Abstract: The present invention provides a method for easily producing an (R)-3-[4-(trifluoromethyl)phenylamino]-pentanoic acid amide derivative useful for an intermediate for pharmaceutical products, particularly an inhibitor of a cholesteryl ester transfer protein (CETP) from easily available raw materials. In the present invention, (S)-N-[4-(trifluoromethyl)phenyl]-3-hydroxypentanoic acid amide prepared from easily available raw materials leads a production of (R)-4-ethyl-1-[4-(trifluoromethyl)phenyl]-2-azetidinone to give (R)-3-[4-(trifluoromethyl)phenylamino]-pentanoic acid amide. Furthermore, (R)-4-ethyl-1-[4-(trifluoromethyl)phenyl]-2-azetidinone is reacted with a carbamic acid ester to give an (R)-3-[4-(trifluoromethyl)phenylamino]-pentanoic acid amide derivative.

Abstract: The present invention provides pharmaceutically acceptable salts having local anesthetic and anti-inflammatory activities. The preferred pharmaceutically acceptable salt is a diclofenac salt of lidocaine. Diclofenac is a non-steroidal anti-inflammatory drug (“NSAID”). Lidocaine is a local anesthetic. Other NSAID (except the salicylic acid derivatives of NSAID) can be used to replace diclofenac and/or other local anesthetics can be used to replace lidocaine. The pharmaceutically acceptable salts are crystalline compounds, which are distinctively different from either the NSAID alone or the local anesthetic alone, as indicated by differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), High Performance Liquid Chromatography (HPLC) and Fourier-Transformed Infrared Spectroscopy (FTIR) analyses.

Abstract: This invention relates to an improved process for synthesizing (±)-2-Amino-N-[2-(2,5-dimethoxyphenyl]-2-hydroxyethyl acetamide monohydrochloride in good yield and in a cost effective manner from 1-(2,5-dimethoxyphenyl)-2-bromoethanone by reacting the same with hexamine in the presence of novel solvent system comprising Tetrahydrofuran and water. The resulting aminoethanone is acylated with haloacetylchloride and sodium acetate in acetone-water solvent system. This product is reduced selectively first with sodium borohydride and subsequently with stannous chloride. This product is converted in situ to the corresponding hydrochloride salt immediately after reduction on its own.

Abstract: The invention relates to a process for the preparation of ?-aminosubstituted carboxylic acid amide compounds and/or their salts comprising reacting a carboxylic acid amide of a primary amine with a nitrosylating agent in the presence of a base followed by hydrolysis to give a hydroxy imino derivative followed by hydrogenation and if necessary converting a base or acid of the ?-aminosubstituted carboxylic acid amide into one of its salts.

Abstract: A composition of matter is disclosed wherein the composition comprises an N-aromatic substituted acid amide compound selected from the group consisting of compounds of formula (I) wherein A and B are independently selected alkylene groups; R1 is selected from the group consisting of hydrogen, alkyl, alkylether, or ester; R2 is hydrogen if R1 is hydrogen; R2 is an alkyl primary amine if R1 is alkyl, alkylether, or ester; R3 and R4 are independently selected from the group consisting of hydrogen and alkyl; R5 is a sterically hindered phenolic group of formula (II) or formula (III) wherein X is CH2, S, NH, or O; and m, n, and p are independently selected integers equal to 0 or 1. These compositions may be used as such or they may be bound to a polymer backbone via a linking moiety.

Abstract: This invention relates to N-acylamino aryl derivatives of the formula 1

Abstract: A Type IV crystal of (Z)-N-[2-methoxy-5-[2-(3,4,5-trimethoxyphenyl)vinyl]phenyl]-L-serinamide hydrochloride, which can be produced by crystallization using a solvent containing water at 2% by weight at the maximum and which has a X ray powder diffraction pattern containing peaks at least at 13.4°, 18.7°, 19.4°, and 22.5° (2&thgr;), is provided. This compound is useful as an effective ingredient for a carcinostatic agent. The crystal of the present invention has excellent properties desirable from the standpoint of the production of medicinal products, i.e., reduced water adsorption and extremely high stability to water. Also provided are a method for producing the Type IV crystal thereof and a method for use of the crystal.

