Abstract: Described herein is pure amorphous darunavir, methods of making pure amorphous darunavir and pharmaceutical compositions containing amorphous darunavir and a pharmaceutically acceptable excipient.

Abstract: An isosorbide derivative of Formula (I) is provided. In Formula (I), Z is —CH2—CH2—, —CH?CH—, —C?C—, —CH2—O—, —CH2—S—, —CH?N—O—, —CO—O—, —CO—S—, single bond, -ph-, —CO—O-ph- or —CO—O-ph-CO—O—, and ph represents benzene, R1 and R2 are, independently, C1-25 alkyl, —CN, —NCS, —CX3 or —OCX3, and X represents halogen, and m and n are, independently, 0, 1 or 2. The invention also provides a liquid crystal display including the isosorbide derivative.

Abstract: The present invention provides a novel process for preparation of darunavir that involves reduction of [(1S,2R)-3-[[(4-nitrophenyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy -1-(phenylmethyl)propyl]carbamic acid (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ester, of formula (5). The present invention also provides darunavir ethanolate of particle size wherein d0.9 is less than 130 ?m, d0.5 is less than 30 ?m, d0.1 is less than 10 ?m and process for its preparation.

Abstract: The present invention relates to a mixture comprising diesters of the formula (I) where R1 to R8?H or alkyl group having from 1 to 6 carbon atoms, where the R1 to R8 radicals may be the same or different, which is characterized in that at least two different diesters I are present in the mixture, said diesters differing in the structure of at least one of the carboxylic acid radicals C8H17COO present, to a process for preparing diesters of an isosorbide derivative of the formula I, in which a hexahydric alcohol and/or a monoanhydro or dianhydro derivative of the alcohol is esterified with a mixture of at least two different carboxylic acids of the empirical formula C8H17COOH, and to the use of these mixtures in paints, inks or coatings, in plastisols, adhesives or adhesive components, in sealants, as plasticizers in polymers or polymer components, as solvents, as lubricant oil components and as assistants in metal processing, and also PVC compositions or plastisols comprising PVC and from 5 to 250 parts by ma

Abstract: A composition comprising an alkynyl phenoxy compound of Formula (I) as a synergist and a pesticidal active ingredient is described, wherein R1 and R2, similar or different, are (C1-C4)alkyl or R1O— and R2O— together represent a group —O—CH2—O—, —O—CH(CH3)—O, —O—CH2—CH2—O—, —O—CH2—CH2—, R3 is (C1-C6)alkyl, (C3-C6)alkenyl or —B—(CH2-CH2—O)z-R6 where B is —CH2—O— or —O—, z is 0, 1 or 2 and R6 is (C1-C4)alkyl; R4 is hydrogen or methyl; R5 is hydrogen or methyl; x is an integer from 1 to 2; y is 0, 1 or 2; with the proviso that when R3 is —B—(CH2CH2—O)z-R6, y is 1 and 5-(propargyloxy)-benzo[1,3]dioxole is excluded.

Abstract: Presently disclosed are methods and apparatus for separation of reaction products from reaction mixtures in an ionic liquid catalysis process, particularly in conversion of biomass, cellulose, and sugars into chemical intermediates such as 5-hydroxymethylfurfural (HMF). In one embodiment an ion exclusion adsorption mechanism is used for the separation process. The process comprises (i) mixing the ionic liquid-containing reaction mixture with de-ionized water, (ii) flowing the water solution mixture into an adsorption column, (iii) eluting the column with a water- and/or alcohol-based fluid, and (iv) collecting separated fractions at different elution times.

Abstract: The present invention relates to new 3-substituted 6-nitrooxy-hexahydrofuro[3,2-b]furane derivatives possessing a superior pharmacological activity in thrombosis and in coronary ischemia models.

Abstract: The present invention provides isomannide derivatives having structural formula (I) as shown below and certain subgenera or species thereof, as flavoring agents or tastants, flavor or taste modifiers, and/or flavor/taste enhancers, particularly, savory (“umami”) flavoring agent or tastant, savory taste modifiers, and/or savory flavor enhancers, for ingestible compositions. The present invention also provides methods of preparing isomannide derivatives having the structural formula (II) shown below and certain subgenera or species thereof.

