A liquid crystal composition including a dioxolane compound represented by the general formula (G1) as a chiral agent is provided. In the general formula (G1), R1 and R2 individually represent any of hydrogen, an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 20 carbon atoms, an aryl group having 6 to 12 carbon atoms, and an alkyl group having 1 to 20 carbon atoms and having a phenyl group as a substituent; R1 and R2 may be bonded to each other to form a ring; R3 and R4 individually represent any of hydrogen, an alkyl group having 1 to 6 carbon atoms, and a cycloalkyl group; and R5 to R40 individually represent any of hydrogen, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, and an aryl group having 6 to 12 carbon atoms.

The present invention provides a diaryl sulfone compound represented by Formula (1) below: wherein R1 to R4 and R1' to R4' are the same or different; each represents hydrogen, C1-4 alkyl, or halogen; and R5 is (thio)glycidyl, acryloyl, or the like; and a method for producing the same. According to the present invention, a novel compound useful as a monomer for producing synthetic resin having a high refractive index and excellent transparency for optical materials can be efficiently produced with a simple production process, using an inexpensive material as a starting material.

An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives.

Disclosed in the present invention is a novel histone deacetylase inhibitor of benzamides and use thereof. The inhibitor has good efficacy in treating diseases caused by abnormal gene expression, such as tumors, endocrine disorders, immune system diseases, genetic diseases and nerve system diseases. The histone deacetylase inhibitor of benzamides is a compound of the following general chemical structural formula (I) or a salt thereof.

Provided is a method of producing an organic transistor, including collectively forming a gate insulating film and an organic semiconductor film by applying, onto a gate electrode, a solution including a polymer and at least one of compounds represented by General Formulas 1 to 4 and 5 to 7, a compound having a structure represented by General Formula 4, a compound having a structure represented by General Formula 5 or 6, and forming a source electrode and a drain electrode on the organic semiconductor film. (where R is a linear or branched alkyl group) (where R is an alkyl group) (where R is an alkyl group) (where A1 and A2 are represented by Formula 8) (where R is an alkyl group or another substituent).

The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.

The invention includes halichondrin B analogs having pharmaceutical activity; in some cases, crystalline forms thereof, and in some cases, halichondrin B analogs having a further utility as synthetic intermediate.

Bromoacetoxycalcidiol (B3CD), which is structurally related to calcidiol, exhibits cytotoxic and apoptotic activity toward cancer cells, including highly aggressive neuroblastoma cells. A series of small molecules designed around the structure of B3CD is expected to have growth inhibitory and apoptogenic activities toward a wide range of malignancies. B3CD shows no apparent toxicity in vivo, indicating potential value as a chemotherapeutic agent which will be particularly useful in treating highly aggressive tumors.

Steroid compounds having increased resistance against metabolism and increased water solubility are disclosed, together with methods for their production. These substances are suitable for the manufacture of pharmaceuticals for the treatment of steroid related or steroid induced CNS disorders and for use in methods of prevention, alleviation or treatment of such disorders.

The present invention relates to a process for the preparation of 17α-(3-hydroxypropyl)-17β-hydroxysteroids of the formula I starting from 17-ketosteroids of the formula III via the intermediates of the formula V wherein the radicals R3, R5, R6, R7, R10, R13, R15, R16, R40, R41 and R42 have the meaning indicated in the description.

A topical therapeutic hydrophobic breakable composition includes a carrier comprising (a) about 60% to about 99% by weight of at least one hydrophobic oil; (b) at least one viscosity-modifying agents selected from the group consisting of a fatty alcohol, a fatty acid and a wax; and (c) a tetracycline antibiotic, characterized in that at least part of the tetracycline antibiotic is suspended in the composition; the viscosity of the composition is at least about 30% higher than the viscosity of the carrier without the tetracycline antibiotic; and is higher than the viscosity of the hydrophobic oil and the tetracycline antibiotic without the viscosity modifying agents. The tetracycline is chemically stable in the composition for at least six months; wherein more than about 90% of the tetracycline has not broken down. The composition is packaged as a breakable foam that breaks easily upon application of shear force.

