Abstract: Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

Abstract: An object of the present invention is to provide a base generator which has sensitivity and is applicable to a wide range of applications, and a photosensitive resin composition which is applicable to a wide range of applications due to the structure of a polymer precursor in which reaction into a final product is promoted by a basic substance or by heating in the presence of a basic substance. The base generator generates a base by exposure to electromagnetic radiation and heating. The photosensitive resin composition comprises a polymer precursor in which reaction into a final product is promoted by the base generator and a basic substance or by heating in the presence of a basic substance.

Abstract: Provided is a new photochemical process for preparing artemisinin. Also provided are certain dihydroartemisinic acid derivatives useful for preparing artemisinin.

Abstract: The invention relates to the use of di-aspirin (bis(2-carboxyphenyl)succinate) and its derivatives in the treatment of colon and colorectal cancer. It also relates to novel derivatives of di-aspirin and to a method of synthesis of the di-aspirin and its derivatives.

Abstract: A printing or coating composition has a non-volatile liquid vehicle carrying a conductive polymer to be deposited on a substrate and is cleavable by heat or acidification without decomposition of said material, cleavage of said vehicle producing decomposition products that are more volatile than said vehicle and which can be evaporated to dry the composition. Suitably, that vehicle is a carbonic acid diester or a malonic acid diester, e.g. of the formula: wherein R2 is an organic substituent such that R2—OH is a volatile alcohol; R1 is an aliphatic or aromatic substituent of more than three carbon atoms such that is volatile; and R3 is C1-3 alkyl.

Abstract: It comprises compounds which are derived from a drug or a substance with therapeutic properties, and useful as reagents for the synthesis of biostable polymers including said drug in their backbone, namely polyurethanes, polyureas or polyurea urethanes that are biocompatible and biostable. It also comprises the processes for preparing the compounds and the polymers, as well as to the use of these polymers for the manufacture of medical devices.

Abstract: The present invention describes a series of therapeutically active compounds of formula I, X—Y—Z??(I) that are useful for treating a disorder in a mammal. In the formula I, X and Z, which may be same or different, are independently selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted heterocyclic group or substituted or unsubstituted heterocyclylalkyl; and Y is a linker selected from —O—, —S—, —NH—, —(CH2)n—, —CO—, —CONRa—, —NRaCO—, —NRaCOO—, —COO—, —CONRaCO—, —CONRaCOO— and —COOCOO—.

Abstract: Novel fenicol compounds having useful properties as antibiotic prodrugs, are provided, together with methods of making and using these new compounds.

Abstract: A new family of therapeutics which provides a controlled-release delivery platform for non-steroidal anti-inflammatory agents on an ester or an ester-carbonate backbone is disclosed herein. These agents are reversible inhibitors of acetylcholinesterase and are thus useful for clinical conditions benefiting from inflammation suppression and cholinergic intervention. These compounds are of the general formula wherein n=0, 1; X?C, Si, and N+ and NSAID=ibuprofen, naproxen, indomethacin and diclofenac. Other embodiments are also disclosed.

Abstract: A method of treating an ocular surface disorder in a subject in need of such treatment is provided. The method includes exposing conjunctival tissue of the subject to an effective amount of a vasopermeability agent that increases conjunctival vascular permeability. In some embodiments, the agent is a nitric oxide donor, which may be in a sustained release form. A method of screening a substance for treating an ocular surface disorder is also provided.

Abstract: A process for preparing compounds of the formula (I) in which R1 and R2 are as defined in the description.

