The present invention provides novel 16,23-diene 25-oxime ether analogs of 1,25-dihydroxy vitamin D3, compositions comprising these compounds and methods of using these compounds as inhibitors of CYP24. In particular, the novel compound of the invention are useful for treating diseases which benefit from a modulation of the levels of 1,25-dihydroxy vitamin D3, for example, cell-proliferative disorders.

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.

Provided are methods for the treatment of a rheumatic disease, such as rheumatoid arthritis, ankylosating spondylitis and/or polymyalgia rheumatic, by administering a delayed-release dosage form of a glucocorticoid to a subject in need thereof wherein the treatment is administered once daily for at least about two weeks. Also provided are methods for the treatment of osteoarthritis by administering a delayed-release dosage form of a glucocorticoid to a subject in need thereof wherein the treatment is administered once daily for at least about two weeks.

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.

Several different pyrrolysine analogs are disclosed in this application. Those analogs have distinct chemical and biophysical properties. Some analogs are useful in chemical ligation applications. Methods of making and using are also disclosed.

The invention relates to nitrooxyderivative of corticosteroids of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof R—(Z)a—Rx (I) wherein R is the corticosteroid residue of formula (II): wherein: R1 is OH, R2—CH3, or R1 and R2 are taken together to form a group of formula (III) R3 is Cl or F;R4 is H or F; wherein R1, R2, R3 and R4 can be linked to the correspondent carbon atoms of the steroidal structure in position α or β; with the proviso that: when R1 and R2 are the group of formula (III) then R3 is F and R4 is H or F; The compounds are useful in the treatment of respiratory diseases, inflammatory diseases, dermatological diseases and ocular diseases.

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.

Provided are compounds of Formula I wherein R1, R2, Y, Z and G are as defined herein, that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.

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.

Methods for the synthesis and purification of 9-amino alkyl tetracycline compounds are described.

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.

There is intended to provide the novel compounds which generate a base easily when irradiated with long wavelength light (active energy rays), a photobase generator containing the compounds and a photobase generation method, and the present invention relates to the compounds represented by the general formula [1], a photobase generator containing the compounds and a photobase generation method: (wherein, Ar represents any of groups with specific structures selected from the group consisting of an anthracenyl group, an anthraquinonyl group and a pyrenyl group; R1 and R2 each independently represent a hydrogen atom or a linear, branched or cyclic alkyl group having 1 to 10 carbon atoms, or represent ones which can form an alicyclic ring containing nitrogen atom(s) or an aromatic ring containing nitrogen atom(s) together with a nitrogen atom to which they are bound, which the rings having 3 to 8 carbon atoms which may have a substituent, R3 and R4 each independently represent a hydrogen atom, a linear, branched or acyclic alkyl group having 1 to 10 carbon atoms).

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.

A hydrophobic cationic steroidal anti-microbial (ceragenin) compound forms an amphiphilic compound having a hydrophobic sterol face and a hydrophilic cationic face. The hydrophobic CSA also includes a hydrophobic substituent that gives the ceragenin compound a CLogP value of at least 6.5.

This invention discloses N-cyclopropyl-(20R)-2-methylene-19,26,27-trinor-25-aza-vitamin D analogs, and specifically N-cyclopropyl-(20R)-2-methylene-19,26,27-trinor-25-aza-1α-hydroxyvitamin D3 and pharmaceutical uses therefor. This compound exhibits relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent especially for the treatment or prevention of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer.

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.

This invention discloses 3-desoxy-2-methylene-19-nor-vitamin D analogs, and specifically (20S)-3-desoxy-2-methylene-1α,25-dihydroxy-19-nor-vitamin D3 and (20R)-3-desoxy-2-methylene-1α,25-dihydroxy-19-nor-vitamin D3 as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to monocytes thus evidencing use as anti-cancer agents especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. These compounds also exhibit relatively high calcemic activity evidencing use in the treatment of bone diseases.

It is reported herein that certain muscle diseases and conditions, including forms of muscular dystrophy, are characterized by impaired insulin-dependent signaling in the muscle tissue, in essence, a form of insulin resistance. The present disclosure relates to therapeutic agents, compositions and methods for treating a muscle disease or condition characterized by impaired insulin-dependent signaling by targeting components of the defective insulin signaling pathway. The disease or condition may be treated by administering a therapeutic agent that activates the insulin signaling pathway, in particular, therapeutic agents that act post-insulin receptor to modulate intracellular effector molecules. An exemplary modulator is metformin. Metformin may be administered alone or may be coadministered with another therapeutic agent for treating the muscle disease or condition, such as a corticosteroid.

The invention relates to compounds of Formula (A): (A) or a salt, solvate, hydrate, or amino acid conjugate thereof. The compounds of formula A are TGR5 modulators useful for the prevention and treatment of disease.

The present invention pertains to tetracycline compounds of formula (VIIa): R5*, R5*', R7r*, and R9m* are defined herein. These tetracycline compounds can be used to treat tetracycline compound-responsive states, such as multiple sclerosis and rheumatoid arthritis.

The invention discloses a method for producing 30-halogenated betulinic acid. Betulin is used as a raw material and selectively oxidized and halogenated to generate 30-betulinic acid, and the selected oxidation and halogenation agent has high selectivity and does not affect C-3 hydroxyl or carbon-carbon double bonds. Oxidation and halogenation are completed in one step, so the process route is short, the treatment method is simple, and the product is purified easily.

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.

Tissue slices and whole organisms offer substantial challenges to fluorescence imaging. Autofluorescence and absorption via intrinsic chromophores, such as flavins, melanin, and hemoglobins, confound and degrade output from all fluorescent tags. An “optical window,” farther red than most autofluorescence sources and in a region of low hemoglobin and water absorbance, lies between 650 and 900 nm. This valley of relative optical clarity is an attractive target for fluorescence-based studies within tissues, intact organs, and living organisms. Novel fluorescent tags were developed herein, based upon a genetically targeted fluorogen activating protein and cognate fluorogenic dye that yields emission with a peak at 733 nm exclusively when complexed as a “fluoromodule”. This tool improves substantially over previously described far-red/NIR fluorescent proteins in terms of brightness, wavelength, and flexibility by leveraging the flexibility of synthetic chemistry to produce novel chromophores.

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.

N-Substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximines are effective at controlling insects.

The present invention relates to an pesticidal composition comprising an effective amount of a sulphur; an effective amount of at least one insecticide selected from the group consisting of cartap fipronil, pirimicarb, buprofezine, thiachloprid, acetamiprid, clothianidin, diafenthiuron, novaluron, flubendiamide, spirotetramat, thiamethoxam, imidacloprid or salts thereof, and at least one agrochemically acceptable excipient.

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 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.