Abstract: The present invention relates to compounds of formula (I) that have CYP450 inhibiting properties and are useful as boosting agents when used with HIV treatments. These compounds are represented by formula including the salts and stereoisomeric forms thereof, wherein R1 is 5-thiazolyl or 3-pyridinyl; R2 is iso-butyl, 2,2-dimethylpropyl; 2-hydroxy-2-methyl-propyl or cyclohexylmethyl; R3 is phenyl optionally substituted with one or more halogens, trifluoromethyl, C1-6-alkyl or C1-6-alkoxy wherein optionally two of said alkoxy groups are be linked to each other to form a 5 or 6-membered ring; heteroaryl; C3-7cycloalkyl optionally substituted with one or more halogens; C1-6alkyl optionally substituted with heteroaryl; —O—CH2— (heteroaryl). As boosting agents they are able to increase at least one of the pharmacokinetic variables of certain drugs when co-administered, or improve the bioavailability of certain drugs.

Abstract: Provided are compounds and compositions of general Formula IX: E1-L-Ar—X-PA, that may be utilized in bioconjugation procedures, where Ar is a chromophore and PA is a functional group capable of being attached to any bioactive molecule of interest. The present invention provides Formulas I-III that are capable of being attached to a bioactive vector for the selective delivery of said photoactive pyrazine derivatives to a desired biological target.

Abstract: This invention relates to ruthenium complex-based photosensitizer dyes for dye-sensitized solar cells, which have a general structural formula represented by formula (I).

Abstract: A light-emitting element having excellent light-emitting properties and with which it is possible to emit blue light at a high luminance for a long period of time, and an iridium complex for realizing the same. The light-emitting element has an external quantum efficiency of at least 5% and a light emission maximum wavelength ? max of no more than 500 nm. Further, there is provided a light-emitting element including a light-emitting layer or a plurality of organic compound layers having the light-emitting layer, with at least one of the compound layers including at least one kind of a compound having a partial structure represented by the general formula K-0. In the general formula K-0, R1 to R7 each independently represents a hydrogen atom or a substituent, provided that if R2 is a fluorine atom, R3 is not a hydrogen atom.

Abstract: The present invention relates to a process of separation of 4-aza-androst-1-ene-17-oic acid from 4-aza-androstan-17-oic acid, which brings to 4-aza-androst-1-ene-17-oic containing less than 0.05% w/w of 4-aza-androstan-17-oic acid, with high yield and productivity. In particular, the present invention relates to a process for the separation of 4-aza-androstan-17-oic acid from 4-aza-androst-1-ene-17-oic acid, comprising the steps of treating the crude 4-aza-androst-1-ene-17-oic acid with formic acid and recovering the purified 4-aza-androst-1-ene-17-oic acid containing 4-aza-androstan-17-oic acid in w/w % less than 0.05%.

Abstract: A method of staining a poly(amino acid) by contacting a poly(amino acid) with an overall neutral or overall cationic complex of at least one of transition metal ion, and a plurality of donor ligands each of which is fully coordinated to the transition metal ion and is either a nitrogen donor ligand or a cyclometalated donor ligand, such that at least one of the donor ligands is a cyclometalated donor ligand. Nitrogen donor ligands will contain heteroaryl ring systems having from 10 to 40 ring atoms, wherein each nitrogen donor ligand is substituted with from 0 to 4 R1 groups. Cyclometalated donor ligands will likewise contain heteroaryl ring systems having from 10 to 40 ring atoms, such that at least one ring atom is N, wherein each cyclometalated donor ligand is substituted with from 0 to 4 R1 groups. R1, R2, R3 and R4 groups are defined herein.

Abstract: The present invention is directed to a novel form of a pyrrolopyridine-2-carboxylic acid amide of formula (I), which is an inhibitor of glycogen phosphorylase, compositions containing it and their use in therapy. The invention is also directed to processes for production of the novel form, novel intermediates used in said processes and processes for the production of said intermediates.

Abstract: Methods for producing moxifloxacin hydrochloride compounds having very low levels of impurities are provided. Compounds produced using such methods and pharmaceutical compositions including such compounds are also provided.

Abstract: The present invention relates to sodium channel inhibitors of Formula (I): in which R1, R2, R3, R4, R5, X, Y, and Z are as defined herein, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.

Abstract: Triphenylamine derivatives useful as fluorophores in biology, in particular for two-photon microscopy; and compositions comprising these derivatives, to the use of these compositions and of the derivatives themselves for labelling biological molecules (or “biomolecules”) such as nucleic acids, oligonucleotides, proteins, polypeptides, plasmids, and the like, for their examination in particular by two-photon microscopy, and to biomolecules labelled with the said derivatives.

