Abstract: The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D1 and D2 as well as the 5HT2 receptors in the central nervous system, to medicaments comprising such compounds as active ingredients, to the use of such compounds in the treatment of diseases in the central nervous system, and to methods of treatment comprising administration of such compounds.

Abstract: Disclosed are compounds of Formula (I) or stereoisomers or salts thereof, wherein: X1, X2, X3, W, Q1, Q2, and G2 are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

Abstract: The invention relates to novel quinazolinone compounds and their use as inhibitors of PI3 kinases, for example, PI3K?, for treating and/or preventing diseases, disorder, and conditions associated with modulating PI3 kinase activity. Novel 3-aryl-2-((arylamino)methyl)quinazolin-4(3H)-one derivatives and pharmaceutically acceptable salts or solvates thereof and their use for the treatment or prevention of diseases, disorders, and conditions associated with the activity of one or more PI3 kinase, such as PI3K?, are disclosed.

Abstract: The present invention relates to a non-solvated crystalline Darunavir, process for its preparation and pharmaceutical composition comprising it. The present invention also relates to a process for the preparation of amorphous Darunavir from a non-solvated crystalline Darunavir.

Abstract: The present invention relates to a method for producing a furan-based compound using an ion exchange resin in the presence of an organic solvent. In the method for producing a furan-based compound according to the present invention, a furan-based compound is made from an aldose-type hexose compound in the presence of an organic solvent by using an anion exchange resin and a cation exchange resin. Thus, the aldose-type hexose compound obtained from biomass by simultaneously or consecutively using the anion/cation exchange resins as catalysts can be made into 5-hydroxymethyl-2-furfural (HMF) or alkyl ether derivatives thereof such as 5-alkoxymethyl-2-furfural (AMF) without using an expensive reagent. Also, since the selection of an organic solvent is not limitative and a heterogeneous catalyst can be used, separation and purification is easy and chemically stable AMF can be directly obtained.

Abstract: Novel chroman derivatives and intermediate compounds, compositions containing same, methods for their preparation and uses thereof as therapeutic agents particularly as anti-cancer and chemotherapeutic selective agents are described.

Abstract: The invention relates to (among other things) non-ring hydroxy substituted taxanes and methods for synthesizing the same. The invention further relates to conjugating the non-ring hydroxyl substituted taxanes to a water-soluble, non-peptidic polymer.

Abstract: In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.

Abstract: Disclosed embodiments relate to improved methods for the synthesis of activated fumarate intermediates and their use in chemical synthesis. Disclosed embodiments describe the synthesis of activated fumarate esters including those derived from activating groups including: 4-nitrophenyl, diphenylphosphoryl azide, pivaloyl chloride, chlorosulfonyl isocyanate, p-nitrophenol, MEF, trifluoroacetyl and chlorine, for example, ethyl fumaroyl chloride and the subsequent use of the activated ester in situ. Further embodiments describe the improved synthesis of substituted aminoalkyl-diketopiperazines from unisolated and unpurified intermediates allowing for improved yields and reactor throughput.

Abstract: Disclosed are intermediates of Sitagliptin, a preparation process thereof, and a process for synthesizing Sitagliptin using these intermediates. Sitagliptin is synthesized by using chiral amino compounds as a raw material, without having to build a chiral center with a chiral asymmetric catalytic hydrogenation, and high-pressure hydrogenation is avoided.

Abstract: A process which isolates tetrahydrofuran from a stream of tetrahydrofuran, alkanol and high boilers, by: (a) separating off a first stream of tetrahydrofuran and alkanol as azeotrope in a first distillation stage; (b) feeding part of the first stream into a reactor for esterifying maleic anhydride, giving a second stream of tetrahydrofuran and monoalkyl maleate; (c) separating the second stream into a third stream of monoalkyl maleate and a fourth stream of tetrahydrofuran in a second distillation stage; (d) feeding the fourth stream of tetrahydrofuran from the second distillation stage and the part of the first stream from (a) which is not fed to the reactor into a third distillation stage to obtain a product stream of tetrahydrofuran and a sixth stream of tetrahydrofuran and alkanol; (e) recirculating the sixth stream from the third distillation stage into the first distillation stage or the reactor in (b).

Abstract: Gambogenic acid derivatives having a structure shown as Formula (I) or (II), salts, preparation method and application thereof in the treatment of tumor. Compared with gambogenic acid, the gambogenic acid derivatives exhibit more potent anti-tumor activities.

Abstract: Furfural is produced by mixing an aqueous feedstock solution containing C5 sugar and/or C6 sugar with a heated, high boiling, water-miscible solvent, such as sulfolane, and a soluble acid catalyst. Furfural product and water are distilled off through a multistage distillation column, leaving non-volatile solvent behind. Typical furfural yields with sulfolane as the reaction solvent are about 80% at as high as 99% conversion. Also, certain by-products (e.g., humins) solubilized in the reaction solvent can be precipitated by addition of water or aqueous feedstock solution and then removed by filtration, thereby providing a convenient and effective way of removing these undesirable byproducts from the reaction mixture.

Abstract: Furfural is produced by mixing an aqueous feedstock solution containing C5 sugar and/or C6 sugar with a heated high boiling, water-miscible solvent, such as sulfolane, and a solid acid catalyst. Furfural product and water can be distilled off, leaving non-volatile solvent behind. Furfural yields of over 70% at as high as 99% conversion have been obtained with this process with sulfolane as the reaction solvent and zeolite beta as the solid acid catalyst. Also, certain by-products (e.g., humins) solubilized in the reaction solvent can be precipitated by addition of water or aqueous feedstock solution and then removed by filtration, thereby providing a convenient and effective way of removing these undesirable byproducts from the reaction mixture.

Abstract: There is provided a compound having a good miscibility with another liquid crystal compound and having a combination of a low viscosity (?), high storage stability, and high T?i even after being used to produce a liquid crystal composition. In particular, it is a compound having a 2-fluorophenyloxymethane structure is provided. Since the compound having a 2-fluorophenyloxymethane structure is highly miscible with another liquid crystal compound, using the compound having a 2-fluorophenyloxymethane structure as a component of a liquid crystal composition enables a production of a liquid crystal composition which exhibits a liquid crystal phase at low viscosity and in a wide temperature range and which has a high storage stability and enables production of a liquid crystal display device which responds fast and which has excellent display characteristics.

Abstract: Processes for making furfural and 5-hydroxymethylfurfural from sugars are provided. The processes can be carried out using a batch process or a continuous mode of operation. An aqueous sugar solution is pressurized with CO2, thereby producing carbonic acid in situ that catalyzes the dehydration reaction to produce furfural from C5 sugars and 5-methylhydroxyfurfural from C6 sugars.

Abstract: This disclosure relates to a process for the preparation of N-[2-n-butyl-3-{4-[(3-dibutylamino)-propoxy]-benzoyl}-1-benzofuran-5-yl]-methane-sulfonamide of formula I and its pharmaceutically acceptable salts, wherein one of the methylsulfonyl groups of the 2-n-butyl-3-[(di-n-butylamino-3-propoxy)-benzoyl]-5-bis-(methylsulfonamido)-benzofuran of formula II is selectively cleaved and if desired, the resulting compound of formula I is transformed into its salt.

Abstract: Provided in some embodiments are compositions comprising a compound having a structure according to Formula A or Formula B: or a pharmaceutically acceptable salt, tautomer or hydrate thereof, where X2 is a bond or linker, X3 is bond or —PO4—, and X1, R1, R2, R3, and n are described herein. Also provided in some embodiments are methods for making and using such compounds and compositions.

Abstract: The invention relates to a novel process for preparation of dronedarone (I) and pharmaceutically acceptable salts thereof where the compound of formula (II) or salt thereof is reacted with a compound of formula L-(CH2)3—CH3 (III), where L is a leaving group, and isolating the obtained product and, if desired, converting it into a pharmaceutically acceptable salt thereof. The invention also relates to some novel intermediary compounds and the preparation thereof.

Abstract: The present invention generally relates to methods for the synthesis of catalysts, including epoxidation catalysts, and related compounds and catalyst compositions. Embodiments described herein may provide efficient processes for providing catalysts (e.g., epoxidation catalysts) in large quantities and using simplified methods.