A process for the preparation of a chiral compound, in particular posaconazole, wherein the process comprises mixing and reacting the compounds of formula (I) Y3—NH2; of formula (IIa) 0=C═N—Y0 and/or of formula (IIb) and of formula (III) in a solvent in any order to obtain a reaction mixture containing a chiral compound of formula (IV) and/or formula (V).

The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases are therapeutically useful.

The invention relates to oxazolopyrimidine compounds of formula I, where A, R1 and R2 are defined as stated in the claims. The compounds of formula I are suitable, for example, for wound healing.

The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, T, V, W, X, Y, Z, ring A, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and m are defined herein. There novel pyrrolopyrimidine and purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.

The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R1 represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C1-5alkylR3, wherein R3 is piperidinyl-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C1-4alkyl, C1-4hydroxyalkyl and C1-4alkoxy; 2) C2-5alkenylR3, wherein R3 is as defined herein; 3) C2-5alkynylR3, wherein R3 is as defined herein; and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof; processes for their preparation; pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.

The present invention provides a compound useful as an agent for the prevention or treatment of a sex hormone-dependent disease or the like. That is, the present invention provides a fused heterocyclic derivative represented by the following general formula (I), a pharmaceutical composition containing the same, a medicinal use thereof and the like. In the formula (I), ring A represents 5-membered cyclic unsaturated hydrocarbon or 5-membered heteroaryl; RA represents halogen, alkyl, alkenyl, alkynyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like ; ring B represents aryl or heteroaryl; RB represents halogen, alkyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like; E1 and E2 represent an oxygen atom or the like; U represents a single bond or alkylene; X represents a group represented by Y, —SO2—Y, —O—(alkylene)—Y, —O—Z in which Y represents Z, amino or the like; Z represents cycloalkyl, heterocycloalkyl, aryl, heteroaryl or the like; or the like.

The presently-disclosed subject matter relates to compounds of the formula: and methods for use thereof. The presently-disclosed subject matter relates methods of selectively differentiating a stem cell, and methods of screening for compounds useful for enhancing terminal differentiation of committed cardiac progenitor cells.

The present invention is related to methods for the preparation of pharmaceutically acceptable salts of (+)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(methanesulfonyl-methyl-amino)-pyrimidin-5-yl]-(3R,5S,6E)-dihydroxy-hept-6-enoic acid, intermediates thereof and methods for producing said intermediates.

A composite sheet of the present invention comprises an oxetane-epoxy-based compound, represented by chemical formula 1, as a binder.

Disclosed are oil-extended olefin block copolymer compositions with precipitated silica. The precipitated silica reduces oil-bleed while maintaining composition softness.

The object of the present invention is to provide an intermediate film for laminated glass which prevents reductions of transparency and appearance property caused by permeation of moisture and water. The above object is attained by the present invention, i.e., a composition for forming an intermediate film for a laminated glass which comprises ethylene-vinyl acetate copolymer and a compound having alkyleneoxy group. The composition of the present invention enables the formation of an intermediate film for a laminated glass that restrains white spots from occurring by the permeation of moisture and water.

Polyamide molding materials for transparent molding parts. The materials comprise transparent copolyamides that contain: (A) 40 to 100 wt % of at least one transparent copolyamide with a glass transition temperature (Tg) of at least 80° C. and not more than 150° C., composed of at least two diamines that are different from each other, wherein the at least two diamines are a mixture of (a) 50 to 90 mol % bis-(4-amino-3-methylcyclohexyl)methane (MACM) and/or bis-(4-amino-3-ethylcyclohexyl)methane (EACM) and/or bis-(4-amino-3,5-dimethylcyclohexyl)methane (TMACM) and b) 10 to 50 mol % aliphatic diamine having 9 to 14 carbon atoms, in particular decandiamine, particularly preferably at least 20 mol % decandiamine, each relative to the total amount of diamines, and of one or more aliphatic dicarboxylic acids, having 6 to 36 carbon atoms, (B) 0 to 60 wt % of at least one further polymer, (C) 0 to 10 wt % of additives, the sum of the components (A), (B) and (C) totaling 100% by weight.

Composite material that contain epoxy resin which is toughened and strengthened with thermoplastic materials and a blend of insoluble particles. The uncured matrix resins include an epoxy resin component, a soluble thermoplastic component, a curing agent and an insoluble particulate component composed of elastic particles and rigid particles. The uncured resin matrix is combined with a fibrous reinforcement and cured/molded to form composite materials that may be used for structural applications, such as primary structures in aircraft.

Formulations comprising an isosorbide-modified unsaturated polyester comprising maleic acid, fumaric acid, itaconic acid or maleic anhydride and isosorbide and one or more low profile additives. The formulations exhibit better shrink control in molding compound formulations with standard low profile additives than their non-isosorbide-modified analogues. These isosorbide-modified unsaturated polyester resins may be applied in molding compounds like sheet molding compounds or bulk molding compounds and may be components of fiber reinforced composites or other composite materials.

The invention relates to radiation curable coating systems on the basis of aqueous polyurethane dispersions, to a method for the production thereof, to the use of the coating systems as paints and/or adhesives, and to objects and substrates provided with said paints and/or adhesives.

Disclosed is an adhesive for a polarizing plate that comprises a polyvinyl alcohol-based resin with an acetoacetyl group and an amine-based metal compound crosslinking agent, and a method of manufacturing the same.

Injection molded articles and process of forming the same are described herein. The processes generally include providing a polyolefin including one or more propylene heterophasic copolymers, the polyolefin having an ethylene content of at least 10 wt. % based on the total weight of the polyolefin; contacting the polyolefin with a polylactic acid and a reactive modifier to form a compatiblized polymeric blend, wherein the reactive modifier is produced by contacting a polypropylene, a multifunctional acrylate comonomer, and an initiator under conditions suitable for the formation of a glycidyl methacrylate grafted polypropylene (PP-g-GMA) having a grafting yield in a range from 1 wt. % to 15 wt. %; and injection molding the compatibilized polymeric blend into an article.

The present invention relates to a solid composition containing calcium silicate hydrate and at least one water-swellable polymer which can form a hydrogel, and also to a process for preparing the composition, to the use thereof as a setting accelerator, and as a grinding aid in cement production. It also relates to building material mixtures which comprise the compositions.

A rubber composition for manufacturing tyres is based on one or more diene elastomers, one or more reinforcing fillers, and a vulcanization system. The vulcanization system includes one or more 1,2,4-triazine compounds chosen from compounds of formula I and compounds of formula II: Certain specific 1,2,4-triazine derivatives are described.

An aqueous dispersion includes particles at least partially encapsulated in a microgel where the microgel is prepared from a hyperbranched acrylic polymer. In addition, a method for making an aqueous dispersion includes: (1) mixing in an aqueous medium: (a) particles, (b) at least one ethylenically unsaturated monomer, and (c) a water-dispersible hyperbranched acrylic polymer having ethylenic unsaturation; and (2) polymerizing the at least one ethylenically unsaturated monomer and water-dispersible hyperbranched acrylic polymer having ethylenic unsaturation to at least partially encapsulate the particles in a microgel.

A primer solution for enhanced adhesion to a rigid substrate for aviation and aerospace applications includes an aminosilane-capped polyurethane prepolymer and a first solvent. The first solvent reacts with or modifies the surface of the rigid substrate, enabling the primer solution including the aminosilane-capped polyurethane prepolymer to become a part of the surface of the rigid substrate.

Disclosed are polymeric compositions with improved breakdown strength. The polymeric compositions contain a polyolefin and a voltage stabilizing agent. The voltage stabilizing agent contains a triazine. The triazine may include a substituent that enables keto-enol tautomerism, which provides the voltage stabilizing agent with additional energy dissipation capacity. The present polymeric compositions exhibit improved breakdown strength when applied as an insulating layer for power cable.

The present invention pertains to an additive combination comprising at least two sterically hindered amines, at least one further stabilizer, a dispersing agent and a plasticizer. The present invention also pertains to a composition comprising an organic material susceptible to degradation by light, oxygen and/or heat, and the additive combination and to the use and the process for stabilizing organic material against degradation by light, oxygen and/or heat by the additive combination.