Abstract: Disclosed are isosorbide glyceryl ether derivatives according to the following general formula (I), wherein R or R? represent a hydrogen atom, or an alkyl or an acyl group with 6 to 22 C-atoms, and n and m represent independent from each other zero, or a number from 1 to 4, and the use thereof in cleansers or detergents or personal care applications.

Abstract: The present invention provides processes for catalytically converting biomass to oxygenated compounds suitable for use in bioreforming processes.

Abstract: The present invention relates to new 3-substituted 6-nitrooxy-hexahydrofuro[3,2-b]furane derivatives possessing a superior pharmacological activity in thrombosis and in coronary ischemia models.

Abstract: Compounds having the formula wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of aniline and capable of inhibiting the lethal effects of infection by anthrax bacteria and are useful in the treatment of poisoning by anthrax.

Abstract: Provided herein are isosorbide-based bisphenol polymer structural units and methods of making the same. These structural units may be polymerized with one or more other types of structural units to form polymers, such as polycarbonates.

Abstract: A dianhydrohexitol diester composition is obtained by esterifying a dianhydrohexitol composition with a carboxylic acid in the presence of an acid catalyst and hypophosphorous acid. Preferably, the hypophosphorous acid is introduced in an amount between 0.05 and 2 wt. percent of dianhydrohexitol, and in a hypophosphorous acid/acid catalyst weight ratio of less than 1/1. Dianhydrohexitol diester compositions, for example isosorbide diesters, isomannide and/or isoidide rich in diester(s), and having a low yellow index (YI), are useful in numerous industrial applications, in particular in plastic compositions.

Abstract: A process is disclosed for converting a polysaccharide-containing biomass material to platform chemicals. The process comprises dissolving the polysaccharides in an inorganic molten salt hydrate, converting the polysaccharides to monosaccharides, and converting the monosaccharides to derivatized (di)anhydro sugars that are easily separable from the inorganic molten salt hydrate. The derivatized (di)anhydro sugars are useful as fuel additives and fuel substitutes.

Abstract: Methods for the preparation of hexahydrofuro[2,3-b]furan-3-ol and especially its enantiomer (3R,3aS,6aR) hexahydrofuro[2,3-b]furan-3-ol, as well as certain novel intermediates for use in such methods are disclosed.

Abstract: The invention relates to reactive derivatives on the basis of dianhydrohexitol-based isocyanates.

Abstract: The invention relates to the use of 2,5-diisocyanato-1,4:3,6-dianhydro-2,5-dideoxy-D-manitol (I), 2,5-diisocyanato-1,4:3,6-dianhydro-2,5-dideoxy-D-glucitol (II), and/or 2,5-diisocyanato-1,4:3,6-dianhydro-2,5-dideoxy-L-iditol (III).

Abstract: The present invention relates to a marking of polymeric liquid crystal material having determined optical characteristics allowing its authentication and reading by a machine and its authentication by the human eye. The marking is applied onto an item, good or article by a variable information printing process. The marking is in the form of indicia representing a unique code which allows for an easy authentication by the human eye and a secure tracking and tracing of the marked item, good or article throughout is life cycle.

Abstract: A method for preparing a dianhydrohexitol diester composition, characterized in that it comprises a step which consists in esterifying a dianhydrohexitol composition with a carboxylic acid in the presence of an acid catalyst and hypophosphorous acid. Preferably, the hypophosphorous acid is introduced in an amount ranging between 0.05 and 2 wt. % of dianhydrohexitol, and in a hypophosphorous acid/acid catalyst weight ratio less than 1/1. The method enables novel dianhydrohexitol diester compositions, for example isosorbide diesters, isomannide and/or isoidide richer in diester(s) and/or less colored, useful in numerous industrial applications, in particular in plastic compositions, to be obtained.

Abstract: [Problem] There is provided a method for producing an oxygen-containing compound safely and with improved reaction efficiency, in which an undesired peroxide is unlikely to be produced, and efficient heat exchange of the ozonization can be achieved.

