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.

Provided is a compound which has strong and sustaining intraocular pressure lowering action and, further, has no fear of side effect on eyes. Since a compound represented by the formula (I): wherein definition of each group is as described in the specification, or a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering action and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.

Disclosed is a process to produce a dry purified carboxylic acid product comprising furan-2,5-dicarboxylic acid (FDCA). The process comprises oxidizing at least one oxidizable compound selected from the following group: 5-(hydroxymethyl)furfural (5-HMF), 5-HMF esters (5-R(CO)OCH2-furfural were R alkyl, cycloalkyl and aryl), 5-HMF ethers (5-R'OCH2-furfural, where R'=alkyl, cycloalkyl and aryl), 5-alkyl furfurals (5-R″-furfural, where R″=alkyl, cycloalkyl and aryl), mixed feed-stocks of 5-HMF and 5-HMF esters and mixed feed-stocks of 5-HMF and 5-HMF ethers and mixed feed-stocks of 5-HMF and 5-alkyl furfurals to generate a crude carboxylic acid slurry comprising FDCA.

A process for the manufacture of dialkyl furan-2,5-dicarboxylate (DAFD) vapor composition by feeding furan-2,5-dicarboxylic acid (“FDCA”) to an esterification reactor and in the presence of an alcohol compound such as methanol, conducting an esterification reaction to form an esterification vapor containing DAFD, unreacted alcohol compound, 5-(alkoxycarbonyl)furan-2-carboxylic acid (ACFC), and water, and continuously passing the esterification vapor through an ACFC condensing zone, that can be integral with the esterification reactor, in which at least a portion of the ACFC in the esterification vapor is converted to a liquid phase condensate, and continuously discharging the esterification vapor from the ACFC condensing zone as a DAFD vapor. There is also a DAFD vapor composition containing DAFD, water, unreacted alcohol, and by-products.

Described herein are compounds generally comprising an indeno[2',3':3,4]naptho[1,2-b]pyran structure. Such compounds may be useful for their photochromic properties, and be used in certain photochromic compositions. Such compositions may further comprise other photochromic compositions and/or materials. Additionally, such compounds and/or compositions may be suitable for preparing certain photochromic articles. Also described herein are methods for preparing certain photochromic compounds, compositions, and articles.

The present invention relates to new salts of 6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol(rotigotine), their use as a medicament, for example for the treatment of CNS disorders like Parkinson Disease, RLS, fibromyalgia and/or depression, in particular through electromotive administration. The present invention relates to pharmaceutical formulations suitable for iontophoresis that provide enhanced iontophoretic delivery of rotigotine to at least one target tissue. The formulations are further characterized by good to excellent solubility of the salts in aqueous solutions.

A polymer composition for solar cell and flexible electronics devices, where the polymer is a p-type conducting polymer. The p-type polymer comprises a benzothiadiazole acceptor and indeno-fluorene donor. Further, a solar cell and flexible electronic device article may be made from the polymer.

A catalyst for an organic reaction and a method of using a catalyst in an organic reaction are provided. The catalyst for an addition or condensation reaction includes a graphene oxide including an oxygen functional group, and the catalyst is configured to promote the addition or condensation reaction by bonding the oxygen functional group with an alkali metal ion or alkali earth metal ion during the addition or condensation reaction.

Lactic acid equivalents are recovered from a starting lactide stream by catalytically racemizing a portion of the lactide in the stream at a temperature of 180° C. or below. This increases the proportion of two species of lactide (i.e., at least two of S,S-, R,R- or meso-lactide) at the expense of the third species. The racemized mixture so obtained can be separated to recover some or all of one or more of the lactide species from the remaining lactide species, by a process such as melt crystallization or distillation. Impurities in the starting lactide stream usually are retained mostly in the remaining meso-lactide, so a highly purified S,S- and/or R,R-lactide stream can be produced in this manner. Such a purified S,S- and R,R-lactide stream is suitable for polymerization to form a polylactide.

Provided are a method of preparing a chlorohydrin composition and a method of preparing epichlorohydrin by using a chlorohydrin composition prepared by using the method. The method of preparing chlorohydrins in which polyhydroxy aliphatic hydrocarbon is reacted with a chlorination agent in the presence of a catalyst includes performing at least one combination of a series of unit operations comprising a first reaction step, a water removal step, and a second reaction step in this stated order, wherein the method further includes mixing a chlorohydrin concentrate obtained by purifying the reaction mixture discharged from the final reaction step from among the reaction steps and a water-rich layer discharged from the water-removal step and diluting the mixture with water. The method of preparing epichlorohydrin includes contacting the chlorohydrin composition prepared by using the method of preparing a chlorohydrin composition with an alkaline agent.

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.

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 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.

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.

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.

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.

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.

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.

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.

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.

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.

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 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 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.

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.

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 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 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.

