187 results about "Benzopyrans" patented technology

Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: wherein j is 0 or 1, k is 0 or 1, m is 0, 1, or 2; n is 1 or 2; A is selected from the partial Formulas: where q is 1, 2, or 3, W3 is -O-; -N(R9)-; or -OC(=O)-; R7 is selected from -H; -(C1-C6) alkyl, -(C2-C6) alkenyl, or -(C2-C6) alkynyl substituted by 0 to 3 substituents R10; -(CH2)u-(C3-C7) cycloalkyl where u is 0, 1 or 2, substituted by 0 to 3 R10; and phenyl or benzyl substituted by 0 to 3 R14; R8 is tetrazol-5-yl; 1,2,4-triazol-3-yl; 1,2,4-triazol-3-on-5-yl; 1,2,3-triazol-5-yl; imidazol-2-yl; imidazol-4-yl; imidazolidin-2-on-4-yl; 1,3,4-oxadiazolyl; 1,3,4-oxadiazol-2-on-5-yl; 1,2,4-oxadiazol-3-yl; 1,2,4-oxadiazol-5-on-3-yl; 1,2,4-oxadiazol-5-yl; 1,2,4-oxadiazol-3-on-5-yl; 1,2,5-thiadiazolyl; 1,3,4-thiadiazolyl; morpholinyl; parathiazinyl; oxazolyl; isoxazolyl; thiazolyl; isothiazolyl; pyrrolyl; pyrazolyl; succinimidyl; glutarimidyl; pyrrolidonyl; 2-piperidonyl; 2-pyridonyl; 4-pyridonyl; pyridazin-3-onyl; pyridyl; pyrimidinyl; pyrazinyl; pyridazinyl; indolyl; indolinyl; isoindolinyl; benzo[b]furanyl; 2,3-dihydrobenzofuranyl; 1,3-dihydroisobenzofuranyl; 2H-1-benzopyranyl; 2-H-chromenyl; chromanyl; benzothienyl; 1H-indazolyl; benzimidazolyl; benzoxazolyl; benzisoxazolyl; benzothiazolyl; benzotriazolyl; benzotriazinyl; phthalazinyl; 1,8-naphthyridinyl; quinolinyl; isoquinolinyl; quinazolinyl; quinoxalinyl; pyrazolo[3,4-d]pyrimidinyl; pyrimido[4,5-d]pyrimidinyl; imidazo[1,2-a]pyridinyl; pyridopyridinyl; pteridinyl; or 1H-purinyl; or A is selected from phosphorous and sulfur acid groups; W is -O-; -S(=O)t-, where t is 0, 1, or 2; or -N(R3)-; Y is =C(R1a)-, or -[N<custom-character file="US20020111495A1-20020815-P00900.TIF" wi="20" he="20" id="custom-character-00001" / >(O)k] where k is 0 or 1; R4, R5 and R6 are (1) -H; provided that R5 and R6 are not both -H at the same time, -F; -Cl; -(C2-C4) alkynyl; -R16; -OR16; -S(=O)pR16; -C(=O)R16, -C(=O)OR16, -C(=O)OR<highlight><sup

A class of benzopyrancarboxylic acid derivatives comprises compounds that are potent agonists of PPAR alpha and / or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and / or gamma mediated diseases, disorders and conditions.

A class of benzopyrancarboxylic acid derivatives comprises compounds that are potent agonists of PPAR alpha and / or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and / or gamma mediated diseases, disorders and conditions.

This invention relates to dibenzothiophene, dibenzofuran, dibenzopyran, and dibenzothiapyran compounds. This invention also relates to layers and devices including at least one of the above compounds.

The present invention relates to substituted benzopyran derivatives, stereoisomers, and pharmaceutical acceptable salts thereof and processes for the preparation of the same. The compounds of the present invention are useful as Estrogen Receptor ? agonists. Such agonists are useful for the treating Estrogen Receptor ? mediated diseases such as prostate cancer or BPH.

The present invention is directed to novel benzopyran derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders related to potassium channel.

Compositions for protection against SVFS induced by niacin, a carcinoid, mesenteric traction, serotonin, post-menopause, alcohol, monosodium glutamate, mastocytosis, atopic dermatitis, food-allergy or food intolerance, and mast cell activation syndrome, or against individual symptoms of SVFS, superficial vasodilation, feeling of warmth, itching (pruritus) and hives, comprising a flavonoid compound of the structure 2-phenyl-4H-1-benzopyran or 2-phenyl-4-keto-1-benzopyran or glycosides thereof, or chalconoid compounds, with appropriate substitutions of their hydroxyl groups to render them water soluble or in combination with a pshospholipid or cyclodextrin to render them to have higher oral absorption, administered alone or together with an anti-superficial vasodilation dose of one or more of, olive kernel oil, a serotonin inhibitor, a prostaglandin inhibitor, willow bark extract. A composition for treating cardiovascular disease with niacin, but without eliciting the SVFS effects of niacin, has also been invented.