The present invention is directed at a binder for a battery electrode comprising an ethylene oxide-containing copolymer including a first monomer of ethylene oxide (EO) and at least one additional monomer selected from an alkylene-oxide that is different from the first monomer of EO, an alkyl glycidyl ether, or a combination thereof; wherein the ethylene oxide-containing copolymer has a weight average molecular weight less than about 200,000 g/mole (e.g., from about 10,000 to about 100,000), the molar fraction of the first monomer of EO (XEo) in the ethylene oxide-containing copolymer is greater than 0.80 (e.g., from about 0.80 to about 0.995), and the ethylene oxide-containing copolymer has a peak melting temperature (Tp), in ° C., for a selected XEO in the range of about 0.80 to about 0.995, which is below a maximum value of Tpmax, at the selected XEO, which is calculated using the equation Tpmax=(60−150 (1−XEO)).

Non water-soluble polymers with a comb structure and a (meth)acrylic skeleton on which are grafted side chains containing at least one hydrophobic monomer of the styrene or (meth)acrylic ester type on C1 to C4, and at least one hydroxy or methoxy polylakylene glycol monomer. The levels of monomers are such that the polymer is amphiphilic because it is both rich in hydrophobic monomer and polylakylene glycol monomer. These products, used in paper coating dispersions, enable an increase in their Brookfield™ viscosity, a reduction in their ACAV viscosity, and an improvement in their water retention, which makes them particularly well suited for dry extract and/or high deposit speed coatings.

A platinum complex having the following formula (I) is disclosed, ##STR1## wherein R1 and R2 may be the same or different and each independently represents a methyl group or an ethyl group, and the configuration of 1,2-diaminocyclohexane is either cis-, trans-l-, trans-d-, or trans-dl-.The compound possess excellent antitumor activity with a high therapeutic index and abundant water solubility, and thus are effective as an antitumor agent.

The invention relates 6-acyl-(6H)-dibenz[c,e][1,2]oxaphosphorin-6-oxides of the formula ##STR1## wherein each of R1, R2 and R3 may be present one or more times and R1, R2 and R3 represent halogen having an atomic number of from 9 to 35, alkyl or alkoxy each having from 1 to 6 carbon atoms and wherein Ar represents an aromatic hydrocarbon group having from 6 to 10 carbon atoms.The invention further relates to a process for the preparation of the afore-mentioned compounds and polymerizable compositions containing them as an essential ingredient as a photo-initiator. Finally the invention relates to 6-alkoxy-(6H)-dibenz[c,e][1,2]oxaphosphorin of the formula II ##STR2## wherein each of R1 and R2 may be present once or more times and R1 and R2 represent halogen having an atomic number of from 9 to 35, alkyl or alkoxy each having from 1 to 6 carbon atoms, at least one R1 being, however, halogen and wherein R4 represents alkyl having from 1 to 6 carbon atoms.

Beta-lactamase inhibiting compounds of the formula ##STR1## or a pharmaceutically acceptable acid addition or carboxylate salt thereof; where n is zero, 1 or 2; X3 is H or Br, R1 is H, the residue of certain carboxy-protecting groups or the residue of an ester group readily hydrolyzable in vivo; one of R12 and R13 is H and the other is vinyl, certain aryl, alkylthio, alkylsulfonyl or certain heterocyclyl, aminomethyl, thiocarboxyamido or amidino groups; one of R2 and R3 is H and the other is as disclosed for the other of R12 and R13, or is Cl or CH2 OH, and R18 is H or certain acyl groups; intermediates useful in their production, methods for their preparation and use, and pharmaceutical compositions containing them.

1,4-Dihydropyridine-3-carboxylate derivatives are produced having vasodilating and hypotensive action.

A glycerol derivative which is effective to reduce blood pressure and has the formula: ##STR1## wherein R1 is an alkyl group having 10-22 carbon atoms, R2 is a lower acyl group or benzoyl, each of R3 and R4 independently is hydrogen or a straight or branched chain alkyl group having 1-6 carbon atoms; each of R5, R6 and R7 independently is hydrogen, a straight or branched chain alkyl group having 1-6 carbon atoms, an aryl group or an aralkyl group; and each of m and n independently is 0 or a positive integer under the condition of m+n=2-8.

