Abstract: The present invention relates to an improved process for the preparation of (1S,3S,5S)-242(S)-2-amino-2-(3-hydroxy-1-adamantan-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile and its intermediates.

Abstract: The present disclosure relates to surface-modified zirconia nanoparticles, methods for making and using the same, and high index of refraction films made therefrom. The provided zirconia nanoparticles are surface modified with ligands that include N-hydroxyurea functionalities. The provided ligands also can contain compatibilizing groups that allow the provided surface-modified zirconia nanoparticles to be incorporated into an organic matrix. High index of refraction films can be made using these organic matrices.

Abstract: The present invention relates to macrolactam compounds, intermediates useful in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing and modifying macrolactams. One use of the compounds and methods described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. An example of an HCV inhibitory compound that can be synthesized using the procedures described herein is Compound A and derivative thereof.

Abstract: A polyurethane or polyurea coating for use in protecting a leading edge substrate on an airfoil against liquid or solid particle erosion, the composition made from an isocyanate-terminated prepolymer and curing agents, such as polyaspartic esters, aldimines and ketimines with optional flatting agent for matte coatings.

Abstract: A polyether polyol composition comprising: a polyether polyol, a phosphoric acid compound selected from the group consisting of at least one of orthophosphoric acid, polyphosphoric acid, polymetaphosphoric acid, and partial esters thereof in an amount raning from 0.5 to 100 ppm based on the polyether polyol metals derived from a composite metal cyanide complex catalyst in an amount ranging from 1 to 30 ppm based on the polyether polyol; a method for producing this polyether polyol composition; and methods of making polyurethane or isocyanate group-terminated prepolymers.

Abstract: Peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH) are provided. The compounds can suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). Despite their relative inability to access brain and spinal cord, the compounds attenuate behavioral responses indicative of persistent pain in rodent models of inflammation and peripheral nerve injury, and suppresses noxious stimulus-evoked neuronal activation in spinal cord regions implicated in nociceptive processing. CBi receptor blockade prevents these effects. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the inhibition of peripheral FAAH would be of benefit. The compounds of the invention are according to the formula (I): in which R1 is a polar group. In some embodiments, R1 is selected from the group consisting of hydroxy and the physiologically hydro lysable esters thereof.

Abstract: A resist composition according to the present invention includes at least a base resin, a photoacid generator and a solvent, wherein the photoacid generator comprises a fluorine-containing sulfonic acid salt of the following general formula (4). In the formula, X independently represents a hydrogen atom or a fluorine atom; n represents an integer of 1 to 6; R1 represents a hydrogen atom, or an alkyl, alkenyl, oxoalkyl, aryl or aralkyl group; any of hydrogen atoms on carbons in R1 may be substituted with a substituent; R2 represents RAO or RBRCN; and A represents a divalent group. This fluorine-containing sulfonic acid salt can serve as a photoacid generator having high solubility in a resist solvent and thus can suitably be used for a resist composition such that the resist composition shows high resolution, wide DOF, small LER and high sensitivity to form a good pattern shape in lithographic processes.

Abstract: The invention relates to addition compounds which are obtainable by reacting a) one or more polyisocyanates containing uretdione groups with b) one or more compounds of the formula (I) Y—(XH)n??(I) with the proviso that at least 50% of the free isocyanate groups of component a) are reacted with the compounds of the formula (I) to give an intermediate which contains uretdione groups, and subsequently the intermediate is reacted with c) one or more compounds of the general formula (II) Z—NHRm??(II) with the proviso that all free NCO groups optionally still present and at least 20% of uretdione groups originally used are reacted with Z—(NHR)m. The invention further relates to the use of the addition compounds as dispersants and dispersion stabilizers, and to a process for preparing them.

Abstract: A resist composition including a base component (A) which exhibits changed solubility in a developing solution, and an acidic compound component (J) which is decomposed by exposure to exhibit decreased acidity, wherein the acidic compound component (J) contains a compound represented by formula (J1) [in the formula, R1 represents H, OH, halogen atom, alkoxy group, hydrocarbon group or nitro group; m represents 0-4; n represents 0-3; Rx represents H or hydrocarbon group; X1 represents divalent linking group; X2 represents H or hydrocarbon group; Y represents single bond or C(O); A represents alkylene group which may be substituted with oxygen atom, carbonyl group or alkylene group which may have fluorine atom; Q1 and Q2 represents F or fluorinated alkyl group; and W+ represents primary, secondary or tertiary ammonium coutercation which exhibits pKa smaller than pKa of H2N+(X2)—X1—Y—O-A-C(Q1)(Q2)—SO3? generated by decomposition upon exposure].

Abstract: A phenyl alkyl carbamate derivative compound and a pharmaceutical composition containing the compound are provided. More specifically, the phenyl alkyl carbamate derivative compound and a pharmaceutically acceptable salt thereof, a composition for muscle relaxation containing the phenyl alkyl carbamate derivative compounds and/or pharmaceutically acceptable salt thereof as an active ingredient, and a method of muscle relaxation comprising administering a pharmaceutically effective amount of the phenyl alkyl carbamate derivative compound and/or a pharmaceutically acceptable salt thereof to a subject in need of to a subject in need of, are provided.

Abstract: The present invention relates to the cosmetic, dermatological or therapeutic use of certain cyclohexyl carbamate compounds of formula (I) given below, preferably as skin and/or hair lightening (whitening) actives. The invention further relates to compositions and cosmetic, dermatological or therapeutic products comprising one or more compounds of formula (I) suitable for lightening human skin and/or hair and corresponding methods.

Abstract: A prepolymer system has a monomeric isocyanate content of no greater than about 10% by weight based on 100 parts by weight of the prepolymer system. The prepolymer system comprises a diluent component and a prepolymer component different than and separate from the diluent component. The diluent component has an excess of isocyanate (NCO) functional groups, and comprises the reaction product of a monohydric isocyanate-reactive component and an excess of a first isocyanate component. The first isocyanate component comprises monomeric isocyanates reactive with the monohydric isocyanate-reactive component. The prepolymer component also has an excess of NCO functional groups, and comprises the reaction product of a polyol component and an excess of a second isocyanate component. The prepolymer system can be used to prepare foams via reaction with water. The foams have low density and have excellent adhesion and sound dampening properties for use in cavities of automobile bodies.

Abstract: The present invention relates to the cosmetic, dermatological or therapeutic use of certain cyclohexyl carbamate compounds of formula (I) given below, preferably as anti-cellulite actives.

Abstract: The present invention pertains to a novel method for preparing a carbamate, in which the method comprises reacting an aliphatic substituted urea and/or its derivatives, with a hydroxyl group containing compound to obtain a carbamate. In addition, the present invention provides a novel catalyst which is suitable for catalyzing the reaction to form a carbamate, and a method for preparing the novel catalyst. The method of the present invention for preparing a carbamate does not involve the application of carbon monoxide which is toxic, and the reaction conditions are relatively mild with high catalytic activity, high reaction selectivity of the catalyst, and a relatively short reaction time. Furthermore, the catalyst is separated from the reaction system and reused easily, which will facilitates scale up and industrial application.

Abstract: The present invention relates to a process for preparing polyisocyanates by oligomerization of isocyanates.

Abstract: The present invention relates to a catalyst for the synthesis of organic carbonates, the preparation of the catalyst and the application of this catalyst in the synthesis of organic carbonates from reacting urea and hydroxyl group containing compounds. The catalyst provided in this invention is a calcinate of hydrous salt containing rare earth element at a moderate calcining temperature.

Abstract: The invention relates to a carbodiimide compound or mixture of carbodiimide compounds derived from a carbodiimidization reaction of at least one oligomer having at least one isocyanate group and comprising at least two repeating units deriving from one or more ethylenically unsaturated monomers.

Abstract: The present invention relates to a method for manufacturing an isocyanate group-terminated prepolymer, comprising the following steps (a) to (d): (a) a step of ring-opening polymerizing an alkyleneoxide-containing cyclic compound by using an initiator in the presence of a composite metal cyanide complex catalyst, thereby obtaining a polyol composition containing the catalyst; (b) a step of, without removal of the composite metal cyanide complex catalyst from the polyol composition obtained in the step (a), adding water and performing a heat treatment in a closed system; (c) a step of subjecting the hydrous polyol composition after the step (b) to a dehydration treatment; and (d) a step of adding a polyisocyanate compound to the polyol composition after the step (c) and subjecting to a reaction with the polyol in the polyol composition.

Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.

Abstract: A method of providing a patient with controlled release of tapentadol using a prodrug capable, upon enzymatic activation and intramolecular cyclization, of releasing tapentadol is disclosed. The disclosure also provides such prodrug compounds and pharmaceutical compositions comprising such compounds. Such pharmaceutical compositions can optionally include an enzyme inhibitor that interacts with the enzyme(s) to mediate the enzymatically-controlled release of tapentadol from the prodrug so as to modify enzymatic cleavage of the prodrug. Also included are methods to use such compounds and pharmaceutical compositions.

Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable, stereoisomers, salts or solvates thereof to methods for their synthesis, and use in the treatment of pain.

Abstract: The present disclosure relates to surface-modified zirconia nanoparticles, methods for making and using the same, and high index of refraction films made therefrom. The provided zirconia nanoparticles are surface modified with ligands that include N-hydroxyurea functionalities. The provided ligands also can contain compatibilizing groups that allow the provided surface-modified zirconia nanoparticles to be incorporated into an organic matrix. High index of refraction films can be made using these organic matrices.

Abstract: Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

Abstract: A process for oligomerizing isocyanates includes a step of continuous conversion of an isocyanate monomer into polyisocyanate containing carbamate and/or allophanate groups, in the presence of a catalyst, wherein the conversion step is carried out in a reactor having a specific heat exchange coefficient of greater than or equal to approximately 200 kW/m3/° C.

Abstract: The present invention provides addition compounds, which suitable as dispersants and as dispersion stabilizers, and to the salts of the said compounds. The invention further provides processes for preparing these addition compounds, to their use as dispersants and dispersion stabilizers for organic and inorganic pigments and also fillers in organic and aqueous systems, and to pulverous or fibrous solids coated with such dispersants and intended for incorporation into liquid systems.

Abstract: The present invention relates to a method of producing a carbamate compound, comprising reacting a fluorine-containing carbonic diester compound represented by formula (1) and a non-aromatic diamine compound represented by formula (2) without using a catalyst, to thereby produce a carbamate compound represented by formula (3), and a method of producing an isocyanate compound represented by formula (20) from the carbamate compound without using a catalyst, wherein R represents a fluorine-containing monovalent aliphatic hydrocarbon group, and A represents a divalent aliphatic hydrocarbon group, a divalent alicyclic hydrocarbon group or a divalent aromatic-aliphatic hydrocarbon group.

Abstract: A novel phenylcarbamate compound and a pharmaceutical composition containing the same are provided. More specifically, a novel phenylcarbamate compound, a composition for muscle relaxation containing the phenylcarbamate compound as an active ingredient, and a method of muscle relaxation comprising administering a therapeutically effective amount of the phenylcarbamate compound, are provided.

Abstract: Provided is an enantioselective, palladium-catalyzed method for the preparation of ?-amino-?,?-unsaturated carboxylic acid derivatives having the formulas II, III, VII and VIII:

Abstract: A novel bis-phosphate compound is provided which can be applied to a wide range of reactive substrates and reactions as an asymmetric reaction catalyst and can realize an asymmetric reaction affording a high yield and a high enantiomeric excess. The bis-phosphate compound has a tetraaryl skeleton represented by General Formula (1). In an asymmetric reaction, an amidodiene and an unsaturated aldehyde compound are reacted with each other in the presence of the optically active bis-phosphate compound to give an optically active amidoaldehyde. The invention allows a reaction such as an asymmetric Diels-Alder reaction to proceed efficiently, which has been difficult with conventional mono-phosphate compounds.

Abstract: Disclosed is a thickener based on an aqueous preparation of a nonionic, water-dispersible or water-soluble polyurethane, obtained by reacting: (a) hydrophilic polyols containing at least two OH groups and at least two functional groups selected from ether and ester, of molecular weight at least 300; (b) hydrophobic compounds containing at least one zerewitinoff-active hydrogen atom, of molecular weight about 100 to about 500, with at least one linear or branched, saturated or unsaturated alkyl chain having at least five consecutive carbon atoms not linked to a hetero atom; and (c) at least difunctional isocyanates, where the components are reacted in equivalent ratios OHa):ZHb):NCOc) of 1:(1+x):2(1+y), with the provisos that x is 0.05-1.2, y is (0.2-1.05)x, and more than one equivalent of NCOc) is present versus the sum of OHa) and ZHb).

Abstract: Compounds of Formula II wherein R1a is H; and R1b is C1-C6alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10 alkyl chain, C2-C4haloalkyl or —CH2C3-C7 cycloalkyl; R4? is C1-C6alkyl, C1-C6haloalkyl or oxetany-3-yl. for use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.

Abstract: To provide a method whereby a 2-azaadamantane can easily be obtained in good yield. A method for producing a 2-azaadamantane represented by the formula (1), which comprises cyclizing a compound represented by the following formula (2) in the presence of an acid.

Abstract: This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists.

Abstract: The present invention provides a dental material, a dental material composition and a dental restorative material that exhibit small polymerization shrinkage particularly during curing and are producible at low cost on the industrial scale. The dental material of the present invention includes a specific urethane (meth)acrylic compound represented by Formula (1) described below.

Abstract: The present invention provides a novel compound and a composition including the compound that exhibit small polymerization shrinkage particularly during curing and are producible at low cost on the industrial scale.

Abstract: A multi-component curable composition which is reactive upon admixing of the components and wherein the composition comprises: A. a first component which comprises: (i) a first amine functional adduct which comprises the reaction product of a stoichiometric excess of a diamine and a compound having an epoxide group and an alpha, beta unsaturated carbonyl group; B. a second component which comprises: (i) at least one compound having an average of more than 2.0 groups per molecule which are reactive with amines.

Abstract: A multi-component curable composition which is reactive upon admixing of the components and wherein the composition comprises a first component which comprises a first amine functional adduct and a second amine functional adduct; and a second component which comprises at least one compound having an average of more than 2.0 groups per molecule which are reactive with amines.

Abstract: The present disclosure relates to methods of synthesizing 1-(acyloxy)-alkyl carbamate prodrugs and to intermediates used in the methods.

Abstract: A one-component polyurethane composition includes at least one polyurethane prepolymer having terminal isocyanate groups which is prepared from at least one polyisocyanate and at least one polyol, and to at least one catalyst system which is obtainable from at least one bismuth compound and at least one aromatic nitrogen compound. The polyurethane composition may be used as an adhesive, sealant, coating or lining. Finally, catalysts for polyurethane compositions are disclosed which represent coordination compounds between bismuth and at least one aromatic nitrogen compound.

Abstract: Disclosed is an adamantanamine derivative which is useful as a significant intermediate of an 11?HSD-1 inhibitor. Disclosed is a compound represented by the formula (II): wherein R10 is a group represented by the formula: —(CR13R14)m-NR12—R11 or the like.

Abstract: Disclosed is a fluorinated sulfonic acid salt or fluorinated sulfonic acid group-containing compound having a structure represented by the following general formula (A). In the formula, n indicates an integer of 1 to 10; R indicates a substituted or unsubstituted C1-C20 linear, branched or cyclic alkyl group, a substituted or unsubstituted C1-C20 linear, branched or cyclic alkenyl group, a substituted or unsubstituted C6-C15 aryl group, or a C4-C15 heteroaryl group; and a indicates 1 or 0. A photoacid generator containing the above fluorinated sulfonic acid salt or fluorinated sulfonic acid group-containing compound shows high sensitivity to an ArF excimer laser or the like, presents no concerns about human body accumulation, can generate an acid (photoacid) of sufficiently high acidity, and exhibits high solubility in a resist solvent and good compatibility with a resist resin.

Abstract: Gabapentin enacarbil was prepared and purified from intermediates such as 1-haloalkyl carbamate or carbonate and diacid acetal skeleton. For example, a 1-haloalkyl carbonate or carbamate was prepared by combining a C1 to C10 alcohol or C1 to C10 primary amine, a solvent selected from the group consisting of: acetonitrile, C3 to C7 ketone, C5 to C10 ether, C2 to C7 ester, C5 to C10 hydrocarbon and a combination thereof; a 1-haloalkyl haloformate of the following formula: wherein each X is independently selected from Br, I, or Cl; R1 is alkyl or H; and a C6 to C21 tertiary amine.

Abstract: Three unique subtypes of N-hydroxyamides and N-hydroxycarbamates containing both the vanilloid moiety (4-hydroxy-3-methoxybenzyl) and a lipophilic aliphatic moiety. Also disclosed are direct syntheses of these vanilloid fatty hydroxamates. The compounds possess inhibitory activity against the enzymes fatty acid amide hydrolase (FAAH) and matrix metallo-proteinase 9 (MMP-9). In addition, these substances bind to the calcium channel protein TRPV1 and inhibit vesicant-induced inflammation in skin and cornea. The compounds have utility in treating topical or systemic inflammatory processes in the skin and/or eye.

Abstract: The invention provides a method for producing 2-azaadamantanes represented by formula (1) in good yields. The method includes cyclizing a compound represented by formula (2) in the presence of an acid.

Abstract: In one aspect, the present invention provides a composition of a covalent conjugate of a GABA analog with a drug. In another aspect, the present invention provides methods for treating pain and neurological disorders using the conjugates of GABA analogs.

Abstract: A process of producing a urethane (meth)acrylate monomer having a low acid value and a low content of a hardly soluble high-molecular weight impurity which is crosslinked high-dimensionally, comprising the steps of: (1) contacting a first solution containing a urethane (meth)acrylate monomer having an acid value of more than 0.2 mgKOH/g and an organic solvent to a water-containing adsorbent capable of adsorbing an acid component to obtain a second solution containing a urethane (meth)acrylate monomer having an acid value of not more than 0.2 mgKOH/g, the organic solvent and more than 5,000 ppm (mass) of water based on the urethane (meth)acrylate monomer; (2) contacting the second solution to a dehydrating agent to obtain a third solution containing not more than 5,000 ppm (mass) of water based on the urethane (meth)acrylate monomer; and (3) removing the organic solvent from the third solution.

Abstract: Tertiary non-vinylic carbamates of molecular weight less than 350 are useful as fragrance ingredients. A method of preparation is also described.

Abstract: Processes useful for the preparation of a Compound of Formula I: Formula (I). Intermediates useful for the preparation of the compound of Formula I, and processes useful for preparing said intermediates are disclosed.

Abstract: The invention provides a compound which is (a) an amino acid derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: wherein R1, R2, L1, Het, A, x, y and W are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.

Abstract: In one aspect, the invention relates to storage-stable and flowable polyurethane compositions comprising (a) one or more isocyanate-terminated polyurethane prepolymers derived from one or more hydrocarbon ring-containing diisocyanates and/or triisocyanates and one or more polyols; (b) one or more metal salt complexes of methylenedianiline; and (c) one or more organic acid halide compounds having one or more acid halide groups, wherein the one or more organic acid halide compounds are in an amount wherein the acid halide groups are present in a minimum concentration of about 100 parts per million by weight of the polyurethane prepolymer. In other aspects, the invention relates to methods for storing the curable polyurethane compositions, as well as methods for producing polyurethane elastomers.