Abstract: The present invention provides a pharmaceutical composition comprising N-(3-chloro-4-morpholin-4-yl)phenyl-N′-hydroxyimidoformamidine and sulfobutyl ether &bgr;-cyclodextrin or a salt thereof, wherein sulfobutyl ether &bgr;-cyclodextrin increases the solubility of N-(3-chloro-4-morpholin-4-yl)phenyl-N′-hydroxyimidoformamidine and improves the photostability.

Abstract: Gamma-hydroxybutryic acid amides are used in the treatment of drug addiction and especially in the treatment of alcoholism.

Abstract: A sprayable analgesic composition containing an analgesic which is absorbed into the bloodstream through the buccal mucosa and a pharmacologically acceptable liquid carrier.

Abstract: The present invention relates to a non-hazardous brominating reagent from an aqueous alkaline bromine byproduct solution obtained from bromine recovery plant and containing 25 to 35% bromine dissolved in aqueous lime or sodium hydroxide containing alkali bromide and alkali bromate mixture having bromide to bromate stoichiometric ratio in the range of 5:1 to 5.1:1 or 2:1 to 2.1:1 and a pH ranging between 8-12 and also relates to a method for borminating aromatic compounds by using the above brominating agent.

Abstract: The present disclosure describes novel compounds of formula (A), wherein R1-R12, X and Y have the meanings given in the specification and compositions containing them which are particularly useful for treating hair loss in mammals, including arresting and/or reversing hair loss and promoting hair growth. The compounds described herein are cardiac-sparing.

Abstract: A method for processing of hydrogen for the reductive acylation of nitro, azido and cyano arenes is disclosed. More particularly, improved process for the preparation of amides and anilides using C3-C7 carboxylic acids as proton source/acylating agents employing Fe3+-montmorillonite as a catalyst is disclosed.

Abstract: The invention provides novel &bgr;2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with &bgr;2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are of the following general formula, where X1, X2, Y, and Z are defined variables: Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.

Abstract: The present invention relates to compounds and their ability to act as potassium channel openers.

Abstract: According to the invention, N-butyryl-4-amino-3-methyl-methyl benzoate is obtained in a particularly advantageous manner by, initially, reacting o-toluidine with butyric acid chloride, by brominating the reaction product and by reacting the bromide obtained therefrom with carbon monoxide and methanol in the presence of a palladium catalyst. The invention also relates to the important novel chemical compound N-(4-bromine-2-methylphenyl)-butanamide.

Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma and bronchitis. They are also useful in the treatment of nervous system injury and premature labor.

Abstract: The invention concerns a halogenation in position meta of a phenol fuction. Said halogenation comprises a step which consists in halogenating an aromatic derivative of a medium or advantageously strong acid, the aromatic radical being a phenyl substituted in ortho and in para by functions attracting electrons by inductive effect. The invention is applicable to organic synthesis.

Abstract: Compounds having a &bgr;-3 adrenaline receptor agonist and are useful as drugs for the treatment and prevention of diabetes, obesity, hyperlipemia, etc., represented by a general formula (I) and salts thereof, and a process for producing these, and their intermediates, wherein R represents hydrogen or methyl; R1 represents hydrogen, halogen, hydroxy, benzyloxy, amino, or hydroxymethyl; R2 represents hydrogen, hydroxymethyl, NHR3, SO2NR4R4′, or nitro; R6 represents hydrogen or lower alkyl; and X represents methylene, R9 represents hydrogen, one of R7 and R8 represent hydrogen, and the other thereof represents hydrogen, amino, acetylamino, or hydroxy.

Abstract: Object of the present invention is to provide a process for producing an amide compound with high efficiency by subjecting an oxime compound to Beckmann rearrangement in a liquid phase under mild reaction conditions. Namely, the invention relates to a process for producing an amide compound such as &egr;-caprolactam by subjecting an oxime compound such as cyclohexanone oxime to Beckmann rearrangement in a liquid phase, characterized in that the reaction is carried out in the presence of (1) a non-fluorine-containing sulfonic anhydride and an N,N-disubstituted amide compound or (2) at least one compound selected from the group consisting of sulfonic acids and anhydrides thereof, an N,N-disubstituted amide compound, and a carboxylic anhydride.