The present invention relates to novel heterocycle-substituted diphosphonic acids, and the pharmaceutically-acceptable salts and esters thereof, in which the diphosphonate-substituted carbon atom moiety is attached to a carbon atom in a nitrogen-containing six membered ring heterocycle, preferably a piperidine ring. The heterocycle-substituted diphosphonic acid compounds have the general structure: ##STR1## wherein Z is a nitrogen-containing six membered ring heterocycle moiety selected from piperidinyl, diazinyl and triazinyl; m, n and m+n are from 0 to 10; Q is a covalent bond or a moiety selected from oxygen, sulfur or nitrogen; and R1, R2, R3 and R4 are substituent groups.The present invention further relates to pharmaceutical compositions containing these novel compounds. Finally this invention relates to methods for treating or preventing diseases characterized by abnormal calcium and phosphate metabolism by utilizing a compound or pharmaceutical composition of the present invention.

Herbicidally active 5-amino-1-phenyl-pyrazoles, most of which are new, of the formula ##STR1##

The invention relates to a process for the preparation of oligonucleotides by the following steps: reaction of a nucleoside with a phosphine derivative, reaction of the nucleotide derivative thus obtained with a nucleoside bonded to a polymeric carrier, oxidation of the carrier-bound nucleoside-nucleotide thus obtained with formation of phosphotriester groups, blocking of free primary 5'--OH groups, elimination of a protective group from the terminal 5'--OH group, where appropriate single or multiple repetition of the abovementioned steps to introduce further nucleoside phosphate or oligonucleoside phosphate units, and cleavage of the nucleoside-carrier bond and, where appropriate, elimination of all protective groups present in the oligonucleoside phosphates. The phosphine derivative used is a compound of the general formula III ##STR1## in which X and L can react with OH groups of the sugar units in the oligonucleotides, and R3 is a protective group which can be liberated by β-elimination.

Carbohydrate substituted dibenzo[d,g][1,3,2]dioxaphosphocin compounds of formula I ##STR1## where A is a carbohydrate residue are effective stabilizers for polymers processed at elevated temperatures and subject to thermal or oxidative degradation.

Carbohydrate substituted dibenzo[d,f][1,3,2]dioxaphosphepin compounds of formula I ##STR1## where A is a carbohydrate residue are effective stabilizers for polymers processed at elevated temperatures and subject to thermal or oxidative degradation.

Antivirally active compounds of formula (I), wherein R1 is hydrogen, hydroxy, mercapto or amino; R2 is hydrogen, hydroxy, fluoro, chloro or amino; R3 and R4 are independently selected from (II), (III), amino, hydroxy or an ether or ester residue thereof, or R3 together with R4 is (IV), wherein M is hydrogen or a pharmaceutically acceptable counterion; and n is 1 or 2; with the proviso that, when R2 is amino and R3 and R4 are hydroxy, R1 is not hydroxy and in addition, when n=1, R1 is not hydrogen, and pharmaceutically acceptable salts thereof; processes for preparation of said compounds, a pharmaceutical composition comprising said compounds, methods for treatments of virus infections as well as use of compounds of formula (I) without the proviso for the manufacture of a medicament for treatment of AIDS. ##STR1##

A method of producing a bis(2-carboxyethyl)-alkyl phosphine oxide represented by the following general formula (1) is disclosed. ##STR1## The method comprises the following Steps 1-4: step 1 wherein phosphine is reacted with acrylonitrile to produce bis(2-cyanoethyl)phosphine and then, in step 2, reacted with an alkene to produce a bis(2-cyanoethyl)alkyl phosphine, and in step 3, reacted with an oxidizing agent to produce a bis(2-cyanoethyl)alkyl phosphine oxide, and in step 4, said bis(2-cyanoethyl)alkyl phosphine oxide is reacted with water or a lower alcohol to give a bis(2-carboxyethyl)alkyl phosphine oxide or a derivative thereof.

Catalyst compositions comprising metallocene complexes having polymerisable olefinic groups substituent on an organic group containing a cyclopentadienyl nucleus may be used for the preparation of polyolefins. The catalyst compositions may be in the form of polymers comprising the metallocene complex and may be suitably supported on inorganic supports. Polymers having a broad range of density and melt indices as well as low hexane extractables and excellent powder morphology and flowability may be obtained by use of the catalyst compositions. Preferred metallocene complexes are zirconium complexes in which the polymerisable olefinic group is vinyl.

