Abstract: The present invention provides compounds having in their molecule a structure contributing to high hydrophilicity, and having high photopolymerizability, as well as polymers of such compounds, and a method for producing the compound. The compounds are diol (meth)acrylate having a urethane bond represented by the formula (1), and cyclic ketal (meth)acrylate having a urethane bond represented by the formula (2): (R1: H, —CH3; R2: —(CH2)n-; R3: —(CH2)m-; n: 1-4; m: 1-8; (AO): C2-C4 oxyalkylene group; x: 0-1000; R4, R5: H, —CH3, —C2H5).

Abstract: A method for forming cascade polymers specifically utilizing the amine monomer of the formula The monomer is made by initially reacting nitromethane and CH2?CHCO2— TBu by nucleophilic addition to form the triester nitrotrialkanoate of the formula and then reducing the nitrosubstituent to afford the said amine monomer.

Abstract: Acyloxyalkyl carbamate prodrugs of ?-amino acids, pharmaceutical compositions thereof, methods of making acyloxyalkyl carbamate prodrugs of ?-amino acids and methods of using acyloxyalkyl carbamate prodrugs of ?-amino acids, and pharmaceutical compositions thereof to treat a disease are disclosed. Acyloxyalkyl carbamate prodrugs of ?-amino acids suitable for oral administration using sustained release dosage forms are also disclosed.

Abstract: An organic polyisocyanate with at least one unsaturated functional group is capable of copolymerizing when exposed to actinic radiation. The polyisocyanate comprises structural units with the formula (1): wherein: X is an electron-attracting group; R1, and R2 are hydrogen atoms, a saturated or unsaturated aliphatic or cycloaliphatic radical, or an aromatic or araliphatic radical; and n is an integer from 0 to 5. A process for producing this polyisocyanate is also disclosed.

Abstract: The present invention discloses compounds of formula (I), their optical isomers or pharmaceutically acceptable salts thereof, their preparation and uses thereof, wherein the definitions of R1, R2, R3 and R4 are shown in the description. These compounds are optical isomers or racemic mixtures. After these compounds are uptaken, they are metabolically transformated in vivo into 1-[2-dimethylamino-1-(4-hydroxyphenyl)-ethyl]-cyclohexanol that has neuropharmacological activity, by interrupting reuptake of 5-hydroxytryptamine (5-HT) and/or norepinephrine (NA), which is used for treating diseases associated with central nerve system, such as depression, etc.

Abstract: Phase change ink carrier compositions comprising an admixture of (1) at least one urethane resin; and/or (2) at least one mixed urethane/urea resin; and/or (3) at least one mono-amide; and/or (4) at least one polyethylene wax are provided. In addition, a phase change colored ink of such carrier compositions comprising a phase change ink compatible colorant are also provided. Embodiments of the present invention also include methods for producing a layer of the above phase change colored ink on the surface of a substrate by either direct or indirect printing. Such methods also encompassing using a polyethylene wax as an overcoat layer above such a phase change ink layer on a printed substrate.

Abstract: The present invention includes insecticidal carbamates that are useful, for example, for the control of insects, such as mosquitoes, which can be used in applications where exposure to and/or contact with humans is likely. The insecticides of the present invention include phenyl N-methyl carbamates and compositions comprising them that exhibit species-selective inhibition of acetylcholinesterase (AChE) and are preferably toxic to mosquitoes but not humans. Of particular interest are compounds of Formula (I) and Formula (II): Compounds of Formula (I) and Formula (II) are especially suitable for insecticide treated nets and indoor residual spraying for mosquito control.

Abstract: The present invention provides novel (meth)acrylic and (meth)acrylamide monomers and polymers produced from those monomers. The monomers of the invention each include only a single vinyl functionality and at least one non-vinyl functionality that can be varied to achieve desired monomer/polymer properties. The invention additionally provides methods of producing polymers from these mono-vinyl monomers.

Abstract: The invention relates to a compound of formula (I): Wherein R1, R2, R3 and R4 are as defined herein. The invention also relates to methods of preparation of compounds of formula (I) as well as to their therapeutic application.

Abstract: A process for the preparation of (S)(+)-3-(aminomethyl)-5-methylhexanoic acid (pregabalin) of formula (I) or a salt thereof, comprising the reaction of a compound of formula (II) with an alcohol ROH, in the presence or absence of enzyme, to give a compound of formula (III) as herein defined the transformation of a compound of formula (III) into a compound of formula (VI) or (VIII) as herein defined, and the subsequent hydrolysis of a compound of formula (VI) or (VIII), to give pregabalin.

Abstract: The invention relates to a compound of formula (I): Wherein m, n, X, Y, R1, R2, R3 and R4 are as defined herein. The invention also relates to the use of same in therapeutics.

Abstract: The present invention provides a novel method for preparing a key intermediate, 3-amino-pentan-1,5-diol (2), which is useful for the preparation of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)-propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidine-7-one (1) a MAP-kinase inhibitor useful in the treatment of rheumatoid arthritis.

Abstract: The invention relates to a compound of formula (I): Wherein m, n, X, Y, R1, R2, R3 and R4 are as defined herein. The invention also relates to the use of same in therapeutics.

Abstract: A method of an enantioselective nucleophilic addition reaction to carbonyl, which enables an asymmetric synthesis of an optically active ?-hydroxy-?-keto acid ester, an optically active ?-hydroxy-?-amino acid ester, hydroxydiketone compounds, etc. being useful as a raw material or synthesis intermediate for producing a pharmaceutical preparation, an agricultural chemical, a fragrance, a functional polymer or the like. In this method, the nucleophilic addition reaction of enamide compound accompanied by hydroxyl (—OH) formation to carbonyl is carried out in the presence of a chiral catalyst with copper or nickel.

Abstract: The present invention provides an improved process for the preparation of carbamates with high selectivity of pharmaceutical interest by an eco-friendly, non-toxic, phosgene-/isocyanate-/CO-free clean route through a reaction of amine, organic halide compound and carbon dioxide in the presence of a solid, reusable catalyst at moderate conditions and does not require additional cocatalyst/promoter as well as solvent.

Abstract: Disclosed is crystalline ladostigil tartrate of a specified density, compositions, including pharmaceutical compositions comprising such ladostigil tartrate, and a process for the manufacture thereof.

Abstract: The invention relates to a process for producing carbamoyloxy (meth)acrylates which comprises transesterification of hydroxyalkyl carbamates with an (meth)acrylate of formula CH2?CR29—COOR30 wherein R29 is hydrogen or methyl and R30 represents an alkyl group comprising from 1 to 8 carbon atoms, in the presence of an organotitanate, an organozirconate catalyst or an organotin catalyst, the carbamoyloxy (meth)acrylates thereby obtained and their use in radiation curable compositions.

Abstract: Electron donor compounds, suitable for use as adhesives or as components in adhesives, contain a carbon to carbon double bond attached to an aromatic ring and conjugated with the unsaturation in the aromatic ring.

Abstract: The present invention concerns a process for producing low-viscosity polyisocyanates or secondary products thereof, which carry activated, radiation-curable double bonds and can optionally also cure thermally, and low-viscosity polyisocyanate mixtures or secondary products thereof and their use in coating compounds.

Abstract: The present invention provides an improved process for the preparation of carbamates with high selectivity of pharmaceutical interest by an eco-friendly, non-toxic, phosgene-/isocyanate-/CO-free clean route through a reaction of amine, organic halide compound and carbon dioxide in the presence of a solid, reusable catalyst at moderate conditions and does not require additional cocatalyst/promoter as well as solvent

Abstract: Hydride process for making acyclic diol intermediates from cyclic intermediates, useful in antibacterial quinolone synthesis.

Abstract: Disclosed is an aromatic compound expressed by the general formula (I), wherein A represents of a fused aromatic hydrocarbon moiety such as triphenylene, X represents a hydrogen-bonding site such as an atomic group containing an amide linkage, Y represents a chain functional group such as an alkyl group having 3 to 18, preferably 10 to 18 carbon atoms, and n represents an integer ranging from 2 to 10. The aromatic compound forms a molecular assembly in which the aromatic rings mutually overlap and exhibits an excellent charge carrier transfer property AX—Y)n.

Abstract: The present invention provides angiogenesis inhibitor compounds comprising a MetAP-2 inhibitory core coupled to a peptide, as well as pharmaceutical compositions comprising the angiogenesis inhibitor compounds and a pharmaceutically acceptable carrier. The present invention also provides methods of treating an angiogenic disease, e.g., cancer, in a subject by administering to the subject a therapeutically effective amount of one or more of the angiogenesis inhibitor compounds of the invention.

Abstract: The present invention relates to new hydrophilicized blocked polyisocyanates, a process for preparing them and their use.

Abstract: Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinational polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.

Abstract: Enzymatic preparation of (meth)acrylic esters containing urethane groups, and their use in radiation-curable compositions.

Abstract: Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinatiorial polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.

Abstract: The present invention provided a norbornene compound with cross-linkable groups and their derivative polymers, wherein said cross-linkable groups were olefin or epoxy groups. Norbornene polymers with cross-linkable side chain and their block copolymers as well as modified derivatives were prepared via living ring-open metathesis polymerization method. The resulting polymers with excellent solubility and optic properties had narrow molecular weight distribution, well-controlled molecular weight, small refraction ration and high transparency. They were also suitable for preparing hybrid materials with high thermal stability and chemical resistance.

Abstract: A method for producing carbamates that enables carbamates to be produced at low costs, with high selectivity and high yield, and in a simple manner, and a method for producing isocyanates that enables isocyanates industrially used to be produced by using the carbamates obtained by the carbamates producing method. Nonaromatic amine selected from the group consisting of aliphatic amine, alicyclic amine, and aralkyl amine is allowed to react with alkylaryl carbonate to thereby produce carbamates. Also, the carbamates thus obtained are thermally decomposed to thereby produce isocyanates. When carbamates are produced in this method, alkyl carbamates can be obtained with high selectivity and at high yield by using simple equipment. Also, when isocyanates are produced in this method, polyisocyanates used industrially as the raw material of polyurethane can be produced in a simple manner and with efficiency.

Abstract: The invention concerns the use as catalyst for transforming carbamates of compounds corresponding to the general formula (I): —Sn (X) (X?) wherein: X? is selected among chloride, bromide, iodide, thiocyanate radicals, sulphonate radicals, advantageously perfluorinated on the carbon bearing the sulphonate function; X is selected among the values of X? and among radicals of formula Y-Z; Y is selected among the chalcogen groups, advantageously light (that is oxygen and sulphur); Z is selected in the group consisting of trisubstituted tin, monosubstituted zinc, and the oxygenated acid radicals after ignoring the OH function. The invention is applicable to the coating industry.

Abstract: Compounds of the formula I, in which M, A1, A2, K1 and K2 have the meanings given in the description are novel effective tryptase inhibitors.

Abstract: The present invention provides angiogenesis inhibitor compounds comprising a MetAP-2 inhibitory core coupled to a peptide, as well as pharmaceutical compositions comprising the angiogenesis inhibitor compounds and a pharmaceutically acceptable carrier. The present invention also provides methods of treating an angiogenic disease, e.g., cancer, in a subject by administering to the subject a therapeutically effective amount of one or more of the angiogenesis inhibitor compounds of the invention.

Abstract: Compounds of the formula (I) in which: R1 is (CH2)nY; n is 1 or 2; Y is NHSO2R2 or X1—W—X2—R3; X1 is O or NH; W is C?O, C?S, C?NH, or SO2; X2 is O or NH, provided that X1 and X2 are not both O; R2 is C1-10 alkyl; C2-10 alkenyl; C2-10 alkynyl; aryl; aryl-C1-10 alkyl; aryl-C2-10 alkenyl; aryl-C2-10alkynyl; C3-8 cycloalkyl or C3-8-cycloalkyl-C1-10 alkyl; and R3 is hydrogen, C1-10alkyl; C2-10 alkenyl; C2-10 alkynyl; aryl; aryl-C1-10 alkyl; aryl-C2-10 alkenyl; aryl-C2-10 alkynyl; C3-8 cycloalkyl; or C3-8-cycloalkyl-C1-10 alkyl; or a salt or ester thereof, modulate metabotropic glutamate receptor function and are useful in treating disorders of the central nervous system.

Abstract: Blocked polyisocyanates and one-component stoving systems containing these blocked polyisocyanates, and the preparation thereof and their use for the preparation of lacquers, paints, adhesives and elastomers. The blocked polyisocyanates are derived from polyisocyanates reacted with secondary amines and cationic, anionic and/or nonionic hydrophilizing agents such that they are incorporated into the polyisocyanate at a ratio of from 20:1 to 1:1, wherein the blocking agents correspond to the formula R1–R4 can be identical or different and independently of one another denote hydrogen, C1–C6-alkyl or C3–C6-cycloalkyl, R5 denotes C1–C10-alkyl, C3–C10-cycloalkyl, and B represents ?wherein R6–R8 can be identical or different and independently of one another denote C1–C6-alkyl and/or C1–C6-cycloalkyl, R9 denotes hydrogen or C3–C6-alkyl or C3–C6-cycloalkyl.

Abstract: This invention provides compositions and methods for treating fibrous substrates to render those substrates durably repellent to water and oil and durably resistant to dry soil comprising a fluorochemical urethane formed by reacting a tri- or higher order isocyanate with a fluorochemical monofunctional compound; and optionally a non-fluorinated aliphatic monofunctional compound.

Abstract: The present invention provides angiogenesis inhibitor compounds comprising a MetAP-2 inhibitory core coupled to a peptide, as well as pharmaceutical compositions comprising the angiogenesis inhibitor compounds and a pharmaceutically acceptable carrier. The present invention also provides methods of treating an angiogenic disease, e.g., cancer, in a subject by administering to the subject a therapeutically effective amount of one or more of the angiogenesis inhibitor compounds of the invention.

Abstract: Disclosed are colorant precursor compounds of the formula wherein R is an alkyl group, an aryl group, an arylalkyl group, or an alkylaryl group, and wherein R can be joined to the phenyl moiety to form a ring, each R?, independently of the others, is a halogen atom, an alkyl group, an alkoxy group, a nitrile group, a nitro group, an amide group, or a sulfonamide group, z is an integer of 0, 1, 2, 3, or 4, n is an integer representing the number of carbon atoms in each repeat alkylene oxide unit, and x is an integer representing the number of repeat alkylene oxide units, wherein said colorant precursor has no more than one —OH, —SH, or primary or secondary amino group per molecule.

Abstract: A blocked polyisocyanate adduct including 5 to 95% by weight of at least one isocyanate component having at least one NCO group, the isocyanate component selected from the group consisting of aliphatic, cycloaliphatic and aromatic isocyanates, wherein the isocyanate has an average molecular weight of up to 1000 g/mol and an average NCO functionality of 2–4; 5 to 70% by weight of at least one hydrophilicizing component containing at least one group which is reactive toward the at least one NCO group; at least one blocking agent for blocking from 95 to 100% of the NCO groups which do not react with the hydrophilicizing component; and up to 15% by weight of at least one neutralizing agent.

Abstract: A readily available and inexpensive natural ?-amino acid is converted into a compound represented by formula (1), which is then reacted with an organometallic reagent represented by formula (2) to give an optically active 5-hydroxyoxazolidine represented by formula (3), which is then treated with an acid to provide an optically active aminoketone represented by formula (4). The product is then converted into an optically active aminoalcohol represented by formula (5) or (6) by, for example reduction.

Abstract: The invention concerns a novel catalyst for forming urethanes. Said catalyst is characterized by the general formula: MY3?q[Z]q, wherein: Z is the radical corresponding to the anion of a super acid whereof the Hamett constant is at least equal to 13 and advantageously more than 13, M representing a trivalent metal, preferably known for forming Lewis acids; Y is an anion or a monovalent anionic function; and q is an integer selected advantageously between 1 and 3, inclusively. The invention is applicable to paint.

Abstract: The present invention provides a pharmaceutical agent having cholesteryl ester transfer protein inhibitory action and useful as a blood lipid lowering agent and the like. The present invention relates to a compound represented by the formula wherein Ar1 is an aromatic ring group optionally having substituents, Ar2 is an aromatic ring group having substituents, OR? is an optionally protected hydroxyl group, R is an acyl group, R? is a hydrogen atom or a hydrocarbon group optionally having substituents, or a salt thereof, and a pharmaceutical composition containing a compound of the formula (I) or a salt thereof or a prodrug thereof.

Abstract: Provided is a compound having one or more structures of the formula: wherein X is a primary carbamate group, Y is a hydroxy or halide group, n is an integer of 2 or more, n? is an integer of 1 or more, and R0, R1, R2, R3, R4 and R5 may be H or a group selected from alkyl groups, aliphatic groups, cycloaliphatic groups, aromatic groups and mixtures thereof, with the provisos that at least one R1 or R2 group is selected from the group consisting of aliphatic groups, cycloaliphatic groups, and aromatic groups, and in substantially all structures primary carbamate group X is attached to a carbon atom having a lower degree of substitution than a carbon atom to which functional group Y is attached. The invention provides a method of making the claimed compound.

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: Electron donor compounds, suitable for use as adhesives or as components in adhesives, contain a carbon to carbon double bond attached to an aromatic ring and conjugated with the unsaturation in the aromatic ring.

Abstract: Catalysts contain, as structural units, at least one tertiary amino group and at least one group which, after its decomposition, is capable of complexing or protonating the tertiary amino group.

Abstract: Using at least one compound selected from the group consisting of a zirconyl compound and a zirconium alcoholate as an allophanation catalyst, an allophanate group-containing polyisocyanate composition is produced from a starting material of at least one isocyanate compound selected from the group consisting of an aliphatic diisocyanate, an alicyclic diisocyanate and an isocyanate pre-polymer obtained therefrom, and another starting material of a hydroxyl group-containing compound.

Abstract: More efficient and/or economical methods for synthesizing heptapeptide alcohol analogs of oxytocin are provided along with novel intermediates which are useful in synthesizing such oxytocin analogs. Efficient and economical methods for synthesizing intermediates useful in synthesizing these oxytocin analogs are also provided.

Abstract: The present invention relates to carboxamide compounds of general formula I 1

Abstract: In one aspect, the invention provides a solid catalyst comprising an active alumina catalyst impregnated with a metal hydroxide. In another aspect, the invention provides a process for preparing the inventive alumina catalyst. In certain embodiments, the catalyst may be used for the protection of amines, alcohols and thiols with a wide variety of protecting agents. This procedure is widely applicable for N-protection of amino acids which finds wide industrial applications. The catalyst is also useful for carrying out nucleophilic substitutions of aromatic halides containing an electron-withdrawing group. A wide variety of nucleophiles chosen from amines, primary and secondary, aromatic and aliphatic, as well as alcohols and thiols have been successfully employed. The methodology involves simple techniques and easy work up procedures and is thus useful for large-scale industrial preparations. Additionally, the reactions avoid the use of harmful solvents and thus satisfy the need for green chemistry.

Abstract: A mutant hydrolase optionally fused to a protein of interest is provided. The mutant hydrolase is capable of forming a bond with a substrate for the corresponding nonmutant (wild-type) hydrolase which is more stable than the bond formed between the wild-type hydrolase and the substrate. Substrates for hydrolases comprising one or more functional groups are also provided, as well as methods of using the mutant hydrolase and the substrates of the invention. Also provided is a fusion protein capable of forming a stable bond with a substrate and cells which express the fusion protein.