Abstract: Universal supports for oligonucleotide synthesis include a support material represented by the following formula: In this formula, substituent A is selected from H, alkyl, aryl, or a polymeric or silica base material; substituent B is selected from acyl, aroyl, or a polymeric or silica base material; and substituent C is selected from a dimethoxytrityl group or a protecting group removable under acidic or neutral conditions. For the supports, one of substituents A or B constitutes the polymeric or silica base material. In use, an oligonucleotide is attached to the support at substituent C.

Abstract: A method for producing compounds of general formula (I): wherein R1 and R2, each time they occur and independently of each other, mean hydroxyl, C1-6-alkyl, C1-6-alkoxy, halogen, phenyl or phenoxy; R3 means hydrogen or C1-6-alkyl; m is a whole number from 0 to 4; and n is a whole number from 0 to 5. According to the method, diketene is reacted with an N-phenyl-p-phenylenediamine of general formula (II): wherein R1, R2, R3, m and n have the meanings given above, in the presence of 3 to 40 percent acetic acid and at temperatures of 20 to 100° C. The compounds (I) with R3 is C1-6-alkyl and the enamines can be obtained from these by reaction with ammonia, and their hydration products.

Abstract: PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.

Abstract: The invention relates to methods of synthesizing libraries of diverse and complex highly substituted 2,4-dioxopiperidine compounds of the general formula: wherein R1, R2 and R3 are as herein described, novel intermediates useful for synthesizing such 2,4-dioxopiperidine compounds and methods for identifying and isolating the compounds.

Abstract: Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.

Abstract: Process for the preparation of a diasteromerically enriched phenylglycine amide derivative in which an enantomerically enriched phenylglycine amide is converted into the corresponding Schiff base with the aid of compound R2—C(O)—R3, and the Schiff base obtained is subsequently converted into the diastereomerically enriched phenyglycine amide derivative with the aid of a cyanide source, a reducing agent or an allyl organometallic compound. The phenylglycine amide derivatives obtained are interesting starting materials for the preparation of for example enantimerically enriched &agr;- and or &bgr;-amino acids and derivatives thereof, such as amides and esters, and amines.

Abstract: This invention relates to &agr;-ammonium ketones, iminium ketones or amidinium ketones in the form of their tetraaryl- or triarylalkylborate salts which can be photochemically converted into amines, imines or amidines as well as to a process for their preparation. This invention also relates to base-polymerisable or crosslinkable compositions comprising these &agr;-ammonium ketones, iminium ketones or amidinium ketones in the form of their tetra- or triarylalkylborate salts, to a process for carrying out photochemically induced, base-catalysed reactions as well as to their use as photoinitiators for base-catalysed reactions.

Abstract: The present invention is a process for the preparation of a compound of Formula (IA) or a pharmaceutically acceptable salt thereof: that includes preparing a diamide of Formula (II) or a pharmaceutically acceptable salt thereof:

Abstract: This invention concerns an enzyme substrate consisting of a target part and a marker part, hydrolysis of the substrate leading to separation of the target part from the marker part, and said target part being specific for the enzyme activity being assayed. It also concerns a formulation containing at least one such substrate, and a method for detecting the bacterial species Pseudomonas aeruginosa.

Abstract: The invention to a pharmaceutical composition comprising as active principle a compound of general formula (I), in which R1, R2, R3, and A are as defined in claim 1. These compositions can be used in the treatment of pathologies associated with insulin resistance syndrome.

Abstract: Disclosed is a method of selecting analgesic agents based on their selective ability to block tetrodotoxin-insensitive sodium channels, particularly in comparison to blocking tetrodotoxin-sensitive sodium channels. Also disclosed is a novel class of compounds that is selective for blocking tetrodotoxin-insensitive sodium channels.

Abstract: This invention relates to a process for the Heck coupling reaction where heterogeneous palladium catalysts are used to activate aryl halides for a carbon-carbon coupling with olefins in the presence a base and an aprotic solvent to produce aryl-olefin compounds. The process, in particular, provides for the use of aryl chlorides substituted with electron-withdrawing or electron-donating group for the cross coupling with olefins.