A method of treating hepatitis virus infection is disclosed. The method comprising administering to a human subject in need of such treatment an effective hepatitis virus-combatting amount of an alkyl lipid or alkyl lipid derivative.

A class of pyridine phosphonate compounds is disclosed that are useful as ligands in the one manufacture of oxidation-reduction catalysts. In particular, pyridine-2,6-disphosphonic acid is a specie of the pyridine phosphonate ligands that can be combined with a polyvalent metal to produce a catalyst to convert hydrogen sulfide to solid sulfur.

A method of treating hepatitis virus infection is disclosed. The method comprising administering to a human subject in need of such treatment an effective hepatitis virus-combatting amount of an alkyl lipid or alkyl lipid derivative.

Metallocene compounds having two fluorenyl ligands bridged with a single silicon or germanium atom, said atom having two substituent groups containing a total of at least four carbon atoms, are useful as catalyst components for the polymerization of olefins. Particularly, it is possible to prepare high molecular weight atactic polypropylene with improved yields with respect to the known catalysts.

Disclosed is a process for preparing bridged Group 4 metal complexes containing a neutral diene ligand starting from the corresponding novel, metal diene containing complexes by reaction thereof with the divalent derivative of a bridged bidentate ligand compound. The novel, intermediate metal diene complexes, their formation from tetravalent metal salts and an integrated process combining both process steps are claimed.

Metal complexes useful as components of addition polymerization catalysts are prepared by oxidizing Group 4 or Lanthanide metal containing complexes using an organic halide oxidizing agent in a unique one electron oxidation.

Methods for removing parasites and in particular ectoparasites of vertebrates, in particular of mammals, and compositions for the implementation of this method.Methods for removing parasites of vertebrates, and in particular arthropods, mainly insects and Arachnida, wherein an effectively parasiticidal amount of a compound of formula (I) ##STR1## in particular of fipronil, is administered to the animal via an administration route which makes possible systemic distribution and good absorption.

A metallocene compound is provided wherein to a transition metal compound is bonded a multidentate compound wherein a substituted cycloalkadienyl ring CA1 having therein a heteroaromatic group Ra containing an oxygen, sulfur or nitrogen atom on a cycloalkadienyl ring, preferably the five-membered ring thereof, and an unsubstituted or substituted cycloalkadienyl group CA2 or --(R1)N--, --O--, --S-- or --(R1)P--, preferably CA2, more preferably a substituted cycloalkadienyl group identical with CA1 are bonded through a divalent linking group. The metallocene compound is suitable as a principal ingredient of a catalyst for the polymerization of olefins, particularly achieving a very high effect in making the molecular weight of a polypropylene higher.

The invention provides an improved process for the synthesis of compounds carrying at least one phosphate group, especially polyalkylene glycol phosphate compounds, said process comprising the steps of: (a) reacting a compound containing at least one primary alcohol moiety with a diaryl- or diaralkyl-halophosphate whereby to form the corresponding diaryl- or diaralkyl-phosphate ester; (b) reductively cleaving the resulting product; and (c) if desired, repeating steps (a) and (b) with the product of step (b) whereby to produce a compound carrying two or more phosphate groups. Advantages of the process in accordance with the invention are that this avoids the production of by-products and results in products which are low in impurities. Also provided are novel diaryl- and diaralkyl-phosphate ester compounds, in particular polyethylene glycol diphenylphosphate ester and derivatives thereof.

A process to prepare an improved fluid rare earth phosphate catalyst composition useful in preparing alkylene oxide adducts of organic compounds having active hydrogen atoms is provided. The catalyst is prepared by dissolving a rare earth salt in a C9-C30 active hydrogen containing organic compound and then adding phosphoric acid to the organic compound rare earth mixture.

This invention relates to a composition comprising antimony trifluoride and silica, a method for the preparation of said composition and use of said composition as a catalyst in a process for the oxidation of cyclohexanone to ε-caprolactone.

The preparation of phosphorescent metalloporphyrin labelling reagents and their use for preparation of phosphorescent conjugates with biomolecules. The labelling reagents obtainable are water soluble monofunctional derivatives of Pt- and Pd-coproporphyrins, where the term “monofunctional” refers to the number of reactive groups in the porphyrin moiety.