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102 results about "Cycloalliin" patented technology

Long-lived homogenous amide containing macrocyclic compounds

A robust compound is provided having the formula: wherein Y1, Y2, Y3 and Y4 are oxidation resistant groups which are the same or different and which form 5- or 6-membered rings with a metal, M, when bound to D. D is a metal complexing donor atom, O or N. Each X is a position for addition of a substituent and, when D is N, each position is (i) not occupied such that a double bond is formed between D and an atom adjacent to D, or (ii) is selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, aryl, alkoxy, phenoxy, halogen, halogenated alkyl, halogenated aryl, halogenated alkenyl, halogenated alkynyl, perhaloalkyl, perhaloaryl, a substituted or unsubstituted cycloalkyl ring, a substituted or unsubstituted cycloalkenyl ring, a substituted or unsubstituted saturated heterocyclic ring, a substituted or unsubstituted unsaturated heterocyclic ring, and at least one X is hydrogen, and when D is O, the position is not occupied.
Owner:CARNEGIE MELLON UNIV

Phenylahistin and the phenylahistin analogs, a new class of anti-tumor compounds

Methods of using a compound, its pharmaceutically acceptable salts, and / or its pro-drug esters, in isolated form, to treat cancer, and methods for isolating, for formulating, and for administering the compound, salt, and / or pro-drug ester as an antitumor agent, wherein the compound, salt, or pro-drug ester has the following structure: wherein:R1, R2, R5, R7, and R8 are each separately selected from the group consisting of a hydrogen atom, a halogen atom, and saturated C1-C24 alkyl, unsaturated C1-C24 alkenyl, cycloalkyl, cycloalkenyl, alkoxy, cycloalkoxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, amino, substituted amino, nitro, substituted nitro, phenyl, and substituted phenyl groups,R3, R4, and R6 are each separately selected from the group consisting of a hydrogen atom, a halogen atom, and saturated C1-C12 alkyl, unsaturated C1-C12 alkenyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, amino, substituted amino, nitro, and substituted nitro groups,X1 and X2 are separately selected from the group consisting of an oxygen atom, and a sulfur atom, andthe dashed bond represents a bond selected from the group consisting of a carbon-carbon single bond and a carbon-carbon double bond. Most preferably, R3 and R4 are hydrogen, and each are involved in hydrogen bonds, and / or the dashed bond is a double bond, such that the chemical backbone of the compound substantially retains a substantially planar conformation.
Owner:BEYONDSPRING PHARMA INC

Oxygen scavenger block copolymers and compositions

An oxygen scavenger composition includes a block co-polymer having at least one block including a polyester condensation polymer segment having cycloalkenyl group(s) or functionality directly or indirectly bonded to the polymer chain of said block, and having at least one second block including a polymer segment of a thermoplastic, film forming material. The block copolymer has been found to act as an oxygen scavenger agent under both ambient and refrigerated conditions, to be compatible with conventional film forming packaging materials, and to provide compositions exhibiting low tack which can be readily formed and processed using conventional film forming equipment. A packaging material, such as a film or laminated product suitable for packaging applications, can include the oxygen scavenger composition.
Owner:CRYOVAC ILLC

4,6-di- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections

This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R2 is hydrogen, NR′R″, C1-7 alkyl, arylC1-7 alkyl or C3-10 cycloalkyl; R4 is amino, C1-7 alkyl, C2-7 alkenyl, C3-10 cycloalkyl, C3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C1-7 alkyl or C3-10 cycloalkyl-C1-7 alkyl; R5 is hydrogen or C1-7 alkyl, or R5 and R4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C1-7alkylene, C2-7 alkenylene or C2-7 alkynylene; R6 is halogen, heteroaryl or aryl; R′ and R″ are each independently hydrogen, C1-7 alkyl-carbonyl or C1-7 alkyl; provided that R4 is not phenyl substituted with morpholino when R2 is H and R5 is H, and provided that when NR4R5 is piperazinyl, said NR4R5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.
Owner:GILEAD SCI INC