Abstract: The invention provides a process for the preparation of 2-amino-N-[2-(2,5-dimethoxyphenyl)-2-hydroxyethyl]acetamide of the formula 1 by hydrogenolysis of substituted 2-dibenzylamino-N-[2-(2′,5′-dimethoxyphenyl)-2-hydroxy-ethyl]acetamide having the formula (5), wherein Ar and Ar′ are aryl groups,

Abstract: The present invention relates to new aminoindane piperidine compounds, the method of using aminoindane compounds as local anesthetics, said compounds having particularly valuable properties as dermal and topical anesthetics in mammals, including man, as well as compositions containing said compounds.

Abstract: Disclosed are compounds of the general formula 1

Abstract: A class of substituted b-amino acids are potent inhibitor of methionine aminopeptidase type 2 (MetAP2) and are thus useful in inhibiting angiogenesis and disease conditions which depend upon angiogenesis for their development such as diabetic retinopathy, tumor growth, and conditions of inflammation. Pharmaceutical compounds containing the compounds and methods of inhibiting methionine aminopeptidase-2, and angiogenesis are also disclosed.

Abstract: The present invention relates to chemically stable, polyfunctional, perfluorinated polyorganosiloxanes (POS) comprising on the one hand fluorinated lateral grafts resulting from the hydrosilylation of perfluorinated olefins with SiH units and having alkyl and/or alkyl ester linkages but not ether linkages, and on the other hand other, non-perfluorinated functional units E capable of giving them diverse and varied physical and chemical properties and opening up avenues in numerous applications. Examples of these POS according to the invention are those of the following formula: According to another of its features, the invention relates to a process for the preparation of these polyfunctional perfluorinated POS. Applications: antifoams, agents for lowering surface tension, dirt repellents, antiadhesives, lubricants, oleophobic and/or hydrophobic agents, coatings etc.

Abstract: This invention features a template for synthesizing combinatorial libraries, methods of synthesizing combiatorial libraries of chemical compounds utilizing the template, and combinatorial libraries of chemical compounds formed by the methods of this invention.

Abstract: The invention relates to derivatives of general formula I ##STR1## as defined in the description. The invention also relates to a process for their preparation and to their therapeutic use, in particular for the treatment of complaints associated with melatonin disorders, and pharmaceutical and cosmetic compositions comprising them.

Abstract: The present invention provides amine/amide catalysts for use in catalyzing the formation of polyurethane. The amine/amide catalysts, which have low fugitivity due to their reactivity with isocyanates, and good catalytic activity, have the structure ##STR1## wherein Q is C.sub.z H.sub.2z+1, or (CH.sub.2).sub.n N(R.sup.3).sub.k T, T is a monovalent C.sub.1 -C.sub.4 alkyl, amino-C.sub.1 -C.sub.4 -alkyl, mono-C.sub.1 -C.sub.4 -alkylamino-C.sub.1 -C.sub.4 -alkyl, or di-C.sub.1 -C.sub.4 -alkylamino-C.sub.1 -C.sub.4 -alkyl group, or T is a divalent alkyl, amine substituted alkyl, alkylaminoalkyl, or alkoxyalkyl group which forms with the nitrogen atom shown in structure (I) to which T is attached a cyclic structure which incorporates up to 6 carbon atoms in the ring as well as the nitrogen atom shown in structure (I), which cyclic structure may be substituted with C.sub.1 to C.sub.4 alkyl;k=0 or 1, being 1 if T is a monovalent group and 0 if T is a divalent group; R.sup.2 .dbd.H or C.sub.z H.sub.2z+1 ; R.sup.3 .dbd.

Abstract: The present invention is directed to N-benzyl-2-amino-3-methoxypropionamide and stereoisomers the use thereof anti-convulsant and an intermediate in the preparation of other anti-convulsants.

Abstract: Compounds of the formula ##STR1## are useful as intermediates to new herbicidal 4-benzoylisoxazoles.

Abstract: A composition suitable for transdermal electrotransport delivery of an agent through a body surface comprises a free acid/base form of an agent to be delivered by transdermal electrotransport, and a salt form of the agent, and optionally a permeation enhancer. Methods of enhancing transdermal electrotransport delivery and of forming a composition for the enhancement of transdermal electrotransport drug delivery, and a transdermal electrotransport delivery device (10) utilizing the compositions of the invention are disclosed.

