodiment, the present invention provides a process for the preparation of an amino alcohol compound of formula (V-i) comprising adding a toluene solution of 2,3-dichloro-5,6-dicyano-1,4-benzoquinone to a toluene solution of a compound of formula (III-i), via a compound of formula (IV-i).

The present invention relates generally to pharmaceutical agents containing a heterocyclic moiety, and in particular, to heterocyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterocyclic MMP-3, MMP-8 and / or MMP-13 inhibiting compounds with a squaramide or benzoxazinone moiety, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.

The invention discloses a benzoxazinone thiophenol fluorescent probe and a preparation method thereof, and belongs to the technical field of analysis and detection. The benzoxazinone thiophenol fluorescent probe has a favorable fluorescent property, can selectively recognize thiophenol in a buffer solution, is quick in response, low in detection limit (only 24 nM), large in Stokes displacement, enhanced in fluorescence, and high in selectivity and anti-interference capability, and can qualitatively or quantitatively analyze thiophenol in real time, thereby being applicable to thiophenol detection in the watery environment.

This invention pertains to a method for controlling lepidopteran, homopteran, hemipteran, thysanopteran and coleopteran insect pests comprising contacting the insects or their environment with an arthropodicidally effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereofwherein A and B and R1 through R8 are as defined in the disclosure.This invention further relates to a bezoxazinone compound of Formula 10wherein R4 through R8 are as defined in the disclosure, useful for preparation of a compound of Formula I.

The invention relates to weeding activity of 2-benzoxazinone-5-cyclohexylaminocarbonyltetrazolylone,Wherein R1 is CH3 and C2H5; R2 is CH3, C2H5, CH2CH=CH2 and propargyl group; and R3 is F and Cl.When 1500g of weedicide per hectare is applied, the weedicide has broad spectrum for cockspur grass, crab grass, amaranth and rape before and after seedling.

Embodiments of the present invention are directed to polymeric compositions of polyethersulfone comprising hindered amine light stabilizer, benzoxazinone-based ultraviolet stabilizer and diphenylacrylate-based ultraviolet stabilizer.

Stabilized photoactive composition comprising: - at least one photoactive organic polymer; - at least one light stabilizer selected from hindered amines; - at least one UV absorber selected from triazines, benzoxazinones, benzotriazoles, benzophenones, benzoates, formamidines, cinnamates or propenoates, aromatic propanediones, benzoimidazoles, cycloaliphatic ketones, formanilides including oxamides, cyanoacrylates, benzopyranones, salicylates, or mixtures thereof. Said photoactive composition can be advantageously used in the construction of photovoltaic devices such as, for example, photovoltaic cells, photovoltaic modules, solar cells, solar modules, on both rigid and flexible supports.

A synthesis method of a 2-substituted benzoxazin ketone compound shown in the chemical formula (I) comprises the following steps: using 2-aryl indole as a raw material, using potassium hydrogen sulfate compound salt 2KHSO5. KHSO4. K2SO4 oxidation as an oxidizing agent, and performing oxidation reaction to obtain the 2-substituted benzoxazin ketone compound, wherein R represents a hydrogen atom, an alkyl of C1-C6, a naphthenic base, an alkoxy of C1-C6, halogen and an aryl group, and R' represents an aryl group or a substituted aryl group, an alkoxy of C1-C6, an aryloxy group, an alkoxy group of C1-C6 and an aryl amine group. The synthesis method has the advantages of green, high efficiency, mild reaction condition, simple operation, wide application range, low manufacturing cost, high synthesis yield and the like.

This invention relates to novel compounds of Formula (I) for use as vascular damaging agents: wherein: X is selected from: —O—, —S—, —S(O)—, —S(O2)—, —N(R4)— or —N(R4)CH2C(O)—; R1 is independently selected from: amino, halo, hydroxy, —OPO3H2, C1-4alkyl, C1-4alkoxy, N-C1-4alkylamino, N,N-di-C1-4alkanoylamino or C1-4alkylthio wherein the amino group is optionally substituted by an amino acid residue and the hydroxy group is optionally esterified; R2 is selected from: hydrogen or C1-4alkyl; R3 is selected from: hydrogen or C1-4alkyl; R4 is selected from: hydrogen or C1-4alkyl; n is 0, 1 or 2; and p is 0, 1, 2 or 3; or a salt, pro-drug or solvate thereof. The invention also relates to methods for preparing compounds of Formula (I), to their use as medicaments (including methods for the treatment of angiogenesis or disease states associated with angiogenesis) and to pharmaceutical compositions containing compounds of Formula (I).