Fluoropolymer compositions containing a nitrogen cure site monomer

A composition of (a) a fluoropolymer having interpolymerized units derived from a nitrogen-containing cure site monomer; and (b) a nonfluorinated catalyst composition that includes a compound having the general formula: {RA}(−){QR′k}(+) or in certain cases the precursors thereof, wherein R is hydrogen, an alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl or aralkyl, A is an acid- or acid-derivative anion, Q is phosphorous, sulfur, nitrogen, arsenic, or antimony, and each R′ is hydrogen or an alkyl, aryl, aralkyl, or alkenyl group, k is the valence of Q; and optionally (c) an alcohol of the formula R2—OH, wherein R2 is an alkyl group which can be partially fluorinated. Also provided are a method of making a fluoropolymer, a method of increasing induction time, and fluoropolymer articles containing curable or cured fluoropolymer compositions.
Owner:3M INNOVATIVE PROPERTIES CO

Anthelmintic compounds, compositions and method of using thereof

The present invention relates to novel anthelmintic compounds of formula (IA) below:wherein, Y is selected from the group consisting of —H, aryl, cycloalkyl, cycloalkenyl, heteroaryl, heterocyclyl, alkyl, haloalkyl, and alkoxyalkyl; and Z is selected from the group consisting of aryl, cycloalkyl, cycloalkenyl, heteroaryl, heterocyclyl, alkyl, haloalkyl, and alkoxyalkyl. Variables Ring A, Ring B, Ring C, X1, X6, and X8 are as defined herein. The invention also relates to parasiticidal compositions comprising the compounds, and methods and uses of the compounds for treating and preventing parasitic infections and infestations in animals.
Owner:BOEHRINGER INGELHEIM ANIMAL HEALTH USA INC

Silicon compounds

The present invention provides a silicon compound represented by Formula (1) and a polymer obtained by using the same, and this makes it possible not only to obtain an organic-inorganic composite material having a distinct structure but also to control the structure of the above polymer as a molecular aggregate. wherein R1 is a group independently selected from hydrogen, alkyl having a carbon atom number of 1 to 40, substituted or non-substituted aryl and substituted or non-substituted arylalkyl; in this alkyl having a carbon atom number of 1 to 40, optional hydrogens may be substituted with fluorine, and optional —CH2— may be substituted with —O—, —CH═CH—, cycloalkylene or cycloalkenylene; in alkylene in this arylalkyl, optional hydrogens may be substituted with fluorine, and optional —CH2— may be substituted with —O— or —CH═CH—; and A1 is a group having an α-haloester bond.
Owner:JNC CORP

m-TERPHENYL COMPOUND DERIVATIVES AND APPLICATION FOR ORGANIC LIGHT EMITTING DIODE

An m-terphenyl derivative has a structure of formula (I) or (II):wherein A and B are five-membered heterocyclic compounds containing nitrogen, each of substituents R, R1 and R2 is a member independently selected from the group consisting of H, halo, cyano, trifluoromethyl, amino, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C20 cycloalkyl, C3-C20 cycloalkenyl, C1-C20 heterocycloalkyl, C1-C20 heterocycloalkenyl, aryl and heteroaryl. The compound of the present invention may have advantages in good electron affinity, low HOMO and thereby achieving hole blocking and may be used for electron transport material and / or electron injection material.
Owner:E INK HLDG INC

4,6-di- and 2,4,6-trisubstituted quinazoline derivatives and pharmaceutical compositions useful for treating viral infections

This invention provides the treatment of viral infections with a 4,6-disubstituted or 2,4,6-trisubstituted quinazoline derivative represented by the structural formula [(I)] wherein: R2 is selected from the group consisting of hydrogen, NR′R″ and C1-7 alkyl; —A is selected from the group consisting of a bond, O, S(O)n, C1-7 alkylene, C2-7 alkenylene and C2-7 alkynylene; R4 is selected from the group consisting of C1-7 alkyl, C2-7 alkenyl, C3-10cycloalkyl, C3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted alkyl and cycloalkyl-alkyl; —Y is selected from the group consisting of a single bond, C1-7 alkylene, C2-7 alkenylene, and C2-7 alkynylene; n is 0, 1 or 2; and R6 is selected from the group consisting of halogen, heteroaryl and aryl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-Λ / -oxide, a solvate or a pro-drug thereof.
Owner:GILEAD SCI INC