Abstract: The subject invention concerns a compound of formula (X), ##STR1## which can be prepared from the starting material L-lysine, and converted to levobupivacaine by cyclization.

Abstract: The present invention is directed to a compound of the following formula: ##STR1## pharmaceutical compositions containing the same and the use thereof as an anticonvulsant.

Abstract: The invention relates to novel amino acid derivatives, to a process for their preparation and to their use as pesticides, in particular as fungicides, and as intermediates for preparing known substituted amino acid derivatives with fungicidal activity.

Abstract: The invention relates to compounds of formula ##STR1## and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.

Abstract: Novel substituted fluorene compunds of Formula I are active as melatonergic agents: ##STR1## wherein: X=H, halogen, OH or OZ;Z=C.sub.1-6 alkyl; --(CH.sub.2).sub.m --CF.sub.3 (m=0-2); CD.sub.3 ; or ##STR2## n=1 or 2; and R=C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl, halogen substituted C.sub.1-6 alkyl, or C.sub.1-6 alkoxy substituted C.sub.1-6 alkyl.

Abstract: L-amino acid amides are converted to the corresponding D-amino acid amides. An amide formed from an L-amino acid and an optically active (S)-.alpha.-alkylbenzylamine is subjected to dehydration condensation with an aryl aldehyde to form a Schiff's base, which is racemized at the amino acid moiety in the presence of a base to yield an N-allylidene-D-amino acid-(S)-amide. The less-soluble diastereomer N-allylidene-D-amino acid-(S)-amide is crystallized from the reaction mixture and recovered by means of solid/liquid separation. The N-allylidene form is readily hydrolyzed into the amino acid-(S)-amide and the starting aldehyde.

Abstract: Stilbene compounds of the following formula (I) or their pharmaceutically acceptable salts are effective as carcinostatics and of low toxicity: ##STR1## wherein X represents a hydrogen atom or a nitrile group, and Y represents an amino acid acyl group.

Abstract: The present invention relates to pyridazino[4,5-b]quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino[4,5-b]quinolines as active ingredient, and methods for the treatment of neurological disorders.

Abstract: A novel process for the preparation of .alpha.-aminoacylanilides comprises the treatment of the corresponding .alpha.-haloacylanilides with a solution of ammonium carbamate in aqueous ammonia. The process is especially useful in the preparation of certain active cardiac antiarrhythmic agents, such as tocainide.

Abstract: Isoxazole-4-carboxamides and hydroxyalkylidenecyanoacetamides, pharmaceuticals containing these compounds and their useIsoxazole-4-carboxamide derivatives and hydroxyalkylidene-cyanoacetamide derivatives are suitable for the treatment of carcinoses. These compounds can be prepared by known processes. Some of the compounds are novel and are additionally suitable for the treatment of rheumatic disorders.

Abstract: Isoxazole-4-carboxamide derivatives and hydroxyalkylidene-cyanoacetamide derivatives are suitable for the treatment of carcinoses. These compounds can be prepared by known processes. Some of the compounds are novel and are additionally suitable for the treatment of rheumatic disorders.

Abstract: A method for synthesizing enantiomerically enriched chemical intermediates with predetermined chirality is described. The method comprises formation of a pseudoephedrine amide, followed by stereoselective alkylation at the alpha carbon. The chiral auxiliary can then be cleaved off, affording chiral end products useful for further transformations. The enantiomeric enrichment of the chiral end products may exceed 98%, and the chiral auxiliary can be recovered. Novel amides of pseudoephedrine used in this method are also disclosed.

