Abstract: A thermostable mutant DNA polymerase; a method for obtaining the thernmostable mutant DNA polymerase by identifying a thermostable mutant polypeptide exhibiting enzymatic activity, wherein the thermostable mutant polypeptide is a variant of DNA polymerase I obtained from Thermus aquaticus; a polynucleotide, an expression vector, and a host cell encoding the thermostable mutant DNA polymerase; and a method of performing a reverse transcription polymerase chain reaction (RT-PCR) utilizing the thermostable mutant DNA polymerase, as well as a kit for facilitating the same.

Abstract: Disclosed herein are amino acid sequences, and encoding nucleotide sequences, of isolated catalytic domains of the LOX and LOXL2 proteins from human and mouse. Methods for the preparation and use of these isolated catalytic domains are also provided.

Abstract: A variant phylogenetic group of HPIV-2, more particularly a novel variant phylogenetic sub-group of HPIV-2, and a means for diagnosing HPIV-2 which take into account this novel group and this novel sub-group.

Abstract: The present invention relates to isolated Solanum Bulbocastanum Bul409 promoter sequences and uses thereof. An exemplary embodiment provides an isolated plant Bul409 promoter comprising a nucleic acid sequence that is at least about 90% identical to nucleotides 1-771 of SEQ ID NO:1, wherein the promoter sequence is capable of controlling transcription in a plant. Other exemplary embodiments provide a method for making a transgenic plant, wherein the method comprises transforming a plant, plant part, or plant cell with an expression vector comprising isolated plant Bul409 promoter operably linked to a heterologous nucleic acid sequence, wherein the isolated plant Bul409 promoter is capable of controlling transcription of the heterologous nucleic acid in a plant, and a transgenic plant made by the method and decendants thereof.

Abstract: The present invention provides compositions, methods and kits for the species-specific detection of Pseudomonas aeruginosa.

Abstract: The invention relates to sense oligonucleotide having a sequence complementary to a single-stranded RNA (antisense transcript) having a sequence complementary to mRNA of iNOS gene in order to control expression of iNOS (inducible nitric oxide synthase). The sense oligonucleotide of the present invention can control expression of iNOS and is useful for biological defense and treatment and prevention of diseases related to excessive production of NO, such as cancerogenesis, inflammatory disease, endotoxin shock by bacterial infection and the like.

Abstract: The invention provides compositions and methods for reducing expression of a target gene in a cell, involving contacting a cell with an isolated double stranded nucleic acid (dsNA) in an amount effective to reduce expression of a target gene in a cell. The dsNAs of the invention possess a single stranded extension (in most embodiments, the single stranded extension comprises at least one modified nucleotide and/or phosphate back bone modification). Such single stranded extended Dicer-substrate siRNAs (DsiRNAs) were demonstrated to be effective RNA inhibitory agents compared to corresponding double stranded DsiRNAs.

Abstract: A method of forming a sucrose-6-ester includes in sequence the steps of: a) contacting sucrose with a organotin-based acylation promoter in a solvent in the presence of a base selected from amines and basic alkali metal salts; b) removing water to form a tin-sucrose adduct; and c) contacting the tin-sucrose adduct with an acylating agent to form the sucrose-6-ester. The sucrose-6-ester may then be converted to sucralose.

Abstract: It discloses a process for refining Aztreonam, comprising the steps of 1) treating Aztreonam material with an alkali metal alkoxylate or an alkali earth metal alkoxylate under heating in the presence of a suitable solvent or a mixture of solvents, followed by adjusting the pH value with a suitable acid and cooling down to precipitate Aztreonam, which provides a primary purified Aztreonam; 2) adsorbing Aztreonam with strongly basic ion exchange resin, followed by eluting the resin and collecting the eluate, to provide a secondary purified Aztreonam after concentration under reduced pressure; 3) adjusting the pH value with a suitable acid to allow crystallization, followed by centrifuging and washing the resultant crystals, to provide a tertiary purified Aztreonam after drying. The refined Aztreonam product has a purity of no less than 99.2%, mostly no less than 99.5%, with little residue on ignition and significantly low content of heavy metals.