Novel heterocyclic derivatives and pharmaceutical composition containing same

Disclosed is a novel compound that acts as an antagonist for P2X3 and / or P2X2 / 3 receptors. Also disclosed is a pharmaceutical composition that acts as an antagonist for P2X3 and / or P2X2 / 3 receptors, said composition containing: a compound represented by formula (I), a pharmacologically permitted salt thereof, or a solvate of either. In the formula, ring A represents a substituted or unsubstituted five-to-seven-membered cycloalkane, a substituted or unsubstituted five-to-seven-membered cycloalkene, or the like; C represents a carbon atom; -X- represents -N(R16)- or the like; R16 represents hydrogen, a substituted or unsubstituted alkyl, or the like; R7 represents a substituted or unsubstituted five- or six-membered heteroaryl or a substituted or unsubstituted six-to-ten-membered aryl; each of Q1 and Q2 independently represents a carbon atom or a nitrogen atom; -L- represents -O-, -S-, or the like; R6 represents a substituted or unsubstituted cycloalkyl, a substituted or unsubstituted cycloalkenyl, or the like; and R2 represents hydrogen, hydroxyl, or the like.
Owner:SHIONOGI & CO LTD

Novel imidazolidine derivative and use thereof

According to the present invention, a compound represented by formula (I):wherein Q is:A is a hydrogen atom, a halogen atom, —ORa or a C1-4 alkyl group which may be substituted by one or more halogen atoms; E is independently selected from a C1-6 alkyl group; m is selected from integers from 0 to 3; R2 and R3 are independently selected from a C1-6 alkyl group; X1 and X2 are independently selected from O and S; Y is selected from an arylene group and a divalent 5- or 6-membered monocyclic or 8- to 10-membered condensed heterocyclic group, wherein the arylene group and the heterocyclic group may be substituted by 1 to 3 substituents independently selected from E1; E1 is independently selected from a hydroxyl group, a halogen atom, a C1-4 alkyl group, a cyano group, a C1-4 alkoky group, a carbamoyl group, a C1-4 alkylcarbamoyl group, a di(C1-4 alkyl)carbamoyl group, an amino group, a C1-4 alkylamino group, a di(C1-4 alkylamino group, a sulfamoyl group, a C1-4 alkylsulfamoyl group and a di(C1-4 alkyl)sulfamoyl group; Z is —CON(—Ra)—, —CO—, —COO—, —NRa—C(═NH)NRb—, —NRa—C(═N—CN)NRb—, —N(—Ra)COO—, —C(═NH)—, —SO2—, —SO2N(—Ra)—, —SO2NR1—, —N(—Ra)CO—, —N(—Ra)CON(—Rb)—, —N(COR1)CO—, —N(—Ra)SO2—, —N(SO2R1)SO2—, —N(—Ra)— or —N(—Ra)SO2N(—Rb)—; R1 is independently a hydrogen atom, a hydroxyl group, a C1-6 alkyl group which may be substituted by one or more substituents, a heterocyclic group which may be substituted by one or more substituents, an aryl group which may be substituted by one or more substituents, a C3-8 cycloalkyl group which may be substituted by one or more substituents or a C3-8 cycloalkenyl group which may be substituted by one or more substituents, or a salt, prodrug or solvate thereof is provided. Furthermore, a pharmaceutical composition containing the compound, and the like are also provided.
Owner:CHUGAI PHARMA CO LTD