Abstract: The present invention is directed to a new class of hydroxamic acid derivatives of formula I, wherein the variables G, T, D, L, R1, R2, R3 are as described herein, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections in a patient in need thereof.

Abstract: A process for preparing 1-(6-methylpyridin-3-yl)-2-[4-(methyl sulfonyl)phenyl]ethanone, an intermediate of the synthesis of Etoricoxib. The synthesis of the intermediates useful for such preparation is also described.

Abstract: The present invention relates to a process for the preparation of S-[2-[1-(2-ethylbutyl)cyclohexylcarbonylamino]-phenyl]2-methylthiopropionate which is useful as a pharmaceutically active compound.

Abstract: A method for producing a 3-halo-1,2-benzisothiazole represented by the general formula (2): wherein R1 is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, an alkoxycarbonyl group having 2 to 5 carbon atoms, a nitro group or a halogen atom, and X is a halogen atom, the method characterized by reacting a 1,2-benzisothiazol-3-one represented by the general formula (1): wherein R1 is the same group as the R1 defined in the above general formula (2), with a thionyl halide in a polar solvent. The 3-halo-1,2-benzisothiazole obtainable according to the method of the present invention is suitably used as production raw materials and the like for a medicament and the like.

Abstract: The object is to provide a stable SM-108 derivative, which is effective as a carcinostatic agent, particularly an SM-108 derivative having good storage stability. An SM-108 compound having good storage stability can be produced by producing an organic sulfonic acid salt compound of SM-108. Further, a crystalline SM-108 compound containing a trace amount of an organic carboxylic acid can be produced by using an aqueous solution of the organic sulfonic acid salt of SM-108, and by adding an alkali metal salt of an organic carboxylic acid to the aqueous solution to neutralize the aqueous solution and then causing the crystal precipitation in the solution.

Abstract: The disclosure provides fluorescence probe compounds of formula I, their preparation methods and applications. These compounds are useful in detecting mercury ions.

Abstract: The present disclosure provides drug-ligand conjugates that are potent cytotoxins and include a linker between the drug and ligand where the linker has a single amino acid. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.

Abstract: Industrial synthesis process for, and crystalline form I of, the compound of formula (I): and also crystalline form I of the associated free base. Medicinal products containing the same which are useful in the treatment of disorders of the histaminergic system.

Abstract: The present invention relates to a new process for the preparation of (poly)aminoalkylaminoacetamide derivatives of epipodophyllotoxin and salts thereof, characterized in that it comprises a step of peptide coupling of 4-amino-4?-demethylepipodophyllotoxin with an amine-containing reactant having protecting groups.

Abstract: The invention relates to a fluorescent dye of general formula I or II wherein R1, R2, R3 and R4 are independently hydrogen or a branched or unbranched, saturated or unsaturated, aliphatic or aromatic, functionally substituted, or unsubstituted hydrocarbon radical, wherein at least one of the R1 or R2 radicals and one of the R3 or R4 radicals is not hydrogen and the R1 and R3 radicals and/or R2 and R4 radicals in formula I can be bridged to each other, and X and Y independently represent a substituted or unsubstituted C1 or C2 hydrocarbon radical wherein any one carbon unit can be replaced by an N or S heteroatom. The dye is remarkable for its high fluorescence intensity and large Stokes shift in combination with a long fluorescence lifetime.

Abstract: Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)—O—C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)—O—C(O)-heteroaryl and a basic tertiary amine.

Abstract: The present invention relates to an epoxidation process for the preparation of alkylene oxide comprising contacting a hydroperoxide with an olefin in the presence of a catalyst, wherein the catalyst is a titanium containing catalyst obtainable by a method comprising the steps of (a) making a support by a method comprising reacting a silicate with water in the presence of a surfactant selected from block copolymers based on ethylene oxide (EO) and propylene oxide (PO), and calcining the obtained reaction product; and (b) impregnating the support of step (a) with a titanium containing agent.

Abstract: An epoxy compound of high-purity N,N,N?,N?-tetraglycidyl-3,4?-diaminodiphenyl ether is produced by: an addition reaction step of reacting 3,4?-diaminodiphenyl ether with epichlorohydrin in a polar protic solvent at 65 to 100° C. for 12 hours or longer to form N,N,N?,N?-tetrakis(3-chloro-2-hydroxypropyl)-3,4?-diaminodiphenyl ether; and a cyclization reaction step of reacting the N,N,N?,N?-tetrakis(3-chloro-2-hydroxypropyl)-3,4?-diaminodiphenyl ether with an alkali compound for dehydrochlorination.

Abstract: According to the present invention, a process for producing an epoxy compound, where an epoxy compound can be selectively produced from olefins with good yield at low cost in a safe manner by a simple operation under mild conditions without using a quaternary ammonium salt or a metal compound, is provided. The present invention relates to a process for producing an epoxy compound, comprising epoxidizing a carbon-carbon double bond of an organic compound having a carbon-carbon double bond by using hydrogen peroxide as an oxidant, wherein the epoxidation is carried by out using an organic nitrile compound and an organic amine compound.

Abstract: A process for preparing (meth)acrylates of C17-alcohol mixtures by reacting (meth)acrylic acid with a C17-alcohol mixture in the presence of at least one acidic catalyst and of at least one polymerization inhibitor and in the presence of a solvent which, with water, forms an azeotrope in which the esterification is performed in a reactor with a circulation evaporator, the azeotrope is distilled off and condensed, and the condensate splits into an aqueous phase and an organic phase, wherein the C17-alcohol mixture has a mean degree of branching (iso index) of 2.8 to 3.7.

Abstract: The present invention describes a process for the production of alkyl esters of fatty acids and glycerine employing, in a reaction section, at least one transesterification reaction between an animal or vegetable oil and an aliphatic mono-alcohol, and using a heterogeneous solid catalyst, in which the energy balance is improved by thermal integration of the energy released during the mono-alcohol condensation step.

Abstract: The invention provides for a process for the preparation of a silylferrocene compound, comprising the steps of treating ferrocene with a 4-chloroalkyryl chloride in the presence of an lewis acid catalyst and an organic solvent to obtain the acylated product, reducing the acylated product to obtain the 4-chloralkylferrocene, treating the 4-chloroalkylferroce with a metal under Grignard reaction conditions to form its corresponding Grignard intermediate compound; and reacting with chloroalkylsilane in-situ to give the silylferrocene compound. The silylferrocene compound 4-(dimethylsilyl)butylferrocene can be prepared by the process of the invention.

Abstract: The invention relates to a method for producing mono-carboxyfunctionalized dialkylphosphinic acids and esters and salts thereof, characterized in that a) a phosphinic acid source (I) is reacted with olefins (IV) to yield an alkylphosphonic acid, salt or ester (II) thereof in the presence of a catalyst A, b) the alkylphosphonic acid thus obtained, salt or ester (II) thereof is reacted with an ?,?-unsaturated carboxylic acid derivative (V) to yield a mono-carboxyfunctionalized dialkylphosphinic acid derivative (III) in the presence of a catalyst B, wherein R1, R2, R3, R4, R5, R6, R7 are the same or different and stand independently of each other, among other things, for H, C1-C18 alkyl, C6-C18 aryl, C6-C18 aralkyl, C6-C18 alkylaryl, and X and Y are the same or different and stand independently of each other for H, C1-C18 alkyl, C6-C18 aryl, C6-C18 aralkyl, C6-C18 alkylaryl, Mg, Ca, Al, Sb, Sn, Ge, Ti, Fe, Zr, Zn, Ce, Bi, Sr, Mn, Cu, Ni, Li, Na, K and/or a protonized nitrogen base, and the catalyst A is formed b

Abstract: This invention provides, but is not limited to, methods of using metal-organic frameworks (MOFs) having repeat units of the formula M2(DHTP) (M is a divalent metal ion; DHTP=2,5-dihydroxyterephthalate) for acetylene storage. Also provided are compositions of the same formula and acetylene, e.g., an acetylene storage material comprising [M2(DHTP)]n and acetylene.

Abstract: A process for producing zinc toluenesulfonate comprising reacting a zinc compound comprising Zn(OH)2 with toluenesulfonic acid and/or a salt thereof in the presence of an alcohol having 1 to 20 carbon atoms in total at a temperature higher than 60° C.

Abstract: A surface modifier comprising an organosilicone compound represented by General Formula (A) and/or General Formula (B): F—(CF2)q—(OC3F4)m—(OC2F4)n—(OCF2)o(CH2)pXX?Si(X?)3-a(R1)a (A) and F—(CF2)q—(OC3F6)m—(OC2F4)n—(OCF2)o(CH2)pXX?(X?)2-a(R1)aSiO(F—(CF2)q—(OC3F6)m—(OC2F4)n—(OCF2)o—(CH2)pXX?(X?)1-a(R1)aSiO)zF—(CF2)q—(OC3F6)m—(OC2F4)n—(OCF2)o(CH2)pXX?(X?)2-a(R1)aSi(B) wherein q is an integer from 1 to 3; m, n, and o are independently integers from 0 to 200; p is 0, 1 or 2; X is oxygen or a bivalent organic spacer group: X? is a bivalent organosilicone spacer group; X? is hydrolysable group; and z is an integer from 0 to 10 when a is 0 or 1.