The invention relates to a synthesis method and application of a novel high-selectivity and high-sensitivity near infrared fluorescence probe for visually detecting hydrogen polysulfide. The method comprises the steps of making benzopyran carbonitrile and p-hydroxy benzaldehyde react to obtain a precursor, and then conducting an esterification reaction with 2-fluoro-5-nitrobenzoic acid to obtain the fluorescence probe. The probe reacts with sodium polysulfide to generate a strengthened fluorescence change, which is that the fluorescence at the 682 nm is strengthened remarkably. Besides, a dynamic experiment result shows that the reaction time of the compound and hydrogen polysulfide is shorter than 5 min, and the interference rejection is strong. Thus, the pyran carbonitrile compound can serve as the application of the near infrared fluorescence probe for detecting hydrogen polysulfide.

The invention discloses a novel preparation method of pranoprofen. The novel preparation method of the pranoprofen has the advantages of being high in yield, having less impurities, and being safe andenvironmentally friendly. The novel preparation method of the pranoprofen comprises the following steps that step 1, 5H-[1]-benzopyran[2,3-b]pyridine and propionyl chloride are directly acylated; step 2, bromination is carried out; step 3, potassium tert-butoxide or sodium tert-butoxide is used for hydrolysis, and finally, rearrangement is carried out to obtain the pranoprofen.

A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I′wherein X, A1, A2, A3, A4, R, R″, R1 and R2 are as described in the specification.

Substituted and unsubstituted flavone or isoflavone glycoside derivatives of the formula [A1-C(═O)O]m—[X—O-Z]—[O—C(═O)-A2]n, wherein [X—O-Z] represents a flavone or isoflavone glycoside structure, particularly a naringin residue, X is a flavone or isoflavone corresponding to formula (IIa) or formula (IIb):wherein the flavone or isoflavone residue is substituted one or more times and / or reduced one or more times; Z represents a mono-, di- or polysaccharide, which is acetally-bound at the benzopyran group to X and ester-substituted by —O—C(═O)-A2; [A1-C(═O)] is an acyl group on the flavone or isoflavone; A1 and A2 independently, represent a polyunsaturated C15-26 alkenyl group containing at least four isolated and / or at least two conjugated double bonds, or an arylaliphatic radical with 1-to-4 methylene groups between the ester group and the aromatic ring; [C(═O)A2] is an acyl group; n is an integer other than 0; m is an integer, including 0; and R1, R2 and R are hydroxyl groups or hydrogen atoms.

The invention discloses new application of a 2-(4-fluorophenyl)-3-nitro-8-O-ethyl-2-hydro-benzopyran compound, in particular application of the compound serving as phosphatidylinositol-3-kinase (PI3K) inhibitor. The PI3K inhibitor can inhibit PI3K and disturb a PI3K / AKT signal channel, has good treatment effect on multiple tumors, particularly malignant hematological diseases, can effectively control the propagation of tumor cells and induce the apoptosis thereof, and has the effect of inhibiting and treating the tumors; and meanwhile, the PI3K has low toxicity.

The present invention relates to a process for separation of desired diastereomeric pair from a mixture of diastereomeric pairs thereby obtaining nebivolol intermediates. Thus, the mixture of (+)-[1S*(R*)]-6-fluoro-3,4-di-hydro-α-[[(phenylmethyl)amino]methyl]-2H-1-benzopyran-2-methanol, (+)-[1S*(S*)]-6-fluoro-3,4-dihydro-2-oxi -ranyl-2H-1-benzopyran and ethanol is heated to reflux temperature and stirred for 8 hours at the same temperature to obtain (±)-[2R*[1S*,5S*(S*)]]+[2R*[1S*,5R*(R*)]]-α,α′-[phenylmethyliminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran ran-2-methanol]. Then the reaction mass is cooled to 10° C., the pH is adjusted to 2 with HCl gas and stirred for 45 minutes at 25° C. to 30° C. Then the separated solid is filtered and dried to give (+)-[2R*[1S*,5S*(S*)]]-α,α′-[phenylmethyliminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol] hydrochloride salt, which can be converted into nebivolol.

This invention provides 6H-[1]benzopyrano[4,3-b]quinoline compounds having the formula I: The invention further provides compositions including the compounds, methods for the use of the compounds, and the methods of preparation of the compounds.

