Abstract: The present invention is directed C2-disubstituted indan-1-ones of the Formula I, 1

Abstract: The invention relates to an improved process for the preparation of N-carboxyanhydrides by reaction of the corresponding amino acid or one of its salts with phosgene, diphosgene and/or triphosgene in a solvent medium, characterized in that at least a portion of the reaction is carried out under a pressure of less than 1000 mbar. The N-carboxyanhydrides are thus obtained with better yields and an improved purity.

Abstract: GABA-related pro-drugs of the formula (III) are provided that when administered to humans or other mammals provide an increased duration of active compound in the plasma compared to compounds of corresponding structure in which labile groups are not present.

Abstract: The present invention provides a method for enantioselectively producing a nonracemic 6,7-dihydroxy geranyloxy compound from a geranyloxy compound. In particular, methods of the present invention involve enantioselectively epoxidizing the geranyloxy compound and hydrolyzing the epoxide moiety under conditions sufficient to produce the nonracemic 6,7-dihydroxy geranyloxy compound.

Abstract: Compounds of formula I are useful for treating conditions associated with hyperglycemia, especially Type II diabetes. These compounds are useful in stimulating the kinase activity of the insulin receptor, activating the insulin receptor, and stimulating the uptake of glucose. Pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.

Abstract: The present invention relates to novel carbamates, ureas, and pharmaceutically acceptable salts thereof, compositions comprising the carbamate, urea, or a pharmaceutically acceptable salt thereof, and methods for treating or preventing cancer, inflammation, or a viral infection comprising administering to a patient in need of such treatment or prevention a therapeutically effective amount of the carbamate, urea, or pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to azo amino acid derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.

Abstract: The present invention provides a commercially profitable process for producing a &bgr;-amino acid ester derivative which comprises reacting an &agr;-amino acid ester derivative with a base and a dihalomethane, reacting the same with a lithium amide and an alkyllithium in succession, and treating the reaction product with an acid in an alcohol.

Abstract: Compounds of formula (I) are disclosed which are diasteroisomers of a known class of protease inhibitors. The compounds inhibit &ggr;-secretase, and find use in the treatment and/or prevention of Alzheimer's disease.

Abstract: The present invention is directed to a transition metal catalyst, comprising a Group 8 metal and a ligand having the structure wherein R, R′ and R″ are organic groups having 1-15 carbon atoms, n=1-5, and m=0-4. The present invention is also directed to a method of forming a compound having an aromatic or vinylic carbon-oxygen, carbon-nitrogen, or carbon-carbon bond using the above catalyst. The catalyst and the method of using the catalyst are advantageous in preparation of compounds under mild conditions of approximately room temperature and pressure.

Abstract: Acylated ketoamides are prepared from sulfonyl amides and aldehydes or their related derivatives by a step of 1

Abstract: The present invention relates to compounds of formula (I): 1

Abstract: The decomposition of di-t-butyl dicarbonate which is a thermally unstable compound is inhibited. To achieve the object, a hydrocarbon compound such as hexane, cyclohexane, 1-hexene or toluene and/or a chain ether compound such as diisopropyl ether or t-butyl methyl ether are/is used as a decomposition inhibitor for di-t-butyl dicarbonate.

Abstract: The process disclosed herein satisfies the need in the art for an industrially viable oxidative carbonylation catalytic system, and is capable of producing carbamates at a significantly higher rate than those processes reported in journal and patent literature. This reaction process takes place via a reaction mechanism that does not involve drastic conditions. Specifically, the catalytic system of the present invention employs Group VIII metal catalysts and/or copper-based catalysts with halide promoters to produce carbamates through heterogeneous oxidative carbonylation at atmospheric pressure and relatively non-drastic temperatures in a gas-solid carbonylation process.

Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

Abstract: The present invention relates to certain resorcinol derivatives and their use as skin lightening agents.

Abstract: 1 Novel urea derivatives of formula I are disclosed: The compounds are inhibitors of &ggr;-secretase, and hence useful in the treatment or prevention of Alzheimer's disease.

Abstract: Compounds represented by the general formula (1):   (where R1 is SR6 or NR7R8, where R6 is typically an alkyl group having 1-6 carbon atoms, R7 is a hydrogen atom, an alkyl group having 1-6 carbon atoms or a nitro group, and R8 is a hydrogen atom or an alkyl group having 1-6 carbon atoms; R2 and R3 are each typically a hydrogen atom or an alkyl group having 1-6 carbon atoms; R4 is a hydrogen atom, an alkyl group having 1-6 carbon atoms or an amidino group of which the amine portion may be substituted by an alkyl or nitro group; R5 is a hydrogen atom or an alkyl group having 1-6 carbon atoms; Y1, Y2, Y3 and Y4 which may be the same or different are each typically a hydrogen atom, a halogen atom or an alkoxy group having 1-6 carbon atoms; n and m are each an integer of 0 or 1), or possible stereoisomers or optically active forms of the compounds or pharmaceutically acceptable salts thereof.