Abstract: The invention concerns a method for the condensation of aromatic derivative(s) or a sulphinic derivative by a perhalogenated, advantageously perfluorinated, carbon atom. Said method is characterized in that it consists in subjecting said sulphinic derivative and said aromatic derivative to the action of a strong acid whereof the pKa is not more that 0. The invention is applicable to organic synthesis.

Abstract: Compounds of formula (I) 1

Abstract: A process for preparing 4-substituted 2-alkylbiphenyls and 2-alkoxybiphenyls of the formula (I), 1

Abstract: A method of efficiently removing the protective group from a protected hydroxyl or amino group with an allyl derivative by one step reaction under neutral conditions. A protected hydroxyl or amino group is converted into a free hydroxyl or amino group in one-step by adding a reducing agent to an allyl derivative in the presence of nickel dichlorobis (diphenylphospino) propane.

Abstract: The invention relates to compounds of formula I 1

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 a process for preparing a compound of the formula wherein b, Y and R3 are defined as above, useful for preparing novel aralkyl and aralkylidene heterocyclic lactams and imides which are selective agonists and antagonists of serotonin 1 (5-HT1) receptors.

Abstract: Pesticidal substituted anilide compounds having the structural formula I and compositions and methods comprising those compounds for the control of insect pests.

Abstract: The instant invention provides a process for the selective N-formylation of N-hydroxylamines.

Abstract: The present invention provides novel compounds of formula I 1

Abstract: The present invention relates to a compound having the formula: 1

Abstract: The invention relates to a process for preparing cis-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthylamine, or racemic sertraline, corresponding to formula (I) in salt form, starting with 4-(3,4-dichlorophenyl)tetralone of formula (II) according to which (a) the 4-(3,4-dichlorophenyl)tetralone of formula (II) is reacted with N-methylformamide in the presence of formic acid, (b) the reaction medium obtained according to (a) is treated with a base, and (c) the racemic sertraline salt is separated out by selective crystallization with an acid. The invention also relates to N-methylformamide-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthylamine and to its use to obtain racemic sertraline.

Abstract: A method for manufacturing a color coupler used in a silver halide photographic light-sensitive material using an ammonium trihalide. Said method for manufacturing the color coupler comprising the following step: a step for halogenating a coupling position of a four equivalent coupler using a halogenating agent, wherein said halogenating agent is said ammonium trihalide.

Abstract: The invention relates to a process for preparing N-(3-amino-4-fluoro-phenyl)-sulphonamides, N-(3-amino-4-fluoro-phenyl)-carboxamides or N-(3-amino-4-fluoro-phenyl)-carbamates of the general formula (I) in which A represents SO2, CO or CO2 and R represents in each case optionally substituted alkyl or aryl, wherein 1-fluoro-2,4-diamino-benzene of the formula (II) is reacted with sulphonyl chlorides, carbonyl chlorides or chlororformic esters of the general formula (III)  in which A and R are as defined above in the presence of an acid acceptor and in the presence of a diluent at temperatures between −20° C. and +100° C.

Abstract: The halogenation of a compound of formula (1) or formula (2′), wherein Q is an NH2 group optionally in the form of an addition salt, or an NHCOCH3 group, and X is a halogen atom, using a compound of formula X2, in a solvent selected from an anhydrous halogenated hydrocarbon, a mixture of water and a halogenated hydrocarbon and optionally the compound of formula (1) itself, gives a 2-amino or 2-acetamido trifluoromethylbenzene halogenated in the 5 position of the benzene ring.