A topical therapeutic hydrophobic breakable composition includes a carrier comprising (a) about 60% to about 99% by weight of at least one hydrophobic oil; (b) at least one viscosity-modifying agents selected from the group consisting of a fatty alcohol, a fatty acid and a wax; and (c) a tetracycline antibiotic, characterized in that at least part of the tetracycline antibiotic is suspended in the composition; the viscosity of the composition is at least about 30% higher than the viscosity of the carrier without the tetracycline antibiotic; and is higher than the viscosity of the hydrophobic oil and the tetracycline antibiotic without the viscosity modifying agents; and the amount of viscosity modifying agents can optionally be reduced by at least an amount by weight that would have increased the viscosity of the carrier without the tetracycline antibiotic by at least 30%; wherein the tetracycline is chemically stable in the composition for at least six months; wherein more than about 90% of the tetracycline has not broken down; wherein when packaged in an aerosol container to which is added a liquefied or compressed gas propellant the composition affords upon release from the container a breakable foam of at least good quality that breaks easily upon application of shear force.

Bile acids and related compositions and methods of synthesis and use. More specifically, deoxycholic acid and related compositions, said compositions being free of all moieties of animal origin and free of pyrogenic moieties.

The invention provides a method for synthesizing 7-Acetyleno quinone methide compounds that is safe and inexpensive. The method avoids the need for extremely cold reaction temperatures and unlike the prior art does not require any highly explosive materials. The method comprises the steps of: a) performing a condensation reaction between 3,5-di-tert-butyl-4-hydroxybenzaldehyde and a secondary amine thereby forming a secondary amine quinone methide intermediate;b) removing water from the secondary amine quinone methide intermediate by azeotropic distillation;c) adding the dehydrated secondary amine quinone methide intermediate to an organic medium containing a metal acetylide to form a Mannich base intermediate; andd) adding a release agent to the Mannich base intermediate to yield a 7-Acetyleno quinone methide.

Disclosed are methods of purifying (20R) and (20S) analogs of 2-methylene-19-nor-22-dimethyl-1α,25-dihydroxyvitamin D3 to obtain the (20R) and (20S) analogs in crystalline form. The method includes the steps of preparing a solvent of either diethyl ether or a mixture of 2-propanol and hexane, dissolving a product containing the (20R) and (20S) analog to be purified in the solvent, cooling the solvent and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of crystals, and recovering the crystals.

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 bicyclic amines of triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.

Use of 9,10-anthraquinone compounds of formula (I) or pharmaceutical salts thereof or plant extracts containing said compounds in the preparation of anti-HCV medicaments is disclosed, in which Y1 are Y2 are independently hydrogen, hydroxyl or groups of formula (II); and R1, R2, R3, R4, R5 and R6 are independently hydrogen, hydroxyl, carboxyl, cyano group, nitro group, groups of formula (III) or groups selected from those substituted or unsubstituted groups: amino, C1-C6 aliphatic hydrocarbon, C3-C7 cyclic aliphatic hydrocarbon, C1-C6 alkoxy, C2-C7 carbalkoxy, C1-C4 acyloxy, C6-C20 aryl, or 5 to 7 members heterocyclic or benzoheterocyclic thereof; or R5 and R6 form the group of formula (IV). The compounds of present invention are cheap, safe and effective because that they mostly come from traditional Chinese medicines and have better anti-HCV effects and lighter side effects.

A way to formulate prasterone to both increase its oral bioavailability, and decrease the variability of its oral bioavailability. In contrast to the approach taught by the prior art, the instant approach is amenable to scale-up to commercial scale. Further, the resulting product is amenable to analysis using standard, known quantitative analytical techniques; thus, unlike the prior art approach, the instant approach may be used to manufacture a product in conformity with applicable regulatory standards.

Disclosed is a photosensitive resin composition for a color filter and a color filter using the same. The photosensitive resin composition for a color filter includes (A) a dye-polymer composite including a structural unit derived from the compound represented by the following Chemical Formula 1, wherein each substituent is the same as defined in the detailed description; (B) an acryl-based photopolymerizable monomer; (C) a photopolymerization initiator; and (D) a solvent.