Isoxazole compounds as inhibitors of heat shock proteins

Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: (A), (B) wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C═O)—, —(C═S)—, —SO2—, —C(═O)O—, —C(═O)NRA—, —C(═S)NRA—, —SO2NRA—, —NRAC(═O)—, —NRASO2— or —NRA— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is (i) a group of formula (IA) above or (ii) a carboxamide radical; or (iii) a non aromatic carbocyclic or heterocyclic ring wherein a ring carbon is optionally substituted, and / or a ring nitrogen is optionally substituted by a group of formula -(Alk1)p-(Z)r-(Alk2)s-Q wherein Q, Alk1, Alk2, Z, p, r and s are as defined above in relation to group (IA); and R3 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C1-C6 alkyl, C1-C6 alkenyl, or C1-C6 alkynyl; or a carboxyl, carboxamide, or carboxyl ester group.
Owner:LIGAND UK DEV LTD +2

Extraction method of coptis detoxifcation decoction active site and use thereof

The invention relates to an extract method of Chinese traditional medicinal compound rhizoma coptidis alexipharmic soup active part and an application of the active part in preparing medicament resisting vascular dementia. The extract method disclosed by the invention adopts industrialized separating and refining technologies, such as microporous membrane and macroporous resin absorption, greatly decreases cream yield of the preparation, maximally retains effective components, improves transforming rate of effective components in raw materials and purity of effective components in the preparation. The extracted active part comprises three kinds of known chemical components: alkaloids, flavonoid glycosides and iridoid glycosides respectively, and has a vascular dementia resisting function.
Owner:NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE

Method for extracting general iridoid glycoside from 'Duyiwei' of Tibet medicine and application

A process for extracting the iridoid glycoside from common lamiophlomis herb includes reflux extracting in alcohol solution, macroreticular resin adsorpotion, and separation. Said iridoid glycoside can be used as the active staltic component.
Owner:中国人民解放军联勤保障部队第九四〇医院

Anthranilamide insecticides

Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein J is a phenyl optionally substituted with one to four substituents independently selected from R5; or J is a heterocyclic ring selected from the group consisting of J-1 to J-8; R4 is C4-C12 alkylcycloalkyl, C5-C12 alkenylcycloalkyl, C5-C12 alkynylcycloalkyl, C4-C12 cycloalkylalkyl, C5-C12 cycloalkylalkenyl, C5-C12 cycloalkylalkynyl, C4-C12 cycloalkenylalkyl or C4-C12 alkylcycloalkenyl; each optionally substituted with one to six substituents selected from CH3 and halogen; or R4 is C3-C5 oxiranylalkyl, C3-C5 thiiranylalkyl, C4-C6 oxetanylalkyl, C4-C6 thietanylalkyl, 3-oxetanyl or 3-thietanyl, each optionally substituted with one to five substituents independently selected from C1-C3 alkyl, C1-C3 haloalkyl, halogen, CN, C2-C4 alkoxycarbonyl and C2-C4 haloalkoxycarbonyl; or R4 is C3-C5 aziridinylalkyl, C4-C6 azetidinylalkyl or 3-azetidinyl, each with R10 attached to the nitrogen atom, and optionally substituted on carbon atoms with one to five substituents independently selected from Cl-C3 alkyl, C1-C3 haloalkyl, halogen, CN, C2-C4 alkoxycarbonyl and C2-C4 haloalkoxycarbonyl; and Rla. R1b, R2, R3 and R5 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
Owner:FMC AGRO SINGAPORE PTE LTD +1

Total effective extractive part of morinda officinalis, as well as preparation method and application thereof