Abstract: Process for the synthesis of the compound of formula (I): wherein R represents a para-methoxybenzyl (PMB) group or the following group: Application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid.

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with the compounds.

Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.

Abstract: Provided herein are quinazoline compounds of formula (I): The compounds are useful for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.

Abstract: Process for the preparation of a mono-N-alkylpiperazine of the formula I in which R1 is C1- to C5-alkyl or 2-(2-hydroxyethoxy)ethyl, by reacting diethanolamine (DEOA) of the formula II with a primary amine of the formula H2N—R1 (III) in the presence of hydrogen and a catalyst molding, where the reaction is carried out in the liquid phase at an absolute pressure in the range from 150 to 250 bar and the amination is carried out by means of a catalyst molding, the precursor of which can be prepared according to a process in which (i) an oxidic material comprising copper oxide, aluminum oxide and lanthanum oxide is provided, (ii) pulverulent metallic copper and/or copper flakes and optionally graphite is added to the oxidic material, (iii) the mixture resulting from step ii is shaped to give a molding, where the oxidic material is obtainable by simultaneous or successive precipitation of the component copper oxide, of the component aluminum oxide and of the component lanthanum oxide and subsequent dry

Abstract: Described herein are platinum and palladium compounds with geometrically distorted charge transfer state, applications and methods for the preparation thereof. The platinum and/or palladium compounds described herein are capable of emitting light and can be used in light emitting devices.

Abstract: The invention relates to a process for the preparation of alkali-metal salts with dihydridodicyanoborate anions by reaction of alkali-metal tetrahydridoborates or trihydridocyanoborates with trialkylsilyl cyanide and further reaction thereof in metathesis reactions.

Abstract: This invention relates to novel compounds of the Formula (I*), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.

Abstract: The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs/compositions of hydrocodone, including benzoates and heteroaryl carboxylic acids, which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

Abstract: The invention provides a series of novel thiochromeno[2,3-c]quinolin-12-one derivatives. Further, the invention also provides the preparation method and application of said derivatives, said application comprises: said derivatives with treating effective amount are prepared into pharmaceutical compositions for inhibition of topoisomerase type I and II, inhibition of cancer cell growth, further treating cancer.

Abstract: The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. Specially, the present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or salt thereof, and a medicament containing the compound or a prodrug thereof, which is an Smo inhibitor or an agent for the prophylaxis or treatment of cancer.

Abstract: Compounds and methods are disclosed that are useful for noninvasive imaging in the near-infrared spectral range. The cyanine compounds of Formula I are presented: wherein Q is a portion of a polymethine bridge selected from the group consisting of: Also included are bioconjugates of the compounds of Formula I, methods of labeling biomolecules with the compounds, and methods of imaging.

Abstract: A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof; compositions contain these compounds as active ingredient and processes for preparing these compounds and compositions.

Abstract: The present invention provides, for example, the following compound: wherein ring Z is pyridine or a carbocycle, each of which is substituted or unsubstituted, ring A is a carbocycle or a heterocycle, each of which is substituted or unsubstituted, R1 is substituted or unsubstituted alkyl or the like, R2a, R2b, R4a and R4b are each independently hydrogen or substituted or unsubstituted alkyl or the like, its pharmaceutically acceptable salt or a solvate thereof having an effect of inhibiting amyloid ? production, especially a BACE1 inhibitory activity, and useful as a medicament for treating diseases induced by production, secretion or deposition of amyloid ? proteins.

Abstract: The present invention relates to the cinchonidine salt useful in the preparation of intermediates for preparing a macrocyclic HCV inhibitor, as well as processes involving this salt.

Abstract: A process for making 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid, and therapeutically acceptable salts thereof, and intermediates used in the process are disclosed.

Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.

Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein A, B and D are each oxygen or sulfur, provided that least one of A, B and D is sulfur; and R1-R8 are each independently hydrogen, hydroxyl, acyl, substituted acyl, acyloxy, substituted acyloxy, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, aryl, substituted aryl, amino, substituted amino, halogen, heterocycloalkyl, substituted heterocycloalkyl, heteroaryl, substituted heteroaryl, or a thio-containing group.

Abstract: The present invention relates to compounds of general formula I, wherein R1, LP, (Het)Ar1, (Het)Ar2 and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.

Abstract: Embodiments of compounds for selectively detecting a thiol are disclosed. In some embodiments, the compounds are bridged viologens, and the compounds are capable of reacting with homocysteine and/or glutathione in a buffered solution to produce a change in the solution's absorbance spectrum and/or emission spectrum. Also disclosed are embodiments of methods and kits for detecting homocysteine and/or glutathione with the disclosed bridged viologens.

Abstract: Photoreactive DNA cleaving conjugate compounds are provided comprising a DNA cleaving moiety which comprises an aryl alkyne group and a polyfunctional pH-regulated DNA-binding moiety which comprises at least one or two amino groups.

Abstract: Pesticidal compositions and their uses are disclosed.

Abstract: Compounds and related compositions and methods as can be used to selectively inhibit neuronal nitric oxide synthase and as can be employed in the treatment of various neurodegenerative diseases.

Abstract: 4-Amino-5-fluoro-3-halo-6-(substituted)picolinates are conveniently prepared from 4,5,6-trichloropicolinates by a series of steps involving fluorine exchange, amination, halogen exchange, halogenation and transition metal assisted coupling.

Abstract: The present teachings provide methods that enable the preparation and purification of radioiodinated vectors without the need for HPLC purification, as well as novel precursors which include biotin-like substituents useful in such methods.

Abstract: A sensor that includes a) a silicon (Si) substrate having a surface; and b) a monolayer of oligoethylene glycol (OEG) bonded to the surface via silicon-carbon bonds. Regions of the OEG monolayer distal to the surface are functionalized with a molecular probe serving as a recognition element for a bioanalyte. A method of making a silicon surface that recognizes a biological specimen includes 1) hydrosilylating with a mixture that includes an oligoethylene glycol (OEG) substituted with an alkene at one end of the OEG and capped at the opposing end of the OEG and an oligoethylene glycol (OEG) substituted with an alkene at one end of the OEG and an alkyne having a protecting group at the opposing end of the OEG and 2) removing the protecting group from the alkyne; and 3) reacting the alkyne with a reagent in a 1,3-dipolar cycloaddition.

Abstract: A batch reactor process for the synthesis of potassium 5,7-dinitro-[2,1,3]-benzoxadiazol-4-olate-3-oxide (KDNP) from 3-bromo-2,4,6-trinitroanisole (ETNA) includes adding BTNA to a reaction vessel containing potassium azide (KN3) and water (H2O). The resulting mixture is heated to 90° C. followed by cooling to room temperature and agitating the final solution. The precipitate KDNP product is recovered by filtration.

Abstract: Provided is a process for the preparation of an N-substituted isothiazolinone derivative having the general formula (I), comprising reacting N-substituted 3-mercaptopropionamides of formula (II) or N,N?-bis-substituted 3,3?-dithiodipropionamides of formula (III) with sulfuryl chloride in the absence of solvents. Also provided is a process for the preparation of a compound having the general formula (III), comprising reacting a methyl ester of formula (IV) with an amine of formula (V) in a solvent of methanol. As no addition solvent is used in the process of the invention, the cost of manufacturing and pollution to the environment can be reduced.

Abstract: This invention provides a method for preparing a 1,2,3-triazole compound comprising contacting an organic azide with a 2-substituted-1-haloalkyne, in the presence of a copper catalyst and a copper-coordinating ligand (preferably a tertiary amine) in a liquid reaction medium, thereby forming a 1,4,5-substituted-1,2,3-triazole compound including a halo substituent at the 5-position of the triazole, the organic portion of the organic azide at the 1-position of the triazole, and the substituent of the 1-iodoalkyne at the 4-position of the triazole. A method for preparing 1-iodoalkynes is also provided.

Abstract: The present process purifies a salt Cat+X?, where Cat+ is any cation and X? is an organic anion having at least 6 carbon atoms. The salt is an impurity in a composition comprising a water-soluble salt (Cat+)nYn?, where Yn? is an inorganic anion or an organic anion, different from X?, with at most 10 carbon atoms. The process involves converting X? into an acid HX by adding an acid (H+)mZm?, forming two phases: an organic phase comprising HX and an aqueous phase comprising the water-soluble salts (Cat+)mZm? and (Cat+)nYn? or acids (H+)nYn?. The organic phase is separated and the aqueous phase passes over a basic anion exchanger which binds Zm? and Yn? and liberates OH?, giving an aqueous mixture comprising Cat+OH?. The organic phase and the aqueous mixture are converted into Cat+X? and H2O, optionally with addition of further HX.

Abstract: This invention is directed to compounds of formula I having the structure which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.

Abstract: The present invention relates generally to an improved process for the preparation of 5-azaspiro[2.4]heptane-6-carboxylic acid and its derivatives which are useful intermediates in the synthesis of biologically active molecules, especially in the synthesis of hepatits C virus NS5A inhibitors.

Abstract: The present invention relates to a stereoselective reduction procedure to obtain, by means of catalytic asymmetric hydrogenation by hydrogen transfer, a compound of formula (I) in which X is S or SO2 and R4 is hydrogen or an SO2NH2 group, from the corresponding ketone precursor, said compound of formula (I) being useful as an intermediate in the preparation of dorzolamide or of the hydrochloride salt thereof.

Abstract: The present disclosure provides a processes for the preparation of a compound of Formula I: which is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of Formula I.

Abstract: The present invention relates to a process for preparing Nebivolol and, more particularly, to an improved method of debenzylation of a compound of formula (II) useful for preparing nebivolol endowed with high purity.

Abstract: The present invention provides a process for obtaining dronedarone or salts thereof characterized in that in an organic phase comprising one or more non-polar solvents, 5-amino-3-[4-(3-di-n-butylaminopropoxy)benzoyl]-2-n-butyl-benzofuran is reacted with methane sulfonyl chloride without the addition of a base. The invention also provides a process for obtaining intermediates of dronedarone environmentally friendly and industrially viable.

Abstract: Embodiments of the present disclosure provide processes and systems for the epoxidation of an olefin using a fixed bed reactor. The fixed bed reactor is maintained at a temperature from 0 to 40 degrees Celsius. The processes and systems regulate a superficial liquid velocity of a non-homogeneous reaction mixture and recycled portion of effluent of the fixed bed reactor.

Abstract: A process for producing propylene oxide comprising reacting propene with hydrogen peroxide in the presence of a catalyst to give a mixture (G1) comprising propylene oxide, unreacted propene, and oxygen; separating propylene oxide from mixture (G1) to give a mixture (GII) comprising propene and oxygen; and adding hydrogen to mixture (GII) and reducing the oxygen comprised in mixture (GII) at least partially by reaction with hydrogen in the presence of a catalyst comprising copper in elemental and/or oxidic form on a support, wherein copper is present on the support in an amount of 30 to 80 wt.-% based on the whole catalyst and calculated as CuO.

Abstract: The subject matter of the invention is a process for synthesizing ?-functionalized acids of formula R—(CH2)n—COOH in which R is COOH or NH2CH2, from a feedstock of natural origin containing hydroxylated fatty acids.

Abstract: The invention describes novel 14-hydroxy docosahexaenoic acid (DHA) analogs, their preparation, isolation, identification, purification and uses thereof.

Abstract: Organometallic complexes and use thereof in thin film deposition, such as CVD and ALD are provided herein. The organometallic complexes are (alkyl-substituted ?3-allyl)(carbonyl)metal complexes.