52 results about "ISOLATE COMPOUND" patented technology

Peptides that are designed to inhibit the biological activity of the IL-1R type 1 receptor and inhibit IL-1R / IL-1RacP related cell signaling and biological activity are disclosed. Compositions comprising IL-1R antagonists of the present invention are useful in the treatment of IL-1 related diseases or conditions such as arthritis, rheumatoid arthritis, osteoarthritis, and inflammatory bowel disease as well as other chronic or acute inflammatory diseases. This invention also discloses an isolated compound having an IL-1R antagonist activity, said compound being selected from the group consisting of: a peptide comprising the amino acid sequence RYTPELX, wherein R, Y, T, P, E, L, refer to their corresponding amino acids, and X is selected from no amino acid and alanine (A); and a derivative of (a) wherein the derivative incorporates one, two or three amino acid modification selected from an amino acid addition, deletion or substitution in the RYTPEL portion of the peptide, and wherein said derivative maintains its antagonist IL-1R activity.

Methods are disclosed for establishing a quantitative relationship between spectral properties of molecules and a biological, chemical, or physical endpoint of the molecules. Spectral data including data from nuclear magnetic resonance, mass spectrometric, infrared, and ultraviolet-visible techniques are used along with endpoint data to train a pattern-recognition program. The training yields a spectral data-activity relationship that may be used to predict the endpoint value of a molecule from its spectral data alone. Methods for rapidly screening isolated compounds or mixtures of compounds based upon their spectral data are included.

The invention provides methods and compositions for the treatment of inflammatory disorders, such as inflammatory bowel diseases (IBDs). The use of bacteria-free, probiotic-derived compounds instead of live bacteria provides a safety advantage over the use of live bacteria. In addition, the administration of isolated compounds will provide more reliable dosing, greater simplicity, and improved consistency than is found in administering probiotics, which is dependent on both establishing and maintaining bacterial colonization.

Treatment of Diseases caused by Disturbances of the Activity of the Androgen Receptor uses of compounds of Formula (I): (as defined herein), for the treatment of diseases caused by disturbances of the activity of androgen receptor are provided: Formula (I). Isolated compounds of Formula (I) are also provided.

A process for preparing Oxcarbazepine III comprising: a) reacting oximinostilbene IV with chlorosulfonyl isocyanate in an inert organic solvent and isolating compound V b) hydrolyzing compound V to form crude Oxcarbazepine III c) purifying oxcarbazepine.

The invention relates to an irradiated crosslinking low-smoke halogen-free flame-retardant insulating compound and a sheathing compound for solar cables, which are characterized by taking ethylene-methyl acrylate copolymer (EMA) or ethylene-butyl acrylate copolymer objects (EBA) as basal resin, taking functionalized polyolefin resin as compatilizer, taking magnesium oxide and silicon resin as fire retardant, and then mixing antioxidant, UV absorbent, anti-copper agent, crosslinking sensitizer and processing agent together. The irradiated crosslinking low-smoke halogen-free flame-retardant isolating compound and the sheathing compound for solar cables have the advantages of higher temperature resistant class, longer service life, excellent squeezing performance and good electrical insulation performance. Cables squeezed from the irradiated crosslinking low-smoke halogen-free flame-retardant insulating compound and the sheathing compound can pass the flood and pressure test.

The invention relates to a damping vibration-isolating compound track bed for a metro and a construction method thereof. The track bed comprises concrete layers and EPS (Expanded Poly Styrol) layers which are arranged at intervals, wherein the quantity of the concrete layers is three or four; the quantity of the EPS layers is two or three; the top layer and the bottom layer are both concrete layers; the EPS layers and the poured concrete layers are fixed by small steel chisels; the concrete layers meet the C35 standard; a demand on the density of the EPS layers is 12-15kg / m<3>; and a grain size of EPS grains is 1-2mm. The damping vibration-isolating compound track bed meets the demands on strength and long-term stability, has certain elasticity, has an obvious damping vibration-isolating function and has the energy attenuation above 50-60dB.

The instant invention provides a live labeling microorganism assay for screening a one-bead one-compound library to identify synthetic anti-adherent compounds for blocking biofilm formation. The compounds of libraries may be peptides, small molecules, nucleic acids, other types of molecules or a combination of the foregoing. The live labeling microorganisms are incubated with a one-bead one-compound library for a long period with fresh-labeled bacteria and nutrition replacement in regular intervals. Those beads without bacterial adhesion are transferred into nutritional agar for the culture. The true anti-adherent beads are isolated and the sequences of each isolated compound-bead are determined with sequencer. The anti-adherent compounds identified in this invention are proved to possess long-term effect of blocking bacterial adhesion and biofilm formation. Thus the instant invention provides a unique and powerful method to identify anti-adherent compounds from library more quickly and reliably than current state-of-the-art technology allows.

The invention provides the application of caffeoylquinic acid and its derivatives in the preparation of anti-complement drugs. The present invention extracts and separates the caffeoylquinic acid compounds obtained from Shamrock, through in vitro experiments, it is confirmed that the cell hemolysis caused by the activation of the classic pathway of the complement system is inhibited, indicating that there is an anti-complement effect. The activity is stronger than that of the total extract of S. sageris, and it is a kind of good complement inhibitor, which can be used to prepare new anti-complement drugs and treat various diseases caused by abnormal activation of complement, and has low effective concentration and low toxicity. The drug is safe, the source of raw materials is abundant, and it has great clinical application value. Caffeoylquinic acid and its derivatives are shown in the following structural formula I: Formula I wherein R1, R2, R3, or R4 can be the same or different, and they are H or caffeoyl respectively, provided that they cannot be H at the same time; R5 is H , CH3, CH2CH3 or CH2CH2CH2CH3.

The present invention in its broadest aspect relates to a method for reducing glycoalkaloid content and turbidity of an aqueous phase comprising compounds selected from two or more of PA, PI, PPO, LipO, pectin, lipid, glycoalkaloid and phenolic compounds of which at least one compound is selected from PA, PI, LipO and PPO; a) providing an aqueous phase comprising compounds selected from two or more of PA, PI, PPO, LipO, pectin, lipid, glycoalkaloid and phenolic compounds of which at least one compound is selected from PA, PI, LipO and PPO; and b) performing one or more steps to reduce the concentration of solanine in the dry matter of the aqueous phase with at least 15 percent, such as at least 20% such as at least 25% and to achieve an optical density at 620 nm of the remaining aqueous phase of less than 0.7; such as less than 0.5; such as less than 0.3; such as less than 0.2 such as less than 0.1 and thereby obtaining an aqueous phase having reduced glycoalkaloid content and turbidity compared to an untreated aqueous phase.

The present invention refers to extracts from the fungus Guignardia sp., and also a new isolate compound from the aforementioned extract, both having antimicrobial activities, particularly antibacterial and antifungal activities, and their use in pharmaceutical compositions. The new compound, isolated from the extract of the fungus Guignardia sp., presents a dioxolanone ring, having the following formula: ##STR1##

Isolated compounds and combinations of isolated compounds isolated from Scutellaria barbata D. Don are effective in the generation of reactive oxygen species, induction of DNA damage and induction of apoptosis in cancer cells. The compounds and combinations may be prepared as pharmaceutical compositions for administration to mammals, such as humans, for the treatment of solid cancers, such as epithelial cancers. Such epithelial cancers include breast cancer and ovarian cancers.

The invention relates to novel antitumor compounds of general formulaas well as their corresponding pharmaceutically acceptable salts, derivatives, prodrugs and stereoisomers. These compounds can be obtained by isolating a sponge from family Theonellidae, genus Theonella and species swinhoei, and forming derivatives from the isolated compounds. These compounds have cytotoxic activity and can be used for the treatment of the cancer.

A simple, cost-effective process for preparation of efavirenz of formula (I) comprising reacting a solution of 5-chloro-α-(cyclopropylethynyl)-2-amino-α-trifluoromethyl) benzene methanol of formula (II) in an organic solvent with triphosgene in the presence of an inorganic base at a temperature range −5° C. to 25° C., adding water and isolating compound of formula (I).

Peptides that are designed to inhibit the biological activity of the IL-1R type 1 receptor and inhibit IL-1R / IL-1RacP related cell signaling and biological activity are disclosed. Compositions comprising IL-1R antagonists of the present invention are useful in the treatment of IL-1 related diseases or conditions such as arthritis, rheumatoid arthritis, osteoarthritis, and inflammatory bowel disease as well as other chronic or acute inflammatory diseases. This invention also discloses an isolated compound having an IL-1R antagonist activity, said compound being selected from the group consisting of: a peptide comprising the amino acid sequence RYTPELX, wherein R, Y, T, P, E, L, refer to their corresponding amino acids, and X is selected from no amino acid and alanine (A); and a derivative of (a) wherein the derivative incorporates one, two or three amino acid modification selected from an amino acid addition, deletion or substitution in the RYTPEL portion of the peptide, and wherein said derivative maintains its antagonist IL-1R activity.

The present invention relates to a novel salt of (3aR,4S,7R,7aS)-2-[((1R,2R)-2-{[4-(1,2-benzisothiazol-3-yl)-piperazin-1-yl]methyl}cyclohexyl)methyl]hexahydro-1H-4,7-methanisoindol-1,3-dione and hydrates thereof, to methods for preparing the novel salt and its hydrates. In one aspect, the present invention provides a compound which is lurasidone dihydrochloride. In another aspect, the present invention provides a process for preparation of lurasidone dihydrochloride comprising: (i) mixing lurasidone free base in an organic solvent system; (ii) subjecting step (i) mixture to acid proton source; and (iii) isolating compound of lurasidone dihydrochloride.

The present invention is directed to a method and device to isolate compounds from plant material using vibrational pulsing, vibrational decanting, vibrational sieving and vibrational rinsing. A susceptible liquid is generated by vibrational agitation, decanted when in a vibrating container and then collected by passing over a series of vibrating screens and then rinsed with water while collected on the vibrating screens and the residue collected. The isolated compound can either be collected in the decant or retained on the screens. In an embodiment of the invention, the vibrational rinsing step reduces unwanted impurities isolated.

A process for preparing Oxcarbazepine IIIcomprising:a) reacting oximinostilbene IV with chlorosulfonyl isocyanate in an inert organic solvent and isolating compound Vb) hydrolyzing compound V to form crude Oxcarbazepine IIIc) purifying oxcarbazepine.

Isolated compounds and combinations of isolated compounds isolated from Epimedium grandiflorum Morr. are estrogenic, and can be used to treat one or more symptoms of menopause and / or ER-positive cancer. The compounds and combinations may be prepared as pharmaceutical compositions for administration to mammals, such as humans, for the treatment of solid cancers, such as epithelial cancers. Such epithelial cancers include breast cancer, uterine cancer, cervical cancer, ovarian cancer, vulvar cancer, endometrial cancer.

The present invention relates to bioactive extracts its fractions and isolation of compound from Rauwolfia tetraphylla. The extracts and fractions are useful for the treatment of psychosis based on in-vivo validation on animal model and proportional binding affinities for dopaminergic-D2, Cholinergic (muscarinic) and Serotonergic (5HT2A) receptors for antipsychotic activity. The present invention relates to novel antipsychotic activity in the leaf alkaloids of Formula 1 and 2 named tetrahydroalstonine, 10-methoxytetrahydroalstonine, isoreserpiline, 10-demethoxyreserpiline, 11-demethoxyreserpiline, reserpiline and α-yohimbine. The present invention also relates to processes for obtaining antipsychotic extracts as well as for the isolation of alkaloids of formula 1 and 2 from the leaves of Rauwolfia tetraphylla. The present invention particularly relates to significant antipsychotic activity in the MeOH extract, ethylacetate and chloroform fractions of R. tetraphylla and in the isolated compounds α-yohimbine, reserpiline and in a mixture 10-demethoxyreserpiline and 11-demethoxyreserpiline in 1:1.5 ratios for treating psychosis without any extra pyramidal symptoms (EPS).

The present invention relates to a process for the preparation of Compound (A):wherein the process comprises contacting atazanavir base (Compound (II))with sulphuric acid in a combination of two or more solvents and isolating compound (A). The present invention also relates to substantially pure Compound (A), and to Compound (A) devoid of mesityl oxide impurity. Mesityl oxide has the following formula:

The invention provides a method for isolating a compound metal grid from a back electrode during large-area preparation of a dye sensitized solar cell (DSSC). The method comprises the following steps of: (1) sputtering a compound metal grid of Ti and Al on transparent conducting glass; (2) preparing a TiO2 nanoparticle film on a transparent conducting substrate by using a TiO2 sizing agent with ascreen printing method; and (3) heating the substrate on which the TiO2 sizing agent is printed to fully vaporize or oxidize organic matters in the TiO2 sizing agent, wherein an oxide of a Ti metal on an upper layer of the compound metal grid is taken as an isolated layer. Due to the adoption of the method provided by the invention, the isolation between an Al metal grid and an electrolyte duringthe encapsulation of the dye-sensitized solar cell is realized effectively, and the problem of internal short circuit of the DSSC is solved; and low-cost metals, i.e., Al and Ti are adopted instead of precious metals, i.e., Pt, Au and the like in the conventional process, so that a firm foundation is laid for the industrial mass production of DSSCs.

The present invention provides novel isolated compounds characterized as metabolites or derivatives of desmethylvenlafaxine including hydroxy-DV metabolites, hydroxy-DV-glucuronide metabolites, N-oxide-DV metabolites, and benzyl-hydroxy-DV metabolites. The invention includes pharmaceutical compositions comprising any of the metabolites or derivatives of the invention in combination with a pharmaceutically acceptable carrier or excipient. The invention also includes a method of treating at least one central nervous system disorder in a mammal comprising providing to a mammal in need thereof an effective amount of the compounds of the invention.

This invention relates to extract, fractions and isolated compound of Rhodiola rosea, and uses thereof for treating neuropathological and neurodegenerative diseases. The extracts and compounds of the present invention inhibit the aggregation of alpha-synuclein. In one embodiment, Rhodiola rosea extracts and compounds of the present invention can be used to treat synucleinopathies including PD, dementia with Lewy bodies, pure autonomic failure, multiple system atrophy, and Alzheimer's disease.

The present invention provides novel isolated compounds characterized as metabolites or derivatives of desmethylvenlafaxine including hydroxy-DV metabolites, hydroxy-DV-glucuronide metabolites, N-oxide-DV metabolites, and benzyl-hydroxy-DV metabolites. The invention includes pharmaceutical compositions comprising any of the metabolites or derivatives of the invention in combination with a pharmaceutically acceptable carrier or excipient. The invention also includes a method of treating at least one central nervous system disorder in a mammal comprising providing to a mammal in need thereof an effective amount of the compounds of the invention.

A Fraxinus excelsior seed extract that can be administered for therapeutic treatment of a subject, including a human, by blocking fat synthesis, activating PPAR-alpha, increasing hypoglycemic activity, reducing bodyweight, controlling fasting plasma insulin levels against hyperinsulinemia, and promoting insulin sensitivity and causing a beneficial acute insulinotropic effect. The Fraxinus excelsior seed extract includes, inter alia, an isolated compound (2S,3E,4S) 2H-Pyran-4-acetic acid-3-ethylidene-2-[(6-O-β-D-glucopyranosyl-β-D-glucopyranosyl)oxy]-3,4-dihydro-5-(methoxycarbonyl)methyl ester, commonly called excelside A, an isolated compound (2S,3E,4S) 2H-Pyran-4-acetic acid-3-ethylidene-2-[(6-O-β-D-glucopyranosyl-β-D-glucopyranosyl)oxy]-3,4-dihydro-5-(methoxycarbonyl) 2-(4-hydroxyphenyl)ethyl ester, commonly called excelside B, and the compounds GI5, GI3, nuzhenide, and oleoside dimethyl ester.

The application of the active ingredient gentiopicroside in the preparation of drugs for inhibiting hepatitis B virus. The active ingredient gentiopicroside is a compound extracted and separated from the commonly used traditional Chinese medicine Gentiana quinquefolium in my country. The active ingredient gentiopicroside is mixed with pharmaceutically acceptable carriers in preparations such as those suitable for enteral and parenteral administration. Organic or inorganic solid or liquid excipients are mixed, and the pharmaceutical preparation can be in solid form such as tablet, capsule, powder, pill, granule, or in liquid form such as injection, emulsion, etc. Gentiopicroside was prepared into injections, and the drug efficacy test showed that ducks infected with duck hepatitis B virus were treated with intramuscular injection of gentiopicroside on the 7th day after infection. The inhibitory effect of duck serum DHBV-DNA level is remarkable, and the statistical processing results have very significant and significant differences, inhibitory effect (P<0.01-0.05), and the inhibitory effect of three batches of experiments can be repeated.

A Fraxinus excelsior seed extract that can be administered for therapeutic treatment of a subject, including a human, by blocking fat synthesis, activating PPAR-alpha, increasing hypoglycemic activity, reducing bodyweight, controlling fasting plasma insulin levels against hyperinsulinemia, and promoting insulin sensitivity and causing a beneficial acute insulinotropic effect. The Fraxinus excelsior seed extract includes, inter alia, an isolated compound (2S,3E,4S) 2H-Pyran-4-acetic acid-3-ethylidene-2-[(6-O-β-D-glucopyranosyl-β-D-glucopyranosyl) oxy]-3,4-dihydro-5-(methoxycarbonyl)methyl ester, commonly called excelside A, an isolated compound (2S,3E,4S) 2H-Pyran-4-acetic acid-3-ethylidene-2-[(6-O-β-D-glucopyranosyl-β-D-glucopyranosyl)oxy]-3,4-dihydro-5-(methoxycarbonyl) 2-(4-hydroxyphenyl)ethyl ester, commonly called excelside B, and the compounds G15, G13, nuzhenide, and oleoside dimethyl ester.

Disclosed herein are isolated compounds or pharmaceutically acceptable salts thereof, which exhibit immunostimulatory or anti-inflammatory effects. The compounds are isolated from the fruiting body of A. camphorata in a solid culture. Also disclosed are methods of stimulating immune responses and / or treating an inflammatory disorder with these compounds and pharmaceutical compositions including the compounds or pharmaceutically acceptable salts thereof.