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-3 cycloalkenyl triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II, III and IV: wherein X can be a C4-8 cycloalkyl, C4-8 cycloalkenyl, C4-9 spirocycloalkyl, C4-9 spirocycloalkenyl, C4-8 oxacycloalkyl, C4-8 dioxacycloalkyl, C6-8 oxacycloalkenyl, C6-8 dioxacycloalkenyl, C6-9 oxaspirocycloalkyl, or C6-9 oxaspirocycloalkenyl ring. These compounds are useful for the treatment of HIV and AIDS.

The present invention relates to novel 4-pregenen-11β-17-21-triol-3,20-dione derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals, as modulators of glucocorticoid or mineralocorticoid receptors. The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat disorders associated with glucocorticoid or mineralocorticoid receptor modulation.

Disclosed is a photosensitive resin composition for a color filter including (A) a dye-polymer composite wherein the dye includes a repeating unit derived from a compound represented by the following Chemical Formula 1, wherein in Chemical Formula 1, each substituent is the same as defined in the detailed description; (B) a binder resin; (C) a photopolymerizable monomer; (D) a photopolymerization initiator; and (E) a solvent.

A stigmasterol-rich phytosterol composition is prepared wherein the composition comprises at least 50% stigmasterol, based on the total weight of phytosterols, no more than 1000 ppm water, no more than 50 ppm ethanol, and wherein stigmasterol is at least 98% in the anhydrous form. A ready-to-freeze beverage is provided comprising the stigmasterol-rich composition and water, with optional additives. A frozen beverage is prepared from the ready-to-freeze beverage as a pourable slush. There are further provided processes to prepare the ready-to-freeze beverage and the frozen slush beverage.

The present invention relates to processes for the crystallisation and for the preparation and isolation of a novel crystalline form of fusidic acid, to the use of said processes in the manufacture of pharmaceutical formulation or medicament, and to the use of said crystalline fusidic acid form for the treatment of bacterial infections.

The disclosure provides compounds and methods of using Apogossypolone derivatives for treating diseases and disorders. In particular, the disclosure provides compounds of Formula I: or a pharmaceutically acceptable salt, hydrate, or solvate thereof, and provides methods for the preparation of compounds of Formula I; and methods for treating cancer, autoimmune diseases, and inflammation by administering a compound of Formula I.

Disclosed are methods of purifying the compound (20R)-2-methylene-19-nor-24-difluoro-1α,25-dihydroxyvitamin D3 to obtain the compound in crystalline form. The methods typically include the steps of dissolving a product containing the compound in a solvent comprising hexane and 2-propanol, cooling the solvent and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of crystals, and recovering the crystals.

The present invention provides for a practical, universal and efficient method to ligate two large macromolecules (e.g., proteins) using the alkyne-azide 1,3-dipolar cycloaddition reaction to produce a conjugated macromolecule, such as a multivalent scFv. The present invention also provides for conjugate macromolecules comprising a plurality of macromolecule components cross-linked through at least one linking group comprising at least one 1,2,3-triazole moiety, wherein at least 50 percent of the macromolecule components in the conjugate macromolecule has only one site available for cross-linking.

In various embodiments, the present invention provides zwitterionic lipids, encapsulants incorporating these zwitterionic lipids and such encapsulants encapsulating one or more bioactive agent. An exemplary bioactive agent is a nucleic acid. Also provided are pharmaceutical formulations of the encapsulants and methods of using such formulations to deliver a bioactive agent to a subject in treating or diagnosing disease in that subject.

The present invention discloses novel process for the preparation of (2R)-2-acetamido-N- benzyl-3-methoxypropanamide of Formula I involving novel intermediates of Formula-XIX and Formula-XX.

The disclosure relates to novel C4 and C6 substituted androst-4-ene diones as well as andros-1,4-diene diones and derivatives thereof, their process of preparation, pharmaceutical compounds containing them, and the use of said compounds for the treatment of hormone-related disorders in mammals. This includes hormone-dependent cancers, particularly those caused by elevated levels of estrogen and its intermediates. These compounds can also be used in the treatment of other hormone-related disorders, including benign prostatic hyperplasia, cardiovascular disease, and neurodegenerative disorders.

The invention relates to 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of formula I with progesterone-antagonizing action and methods of production thereof, use thereof for the treatment and/or prevention of diseases and use thereof for producing medicinal products for the treatment and/or prevention of diseases, in particular uterine fibroids (myomata, uterine leiomyomata), endometriosis, heavy menstrual bleeding, meningiomata, hormone-dependent breast cancers and menopause-associated complaints or for fertility control and emergency contraception.

The invention relates to compounds of formula (I): wherein R is ethyl, propyl or allyl, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.

The present invention relates to a process for the preparation of a compound of formula (I), hydrates or solvates thereof.

The present invention provides a method to label phospholipids in vivo based on the metabolic incorporation of an alkynyl- or azido-labeled metabolic precursor into phospholipids. The resulting phospholipids have alkynyl or azido moieties, which, upon reaction with a labeled azide or alkyne, respectively, form labeled compounds that can be visualized using optical or electron microscopy with high sensitivity and spatial resolution in cells or tissue. The present method provides a valuable tool for imaging phospholipid synthesis, turnover and subcellular localization in cultured cells as well as in animals.

A topical therapeutic hydrophobic breakable composition includes a carrier comprising (a) about 60% to about 99% by weight of at least one hydrophobic oil; (b) at least one viscosity-modifying agents selected from the group consisting of a fatty alcohol, a fatty acid and a wax; and (c) a tetracycline antibiotic, characterized in that at least part of the tetracycline antibiotic is suspended in the composition; the viscosity of the composition is at least about 30% higher than the viscosity of the carrier without the tetracycline antibiotic; and is higher than the viscosity of the hydrophobic oil and the tetracycline antibiotic without the viscosity modifying agents. The tetracycline is chemically stable in the composition for at least six months; wherein more than about 90% of the tetracycline has not broken down. The composition is packaged as a breakable foam that breaks easily upon application of shear force.

The invention relates to a process for the preparation of a compound of formula (I): wherein R1 and R2 are as defined in the description, by reaction of a compound of formula (II) with a base. Compound (I) is an intermediate useful in the preparation of gestodene.

The present invention provides a compound which functions as a selective vitamin D receptor modulator and has action-selectivity or tissue-selectivity such that it does not induce hypercalcemia but causes other effects. There is provided a compound represented by formula (I), a solvate thereof or a prodrug thereof. wherein m and n each independently represent 1 or 0;R represents a hydrogen atom or an alkyl group;Y represents an ethane-1,1-diyl group or an ethyne-1,2-diyl group; andZ1 represents a hydrogen atom and Z2 represents a hydroxyalkoxy group, orZ1 and Z2 jointly form a methylene group.

The invention relates to a solid pharmaceutical composition comprising solid amorphous fulvestrant, said composition being formulated in combination with a solubilizing composition. The invention also relates to a method for preparing said composition and a kit including the composition.

Disclosed are methods of purifying the compound (20R)-19-nor-24-difluoro-1α,25-dihydroxyvitamin D3 to obtain the compound in crystalline form. The methods typically include the steps of dissolving a product containing the compound in a solvent comprising hexane and 2-propanol, cooling the solvent and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of crystals, and recovering the crystals.

The invention relates to a method for producing a protective layer on a surface of a plant, to a protective layer for a surface of a plant, to a plant coated with said protective layer, to a composition for carrying out the method and for producing the protective layer, and to uses of said composition. According to the invention, a method is proposed, wherein at least one sol gel having nano-scale particles is formed by the hydrolysis of at least one precursor in water and at least one nano-scale layer of the sol gel is applied onto the surface of the plant. The protective layer according to the invention comprises a nano-scale SiO2 layer, and the composition according to the invention comprises at least one SiO2-producing substance.

The present invention comprises formulations comprising at least one pesticide and at least one co-polymer comprising a) 1-vinyl-2-pyrrolidinone as comonomer a); and b) 60-99 wt % at least one comonomer b) chosen from the group of laurylacrylate and vinyl ester of neodecanoic acid in polymerized form, methods of combating harmful insects and/or phytopathogenic fungi, a method of controlling undesired vegetation and methods of improving the health of plants based on the afore-mentioned formulations.

Novel active compound combinations comprising a carboxamide of the general formula (I) (group 1) in which A, R1, R2 and R3 are as defined in the description,and the active compound groups (2) to (23) listed in the description have very good fungicidal properties.

Aqueous glyphosate formulations comprising a surfactant derived from metathesized natural oil feedstocks are disclosed. The formulations comprise a glyphosate salt, water, and a surfactant derived from a metathesis-derived C10-C17 monounsaturated acid, octadecene-1,18-dioic acid, or their ester derivatives. The surfactant is selected from C10 or C12 amine oxides, C10 or C12 quats, C10, C12, or C16 amidoamines, C10 or C12 amidoamine oxides, C10 imidazoline quats, C10 or C12 amidoamine quats, C10, C12, or C16 betaines, C16 amidoamine betaines, C18 diamidoamines, C18 diamidoamine oxides, C18 diamidoamine diquats, C18 diamidoamine oxide quats, C18 diamidoamine oxide betaines, Cis diamidoamine monobetaines, C18 diamidoamine monobetaine quats, C18 ester amidoamine quats, and amidoamines and their oxidized or quaternized derivatives made from self- or cross-metathesized palm or soybean oil. The surfactants noted above impart substantial stability to highly concentrated glyphosate formulations at, above, and below room temperature and perform as well or better than commercial alternatives.

The present invention is directed towards microcapsules, uses and methods of microencapsulation with improved properties regarding agglomeration, bleeding and control of the reaction. The invention is especially suitable for chemical compounds with at least one carboxamide group, preferably for microencapsulation of those compounds wherein the carbonyl group is attached to a nitrogen atom or nitrogenated heterocycle and wherein the microencapsulation reaction may be too vigorous. The microcapsules are characterized by a mixed glycoluril-polyurea polymer wall, wherein the polyurea groups come from a urea-formaldehyde resin and not from isocyanate monomers or prepolymers. The process of making such microcapsules a dispersant in the oil phase of the type of block copolymer of vinylpyrrolidone/vinylalkene and/or vinylpyrrolidone/vinyl acetate and the microencapsulation reaction may be carried out without the presence of any polyamine/polyol acting as a catalyst.

The use of substituted fused pyrimidinones and dihydropyrimidinones of the formula (I) or salts thereof where the radicals of the formula (I) are each as defined in the description, for enhancing stress tolerance in plants to abiotic stress, and for invigorating plant growth and/or for increasing plant yield.

The present weed reducing material reduces the necessary weed control work by making joint filling sand a hostile substrate for plant and fungus growth by using an environmentally acceptable slow release mineral additive. The additive, having similar grain size distribution, mechanical and rheological properties, forms an integral part of the joint filling sand. The specific gravity of the additive is lower than quartz sand imparting a tendency for the additive to migrate towards the top part of the joint. The additive leads to pore waters rich in sodium and at high pH, both qualities being maintained over long periods. The mixture of additive and sand is handled and applied using conventional laying techniques and equipment, observing usual precautions for mortar or cement mixes with sand. In the environment, reaction with CO2 in the air or in the soil porosity inactivates the causticity, yielding harmless carbonate salts.

The present invention relates to novel active compound combinations comprising, firstly, at least one known compound of the formula (I) in which R1 and A have the meanings given in the description and, secondly, at least one further known active compound from groups (2) to (27) listed in the description, which combinations are highly suitable for controlling animal pests such as insects and unwanted acarids and also phytopathogenic fungi.

The present invention provides: a composition for controlling pests comprising, as active ingredients, ethaboxam and avermectin; a method for controlling pests which comprises applying effective amounts of ethaboxam and avermectin to a pest, a plant or soil for growing plant; and so on.

The present invention relates to compositions, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.

The present invention generally relates to a method for minimizing the formation of insoluble salts of phenoxy herbicides. The method comprises (1) mixing a compatibility agent, amine salts of phenoxy acid herbicides, and a chemical containing non-amine cations in a aqueous system to form a stable and non-nozzle plugging solution; and (2) application of said stable and non-nozzle plugging solution onto target plants.