The invention discloses a total effective part extractive of morinda officinalis, a preparation method and application thereof in medicaments for treating snoring, and the total effective part comprises the following components in percentage by weight: 50-90 percent of morinda officinalis total polysaccharide, 2-5 percent of morinda officinalis total anthraquinone, 5-30 percent of morinda officinalis total iridoids and the like. The preparation method comprises the following steps of: drying the morinda officinalis, and crushing into 10-100 meshes; heating with water for reflux extraction; processing the extract by using a weak base anion exchange resin column, collecting the cross-flow liquid and water eluent, and condensing and drying to obtain the total polysaccharide; carrying out reflux extraction on the dregs of decoction with petroleum ether or 6# extraction solvent oil or other organic solvents with polarity similar to that of the dregs, and removing low-polarity components, such as essential oil and the like; heating the residual dregs with ethanol water with a certain concentration for reflux extraction, and condensing the extract to prepare the total anthraquinone and total iridoids; and then merging the three components, and drying to obtain the total effective part extractive of morinda officinalis. The product of the invention is used for treating snoring (also called as Sleep apnea syndrome (SAS)), and has the advantages of quick and remarkable curative effect, no toxic or side effect, low price, convenient use and the like.
Owner:仇鑫 +1

Effective part of spreading hedyotis herb and preparation method thereof

The invention discloses an effective part of spreading hedyotis herb and a preparation method thereof. The preparation method comprises the following steps of: purifying the effective part of the spreading hedyotis herb, determining the content of total iridoid glycoside and 6-O-p-coumaroyl scandoside methyl ester in the effective part of the spreading hedyotis herb, and further defining effective anti-tumor ingredients in the effective part; the preparation method is beneficial to increase of the stability of products; meanwhile, mice anti-tumor experiments and the contrast between the effective part and a clinically commonly-used anti-tumor medicine, namely, cyclophosphamide, show that the effective part of the spreading hedyotis herb has an obvious anti-tumor effect.
Owner:CAPITAL NORMAL UNIVERSITY

Flavonols

A compound of the formula (I):whereinR is selected from the group consisting of H, alkyl, alkenyl, alkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl and acyl, each of which may be optionally substituted;R1 is an organic moiety that is capable of being converted into a charged group;each X and Y is independently selected from the group consisting of H, halogen, —CN, —NO2, —CF3, —OCF3, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, heteroalkyl, cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl, heteroarylalkyl, arylalkenyl, cycloalkylheteroalkyl, arylheteroalkyl, heterocycloalkylheteroalkyl, heteroarylheteroalkyl, hydroxy, hydroxyalkyl, alkoxy, alkoxyalkyl, alkoxyaryl, alkenyloxy, alkynyloxy, cycloalkyloxy, heterocycloalkyloxy, aryloxy, heteroaryloxy, arylalkyloxy, phenoxy, benzyloxy, amino, alkylamino, aminoalkyl, acylamino, arylamino, sulfonylamino, sulfinylamino, —COOH, —COR2, —COOR2, —CONHR2, —NHCOR2, —NHCOOR2, —NHCONHR2, C(═NOH)R2, alkoxycarbonyl, alkylaminocarbonyl, sulfonyl, alkylsulfonyl, alkylsulfinyl, arylsulfonyl, arylsulfinyl, aminosulfonyl, SR2 and acyl, each of which may be optionally substituted;each R2 is independently selected from the group consisting of H, alkyl, alkenyl, alkynyl, haloalkyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl, heteroarylalkyl, and acyl, each of which may be optionally substituted;m is an integer selected from the group consisting of 0, 1, 2, 3, 4 and 5;p is an integer selected from 0, 1, 2 and 3;or a pharmaceutically acceptable salt or prodrug thereof.
Owner:WOODMAN OWEN L +2

Concentrated fluoroploymer dispersions

An aqueous dispersion composition of about 30 to about 70 weight % non-melt-processible fluoropolymer particles having a standard specific gravity (SSG) of less than 2.225 and about 2 to about 11 weight % surfactant based on the weight of said fluoropolymer comprising a compound or mixture of compounds of the formula: R(OCH2CH2)nOH wherein R is a branched alkyl, branched alkenyl, cycloalkyl, or cycloalkenyl hydrocarbon group having 8-18 carbon atoms and n is an average value of 5 to 18. The fluoropolymer particles of the dispersion comprise a core of high molecular weight polytetrafluoroethylene and a shell of lower molecular weight polytetrafluoroethylene or modified polytetrafluoroethylene. Preferably, the aqueous dispersion composition comprises about 45 to about 65 weight % non-melt-processible fluoropolymer particles.
Owner:THE CHEMOURS CO FC LLC

