Abstract: A method for producing unprotected or carbamate-protected amines of formulae (II) and (III) or R1—NH2 (II) or R1—NHCO2R2 (III) by reacting hydroxamic acids of formula (I) (R1 CONHOH) with a) alkylpliosphonic acid anhydrite's, b) alcohol R2OH and c) optionally with a base, at a temperature ranging from 100 to +120°C., wherein the hydroxainic acid (I) is produced prior to or during reacting (in situ) and R1 is an optionally substituted linear or branched C1-C12 alkyl radical, substituted C3-C10 cycloalkyl, alkenyl, aryl or heteroaryl radical and R2 is an open-chain, cyclic or branched allyl, aryl or C1 to C12-alkyl radicals, or aryloxy, allyloxy or alkoxy radical possibly substituted with open-chain, cyclic or branched C1 to C12-alkyl radicals.

Abstract: Disclosed are protease inhibitors for coronaviruses and SARS-CoV, or picornaviruses, and the use of these protease inhibitors for preventing, reducing, ameliorating and treating a disease or condition caused by coronaviruses and SARS-CoV, or picornaviruses.

Abstract: Pesticidal compounds having the structural formula wherein: R2 is C1-C6 branched or straight chain alkyl; C1-C4 branched or straight-chain haloalkyl; or C3-C6 cycloalkyl; m is 0, 1, or 2; X is selected from the group consisting of: C1-C6 branched or straight-chain alkoxy; halogen; C1-C6 branched or straight-chain alkyl; or C1-C6 branched or straight-chain alkylthio; n is 0 or 1; A is 0; CH2; or NR?, wherein R? is (C1-C6 alkyl)carbonyl; Y is phenyl; benzyl; thiazolyl; thienyl; pyridyl; or tetrahydrofuranyl, the aromatic ring of each substituent being optionally substituted with one or more of halogen, C1-C6 branched or straight-chain alkyl, or C1-C6 branched or straight-chain haloalkyl; use of the compounds as pesticides and pesticidal compositions comprising the compounds.

Abstract: The invention encompasses processes for the synthesis of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin, and intermediates of (S)-Pregabalin.

Abstract: The present invention relates to a compound of formula (1), wherein R1, R2, R3, n, and X are as defined in the specification, and a process for producing the same. This compound is useful as an intermediate for the synthesis of compounds useful as pharmaceuticals or agricultural chemicals.

Abstract: The invention relates to the use of carboxyamine compounds and salts thereof in the treatment of HDAC dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases.

Abstract: The present invention is substituted amine s of formula (XV) useful in treating Alzheimer's ease and other similar disease.

Abstract: A method of synthesis of a N-10 protected PBD compound of formula (I): via an intermediate of formula (II) or formula (V):

Abstract: A process for the preparation of aromatic carbamates comprising contacting one or more organic carbonates with an aromatic amine or urea in the presence of a catalyst and recovering the resulting aromatic carbamate product, characterized in that the catalyst is a heterogeneous catalyst comprising a Group 12-15 metal compound supported on a substrate.

Abstract: A process of producing a compound of the following formula (3): wherein R1 is a C1-5 alkyl group, R2 is a halogen atom, a C1-5 alkyl group, a C2-5 alkenyl group, a C2-5 alkynyl group, a C1-5 alkyl group, a C1-5 alkoxy group, a nitro group, or a hydroxy group, wherein multiple R2 may be the same or may be different, and a is an integer of from 0 to 4, comprising reacting a compound of the following formula (2): wherein R2 and a are as defined above with a C1-5-alkanesulfonyl chloride or C1-5-alkanesulfonic acid anhydride followed by hydrolyzing an N,N-disulfonated derivative of compound (3) to the compound of formula (3).

Abstract: The present invention relates to novel compounds of Formula (I) wherein ‘X’ represents an amino acid group, ‘n’ is an integer between 1 and 4, ‘R1’ represents benzyl, t-butyl or 9-fluorenylmethyl and ‘R2’ represents a tetramethylmercaptoimidazole derivative or —S+R3R4, wherein R3 and R4 each independently represent lower alkyl, or a pharmaceutically and/or veterinarily acceptable derivative thereof. The present invention further relates to pharmaceutical formulations of said compound and the use thereof in the preparation of a medicament for inhibiting diseases in which transglutaminase has been implicated. Advantageously, the medicament is for treating fibrosis, scarring and/or cancer. Additionally, the invention relates to a method of inhibiting autoimmune diseases such as coeliac disease, neurodegeneration and chronic inflammatory diseases (e.g. of the joints including rheumatoid arthritis and osteoarthritis in a subject).

Abstract: The invention relates to substituted para-trifluoromethyl phenyl ether compounds and its preparation and use thereof especially. The substituted para-trifluoromethyl phenyl ether compounds of the invention having general formula (I): The substitutes see Description. The compounds of present invention have broad-spectrum activity, and may be used to control diseases in all sorts of plants caused by oomycete, basidiomycete, ascomycete pathogens and deuteromycete, and it may also provide good control efficacy at very low dosage because of the high activity. The compounds of the invention have good insecticidal activity and have good activity against many pests, especially for Carmine spider mite. The compounds are fit for synthetical control against many kinds of pests.

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: A monomer with a chromophore group represented by Formula (I): wherein AR1 represents a substituted or unsubstituted aromatic group; AR2 represents a substituted or unsubstituted aromatic group or a substituted or unsubstituted alkyl group; and R represents a substituted or unsubstituted alkyl group, with the proviso that one of R, AR1, and AR2 has a substituent with a polymerizable functional group. The monomer can be advantageously used to prepare polymeric dispersants for pigment dispersion, especially inkjet inks.

Abstract: An improved process for preparing carbamic ester derivatives of the general formula (1) by reaction with carbon monoxide and water in the presence of a palladium catalyst is provided.

Abstract: An improved process for preparing carbamic ester derivatives of the general formula (1) by reaction with carbon monoxide and water in the presence of a palladium catalyst is provided.

Abstract: This invention provides compounds of formula I where Ar1 is a 5- to 10-member mono- or bicyclic aromatic group, optionally substituted; where the —NR3R4 group is situated ortho to the NHC(?X) group; n=1 or 2; X?O or S; Y is O or S; and q=1 or 0. The invention also provides pharmaceutical compositions comprising compounds of formula I and/or salts, esters, and prodrugs thereof. These compounds modulate the activation and inactivation of potassium channels. The compounds are useful for the treatment and prevention of diseases and disorders—such as seizure disorders—which are affected by modulation of potassium ion channels.

Abstract: Pharmacological inhibition of fatty acid amide hydrolase (FAAH) activity leads to increased levels of fatty acid amides. Esters of alkylcarbamic acids are disclosed that are inhibitors of FAAH activity. Compounds disclosed herein inhibit FAAH activity. Described herein are processes for the preparation of esters of alkylcarbamic acid compounds, compositions that include them, and methods of use thereof.

Abstract: Novel compounds of the general formula (I), in which the variables are as defined in claim 1, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? subtype, namely, type 1 diabetes, type 2 diabetes, dyslipidaemia, syndrome X (including the metabolic syndrome, i.e. impaired glucose tolerance, insulin resistance, hyper triglyceridaemia and/or obesity), cardiovascular diseases (including atherosclerosis) and hypercholesterolaemia.

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 disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.

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

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: The invention provides methods for hydroaminating N-alkenoyl carbamates with aromatic amines.

Abstract: Arylcycloalkyl derivatives having branched side chains, processes for their preparation and their use as pharmaceuticals The invention relates to arylcycloalkyl derivatives having branched side chains and to their physiologically acceptable salts and physiologically functional derivatives. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistence is involved.

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

Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.

Abstract: Colchicine derivatives represented by the formula (I) with a halogen or nitric ester group, or pharmaceutically acceptable salts thereof, are described. Pharmaceutical compositions containing the same as effective components are also described. The colchicine derivatives were found to have anticancer, anti-proliferous and immunosuppressive function. Methods for preparing the colchicines derivatives are also provided.

Abstract: The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.

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: 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: The present invention relates to novel selective inhibitors of the urokinase plasminogene activator (uPA, EC 3.4.21.31) of the aryl guanidine type.

Abstract: Urea derivatives of formula I are disclosed: The compounds are inhibitors of ?-secretase, and hence useful in the treatment or prevention of Alzheimer's Disease

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 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: 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: A class of compounds is disclosed which are diasteroisomers of a known class of protease inhibitors. The compound inhibit gamma-secretase, and find use in the treatment of and/or prevention of Alzheimer's disease.

Abstract: Compounds of formula (I) or therapeutically acceptable salts thereof, are selective protein tyrosine kinase-B (PTP1B) inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of disorders using the compounds are disclosed.

Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.

Abstract: Disclosed is a method for synthesizing 1-(acyloxy)-alkyl derivatives of primary or secondary amine drugs from 1-acyl-alkyl derivatives of primary or secondary amine drugs, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amenable to scale-up. For example, 1-acyl-alkyl derivatives of gabapentin and pregabalin are oxidized to yield 1-(acyloxy)-alkyl derivatives of gabapentin and pregabalin, respectively.

Abstract: The present invention relates to compounds of formula (I) wherein R1, R2 and R3 independently represent one or more, same or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, carbamoyl, or phenyl; R1 and R2 further represented by nitro and R3 by carboxy; R4 represents hydrogen, (C1-C3)alkyl, or allyl; Q represents a bond, or —C(R6)(R7)(—O—C?O)—, in which formula R6 and R7 independently represent hydrogen, trifluoromethyl, or (C1-C4)alkyl; Y represents either (C5-C15)alkyl, (C2-C15)olefinic group, (C3-C10)monocyclic hydrocarbon, or phenyl, any of which may be optionally substituted with one or more, same or different substituents represented by the formula R5; or (C1-C4)alkyl substituted with at least one or more substituents with the formula R5; or Y represents a group of formula —CH2—(Z—O)n—Z where Z is a (C1-C3)alkyl,

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: Cold curing polyisocyanate adhesive compositions suitable for use in the preparation of engineered lumber composites. Additionally provided are catalysts comprising tertiary amine alkoxylates that are reduced in or substantially free of isocyanate-reactive hydroxylic or amine hydrogen atoms. Further provided is a process for preparing composites articles using the adhesive compositions and composite articles prepared from the adhesive compositions. Composite articles prepared from the adhesive compositions have a substantially increased resistance to delamination.

Abstract: Positionally isomeric diethyloctanediol dicarbamates and diethyloctanediol diallophanates, processes for preparing them, and their use as synthesis building blocks and constituents of adhesives, sealing compounds, and coating materials.

Abstract: The invention relates to a process suitable for large-scale industrial use for preparing compounds of general formula (I) wherein: R1 denotes a group selected from among methyl, ethyl, propyl, cyclopentyl, cyclohexyl, phenyl, benzyl and —C(Me2)phenyl, each of which is optionally mono-, di- or trisubstituted by hydroxy; and, R2 denotes a group selected from among methyl, ethyl, propyl and benzyl.

Abstract: The invention relates to semicarbazides of the general formula I where R1, R2, R3, R4 and I have the meaning indicated in claim 1. The compounds of the formula I can be employed as pharmaceutical active compounds in human and veterinary medicine, in particular for the control and prevention of thromboembolic disorders such as thrombosis, mycocardial infarct, arteriosclerosis, inflammation, apoplexy, angina pectoris, restenosis after angioplasty and intermittent claudication.

Abstract: The invention relates to derivatives of amidino-benzylamine, especially derivatives of 4-amidino-benzylamine, with two bonded amino acids. These derivatives represent a novel group of highly active and very selective F Xa-inhibitors for treating cardiovascular diseases and thrombotic events.

Abstract: The present invention relates to a process wherein a cyclic carbonate compound bearing an electrophilic group is reacted with a compound containing a nucleophilic group, especially an amine group. Such reactions permit to obtain urethane groups useful in polymer preparation, such as polyurethanes, or other urethane-containing polymers.

Abstract: The invention relates to the inhibition of histone deactylase. 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.