A therapeutic compound has a modified phenolic compound of the general formula (I)wherein at least one of R, R1, R2, R3, and R4 is an electrophilic group chosen from halogen, aldehyde, haloalkane, alkene, butyryl, flurophenol, sulfonamide, flurophenol sulfoxide and the remaining R, R1, R2, R3, and R4 is are each independently hydrogen, a hydroxyl group, an alkoxy group, a rutinosyl group, a carboxyl group, chromone, benzopyran, a rhamnosyl group, a substituted alkoxy group or a substituted acyloxy group wherein the substituent is chosen from hydroxyl, alkoxy, aryloxy, phenyl, halogen, and amido group. The compound can be used in a therapeutic treatment of inflammatory related diseases and condition.

The invention relates to dibenz, naphthopyrans and dibenz and dibenz spiropyran compound, and the method for preparing the same. Said method comprises: dibenzofuran or naphthofurans reacting with lithium with molar ration being 1:2-2.4, opening loop, reacting with aldehyde, ketone, ester or amide at temperature of -70 to -80 Deg. C, the molar ratio between dibenzofuran or naphthofurans and aldehyde, ketone, ester or amide is 1:0.7-1, dewatering and closing loop, and getting final product. The invention is characterized by cheap raw material, simple process, high productivity, and multiple kinds of products.

The invention provides a benzopyranyl-3-alcohol esterified derivative and a preparation method of the benzopyranyl-3-alcohol esterified derivative. The benzopyranyl-3-alcohol esterified derivative is shown as the following formula I, wherein in the formula I, R represents one or more of hydrogen, hydroxy, alkoxy, alkyl amino, alkyl acylamino, fluorine or benzoyl; the benzoyl contains one or more of hydroxy, alkoxy, alkyl amino, alkyl acylamino or fluorinated substituents, wherein alkyl in alkoxy, alkyl amino and alkyl acylamino is C1 to C10 straight chain or branched chain alkyl; X in the formula represents hydrogen or oxygen; and Y in the formula represents oxygen or nitrogen and hydrogen. The benzopyranyl-3-alcohol esterified derivative is low-toxic, has excellent antineoplastic multidrug resistance activity and can be used for preparing a medicament for treating breast cancer, colon cancer, prostatic cancer, leukemia, myeloma, pancreatic cancer and the like.

The invention provides a coumarin-benzopyranium salt derivative as well as a synthesis method and application thereof. The Chinese name of the derivative is called (E)-2-(4-(4-(2-cyano-3-(7-(diethylamino)-2-oxo-2H-chrom-3-yl) acryloyl) piperazine-1-yl) phenyl)-7-(diethylamino) chromium perchlorate, the English name is (E)-2-(4-(4-(2-cyano-3-(7-(diethylamino)-2-oxo-2H-chrom-3-yl) acryloyl) piperazine-1-yl) phenyl)-7-(diethylamino) chromenium perchlorate, and the is derivative is named as CM-BP. The invention also provides a synthetic method of the coumarin-benzopyranium salt derivative, a method for distinguishing, identifying and detecting glutathione and sulfur dioxide, and an application of the coumarin-benzopyranium salt derivative in sulfur dioxide metabolic imaging. The contents of glutathione and sulfur dioxide can be quantitatively detected by a fluorospectro photometer in a PBS solution with the pH value of 7.4. The detection process is simple, sensitive and rapid, and the detection result is high in accuracy.

The present invention discloses liquid crystal compounds having dibenzopyran derivatives with cycloalkyl groups, and preparation methods and application thereof. The liquid crystal compounds having dibenzopyran derivatives with cycloalkyl terminal groups, shown in formula I, exhibit better miscibility and a very large negative dielectric constant, compared to those having a flexible alkyl chain as a terminal group, therefore the compounds of the present invention, shown in formula I, may improve the miscibility of liquid crystal compounds and broaden the application range of liquid crystal mixtures. In addition, the compounds may also increase the negative dielectric constants of liquid crystal mixtures, having an important application value.

The invention discloses a benzopyranone compound, as well as a preparation method and an application thereof, belonging to the field of synthesis of medicaments. The method comprises the following steps of: based on 1, 4-benzopyrandione and p-tert-butyl cyclohexyl acetaldehyde as raw materials, performing condensation reaction to get 3-((4-tert-butyl-cyclohexyl) dimethylene)-1, 4-benzopyrandione. The invention further discloses the method for preparing buparvaquone by utilizing the compound. The method has the characteristics of simple synthesis method, effect of avoiding the use of AgNO3, high total yield and the like.

The invention relates to a method of treating a diabetic condition by administering a therapeutically effective amount of a histamine-3 receptor antagonist, including benzofuran and benzopyran derivatives of formula (I), aminoalkoxybiphenylcarboxamide compounds of formula (III), and aminoetherbiphenyl compounds of formula (IV) as described herein.

The invention relates to a composition comprising a lupin total extract consisting of a lupin sugar extract, comprising at least 50 % galactooligosacharides by weight, in relation to the weight of dry matter, and a lupin peptide extract. The composition can also contain a chromane derivative or a chromene derivative. The invention also relates to a pharmaceutical and / or cosmetic composition comprising said lupin total extract, used advantageously as an anti-inflammatory agent, which repairs the cutaneous barrier and heals, used particularly in the prevention and / or treatment of erythemas.

Provided are benzopyran compounds of formula I, for example, pomiferin-3′,4′-dimethyl ether, and the use of such compounds and compositions thereof to modulate (e.g., inhibit) melanogenesis and pigmentation.wherein R3, R4, R5, R6, R7 and R8 are described herein. Also provided are plant extracts containing a compound of formula I, and the use of such a plant extract to modulate (e.g., inhibit) melanogenesis and pigmentation. The compound or plant extract may be prepared as pharmaceutical and cosmetic compositions, and may be used for the prevention and treatment of conditions that are related to aberrant melanogenesis activity.

The invention provides a method for manufacturing a smart light-controlled insulating window membrane, which aims to solve the problems of low efficiency for blocking ultraviolet and infrared rays, low speed of light-controlled color-changing and recovery, poor using comfortable feeling and the like in the prior art. According to the technical scheme, the method is characterized by comprising the following steps: manufacturing a first functional membrane; manufacturing a second functional membrane; combining the first functional membrane and the second functional membrane; coating a transparent wearing layer; and coating a pressure-sensitive adhesive layer and a composite release type PET membrane, wherein the top surface of a first optical PET membrane which is subjected to corona treatment or coated with a PU easy bonding layer is coated with a metal oxide insulating coating mixed with stannic oxide and antimony trichloride particles, and is coated with an intelligent light-controlled color-changing coating mixed with tungsten trioxide particles and benzopyran when the first functional membrane is manufactured; and when the second functional membrane is manufactured, an ultraviolet absorber is added in the process of forming a second optical PET membrane, or a nichrome metal insulating layer is plated to the bottom of the second optical PET membrane.

The present invention relates to substituted benzopyran derivatives, stereoisomers, and pharmaceutical acceptable salts thereof and processes for the preparation of the same. The compounds of the present invention are useful as Estrogen Receptor β agonists. Such agonists are useful for the treating Estrogen Receptor β mediated diseases such as prostate cancer.

A preparing method of tetrahydro benzopyran derivatives is disclosed. The method adopts cyclodextrin as a catalyst, adopts aromatic aldehyde, dimedone and malononitrile as raw materials and adopts water, ethanol or methanol as a solvent. A reaction is performed at 15-30 DEG C, and the tetrahydro benzopyran derivatives can be prepared by recrystallization or column chromatography separation after the reaction is finished. The method is mild in reaction conditions, short in process steps, simple and convenient in operation, low in cost and high in yield, and has a good industrial application prospect.

The invention discloses a preparing method of (E)-N'-arylmethylene-4-(coumarin-3-yl)thiazole-2-hydrazide compound and its application. A formula (I) of the compound is shown as below. The preparing method includes: making salicylic aldehyde and ethyl acetoacetate into 3-acetylindole-2H-chromene-2-one, allowing bromization, cyclization and hydrazinolysis to obtain 4-(2-oxo-2H-chromene-3-yl)thiazole-2-hydrazine, and allowing the 4-(2-oxo-2H-chromene-3-yl)thiazole-2-hydrazine to react with substituted benzaldehydes to obtain the target compound. The compound can serve as a raw material for antiseptic medicine; the preparing method has the advantages that the raw materials are simple and easy to obtain and operating is convenient.

The invention discloses a preparation method of buparvaquone and belongs to the field of medicine synthesis. The preparation method comprises the following step of: with 1,4-benzopyran diketone and p-tert-butylcyclohexyl acetaldehyde as raw materials, performing condensation and rearrangement to prepare pharmaceutical grade buparvaquone. According to the preparation method of buparvaquone, provided by the invention, use of an expensive catalyst AgNO3 is avoided, and a total synthesis yield is increased to about 65% as compared with the prior art. The route is green and environment-friendly, and easy to industrialize.