The invention discloses a method for chiral spirophosphonate catalyzed synthesis of an optically active 2H-1,4-benzoxazine-2-one derivative. The method is characterized in that the 2H-1,4-benzoxazine-2-one derivative is prepared through a complete reaction of a benzoxazinone compound and a pyrrole compound as raw materials in an organic catalyst with chiral spirophosphonate as a catalyst. The method using an asymmetric catalysis aza Friedel-Crafts alkylation reaction technology to synthesize the optically active 2H-1,4-benzoxazine-2-one derivative containing a trifluoromethyl quaternary stereo center has the advantages of mild reaction conditions, simple process and convenient operation, and the above obtained product has potential good bioactivity and is of great significance to screen new drugs, and obtained chiral compounds can be used as a drug synthesis intermediate.

[PROBLEMS]To provide a compound useful as an agent for the treatment of circulatory diseases, nervous system diseases, metabolic diseases, reproductive system diseases, and digestive tract diseases.[MEANS FOR SOLVING PROBLEMS]The compound, which is for use as an active ingredient, is represented by the formula (I):[wherein R1 represents optionally halogenated C1-6 alkyl, etc.; R2 represents, e.g., a group represented by the formula (II-1) or (II-4)(wherein W represents C1-6 alkylene, etc. and R represents C1-6 alkyl, etc.); R3 represents hydrogen, C1-6 alkyl, etc.; X represents —O—, —NH—, etc.; and Y1, Y2, Y3, and Y4 each independently represents —CH—, —N—, etc.].

The invention discloses a preparation method of chlorantraniliprole and an intermediate of chlorantraniliprole, which comprises the following steps: in the presence of an alkali and a solvent, mixing3-bromo-1-(3-chloro-2-pyridyl)-1H-pyrazole-5-carboxylic acid and 2-amino-5-chloro-3-methylbenzoic acid together to form a material I; and mixing the methylsulfonyl chloride with the material I, and carrying out a reaction so as to obtain a 2-[3-bromo-1-(3-chloro-2-pyridyl)-1H-pyrazol-5-yl]-6-chloro-8-methyl-4H-3, 1-benzoxazine-4-one intermediate, i.e., a chlorantraniliprole intermediate. The method is easy to operate, the benzoxazinone intermediate generated in the reaction process does not need to be further treated, can be adopted in a next step of reaction directly without drying for preparation of chlorantraniliprole; the method has the advantages that the method is simple in process and high in total yield and product quality, a filtrate can be used by the aid of synchronous and continuous application processes, accordingly, the usage amount of the solvent can be reduced to a great extent, and the method is suitable for industrial production.

A benzoxazinone compound having the following formula (I):whereinone of R1 and R2 is H, and the other of R1 and R2 is a halogen group, and R1 and R2 cannot be the same at the same time; andR3, R4, R5, R6, and R7 are independently selected from the group consisting of H, a halogen group, a C1-C4 alkyl group, and a C1-C4 alkoxyl group.

The invention provides an N-(arylaminoethyl)-3,1-benzoxazine-2-one compound for crop bacteriostasis, a preparation method and application thereof. The compound is prepared by reacting N-(2-chloroethyl)-3,1-benzoxazine-2-one with substituted aniline in the presence of a phase transfer catalyst and an alkali. The preparation method has the advantages of easily available raw materials, low productioncost and high yield. The compound has a good inhibition effect on the activity of crop germs and particularly has a remarkable inhibition effect on the activity of germs such as fusarium graminearum,botrytis cinerea, phytophthora capsici, sclerotinia sclerotiorum, rhizoctonia solani or magnaporthe oryzae and the like.

It is an object of the present invention to provide a bisbenzoxazinone compound which does not substantially contain an alkali metal salt, has high purity and provides a resin composition having excellent resistance to hydrolysis when it is contained in a resin, a production method thereof, and a resin composition comprising the compound.The present invention is a bisbenzoxazinone compound represented by the following formula (4):(R1 and R2 are each independently a hydrogen atom, hydroxyl group, alkyl group having 1 to 3 carbon atoms, or the like), and has (i) a purity of 98% or more, (ii) a content of a compound represented by the following formula (7) of less than 0.15 wt %:(iii) a maximum peak in the measurement of the light reflectance at a visible range of its powder at 380 to 480 nm and a maximum light reflectance of 100 to 120%,(iv) a metal sodium content of less than 50 ppm and(v) a YI value of −10 to 10.