There is provided a compound having an excellent controlling effect on pests represented by the formula (1): wherein, A1 represents —NR7—, etc., A2 represents a nitrogen atom, etc., A3 represents a nitrogen atom, etc., R1 represents a C1-C6 chain hydrocarbon group optionally substituted by one or more atoms or groups selected from Group X, etc., R2, R3 and R4 are the same or different and each represents a C1-C6 chain hydrocarbon group optionally substituted by one or more halogen atoms, etc., R5 and R6 are the same or different and each represents a C1-C6 chain hydrocarbon group optionally substituted by one or more atoms or groups selected from Group X, etc., R7 represents a C1-C6 chain hydrocarbon group optionally substituted by one or more atoms or groups selected from Group W, etc., n represents 0, 1 or 2, or an N-oxide thereof.

A pesticidal composition comprising (a) a pesticidal effective amount of at least one compound of formula I in which Q is i or ii or iii or an agrochemically acceptable salt or an N-oxide thereof, and (b) a plant growth regulator, where the ratio of compound of formula I to plant growth regulator is from 20:1 to 1:25.

This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.

A compound of the formula (1) wherein the substituents are as defined in claim 1, are useful as a pesticides.

The present invention discloses a method of inhibiting an ethylene response in a plant, comprising step of applying to at least one portion of the plant an effective ethylene response-inhibiting amount of a H1-cyclopropene-1-propanoic acid salt (CPAS). A method of prolonging the life of a cut flower, comprising applying to the cut flower an effective life-prolonging amount of CPAS and a method for the production a CPAS, comprising steps of (i) preparing 4-bromo-4-pentenoic acid or derivatives thereof; (ii) producing 1-cyclopropene-1-propanoic acid; and (iii), converting this acid into its water soluble salt, especially its sodium salt are presented. Additionally, a new family of water soluble CPAS inhibitors for ethylene response in a plant is disclosed.

Compounds which are trehalose-6-phosphate or trehalose-6-phosphonate precursors of formula (I) or agriculturally acceptable salts thereof are provided: (I) The compounds are useful in increasing starch production in plants.

Compositions and methods, including novel homogeneous microparticulate suspensions, are described for treating natural surfaces that contain bacterial biofilm, including unexpected synergy or enhancing effects between bismuth-thiol (BT) compounds and certain antibiotics, to provide formulations including antiseptic formulations. Previously unpredicted antibacterial properties and anti-biofilm properties of disclosed BT compounds and BT compound-plus-antibiotic combinations are also described, including preferential efficacies of certain such compositions for treating certain gram-positive bacterial infections, and distinct preferential efficacies of certain such compositions for treating certain gram-negative bacterial infections.

Penoxsulam, 2-(2,2-difluoroethoxy)-N-(5,8-dimethoxy[1,2,4]-triazolo[1,5-c]pyrimidin-2-yl)-6-(trifluoromethyl)benzenesulfonamide, is useful in controlling broadleaf weeds and sedges in turfgrass and in vine and orchard floors.

The present invention relates to a pyridazinone compound of the formula (I): wherein R1 represents hydrogen, a C1-6 alkyl group, and the like, R2 represents halogen, a cyano group, a nitro group, a C1-6 alkoxy group, and the like, G represents hydrogen, and the like, Z represents halogen, a cyano group, a nitro group, a C1-6 alkyl group, and the like, and n represents an integer of 1-5 useful as an active ingredient in a herbicide and a noxious arthropod controlling agent.

Disclosed herein are mesocapsules that include agriculturally active ingredients. These mesocapsules are comprised of a polyurea shell and include hydrophilic groups on their surfaces and have a volume-average diameter of about 500 nm or less and some of them have a volume-average diameter on the order of about 300 nm or less. These mesocapsules are suited for delivering active ingredients that are not very soluble in water. Methods for making these mesocapsules include interfacial polycondensation reactions carried out in the presence of surfactants and other methods in which all or most of the surfactant is replaced by adding amino acids to the aqueous phase of the interfacial reaction mixture before forming the final emulsion.

Bioactive agrichemical concentrates and compositions having improved bioactivity comprising combinations of acid solutions and conventional bioactive agrichemical actives or formulations.

New phenylamidines are described, having general formula (I): and their use for the control of phytopathogenic fungi.

Herbicidal injury caused by 6-trisubstituted phenyl)-4-amino-2-pyridinecarboxylates in wheat and barley is reduced with the use of low rates of cloquintocet.

Provided herein are herbicidal compositions containing (a) aminopyralid or an agriculturally acceptable salt or ester thereof and (b) propanil. The compositions provide synergistic weed control of undesirable vegetation, e.g., in rice, wheat, barley, oats, rye, sorghum, corn or maize, oilseed rape/canola, vegetables, pastures, grasslands, rangelands, fallowland, turf, tree and vine orchards, industrial vegetation management or rights-of-way.