Abstract: A method for preparing dialkyl carbonates of dianhydrohexitol, includes the following steps: (a) preparing an initial reaction mixture containing at least one dianhydrohexitol, at least two mole equivalents of a dialkyl carbonate of formula and a transesterification catalyst; (b) heating the reaction mixture to a temperature greater than or equal to the boiling temperature of the formed alcohol, or of the azeotrope thereof, in a reaction chamber preferably provided with a rectification column including a sufficient number of theoretical distillation plates to separate the resulting alcohol from the reaction mixture. Certain dialkyl carbonates of dianhydrohexitols produced by the method and the use thereof for synthesizing synthetic polymers are also described.

Abstract: The invention relates to a method for the amination of at least one keto group in a multicyclic ring system comprising at least one keto group into an amino group, using at least one enzyme E having transaminase activity.

Abstract: The present invention provides new pseudopolymorphic forms of darunavir as well as a novel amorphous form of darunavir, pharmaceutical compositions comprising these compounds, methods for their preparation and use thereof in treating retroviral infections, in particular, HIV infection.

Abstract: Isosorbide monoesters according to the general formula (I) wherein R? or R? represent a hydrogen atom, or an group CO—R??, with the proviso that one group R? or R? is a hydrogen atom, and R?? represents linear or branched, saturated or unsaturated alkyl- or alkenyl groups with 6 to 22 C-atoms are useful compounds in the preparation of all kind of detergents, in particular dish washing detergents or of cosmetic preparations.

Abstract: This invention relates to a new method for the stereospecific thiocarboxylation and nitration of organic compounds for the preparation of compounds according to formula (I): comprising the following steps: (a) reacting a compound of formula (II): with a sulfonic derivative of formula (III) wherein the R is chosen from the groups C1-3-alkyl, C1-3-alkyl substituted with 1 to 3 halogen atoms, phenyl, C1-3-alkyl-phenyl and C1-3-alkyl-phenyl wherein the alkyl is substituted with 1 to 3 halogen atoms and G is a halogen atomo or a group —O—SO2—R wherein R is as hereinabove defined to yield a compound of formula (IV) (b) treating compound (IV) with a thiocarboxylic acid of formula (V) or a salt thereof: wherein Z is as defined above, to yield compound (VI) and (c) treating compound (VI) with tetrabutylammonium nitrate to yield a compound of formula (I).

Abstract: A cosmetic composition for nails containing a plasticizer of natural origin, a derivative of sorbitol, and the use of isosorbide diester as a plasticizer in cosmetic compositions for nails.

Abstract: The present invention concerns substituted aminophenylsulfonamide compounds, their use as protease inhibitors, in particular as broad-spectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present substituted aminophenylsulfonamide compounds with another anti-retroviral agent. It further relates to their use in assays as reference compounds or as reagents.

Abstract: The present invention provides novel solvated forms of darunavir and processes for there preparation. The present invention also provides novel process for preparation of darunavir amorphous form and pharmaceutical composition comprising it. Thus, for example, darunavir 2-methyl-2-butanol solvate was dissolved in methylene dichloride, distilled under vacuum at 45° C. to obtain a residue, cyclohexane was added to the residue and stirred for 30 hours at 20 to 25° C., and the separated solid was filtered, washed with cyclohexane and dried under vacuum at 50° C. for 12 hours to yield darunavir amorphous form.

Abstract: A process for the preparation of N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide derivatives in which a (1-benzyl-2-hydroxy-3-isobutylamino-propyl)-carbamic acid derivative is reacted with a p-nitrophenylsulfonyl halide to provide the desired product in a high yield and degree of purity.

Abstract: 3,9-diazabicyclo[3.3.1]nonane derivatives, useful as monoamine neurotransmitter re-uptake inhibitors. Also, use of these compounds in a method for therapy and in pharmaceutical compositions comprising the compounds. The 3,9-diazabicyclo[3.3.1]nonane derivatives have the formula wherein Ra and Rb are as described in the application. Also disclosed are stereoisomers and pharmaceutically acceptable salts of the compounds.