Abstract: A process for isolating and purifying oxadimethacrylics of the general formula ICH.sub.2 .dbd.C(A)CH.sub.2 --O--CH.sub.2 C(B).dbd.CH.sub.2 Iwhere A and B are selected from the group consisting of --COOR.sup.1, --COR.sup.1, --CONR.sup.2 R.sup.3 and --CN and R.sup.1, R.sup.2 and R.sup.3 are each defined as follows:R.sup.1 is hydrogen, alkyl, substituted or unsubstituted cycloalkyl or cycloalkylalkyl, hydroxyalkyl, aminoalkyl, N-alkylaminoalkyl, N,N-dialkylaminoalkyl, substituted or unsubstituted aryl or arylalkyl,R.sup.2 and R.sup.3 are each hydrogen, alkyl, substituted or substituted cycloalkyl or cycloalkylalkyl, substituted or unsubstituted aryl or arylalkyl,comprises precipitating or crystallizing them from their solutions that contain at least one liquid hydrocarbon compound.

Abstract: 5,6-Dehydronorketamine and derivatives retaining the .alpha.,.beta.-unsaturated carbonyl are disclosed. These end other Michael or Michael-type acceptors and adducts are shown to influence the replication, differentiation or maturation of blood cells, especially platelet progenitor cells. Accordingly, these compounds are used for treatment of thrombocytopenia.

Abstract: Compounds are provided of the following general structure: ##STR1## wherein B is hydrogen or lower alkyl (C.sub.1 -C.sub.4), R.sub.1 is hydrogen or methyl, R.sub.2 is lower alkyl (C.sub.1 -C.sub.4), phenylmethyl or 2-(aminocarbonyl)ethyl, R.sub.3 is H or lower alkyl (C.sub.1 -C.sub.4) and where W and Q are independently selected from phenyl or 4-fluorophenyl. They are useful for providing sedative and antiepileptic activity.

Abstract: The present invention provides the compound having the structure: ##STR1## wherein each of R.sub.1 and R.sub.2 are independently the same as or different from each other; when R.sub.1 and R.sub.2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, wherein each of R.sub.3 and R.sub.4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R.sub.3 and R.sub.4 bond together to form a piperidine group and R.sub.2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8.

Abstract: Compounds of the formula: ##STR1## in which: A represents ##STR2## R represents linear or branched lower alkyl, R.sub.1 represents hydrogen or linear or branched lower alkyl, andR.sub.2 represents aryl or lower arylalkyl or aryl or lower arylalkyl substituted by lower alkyl, lower alkoxy, trifluoromethyl, or halogen, aryl means phenyl or naphthyl, as well as optical isomers, epimers and diastereoisomers and addition salts thereof with a pharmaceutically-acceptable acid, lower alkyl and lower alkoxy having 1 to 6 carbon atoms inclusive, andmedicaments containing the same which are useful for the treatment of disorders of the melatoninergic system.

Abstract: A gasoline detergent additive composition comprising a) the reaction product of a 4-alkyl-2-morpholinone and an alkylphenoxypolyoxyalkylene amine; b) the reaction product of a polyalkenyl succinic acid anhydride and a polyethylene polyamine; and c) a polyalphaolefin. A motor fuel composition is also provided.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or methyl, R.sup.2 is ethyl, propyl, isopropyl, imidazol-2-yl, imidazol-4-yl, pyrazol-3-yl, thiazol-4-yl, thien-2-yl, ethoxycarbonyl, t-butylcarbonylmethyl, benzyloxycarbonylmethyl or t-butoxy, R.sup.3 is isobutyl, cyclohexylmethyl or benzyl, R.sup.4 is nitro, amino or a group of the formula --N(R.sup.5)(R.sup.6) and A is one of the groups ##STR2## wherein R.sup.5 and R.sup.6 is alkyl or alkoxyalkyl; or optionally substituted phenyl, phenylalkyl or phenylsulfonylalkyl among others with the proviso that A is not group (b) when R.sup.6 is alkanoyl, alkoxycarbonyl or arylalkoxycarbonyl, the dotted line can be an additional bond, R.sup.7 is phenyl or substituted phenyl and R.sup.8 is hydrogen or organocarbonylalkyl, with the proviso that R.sup.8 is not alkoxycarbonylamino or arylalkoxycarbonylamino when R.sup.7 is phenyl, benzyl or .alpha.

Abstract: The present invention provides the compound having the structure: wherein each of R1 and R2 are independently the same as or different from each other; when R1 and R2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R1 and R2 are different, R1=R3—N—R4, wherein each of R3 and R4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R3 and R4 bond together to form a piperidine group and R2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8. The present invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells.