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194 results about "Acepyrylene" patented technology

Crystalline forms of 1-chloro-4-(beta-D-glucopyranos-1-yl)-2-[4-ethynyl-benzyl)-benzene, methods for its preparation and the use thereof for preparing medicaments

The invention relates to a crystalline hydrate of 1-chloro-4-(β-D-glucopyranos-1-yl)-2-(4-ethynyl-benzyl)-benzene and to crystalline complexes between 1-chloro-4-(β-D-glucopyranos-1-yl)-2-(4-ethynyl-benzyl)-benzene and a natural amino acid, to methods for the preparation thereof, as well as to uses thereof for preparing medicaments.
Owner:BOEHRINGER INGELHEIM INT GMBH

Structural modification of 19-norprogesterone I: 17-α-substituted-11-β-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents

The present invention relates, inter alia, to compounds having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —NC4H8, —NC5H10, —NC4H8O, —CHO, —CH(OH)CH3, —C(O)CH3, —O(CH2)2N(CH3)2, and —O(CH2)2NC5H10; R2 is a member selected from the group consisting of hydrogen, halogen, alkyl, acyl, hydroxy, alkoxy (e.g., methoxy, ethoxy, vinyloxy, ethynyloxy, cyclopropyloxy, etc.), acyloxy (e.g., acetoxy, glycinate, etc.), alkylcarbonate, cypionyloxy, S-alkyl, —SCN, S-acyl and —OC(O)R6, wherein R6 is a functional group including, but not limited to, alkyl (e.g., methyl, ethyl, etc.), alkoxy ester (e.g., —CH2OCH3) and alkoxy (—OCH3); R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R4 is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of ═O and ═N—OR5, wherein R5 is a member selected from the group consisting of hydrogen and alkyl.In addition to providing the compounds of Formula I, the present invention provides methods wherein the compounds of Formula I are advantageously used, inter alia, to antagonize endogenous progesterone; to induce menses; to treat endometriosis; to treat dysmenorrhea; to treat endocrine hormone-dependent tumors; to treat meningiomas; to treat uterine leiomyomas; to treat uterine fibroids; to inhibit uterine endometrial proliferation; to induce cervical ripening; to induce labor; and for contraception.
Owner:HEALTH & HUMAN SERVICES THE GOVERNMENT OF THE US SEC THE DEPT OF

Industrial process for the synthesis of 17a-acetoxy-11ss-[4-(n,n-dimethyl-amino)- phenyl]-19-norpregna-4,9-diene-3,20-dione and new intermediates of the process

The present invention relates to a new industrial process for the synthesis of solvate- free 17a-acetoxy-11ss-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione [CDB -2914] of formula (I) which is a strong antiprogestogene and antiglucocorticoid agent. The invention also relates to compounds of formula (VII) and (VIII) used as intermediates in the process. The process according to the invention is the following: i) 3-(ethylene-dioxy)-estra-5(10),9(11)-diene-17-one of formula (X) is reacted with potassium acetilyde formed in situ in dry tetrahydrofuran by known method, ii) the obtained 3-(ethylene-dioxy)-17a-ethynyl-17ss-hydroxy-estra-5(10),9(11)-diene of formula (IX) is reacted with phenylsulfenyl chloride in dichloromethane in the presence of triethylamine and acetic acid, iii) the obtained isomeric mixture of 3-(ethylene-dioxy)-21-(phenyl-sulfinyl)-19-norpregna-5(10),9(11),17(20),20-tetraene of formula (VIII) is reacted first with sodium methoxide in methanol, then with trimethyl phosphite, iv) the obtained 3-(ethylene-dioxy)-17a-hydroxy-20-methoxy-19-norpregna-5(10),9(11),20-triene of formula (VII) is reacted with hydrogen chloride in methanol, then v) the obtained 3-(ethylene-dioxy)-17a-hydroxy-19-norpregna-5(10),9(11l); -diene-20- one of formula (VI) is reacted with ethylene glycol hi dichloromethane in the presence of trimethyl orthoformate and p-toluenesulfonic acid by known method, vi) the obtained 3,3,20,20-bis(ethylene-dioxy)-17a-hydroxy-19-norpregna- 5(10),9(11)-diene of formula (V) is reacted with hydrogen peroxide in a mixture of pyridine and dichloromethane in the presence of hexachloroacetone by known method, vii) the obtained 3,3,20,20-bis(ethylene-dioxy)-17a-hydroxy-5,10-epoxy-19-norpregn-9(11)-ene of formula (IV), containing approximately a 1:1 mixture of 5a,10a- and 5ss,10ss-epoxides, is isolated from the solution and reacted with a Grignard reagent obtained from 4-bromo-N,N-dimethyl-aniline in tetrahydrofuran.
Owner:RICHTER GEDEON NYRT

Compounds, compositions, kits and methods of use to orally and topically treat acne and other skin conditions by administering a 19-nor containing vitamin d analog with or without a retinoid

InactiveUS20080261925A1Reduce areaBiocideOrganic active ingredientsBenzoic acidCis-Retinoic Acid
Oral and topical pharmaceutical compositions, kits and methods of treatment thereof for treating various skin disorder including acne, psoriasis, ichthyosis, photoaging, photodamaged skin, and, skin cancer. Exemplary vitamin D analogs as active pharmaceutical ingredients include 2-methylene-19-nor-20(S)-1α-hydroxy-bishomopregnacalciferol, 19-nor-26,27-dimethylene-20(S)-2-methylene-1α,25-dihydroxyvitamin D3, 2-methylene-1α,25-dihydroxy-(17E)-17(20)-dehydro-19-nor-vitamin D3, 2-methylene-19-nor-(24R)-1α,25-dihydroxyvitamin D2, 2-methylene-(20R,25S)-19,26-dinor-1α,25-dihydroxyvitamin D3, 2-methylene-19-nor-1α-hydroxy-pregnacalciferol, 1α-hydroxy-2-methylene-19-nor-homopregnacalciferol, (20R)-1α-hydroxy-2-methylene-19-nor-bishomopregnacalciferol, 2-methylene-19-nor-(20S)-1α-hydroxy-trishomopregnacalciferol, 2-methylene-23,23-difluoro-1α-hydroxy-19-nor-bishomopregnacalciferol, 2-methylene-(20S)-23,23-difluoro-1α-hydroxy-19-nor-bishomopregnancalciferol, (2-(3′hydroxypropyl-1′,2′-idene)-19,23,24-trinor-(20S)-1α-hydroxyvitamin D3, 2-methylene-18,19-dinor-(20S)-1α,25-dihydroxyvitamin D3, a stereoisomer thereof, a prodrug thereof in oral compositions, a salt thereof, and / or a solute thereof. Compounds that activate retinoic acid receptors, such as retinoyls and retinoyl esters, include 13-cis-retinoic acid, all-trans-retinoic acid, (2E,4E,6Z,8E)-3,7-dimethyl-9-(2,6,6-trimethyl-1-cyclohexeneyl)nona-2,4,6,8-tetraenoic acid, 9-(4-methoxy-2,3,6-trimethyl-phenyl)-3,7-dimethyl-nona-2,4,6,8-tetraenoic acid, 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-napthoic acid, 4-[1-(3,5,5,8,8-pentamethyl-tetralin-2-yl)ethenyl]benzoic acid, retinobenzoic acid, ethyl 6-[2-(4,4-dimethylthiochroman-6-yl)ethynyl]pyridine-3-carboxylate, retinoyl t-butyrate, retinoyl pinacol, retinoyl cholesterol, an isomer thereof, a prodrug thereof for oral compositions, an ester thereof, a salt thereof, and / or, a solute thereof. Combinations of such active ingredients demonstrate synergistic efficacy.
Owner:WISCONSIN ALUMNI RES FOUND

Semi-conductive internal shielding material composition, semi-conductive internal shielding material and manufacturing method thereof, as well as medium and low-pressure and 110KV cable

The invention relates to a semi-conductive internal shielding material composition. The composition contains an ethylene-butyl acrylate copolymer, an ethylene-vinyl acetate copolymer, an antioxidant, a cross-linking agent, a dispersant, lubricating oil, an anti-copper agent and acetylene carbon black, wherein relative to 100 parts by weight of ethylene-acrylate, the content of the ethylene-vinyl acetate copolymer is 50-65 parts by weight, the content of the acetylene carbon black is 50-72 parts by weight, the content of the antioxidant is 0.1-1.5 parts by weight, the content of the cross-linking agent is 0.5-2.5 parts by weight, the content of the dispersant is 1-10 parts by weight, the content of the lubricating oil is 1-12 parts by weight, and the content of the anti-copper agent is 0.05-1.2 parts by weight. The invention further relates to a semi-conductive internal shielding material for a medium and low-pressure and 110KV cable and a manufacturing method thereof, as well as the medium and low-pressure and 110KV cable. When the semi-conductive internal shielding material provided by the invention is used for extruding the cable, and the phenomenon of scorching can be avoided.
Owner:CHINA PETROLEUM & CHEM CORP +1

Deuterated acetylenic derivative, pharmaceutical composition and application thereof

The invention discloses a deuterated acetylenic derivative, a pharmaceutical composition and application thereof. The deuterated acetylenic derivative comprises one or more of the deuterated acetylenic derivative (I) with curative effective dose, pharmaceutically-acceptable salt, a stereoisomer, solvate, a polymorphic substance, tautomer, metabolite and prodrugs thereof and at least one pharmaceutically-acceptable auxiliary material. The invention also provides the deuterated acetylenic derivative (I), the pharmaceutically-acceptable salt, the stereoisomer, the solvate, the polymorphic substance, the tautomer, the metabolite or the prodrug thereof, or application of the pharmaceutical composition in preparing one or more protein kinase inhibitors and application in preparing drugs for treating and / or preventing tumors. The deuterated acetylenic derivative (I) disclosed by the invention has the advantages that the activity of protein kinase and the growth of tumor cells can be effectively inhibited, and excellent pharmacokinetic properties and in-vitro and in-vivo pharmaceutical effect are expressed. The formula (I) is as shown in the specification.
Owner:SHANGAI PHARMA GRP CO LTD

Method for continuously preparing 2-aryl-benzothiophene/furan compound by utilizing electrochemical micro-channel reaction device

The invention discloses a method for continuously preparing a 2-aryl-benzothiophene / furan compound by utilizing an electrochemical micro-channel reaction device. The preparation method comprises the following steps: dissolving ethynyl thioanisole / phenylethynyl anisole and an iodine-containing electrolyte in water and acetonitrile to prepare a homogeneous solution, then introducing the prepared homogeneous solution into a feeding hole of an electrochemical micro-channel reaction device by utilizing an injection pump in single-strand sample introduction, and reacting under the action of a direct-current power supply to obtain the product 2-aryl-benzothiophene / furan compound; wherein the electrochemical micro-channel reaction device comprises an anode electrode, a cathode electrode, an electrolytic tank bracket, a reaction tank, the direct-current power supply and a temperature control module; wherein the reaction tank is positioned between the anode electrode and the cathode electrode, and a closed serpentine flow path is formed between the anode electrode and the cathode electrode; the anode electrode and the cathode electrode are arranged on the electrolytic tank bracket; one endsof the anode electrode and the cathode electrode are connected with each other and are connected with the direct-current power supply; and the temperature control module is embedded in the electrolytic tank bracket and is used for controlling the temperature of liquid in the reaction tank.
Owner:NANJING UNIV OF TECH

Quickly-dried oily osmosis film forming type nano composite protective agent as well as preparation method and application thereof

ActiveCN104231918AMacroscopic hydrophobicityHigh water contact angleCoatingsSolventPlatinum catalyst
The invention belongs to the field of coating, and discloses a quickly-dried oily osmosis film forming type nano composite protective agent, as well as a preparation method and application thereof. The preparation method comprises the following steps: mixing methylsilicone oil with high hydrogen content, long-chain alkyl acrylic ester, a platinum catalyst and an inert anhydrous solvent, performing reaction under the temperature of 70-90 DEG C for 2-6 hours, performing cooling, adding acetenyl cyclohexanol serving as an inhibitor, and naturally volatilizing to remove the solvent so as to prepare long-chain alkyl modified polymethylsiloxane containing active silicon hydrogen keys; then diluting the long-chain alkyl modified polymethylsiloxane containing the active silicon hydrogen keys by the inert anhydrous solvent, then adding nano MQ silicon resin, a silane coupling agent and a titanate coupling agent for uniform mixing to obtain a mixture, and diluting the mixture by the inert anhydrous solvent until the effective mass content is 1-10 percent so as to obtain the quickly-dried oily osmosis film forming type nano composite protective agent. The surface of an inorganic multihole base material is coated with the product, so that excellent osmosis film forming property and quick dryness are achieved; the quickly-dried oily osmosis film forming type nano composite protective agent is high in antifouling property and acid-alkali resistance performance.
Owner:GUANGZHOU CHEM CO LTD CHINESE ACADEMY OF SCI

High-performance polyimide film and preparation method thereof

The invention provides a preparation method of a high-performance polyimide film. The method comprises the following steps: in an inert atmosphere, adding diamine POSS, ethynyl-containing diamine andfluorine-containing diamine into a phenolic solvent; after dissolving of the above substances, adding rigid and straight dianhydride and twisted dianhydride; carrying out reacting, then adding ethynyl-containing monoamine; performing imidization by adopting a one-step method or a two-step method; pouring the obtained polyimide resin solution into a precipitant for precipitation; dissolving a precipitate obtained in the previous step in an amide solvent to obtain a glue solution; and subjecting the glue solution to tape casting on a stainless steel plate, and performing gradient heating to obtain the high-performance polyimide film. According to the method, ethynyl functional group-containing diamine is introduced into the middle part of a molecular chain structure, monoamine with an acetenyl group is introduced to the tail end of a molecular chain, cross-linking curing is achieved through a cage structure of diamine POSS and an acetenyl group at a certain temperature, a network-shapedmolecular structure is formed, and the solvent resistance, the mechanical property and the heat resistance of the transparent polyimide film are comprehensively improved.
Owner:株洲时代华鑫新材料技术有限公司

Method for continuously preparing 2-aryl-3-halogenated-benzofuran compounds by using electrochemical microchannel reaction device

The invention discloses a method for continuously preparing 2-aryl-3-halogenated-benzofuran compounds by using an electrochemical microchannel reaction device. The method for preparing benzofuran compounds comprises dissolving ethynyl anisole and electrolyte containing iodine or bromine in water and acetonitrile to prepare a homogeneous solution, then introducing the prepared homogeneous solutioninto the feed port of the electrochemical microchannel reaction device by a syringe pump in single feeding way, and reacting under the action of a DC power supply to obtain the product 2-aryl-3-halogenated-benzofuran compounds; wherein the electrochemical microchannel reaction device comprises an anode electrode, a cathode electrode, an electrolytic cell support, a reaction tank, a DC power supplyand a temperature control module; the reaction tank is located between the anode electrode and the cathode electrode, and a closed serpentine flow path is formed between the anode electrode and the cathode electrode; the anode electrode and the cathode electrode are installed on the electrolytic cell bracket; one ends of the anode electrode and the cathode electrode are connected with each otherand is connected with a DC power supply; the temperature control module is embedded in the electrolytic cell bracket and is used for controlling the temperature of the liquid in the reaction tank.
Owner:NANJING UNIV OF TECH

Surfactant composition, coating solution containing the surfactant composition, and rubber article treated by the coating solution

A surfactant composition is provided. The composition comprises (A) an acetylenediol ethoxylate capped by a glycidyl ether represented by the following structural formula (I):wherein R1 is hydrogen atom, or a C1-6 straight chain, branched or cyclic alkyl group, R2 is a C1-12 straight chain, branched or cyclic alkyl group, R3 is —CH2OR4, R4 is a C2-30 straight chain, branched or cyclic alkyl group, alkenyl group, aryl group, or aralkyl group, n, m, p, and q are a positive number with the average of (n+m) being 1 to 100, and the average of (p+q) being 0.5 to 5), and (B) a silicone surfactant. The coating solution prepared by blending the surfactant composition of the present invention can be coated without causing inconsistency since it does not experience foaming when coated on the rubber article, and industrially advantageous production of a rubber article with non-sticky surface is thereby enabled.
Owner:NISSHIN CHEM IND CO LTD +1

Preparation method of erlotinib hydrochloride crystal form A

The invention provides a preparation method of an erlotinib hydrochloride crystal form A, which belongs to the technical field of the preparation of a drug compound. The preparation method comprises the following steps: enabling 2-amino-4,5-di(2-methoxy ethyoxyl) cyanophenyl and N, N-dimethyl amide dimethyl acetal to react; re-crystallizing and purifying the obtained Schiff base intermediate, and then synthesizing with aminophenylacetylene to obtain erlotinib free alkali; and adding a hydrochloric acid solution, and recrystallizing to obtain the erlotinib hydrochloride crystal form A. According to the scheme of the invention, the process route is short, the product purity is high, the repeatability is good, and the operation is simple and easy to implement, and therefore, the preparation method is suitable for large-scale industrial production.
Owner:NANJING YOUKE BIOLOGICAL MEDICAL RES

High-strength PVC (polyvinyl chloride) pipe material and processing process thereof

ActiveCN110425345AImprove internal support strengthEasy to useRigid pipesTubular articlesFiberPolyvinyl chloride
The invention discloses a high-strength PVC (polyvinyl chloride) pipe material. The high-strength PVC pipe material comprises a PVC layer, a bonding layer and a carbon fiber cloth layer; the carbon fiber cloth layer wraps the outer part of the PVC layer through the bonding layer; a plurality of reinforced connecting grooves are formed in the surface of the outer side of the PVC layer; four reinforced ribs are horizontally arranged on the inner side of the PVC layer; the PVC layer comprises the following raw material componentsincluding, by weight,30-35 parts of PVC resin, 15-20 parts of chlorinated polyethylene, 10-15 parts of ethylene-propylene rubber, 5-8 parts of acetylene-propylene copolymer, 2-4 parts of a stabilizer, 8-12 parts of filler and 1-3 parts of beta-cyclodextrin. Through the reinforced ribs, the internal supporting strength of the PVC pipe is enhanced and use in actual life is facilitated; and through the carbon fiber cloth layer, the carbon fiber cloth layer has high strength, low density and small thickness, does not increase the self-weight of a reinforcing component and the section size, is suitable for various structure types and greatly enhances the external supporting strength of the PVC pipe.
Owner:南塑建材塑胶制品(深圳)有限公司

Acetylene Derivatives And Their Use For Binding And Imaging Amyloid Plaques

The invention relates to radiolabeled compounds and their use in methods of imaging amyloid deposits, as well as to methods of their manufacture. The invention also relates to compounds for inhibiting the aggregation of amyloid proteins that form amyloid deposits, methods for delivering therapeutic agents to amyloid deposits, as well as methods of making compounds that inhibit the aggregation of amyloid proteins.
Owner:THE TRUSTEES OF THE UNIV OF PENNSYLVANIA

(S)-/(R)-difurodinaphthalene as well as derivatives thereof and preparation method

The invention discloses (S)-/(R)-difurodinaphthalene as well as derivatives thereof and a preparation method. The compounds have two spatial configurations which are (S)-/(R)-, and in the structure, the site 2 of furan has substituent groups which are hydrogen, and linear or branched alkyl groups or phenyl groups of C4 or below. The preparation method comprises the following steps of: reacting (S)-/(R)-binaphthol as a raw material and potassium carbonate as alkali with iodomethane in acetone so as to obtain (S)-/(R)-2, 2'-dimethoxy-1, 1'-dinaphthalene; then carrying out diiodo-reaction of a product obtained in the previous step, removing protecting groups of phenolic hydroxyl groups, and esterifying with acetic anhydride, thus obtaining (S)-/(R)-3, 3'-diiodo-2, 2'-diacetoxy-1, 1'-dinaphthalene; carrying out Sonogashira coupled reaction of (S)-/(R)-3, 3'-diiodo-2, 2'-diacetoxy-1, 1'-dinaphthalene with alkyne under the catalysis action of palladium to obtain a series of (S)-/(R)-3, 3'-di(trimethylsilylacetylene, hexynyl or phenyl ethynyl)-2, 2'-diacetoxy-1, 1'- dinaphthalene; and finally under the action of cesium carbonate, carrying out ring closing reaction to obtain the (S)-/(R)-double furodinaphthalene and derivatives thereof. A series of compounds provided by the invention broaden the range of organic electroluminescence materials.
Owner:EAST CHINA NORMAL UNIV
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