Abstract: The present invention provides a compound having the structure (I) and processes for the production thereof and the intermediates used in such process.

Abstract: A process for preparing crystalline Form A of tadalafil (I), comprising crystallization from a solution of tadalafil in a solvent comprising a C3-C7 ester, a ketone, dimethylformamide, dimethylsulfoxide, ethanol, acetonitrile, a chlorinated hydrocarbon, t-butanol, N,N-dimethylacetamide, dioxane, N-methyl pyrrolidone, or a mixture of any two or more thereof.

Abstract: The invention provides protease inhibitors that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the protease inhibitors not attached to the water-soluble oligomer.

Abstract: The invention relates to a method for producing 2,6-dioxabicyclo-(3.3.0)-octane-4,8-dione (I), comprising the oxidation of dianhydrohexitols (II-IV), or of corresponding hydroxy ketones, with an oxygen-containing gas in the presence of a catalyst composition, the reaction proceeding without the addition of halogen sources.

Abstract: The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them and to methods of using the prodrugs.

Abstract: This invention relates to novel hydroxyethylamino sulfonamides and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a compound with the ability to act as an HIV (human immunodeficiency virus) protease inhibitor.

Abstract: Asymmetrically substituted compounds of bisanhydrohexitols are described, including the bisanhydrohexitol isosorbide. The compounds are useful as monomers. The synthesis of polymers from the monomers is also described.

Abstract: This invention relates to a new method for the stereospecific thiocarboxylation and nitration of organic compounds for the preparation of compounds according to formula (I): comprising the following steps: (a) reacting a compound of formula (II): with a sulfonic derivative of formula (III) wherein the R is selected from the groups C1-3-alkyl, C1-3-alkyl substituted with 1 to 3 halogen atoms, phenyl, C1-3-alkyl-phenyl and C1-3-alkyl-phenyl wherein the alkyl is substituted with 1 to 3 halogen atoms and G is a halogen atom or a group —O—SO2—R wherein R is as hereinabove defined to yield a compound of formula (IV) (b) treating compound (IV) with a thiocarboxylic acid of formula (V) or a salt thereof: wherein Z is as defined above, to yield compound (VI) and (c) treating compound (VI) with tetrabutylammonium nitrate to yield a compound of formula (I).

Abstract: Novel spatially-defined macrocyclic compounds containing specific conformational control elements are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle species that exhibit a specific interaction with a particular biological target. In particular, compounds according to the invention are disclosed as agonists or antagonists of a mammalian motilin receptor and a mammalian ghrelin receptor.

Abstract: Disclosed are derivatives of isosorbide having formula (1) wherein R? and R? represent hydrogen or a polymeric ether moiety (CH2—CHR1—O)x—H, where R1 represents hydrogen, or an alkyl or alkenyl moiety having 1 to 33 carbon atoms, which is saturated or unsaturated, branched or linear. This polymeric ether moiety can be a homopolymer or a copolymer, with x being the total degree of polymerization (DP). Preferred is a block copolymer composed of monomer A (DP=a), preferably ethylene oxide or propylene oxide, and monomer B (DP=b), preferably a saturated or unsaturated, branched or linear alkyl or alkenyl moiety having 1 to 33 carbon atoms, where x=a+b. x is a number from 0 to 50, with the proviso that R? and R? are not both hydrogen. The isosorbide derivatives are useful as components of detergent, cleanser, cosmetic and agricultural compositions.

Abstract: In one aspect, the present disclosure encompasses polymerization systems for the copolymerization of CO2 and epoxides comprising 1) a catalyst including a metal coordination compound having a permanent ligand set and at least one ligand that is a polymerization initiator, and 2) a chain transfer agent having two or more sites that can initiate polymerization. In a second aspect, the present disclosure encompasses methods for the synthesis of polycarbonate polyols using the inventive polymerization systems. In a third aspect, the present disclosure encompasses polycarbonate polyol compositions characterized in that the polymer chains have a high percentage of —OH end groups and a high percentage of carbonate linkages. The compositions are further characterized in that they contain polymer chains having an embedded polyfunctional moiety linked to a plurality of individual polycarbonate chains.