Abstract: A compound of the present invention is represented by the formula (A); wherein R1 represents a hydrogen atom or a C1 to C6 alkyl group; Z1 represents a single bond, —CO—O—* or —CO—O—(CH2)k—CO—O—*; Z2 represents a single bond, *—O—CO—, *—CO—O—, *—O—(CH2)k—CO—, *—CO—(CH2)k—O—, *—O—(CH2)k—CO—O—, *—O—CO—(CH2)k—O— or *—O—CO—(CH2)k—O—CO—; k represents an integer of 1 to 6; * represents a binding position to W; W represents a C4 to C36 (n+1) valent alicyclic hydrocarbon group or a C6 to C18 (n+1) valent aromatic hydrocarbon group, one or more hydrogen atoms contained in the alicyclic hydrocarbon group and the aromatic hydrocarbon group may be replaced by a halogen atom, a C1 to C12 alkyl group, a C1 to C12 alkoxy group, a C2 to C4 acyl group or —OR10; R10 represents a hydrogen atom or a group represented by the formula (R2-2); R2 represents a hydrogen atom, a group represented by the formula (R2-1) or (R2-2); n represents an integer of 1 to 3; R4, R5 and R6 independently represent a C1 to C12 hydrocarbon group

Abstract: The present invention relates to a process for preparing compounds of general formula I wherein R1 and R2 are defined as in claim 1, the pharmaceutically acceptable salts and the solvates thereof, which may be prepared starting from compounds of general formula II wherein R1 is defined as in claim 1.

Abstract: A compound of formula (I), their use as precursors and a method of their production wherein n, Y, R, R2, R3, and R4 has the same meaning as given in the specification.

Abstract: A method for forming a monomeric carbonate includes the step of combining a monofunctional alcohol or a difunctional diol with an ester-substituted diaryl carbonate to form a reaction mixture. Similarly, a method for forming a monomeric ester includes the step of combining a monofunctional carboxylic acid or ester with an ester-substituted diaryl carbonate to form a reaction mixture. These methods further include the step of allowing the reaction mixtures to react to form a monomeric carbonate or a monomeric ester, respectively.

Abstract: The present invention provides propofol prodrugs, methods of making propofol prodrugs, pharmaceutical compositions of propofol prodrugs and methods of using propofol prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as migraine headache pain and post-chemotherapy or post-operative surgery nausea and vomiting.

Abstract: Prodrugs of propofol, methods of making prodrugs of propofol, pharmaceutical compositions of prodrugs of propofol and methods of using prodrugs of propofol and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as migraine headache pain and post-chemotherapy or post-operative surgery nausea and vomiting are disclosed herein.

Abstract: Disclosed herein is a compound having a structure: Therapeutic methods, compositions, and medicaments relating thereto are also disclosed.

Abstract: A process for forming a resist pattern comprises the steps of applying on a substrate to form a photosensitive resist layer a photosensitive composition comprising at least one photosensitive compound having, in the molecule, two or more structural units represented by C6R2-6—CHR1—OR7 or C6R2-6—CHR1—COOR7 where R1 is a hydrogen atom or an alkyl group, at least one of R2, R3, R4, R5, and R6 is a nitro group, and others are selected from the group consisting of a hydrogen atom, a halogen atom, an alkyl, an alkoxy, a phenyl, a naphthyl, and an alkyl in which a part or the entire of hydrogen atoms are substituted by a fluorine atom, and R7 is a substituted or unsubstituted phenylene or naphthylene group dissolved in an organic solvent, irradiating the resist layer selectively with a radiation ray, and developing a portion irradiated by the ray to form a pattern of the resist layer.

Abstract: The invention relates to compounds of the general formula wherein Ar1, Ar2, R4, R5, R6, R7, R8, W, X, a and b have the significances given in the specification, and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling parasites on warm-blooded animals.

Abstract: Novel fenicol compounds having useful properties as antibiotic prodrugs, are provided, together with methods of making and using these new compounds.

Abstract: A compound of Formula I, providing tetrapartate prodrugs is provided wherein: L1 is a bifunctional linking moiety; D is a moiety that is a leaving group, or a residue of a compound to be delivered into a cell; Z is covalently linked to [D]y, wherein Z is selected from the group consisting of: a moiety that is actively transported into a target cell, a hydrophobic moiety, and combinations thereof, Y1, Y2, Y3 and Y4 are each independently O, S, or NR12; R11 is a mono- or divalent polymer residue; R1, R4, R9, R10 and R12 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls and substituted C1-6 heteroalkyls; R2, R3, R5 and R6 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C1-6 alkoxy, phenoxy, C1-8 heteroalkyls, C1-8 heteroalkoxy, substituted C1-6 alkyls, C3-8 cycloalkyls, C

Abstract: Methods and compositions to activate a genetically designated target cell (or population of target cells) artificially, in vivo or in vitro, employ triggering of heterologous stimulus-gated ion channels to activate the cells. The stimulus-gated ion channels are suitably TRPV1, TRPM8 or P2X2. A stimulus which leads to opening or “gating” of the ion channel can be a physical stimulus or a chemical stimulus. Physical stimuli can be provided by heat, or mechanical force, while chemical stimuli can suitably be a ligand, such as capsaicin for TRPV1 or ATP for P2X2, or a “caged ligand,” for example a photolabile ligand derivative, in which case a physical signal in the form of light is used to provide the chemical signal. Selective activation of the cell may be used for various applications including neuronal and neuroendocrine mapping and drug screening.

Abstract: High yields of ester-substituted diary carbonates such as bis-methyl salicyl carbonate were obtained by the condensation of ester-substituted phenols with phosgene in the presence of a phase transfer catalyst (PTC) and optionally a tertiary amine catalyst in a solvent free reaction system comprising an aqueous phase held at a pH of 8.3 or higher. The optimized conditions of the present invention use an excess of ester-substituted phenol relative to phosgene and high conversion of phosgene to ester-substituted diaryl carbonate is observed. The product ester-substituted diaryl carbonate may be conveniently isolated as a solid by filtration or as a liquid in which the excess ester-substituted phenols serves as solvent. The method represents an attractive route for the manufacture of bis methyl salicyl carbonate and ester-substituted diaryl carbonates generally. The ester-substituted diaryl carbonates are useful for the preparation and modification of polycarbonates.

Abstract: Serine carbonates of formula I are precursors for organoleptic compounds, masking agents and antimicrobial agents. Further they are alternative substrates for malodor producing enzymes. The symbols in formula I are defined in claim 1.

Abstract: Fungicidal compounds of formula (I): wherein W is CH3O.

Abstract: A method and catalyst system for economically producing aromatic carbonates from aromatic hydroxy compounds. In one embodiment, the present invention provides a method of carbonylating aromatic hydroxy compounds by contacting at least one aromatic hydroxy compound with oxygen and carbon monoxide in the presence of a carbonylation catalyst system that includes a catalytic amount of an inorganic co-catalyst containing lead and a catalytic amount of an inorganic co-catalyst containing titanium. In various alternative embodiments, the carbonylation catalyst system can include an effective amount of a palladium source and an effective amount of a halide composition. Further alternative embodiments can include catalytic amounts of various inorganic co-catalyst combinations.

Abstract: A method and catalyst system for producing aromatic carbonates from aromatic hydroxy compounds. In one embodiment, the method includes the step of contacting at least one aromatic hydroxy compound with oxygen and carbon monoxide in the presence of a carbonylation catalyst system having an effective amount of a manganese source in the absence of a Group VIII B metal source. In various alternative embodiments, the carbonylation catalyst system can include at least one inorganic co-catalyst, as well as a halide composition and/or a base.

Abstract: A method and catalyst system for producing aromatic carbonates from aromatic hydroxy compounds. In one embodiment, the method includes the step of contacting at least one aromatic hydroxy compound with oxygen and carbon monoxide in the presence of a carbonylation catalyst system having catalytic amounts of the following components: a Group VIII B metal source; a combination of inorganic co-catalysts including a copper source and at least one of a titanium source or a zirconium source; an onium chloride composition; and a base. Alternative embodiments include inorganic co-catalyst combinations of a lead source and at least one of a titanium source or a manganese source.

Abstract: A method and catalyst system for producing aromatic carbonates from aromatic hydroxy compounds. In one embodiment, the method includes the step of contacting at least one aromatic hydroxy compound with oxygen and carbon monoxide in the presence of a carbonylation catalyst system having an effective amount of an iron source in the absence of a Group VIII B metal source. In various alternative embodiments, the carbonylation catalyst system can include at least one inorganic co-catalyst, as well as a halide composition and/or a base.

Abstract: 1-phenyl-3-dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.

Abstract: 1-phenyl-3 -dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.

Abstract: Hydroxyaromatic compounds such as phenol are carbonylated with oxygen and carbon monoxide in the presence of a catalyst system comprising a Group VIIIB metal, preferably palladium; an iodide salt, preferably sodium iodide; and at least one organic bisphosphine such as 1,3-bis(diphenylphosphino)propane or 1,4-bis(diphenylphosphino)butane. The catalyst system also preferably contains a compound of cerium or lead.

Abstract: Hydroxyaromatic compounds such as phenol are carbonylated with oxygen and carbon monoxide in the presence of a catalyst system comprising a Group VIIIB metal, preferably palladium; an alkali metal or alkaline earth metal halide, preferably sodium bromide; and at least one sulfone such as sulfolane. The catalyst system also preferably contains a compound of another metal, preferably lead.

Abstract: A method and catalyst system for producing aromatic carbonates from aromatic hydroxy compounds. In one embodiment, the method includes the step of contacting at least one aromatic hydroxy compound with oxygen and carbon monoxide in the presence of a carbonylation catalyst system having catalytic amounts of the following components: a Group VIII B metal source; a combination of inorganic co-catalysts including a copper source and at least one of a titanium source or a zirconium source; an onium chloride composition; and a base. Alternative embodiments include inorganic co-catalyst combinations of a lead source and at least one of a titanium source or a manganese source.

Abstract: The method of the present invention comprises reaction of a gaseous mixture of oxygen and carbon monoxide with an aromatic hydroxy compound in the presence of a catalyst under controlled pressure, wherein the partial pressure of oxygen is optimized to effect increased yields at reduced overall pressure.

Abstract: A method and catalyst system for economically producing aromatic carbonates from aromatic hydroxy compounds. In one embodiment, the present invention provides a method of carbonylating aromatic hydroxy compounds by contacting at least one aromatic hydroxy compound with oxygen and carbon monoxide in the presence of a carbonylation catalyst system that includes a catalytic amount of an inorganic co-catalyst containing titanium. In various alternative embodiments, the carbonylation catalyst system can include an effective amount of a palladium source and an effective amount of a halide composition. Further alternative embodiments can include catalytic amounts of various inorganic co-catalyst combinations.

Abstract: A method and catalyst system for economically producing aromatic carbonates from aromatic hydroxy compounds. In one embodiment, the present invention provides a method of carbonylating aromatic hydroxy compounds by contacting at least one aromatic hydroxy compound with oxygen and carbon monoxide in the presence of a carbonylation catalyst system that includes a catalytic amount of an inorganic co-catalyst containing lead and a catalytic amount of an inorganic co-catalyst containing titanium. In various alternative embodiments, the carbonylation catalyst system can include an effective amount of a palladium source and an effective amount of a halide composition. Further alternative embodiments can include catalytic amounts of various inorganic co-catalyst combinations.

Abstract: An improved method for producing an aromatic carbonate by reacting an aromatic hydroxy compound, carbon monoxide and oxygen in the presence of a catalyst system comprising at least one of palladium or a palladium compound; at least one lead compound; at least one halide source; and at least one desiccant, wherein the ratio of equivalents of lead co-catalyst relative to equivalents of palladium catalyst is optimized to increase reaction rate, as well as to allow production of aromatic carbonate in an economically feasible continuous process.

Abstract: A method and catalyst system for producing aromatic carbonates from aromatic hydroxy compounds is disclosed. In one embodiment, the method includes the step of contacting at least one aromatic hydroxy compound with oxygen and carbon monoxide in the presence of a carbonylation catalyst system having an effective amount of an iron source as the primary catalyst component in the absence of a Group VIII B metal source. In various alternative embodiments, the carbonylation catalyst system can include at least one inorganic co-catalyst, as well as a halide composition and/or a base.

Abstract: A method and catalyst system for producing aromatic carbonates from aromatic hydroxy compounds is disclosed. In one embodiment, the method includes the step of contacting at least one aromatic hydroxy compound with oxygen and carbon monoxide in the presence of a carbonylation catalyst system having an effective amount of a nickel source as the primary catalyst component in the absence of a Group VIII B metal source. In various alternative embodiments, the carbonylation catalyst system can include at least one inorganic co-catalyst, as well as a halide composition and/or a base.

Abstract: Hydroxyaromatic compounds such as phenol are carbonylated with oxygen and carbon monoxide in the presence of a catalyst system comprising a Group VIII metal having an atomic number of at least 44, preferably palladium; an alkali metal or alkaline earth metal halide, preferably sodium bromide; at least one carboxylic acid amide such as N-methylpyrrolidone or dimethylacetamide; and a cocatalyst which is a compound of one or more metals including copper, titanium, zinc, lead, cerium and manganese.

Abstract: A method and catalyst system for producing aromatic carbonates from aromatic hydroxy compounds. In one embodiment, the method includes the step of contacting at least one aromatic hydroxy compound with oxygen and carbon monoxide in the presence of a carbonylation catalyst system having an effective amount of a manganese source in the absence of a Group VIII B metal source. In various alternative embodiments, the carbonylation catalyst system can include at least one inorganic co-catalyst, as well as a halide composition and/or a base.

Abstract: A method and catalyst system for producing aromatic carbonates from aromatic hydroxy compounds. In one embodiment, the method includes the step of contacting at least one aromatic hydroxy compound with oxygen and carbon monoxide in the presence of a carbonylation catalyst system having an effective amount of a cobalt source in the absence of a Group VIII B metal source. In various alternative embodiments, the carbonylation catalyst system can include at least one inorganic co-catalyst, as well as a halide composition and/or a base.

Abstract: A method and catalyst system for economically producing aromatic carbonates from aromatic hydroxy compounds. In one embodiment, the present invention provides a method of carbonylating aromatic hydroxy compounds by contacting at least one aromatic hydroxy compound with oxygen and carbon monoxide in the presence of a carbonylation catalyst system that includes a catalytic amount of an inorganic co-catalyst containing ytterbium. In various alternative embodiments, the carbonylation catalyst system can include an effective amount of a palladium source and an effective amount of a halide composition. Further alternative embodiments can include catalytic amounts of various inorganic co-catalyst combinations.

Abstract: A method and catalyst system for economically producing aromatic carbonates from aromatic hydroxy compounds. In one embodiment, the present invention provides a method of carbonylating aromatic hydroxy compounds by contacting at least one aromatic hydroxy compound with oxygen and carbon monoxide in the presence of a carbonylation catalyst system that includes a catalytic amount of an inorganic co-catalyst containing copper. In various alternative embodiments, the carbonylation catalyst system can include an effective amount of a palladium source and an effective amount of a halide composition. Further alternative embodiments can include catalytic amounts of various inorganic co-catalyst combinations.

Abstract: The invention relates to a process for the preparation of aromatic oligocarbonates from dihydroxy compounds, CO and O.sub.2 in the presence of a platinum metal catalyst, a cocatalyst, a quaternary salt and a base, which is carried out in an inert organic solvent which, under the reaction conditions, forms an azeotrope with water, and this azeotrope is removed from the reaction mixture.

Abstract: The present invention relates to compounds of the general formula I ##STR1## wherein A is a group of the formula ##STR2## and Z is an O or S atom, to the further processing thereof to form novel sec-amidoalkylcarbonic acid derivatives and to those sec-amidoalkylcarbonic acid derivatives.

Abstract: A method and catalyst system for economically producing aromatic carbonates from aromatic hydroxy compounds. In one embodiment, the present invention provides a method of carbonylating aromatic hydroxy compounds by contacting at least one aromatic hydroxy compound with oxygen and carbon monoxide in the presence of a carbonylation catalyst system that includes a catalytic amount of a combination of inorganic co-catalysts containing manganese and nickel; manganese and iron; manganese and chromium; manganese and cerium; manganese and europium; manganese, cerium, and europium; manganese, iron, and europium; or manganese and thorium. In various alternative embodiments, the carbonylation catalyst system can include an effective amount of a palladium source and an effective amount of a halide composition. Further alternative embodiments can include catalytic amounts of various other inorganic co-catalyst combinations.

Abstract: 1-phenyl-3-dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.