Abstract: A silicone composition comprising a formula: (M1)a(D1)b(D2)c wherein M1=R1R2R3SiO1/2, D1=R4R5SiO2/2; and D2=R6R7SiO2/2; wherein R1 is independently at each occurrence a monovalent hydrocarbon radical comprising a reactive end-group other than an amino group; R6 comprises a monovalent poly(oxyalkyl)hydrocarbon radical; and R2, R3, R4, R5, and R7 are independently monovalent hydrocarbon radicals; wherein a, b, and c are stoichiometric subscripts that are zero or positive subject to the following limitations: a is greater than or equal to 2; c is greater than or equal to 1; and when b=0, a+c is greater than or equal to 3 is disclosed.

Abstract: A process for the preparation of acylated secondary alcohol alkoxylates and a process for making secondary alcohol alkoxy sulfates comprising the steps of:— preparing secondary alcohol alkoxylates by the afore-mentioned process; and sulfating the secondary alcohol alkoxylates is described.

Abstract: Provided is a method for preparing 2,5-dimethylphenylacetic acid, wherein p-xylene is mixed with paraformaldehyde and concentrated hydrochloric acid in a solvent of ion liquid to obtain 2,5-dimethyl benzyl chloride by the chloromethylation reaction. Then, 2,5-dimethyl benzyl chloride is introduced into a reactor with an acid binding agent and a solvent, the carbonylation and hydrolysis reaction is conducted in the presence of a catalyst to obtain 2,5-dimethylphenylacetic acid. The present process has new route, less synthesis steps, simple operation, lower cost, increased yield, and is friendly to the environment. Therefore, the method is suitable for industrial production.

Abstract: Fluorescent compositions having emission under long UV excitation can be utilized as security taggants in printing inks. The fluorescent compositions can be esters of 2-naphthalenesulfonamide, and can be produced as solids in crystal or powder form.

Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.

Abstract: The invention relates to a process for preparing hyperbranched polyhydroxybenzoic acid alkoxylates, comprising the steps of: (a) reacting at least one polyhydroxybenzoic ester with one or more alkylene oxides, optionally in the presence of a basic catalyst, (b) allowing the polyhydroxybenzoic ester alkoxylates formed in step (a) to react with transesterification to form hyperbranched polyhydroxybenzoic acid alkoxylates.

Abstract: The present invention relates to a novel process for preparing substituted and unsubstituted (2,4-dimethylbiphenyl-3-yl)acetic acids and their esters of the formula (I) using homogeneous and heterogeneous palladium catalysts, and also the intermediates 4-tert-butyl-2,6-dimethylphenylacetic acid and 4-tert-butyl-2,6-dimethylmandelic acid, and to processes for their preparation.

Abstract: The present invention relates to the discovery of new class of linear and multiarmed hydrolysable linkers and cross linkers for use in the synthesis of biodegradable polymers such as, polyesters, polyurethanes, polyamides, polyureas and degradable epoxy amine resin. The linear and multiarmed hydrolysable linkers of the present invention include symmetrical and/or unsymmetrical ether carboxylic acids, amines, amide diols, amine polyols and isocyanates.

Abstract: A pentaerythritol tetraester which is a mixed ester of pentaerythritol and carboxylic acids is provided, wherein the carboxylic acids comprise isobutyric acid and 2-ethylhexanoic acid and the molar ratio of isobutyric acid to 2-ethylhexanoic acid in the carboxylic acids is 36/64 to 83/17. The pentaerythritol tetraester may be used in a refrigerant oil or the like which exhibits excellent miscibility with a difluoromethane refrigerant among other properties.

Abstract: An intermediate for preparing (meth)acrylated photoinitiators according to Formula (I): wherein: R1 is selected from the group consisting of hydrogen and a methyl group; A represents a group including at least one photoinitiating moiety; L represents a n+o-valent linking group including at least one carbon atom; n and o each independently represent an integer from 1 to 4; p is equal to 0 or 1; X represents a group selected from the group consisting of CI, Br, I, and R2SO3; and R2 represents an optionally substituted group selected from the group consisting of an alkyl group, an alkenyl group, an alkynyl group, an alkaryl group-, an aralkyl group, an aryl group and a heteroaryl group. Also, a method for the preparation of (meth)acrylated photoinitiators by ?-elimination of HX from the intermediate according to Formula (I).