Abstract: The invention relates to nitric oxide donors of the formula (I) and pharmaceutically acceptable salts or stereoisomers thereof: wherein A and A? are independently selected from the group consisting of H and —(X)s—Y with the proviso that at least one of A or A? is not H; wherein s is 0 or 1; X is selected from the group consisting of: —CO—, —COO—, —CONH— and —SO2— or Y is straight or branched C1-C20 alkyl chain, preferably C1-C10 alkyl chain, substituted with one or two —ONO2; or C1-C6 alkylenoxy-C1-C5 alkyl wherein the alkyl group is substituted by one or two —ONO2 groups. The invention also provides novel compositions comprising at least one compound of the invention and at least one therapeutic agent.

Abstract: A method for preparing a dianhydrohexitol diester composition, characterized in that it comprises a step which consists in esterifying a dianhydrohexitol composition with a carboxylic acid in the presence of an acid catalyst and hypophosphorous acid. Preferably, the hypophosphorous acid is introduced in an amount ranging between 0.05 and 2 wt. % of dianhydrohexitol, and in a hypophosphorous acid/acid catalyst weight ratio less than 1/1. The method enables novel dianhydrohexitol diester compositions, for example isosorbide diesters, isomannide and/or isoidide richer in diester(s) and/or less coloured, useful in numerous industrial applications, in particular in plastic compositions, to be obtained.

Abstract: Provided herein (among other things) are protease inhibitor compounds having enhanced features, along with methods for administering such compounds. For example, the subject compounds can be administered without concomitant administration of a CYP3A4 inhibitor, have increased therapeutic index and/or increased potency, and are low-resistance inducing in nature. Exemplary potent HIV protease inhibitors are mono-m-PEG3-atazanavir, mPEGn-N-darunavir (wherein n is 3 or 5), mPEGn-NHCO-saquinavir (wherein n is 5 or 7), and di-mPEG3-atazanavir.

Abstract: The present inventions to provide a novel polymerizable chiral compound (chiral agent) having high helical twisting power, a polymerizable liquid crystal composition comprising the polymerizable chiral compound and a polymerizable liquid crystal compound, a liquid crystal polymer, and an optically anisotropic body.

Abstract: The invention relates to new reactive mesogenic compounds (RM), polymerisable liquid crystal (LC) mixtures and polymers comprising them, and the use of the compounds, mixtures and polymers in optical, electrooptical, electronic, semiconducting or luminescent components or devices, in decorative, security or cosmetic applications, especially for use in polymer films having high optical dispersion.

Abstract: A process for converting aqueous sorbitol to xylitol and isosorbide in the presence of an acid catalyst, and in the absence of an enzyme or of a hydrogenating catalyst, is disclosed. In the process, a sorbitol solution is reacted with an acid zeolite to produce xylitol and isosorbide.

Abstract: The invention relates to compounds of formula (I): wherein R1 and R2 are each independently selected from the group: H, F, Cl and CH3; n1 and n2 are each independently integers 3 to 20; q and r are each independently integers 0, 1 or 2, with the proviso that q+r is ?1; D is a divalent chiral radical selected from the group: wherein R3 is a C1 to C6 straight or branched chain alkyl group; and each B1 and B2 is a divalent radical independently selected from the group: R4-substituted-1,4-phenyl, wherein R4 is H, —CH3 or —OCH3; 2,6-naphthyl; and 4,4?-biphenyl; with the provisos that when q+r=3, at least one of B1 and B2 is R4-substituted-1,4-phenyl; and when q+r=4, at least two of B1 and B2 are R4-substituted-1,4-phenyl. The invention further relates to liquid crystal compositions comprising compounds of formula (I) and polymer networks derived from the polymerization of the liquid crystal compositions.

Abstract: The present invention relates to a process for the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate as well as novel intermediates for use in said process. (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate is particularly useful as an HIV protease inhibitor.