Thioamides and Salts Thereof and Cytokine Production Inhibitors Containing Both

To provide cytokine production inhibitors useful as preventive or therapeutic medicines for diseases accompanied by hyperactivated immune functions. A cytokine production inhibitor containing, as an active ingredient, a thioamide compound represented by the formula (I) or a salt thereof: wherein A is N, NO, C—NO2 or C—CN; Hal is a halogen; M1 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, heterocyclyl, amino, O, S, SO or SO2; M2 is amino, O, S or a single bond; R1 is a halogen, alkyl or the like; each of R2, R3, R4 and R5 is independently H, alkyl or the like; R6 is a halogen, alkyl or the like; Cy is cycloalkyl, cycloalkenyl, aryl or heterocyclyl; each of k, p and q is independently an integer of from 0 to 3; and r is an integer of from 0 to 5.
Owner:ISHIHARA SANGYO KAISHA LTD

Reworkable epoxidized 1-(cyclo) alkenyl ether/polycarboxylic acid product

The present invention discloses reworkable epoxy compositions suitable for encapsulation of and underfill for electronic components comprising (a) a curable epoxy component which is the reaction product of an epoxidized 1-alkenyl ether or 1-cycloalkenyl ether and a polycarboxylic acid, the reaction product being substantially free of unreacted acid or acid impurities; and (b) a curing agent for the epoxy component, wherein the reaction products of the epoxy composition are reworkable. The cured epoxy compositions of this invention contain thermally labile weak α-alkoxy ester linkages which provide for the reworkable aspect of the invention.
Owner:HENKEL CORP

Method for simultaneously preparing six iridoid glycoside components from jasmine

The invention provides a method for simultaneously preparing six iridoid glycoside components from jasmine flowers efficiently and rapidly. The method comprises the steps that jasmine fruit alcohol extracts are subjected to macroporous resin coarse separation, reverse phase intermediate-pressure preparation solution liquid chromatogram enriched flow separation and reverse phase high-pressure separation and purification, and the six monomer compounds with the purity higher than 95% or above can be obtained. The method can enlarge the laboratory separation scale and improve the purifying efficiency; the preparation technology is simple, the cost is low, the extraction efficiency is high, more importantly, samples are not wasted, and the crystallization purity is high.
Owner:INST OF CHINESE MATERIA MEDICA CHINA ACAD OF CHINESE MEDICAL SCI

Novel Compounds

This invention relates to novel compounds useful in the treatment of diseases associated with TRPV4 channel receptor. More specifically, this invention relates to certain substituted amino-azepines, according to Formula I Specifically, the invention is directed to compounds according to Formula I wherein: R1 is optionally substituted C3-7cycloalkyl, optionally substituted C3-7cycloalkenyl, optionally substituted Het-C3-7alkyl, optionally substituted Het-C3-7alkenyl, optionally substituted aryl, optionally substituted heterocycloalkyl, optionally substituted heteroaryl, or optionally substituted indenyl; R2 is H, optionally substituted C1-6alkyl, C3-6cycloalkyl-C0-6alkyl, Ar—C0-6alkyl, or Het-C0-6alkyl; each R3 is independently H, optionally substituted C1-8alkyl, optionally substituted C2-8alkenyl, optionally substituted C2-8alkynyl, Het-C1-6 alkyl, optionally substituted C3-6cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl, or optionally substituted C1-C6 alkoxy; R4 is H, or optionally substituted C1-C4 alkyl; R5 is H, optionally substituted C1-8alkyl, optionally substituted C2-8alkenyl, optionally substituted C2-8alkynyl, optionally substituted C3-6cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl; R6 is H or C1-6alkyl; and X is SO2, CO, CH2, or CONH, and pharmaceutically acceptable salts, hydrates, solvates and pro-drugs thereof.
Owner:SMITHKLINE BECKMAN CORP

Total glycosides extractive of morinda plants, as well as preparation method and application thereof

The invention discloses a total glycosides extractive of morinda plants, a preparation method thereof and application thereof in medicaments for treating snoring, and the weight percentage of total glycosides in the total glycosides extractive is 50-80 percent. The total glycosides extractive mainly contains the components of iridoids, such as monotropein, asperuloside and the like, morindone-6-O-beta-D-primeveroside) and the like. The preparation method comprises the following steps of: drying the morinda plants (comprising roots, stems, leaves and fruits), and crushing into 10-100meshes; carrying out reflux extraction by using petroleum ether or 6# extraction solvent oil or other organic solvents with polarity similar to that of the crushed morinda plant, and removing low-polarity components, such as essential oil and the like; heating the dregs of decoction with 20-95 percent alcohol for reflux extraction; condensing the extract, and dissolving with 10-30 percent alcohol; standing for 12 hours at 4 DEG C; removing pigment at the upper layer, carrying out vacuum condensing on the lower layer till alcohol has no odor, and processing the condensed liquid by using a macroporous resin column; washing with water to remove polysaccharide, protein and the like, eluting with 20-80 percent alcohol, and collecting the eluent; and condensing and drying to obtain the total glycosides extractive product of the morinda plants. The product of the invention is used for treating snoring (also called as Sleep apnea syndrome (SAS)), and has the advantages of quick and remarkable curative effect, no toxic or side effect, low price, convenient use and the like.
Owner:仇鑫 +1

Azaindole derivative having AMPK-activating effect

A compound useful as an AMPK-activating agent is provided. A compound represented by formula (I) (wherein X represents a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, a substituted or unsubstituted cycloalkyl group, a substituted or unsubstituted cycloalkenyl group or a substituted or unsubstituted heterocyclyl group; R1 represents a hydrogen atom, a halogen atom, a cyano group, a nitro group, a carboxy group, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted acyl group, a substituted or unsubstituted carbamoyl group, a substituted or unsubstituted alkylthio group, a substituted or unsubstituted alkylsulfinyl group, a substituted or unsubstituted alkylsulfonyl group or a substituted or unsubstituted alkyloxycarbonyl group; R2 represents a halogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, a substituted or unsubstituted cycloalkyl group, a substituted or unsubstituted cycloalkenyl group, a substituted or unsubstituted heterocyclyl group or the like; R3 represents a halogen atom, a hydroxy group, a cyano group, a nitro group, a carboxy group, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, a substituted or unsubstituted cycloalkyl group, a substituted or unsubstituted cycloalkenyl group, a substituted or unsubstituted heterocyclyl group or the like; and R4 represents a hydrogen atom, a halogen atom, a hydroxy group, a cyano group, a nitro group, a carboxy group, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group or the like) or a pharmaceutically acceptable salt thereof.
Owner:SHIONOGI & CO LTD

Isolation and identification as well as application of volatile oil elements of Parasenecio firmus leaf

The invention belongs to the technical field of medicine production research development, and relates to isolation and identification as well as application of volatile oil elements of Parasenecio firmus leaf. The isolation and identification of the volatile oil elements of the Parasenecio firmus leaf are realized by the following steps of: weighing dried Parasenecio firmus leaf, and extracting ultrasonically by a water steam distillation method to obtain the volatile oil; and analyzing the obtain volatile oil by utilizing a 6890 / 5973N gas chromatograph-mass spectrometer. The obtain volatile oil mainly comprises the following chemical elements in proportion: 18.98% of n-palmitic acid, 9.89% of 1-tridecylene, 8.05% of caryophyllene epoxide, 6.04% of (S)-undeca-cycloolefin, 3.84% of 9,12,15-octadecatrienoic acid, 2.97% of (-)-spathulenol, 2.83% of kaurene and 2.12% of caryophyllene. The volatile oil is used for preparing pharmaceutical preparation capable of restraining escherichia coli, streptococcus, Salmonella, Pasteurella and staphylococcus aureus.
Owner:SHANDONG UNIV AT WEIHAI
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