Abstract: A method of preparing a carbamate or urea-functional compound is described comprising the step of reacting a lactone or hydroxy carboxylic acid with a compound (A) comprising a carbamate or urea group or a group that can be converted to a carbamate or urea group, and an active hydrogen group capable of reacting with the hydroxy carboxylic acid or in a ring-opening reaction with a lactone. The compound thus prepared is useful in curable compositions.

Abstract: The invention provides novel adamantane compounds having one of the following formulas: 1

Abstract: R or S aminocarnitine and their derivatives with formula (I) where Y is as described in the description, starting with aspartic acid with the same configuration as the aminocarnitine desired. This process has advantage in the type of reactants used, reduced volumes of solvents and the possibility of avoiding purification of intermediate products.

Abstract: A phosgene-free method for preparing a carbamate from a compound containing an amine group involves reacting the compound with an alkylating agent in the presence of carbon dioxide and cesium carbonate. A reaction can take place under standard pressure and temperature conditions and produces carbamates in a high yield with low by-product formation.

Abstract: Compounds of peptide mimetic nature having the general formula I 1

Abstract: A purpose of the present invention is to provide TNF-&agr; production inhibitors being useful as therapeutic agents for autoimmune diseases such as rheumatoid arthritis.

Abstract: The present invention provides compounds and libraries of compounds having formula (I): 1

Abstract: Disclosed are intermediates and processes for preparing epoxides of the formula: 1

Abstract: Described are cyclohexylamine derivatives of Formula I 1

Abstract: The present invention provides an aniline derivative represented by the formula (I) 1

Abstract: A method of preparing a carbamate or urea-functional compound is described comprising the step of reacting a lactone or hydroxy carboxylic acid with a compound (A) comprising a carbamate or urea group or a group that can be converted to a carbamate or urea group, and an active hydrogen group capable of reacting with the hydroxy carboxylic acid or in a ring-opening reaction with a lactone. The compound thus prepared is useful in curable compositions.

Abstract: The invention provides adamantane derivatives of formula (I), a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.

Abstract: Novel anthranilic acid derivatives having an inhibiting activity of cGMP-PDE are represented by the formula I where A is a lower alkylene group: 1

Abstract: This invention relates to intermediates useful in the preparation of CETP inhibitors and methods of preparation thereof.

Abstract: The present invention relates to a compound which is expected to be a synthetic intermediate for medicines and pesticides or a separating agent for chromatography or a enantiomerically resolving agent for racemic bodies. That is, it provides 3-amino-1-indanol represented by the formula (I), a process for synthesizing it, an enantiomerically active compound of 3-amino-1-indanol and a process for enantiomerically resolving 3-amino-1-indanol, and a separating agent for enantiomeric isomers comprising enantiomerically active compound thereof as an effective ingredient.

Abstract: Compounds of formula (I) wherein R1 is C1-C4-alkyl or cyclopropyl; R2 is C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkinyl; or C1-C6-alkyl substituted by 1 to 5 fluorine atoms; R3 is C1-C6-alkyl, C1-C6-alkoxy, C3-C6-cycloalkyl, C3-C6-cycloalkoxy, C2-C6-alkenyl, C2-C6-alkenyloxy, C2-C6-alkinyl, C2-C6-alkinyloxy, C1-C6-alkoxycarbonyl, CN, or aryl, heteroaryl, heterocyclyl, aryloxy, heteroaryloxy or heterocyclyloxy, whereby the above-mentioned groups may be substituted by identical of different substituents, R5 signifies hydrogen or methyl; R6 and R7 are C1-C4-alkyl; have microbicidal, insecticidal and acaricidal activity and may be used for the control of pests and plant-pathogenic fungi in agriculture, horticulture and in the field of hygiene.

Abstract: The invention concerns a compound of formula (I) in which m is to 0 or 1 Iso is the (poly)isocyanate radical (after elimination of an isocyanate function); R10 is selected among: a negative charge; a hydrocarbon-based radical (i.e. a residue containing hydrogen and carbon atoms) having a carbon as it binding point [i.e. the atom carrying the open bond]; R11 is selected among a negative charge. The invention is applicable to organic synthesis.

Abstract: The invention relates to a process for the preparation of N-carboxyanhydrides by reaction of the corresponding amino acid with phosgene, diphosgene and/or triphosgene in a solvent medium, characterized in that the reaction is a least partially carried out in the presence of an unsaturated organic compound which has one or more ethylenic double bonds, one of the carbon of at least one ethylenic double bond of which is completely substituted by substituents other than halogen atoms. The N-carboxyanhydrides are thus obtained with better yields and an improved purity.

Abstract: The invention relates to a process for preparing quinoline-substituted carbonate and carbamate compounds, which are important intermediates in the synthesis of 6-O-substituted macrolide antibiotics. The process employs metal-catalyzed coupling reactions to provide a carbonate or carbamate of formula (I) or (II) or a substrate that can be reduced to obtain the same.

Abstract: Process for the preparation of stable activated derivatives of carbamic acid, comprising at least one protected amino group and an activated carbamic acid function, from an amino acid derivative in which the amino group is protected. The process includes: a) a step of transformation of the —COOH group of the amino acid derivative into a —CON3 group to obtain an acyl azide; b) a step of transformation of the —CON3 group of the acyl azide into a —NCO group to obtain an isocyanate; c) a step of treating the isocyanate to obtain a stable derivative of carbamic acid.

Abstract: The invention relates to a process suitable for large-scale industrial use for preparing compounds of general formula (I) 1

Abstract: The present invention provides a compound according to the formula: CH2═C(R1)—C(O)—R6—NHCO2(CH2)p(CF2)q—O—((CF2)aCFXO)m(CF2)r—Z wherein each R1 is independently selected from —H, —CH3, —F and —Cl, wherein each R6 is independently selected from substituted or unsubstituted C1-C10 alkyl, cyclic alkyl, or aryl groups, wherein each a is independently selected from 0-3, wherein each X is independently selected from —F, —CF3 or —CF2CF3, wherein each p is independently selected from 1-4, each q is independently selected from 1-5, each r is independently selected from 1-5, each m is independently selected from 1-50, each Z is independently selected from —F and —(CH2)sOH, and each s is independently selected from 1-4. The present invention also provides for the use of this compound as a surfactant in highly fluorinated liquid solvents. Latexes of dispersed particles utilizing this surfactant are provided.

Abstract: A phosgene-free method for preparing a carbamate from a compound containing an amine group involves reacting the compound with an alkylating agent in the presence of carbon dioxide and cesium carbonate. A reaction can take place under standard pressure and temperature conditions and produces carbamates in a high yield with low by-product formation.

Abstract: Novel (hydroxyethyl)ureas are described. These compounds are effective inhibitors of certain aspartyl proteases, notably secretases involved in the enzymatic cleavage of amyloid precursor protein (APP) to yield amyloid-&bgr; peptide. Methods are provided for administering the novel compounds to treat &bgr;-amyloid-associated diseases, notably Alzheimer's disease.

Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH-mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

Abstract: A novel calcium receptor active compound having the formula is provided:

Abstract: The present invention relates to novel carbamates and pharmaceutically acceptable salts thereof; compositions comprising the carbamate or a pharmaceutically acceptable salt thereof; and methods for treating cancer, inflammation, or a viral infection comprising administering to a patient in need of such treatment a therapeutically effective amount of the carbamate or pharmaceutically acceptable salt thereof.

Abstract: The invention relates to novel carbazate intermediates of formula (II), and to a process for their preparation, and their usefulness in the preparation of (1,3,4) oxadiazine derivatives useful as pesticides, in particular as anthelminthicides, insecticides, acaricides, and nematicides.

Abstract: Process for preparing optically active &bgr;-amino alcohols represented by a general formula (2): Ra—C*H(OH)—C*H(Rb)—Rc wherein Ra and Rc are each independently hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, Rb is one member selected from among groups represented by the following general formulae; (3) R1CO(R2)N—, and (4) R1CO(R1′CO)N—, and C* is an asymmetric carbon atom, characterized by reacting a racemic &agr;-aminocarbonyl compound represented by the general formula (1): Ra—CO—CH(Rb)—Rc, with hydrogen in the presence of an optically active transition metal compound represented by a general formula (7): MaXY(Px)m(Nx)n wherein Ma represents a metal atom belonging to VIII-group of the periodic law, X and Y represent each independently hydrogen, halogeno, Px represents a phosphine ligand, Nx represents an amine ligand, at least one of Px and Nx is optically active, and m and n each independently represent 0 or an integer of 1 th

Abstract: The present invention relates to substantially solvent-free binder compositions containing a) a polyisocyanate component containing heteroallophanate groups and having aromatically-bound isocyanate groups, i) an NCO content of 3 to 16%, ii) an average functionality of 1.8 to 4, iii) an allophanate group content (calculated as C2N2O3, MW: 101) of 5 to 35% and iv) a hydrocarbon chain content of 10 to 65%, wherein the hydrocarbon chains are attached to allophanate groups via oxygen and have an average of 2 to 23 carbon atoms and b) an isocyanate-reactive component. The present invention also relates to the use of these binder compositions in one- and two-component coating compositions.

Abstract: The invention relates to methods for forming combinatorial libraries. The invention provides methods suitable for the rapid and convenient synthesis of very large combinatorial libraries of small organic molecules. In particular, the invention provides a method for forming combinatorial libraries combining amide bond formation with epoxide opening.

Abstract: Process for the preparation of amino acid derivatives of the general formula I where R1-R4 are as defined herein, from the corresponding malonic acid monoester amides of the general formula II  by Hofmann degradation using a hypohalite in an aqueously basic medium, which comprises carrying out the reaction in the presence of an alcohol or amine and using the hypohalite in amounts of from 1.0 to 1.5 equivalents and the base in amounts of from 0.8 to 4.0 equivalents per mole of starting material II.