Abstract: Use of S-(3-aminopropyl)thiosulfuric acid and/or a metal salt thereof for improving the viscoelastic properties of a vulcanized rubber.

Abstract: The compound 4-[3-(2,6-Dimethylbenzyloxy)phenyl]-4-oxobutanoic acid (DPA) is synthesized from 1-[3-(2,6-Dimethylbenzyloxy)-phenyl]-ethanone (DPE) via the intermediate 4-[3-(2,6-Dimethylbenzyloxy)phenyl]-4-oxobulanoic acid ethyl ester (DPAE).

Abstract: A process for preparing aliphatic carboxylic acids having 3 to 10 carbon atoms by oxidizing the corresponding aldehydes with oxygen or oxygen-containing gases, characterized in that (i) the oxidation is performed in a microreactor at elevated pressure and with an oxygen excess based on the stoichiometrically required amount of oxygen, and (ii) in that the reaction mixture removed from the microreactor is passed through at least one postreactor without further addition of oxygen, and (iii) wherein the oxidation reaction in the microreactor is performed under such conditions that aldehyde and corresponding peracid formed are present in the reaction mixture removed in a molar ratio within a range of 1:(0.9 to 1.1), preferably of 1:(0.95 to 1.05).

Abstract: A method of preparing a liquid lactic acid composition that has a total acid content of at least 94% (w/w) and that does not crystallize at a temperature above 10° C. includes obtaining a starting liquid lactic acid composition that has a total acid content of at least 94% (w/w) and that crystallizes at a temperature above 10° C. and incubating said starting liquid lactic acid composition at a temperature above the crystallization point of the starting liquid lactic acid composition for a time period to obtain the liquid lactic acid composition that does not crystallize at a temperature above 10° C.

Abstract: The present invention relates to a solid bed adsorptive separation of organic acid and/or amino acids from fermentation broths containing organic acid and/or amino acid.

Abstract: A process for producing (meth)acrylic acid, comprising the step of repeating a crystallization operation “n” times (providing “n” is an integer 2 or more) to produce purified (meth)acrylic acid from crude (meth)acrylic acid, wherein a (meth)acrylic acid solution is crystallized and the crystallized (meth)acrylic acid is melted to obtain a (meth)acrylic acid melt in the crystallization operation; wherein a constant amount Ak of the (meth)acrylic acid solution is subjected to the kth crystallization operation (providing “k” is an integer 1 to n?1), and the (meth)acrylic acid melt obtained by the kth crystallization operation is utilized as the (meth)acrylic acid solution for the k+1th crystallization operation without being discharged from a crystallizer or is transferred from the crystallizer to a k+1th storage tank for storing the (meth)acrylic acid solution to be used in the k+1th crystallization operation depending on the stored amount of the k+1th storage tank.

Abstract: An object of the invention is to provide efficient, simple and inexpensive processes for the production of carbonyl difluoride, which is an attractive and important compound as a semiconductor etching gas or a semiconductor cleaning gas. A process for producing carbonyl difluoride of the invention includes a step of reacting phosgene and hydrogen fluoride in a gas phase in the presence of a fluorination catalyst to produce carbonyl difluoride and hydrogen chloride, and a step of mixing a mixture containing the carbonyl difluoride and the hydrogen chloride with an organic solvent that is azeotropic with hydrogen chloride but zeotropic with carbonyl difluoride, and distilling the resultant mixture to separate the carbonyl difluoride.

Abstract: Graphene, a method of fabricating the same, and a transistor having the graphene are provided, the graphene includes a structure of carbon (C) atoms partially substituted with boron (B) atoms and nitrogen (N) atoms. The graphene has a band gap. The graphene substituted with boron and nitrogen may be used as a channel of a field effect transistor. The graphene may be formed by performing chemical vapor deposition (CVD) method using borazine or ammonia borane as a boron nitride (B—N) precursor.

Abstract: A method for preparing Aliskiren and intermediate thereof, which comprises the following steps: reacting 4-bromo-1-methoxy-2-(3-methoxypropoxy)benzene with magnesium isopropyl chloride and n-BuLi to obtain the compound of formula XXII; reacting the product of methylsulfonylation of the compound of formula XIX with anhydrous LiBr to obtain the compound of formula XXI; obtaining the intermediate of Aliskiren shown as formula XV by reacting the compound of formula XXII with the compound of formula XXI in an ether as the solvent and in the presence of a catalyst containing iron; then reacting the compound of formula XV with the compound of formula VII to obtain the compound of formula XXIII, following removing R1 from the amino group and obtaining Aliskiren shown as formula I.