Abstract: This invention relates to very specific oxyalkylene-substituted m-amidoaniline compounds as intermediates for the production of poly(oxyalkylene)-substituted diazo (or other type) colorants. Such an inventive intermediate compound is produced in a single step by reacting an oxyalkylene oxide or alkoxy oxyalkylester having at least three carbon atoms (branched or unbranched), glycidol, or a glycidyl group directly with m-acetoamidoaniline (as a preferred example) at a relatively low temperature. Propylene oxide is the preferred compound. The propylene oxide selectively reacts with the amine group on the base compound without propoxylating the amido group. Such a specific method thus does not require extra time- and cost-consuming steps of protecting the amido nitrogen from attack. After production, this intermediate may be reacted with, for example, a diazotized aromatic amine to ultimately form a diazo colorant.

Abstract: Process for preparing a key intermediate, 2-methyl-3-trifluoromethylaniline (MTA) of Flunixin, as well as novel intermediates thereof are described.

Abstract: Activated aromatic compounds are more economically ring brominated by reacting the compounds with a sulfoxide/HBr brominating agent while removing water from the reaction mixture. The water removal provides high conversions and yields when employing stoichiometric quantities of reactants.

Abstract: Tertiary aminoaryl compounds, such as N,N'dialkylaminoaryl compounds, are prepared using successive reductive steps without isolation therebetween, at high temperature and pressure. A nitroaryl compound is reduced using a ketone as both solvent and reactant in a reductive environment, and the resulting intermediate is further reacted with an aldehyde in the same reaction mixture without isolation to provide the second substituent on the amino group.

Abstract: This invention provides a process for the manufacture of N-acetyl amino phenol, which process comprises reacting an appropriate phenol and an amide in the presence of a heteropoly acid or its alkali metal salt catalyst.

Abstract: Compounds of the formula ##STR1## These compounds are useful for inhibiting the growth or replication of retroviruses such as HIV.

Abstract: The present invention is a process of converting a hydroxy aromatic into a 2-hydroxy-N-arylacetamide, comprising:(1) treating a reaction mixture comprising a salt of a hydroxy aromatic with an alkylating agent; and(2) treating the reaction mixture with a Smiles solvent system and raising the temperature of the reaction mixture.

Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.7 and R.sub.8 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkoxycarbonyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a phenyl group with either two or three substituents of the following formula: ##STR2## wherein the positions of substitution are R.sub.2,R.sub.3 -, R.sub.2,R.sub.4 -, R.sub.2,R.sub.5 -, R.sub.2,R.sub.6 -, R.sub.3,R.sub.4 -, R.sub.3,R.sub.5 -, and R.sub.2,R.sub.4,R.sub.6 - and R.sub.2 is methyl, ethyl, fluoro, chloro, methoxy or trifluoromethyl; R.sub.3 is methyl, ethyl, fluoro, chloro, methoxy or trifluoromethyl; R.sub.4 is methyl, fluoro, bromo, methoxy or cyano; R.sub.5 is methyl, fluoro, chloro, methoxy, cyano or trifluoromethyl; R.sub.

Abstract: Disclosed are intermediates for the preparation of novel aminocoumaran derivatives of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are a hydrogen atom, an acyl group, an alkoxycarbonyl group, an aliphatic group or aromatic group; R.sup.3, R.sup.4 and R.sup.5 are an optionally acylated hydroxyl, optionally substituted amino group, alkoxy group or aliphatic group, or two of R.sup.3, R.sup.4 and R.sup.5 may be linked together to form a carbocyclic group; R.sup.6 and R.sup.7 are an aliphatic group and at least one of them has a methylene group at the .alpha.-position; R.sup.8 and R.sup.9 are a hydrogen atom or an aliphatic group or aromatic group, or a salt thereof is useful for medicines for preventing and treating various diseases such as arterial sclerosis, hepatopathy, cerebrovascular diseases and the like.

Abstract: There are disclosed compounds of formula I,Ar--CH.sub.2 CH.sub.2 --NH--CR.sup.1 R.sup.2 --X--Y Iin whichAr represents a group, ##STR1## X represents a C.sub.1-12 alkylene chain optionally interrupted or terminated by one or more groups selected from --S(O).sub.n --, --O--, --C(Z)--, CR.sup.6 R.sup.7, phenylmethyne, --NR.sup.8 --, --CONH--, --NHCO-- and --NHCONH--,Y represents an optionally substituted aryl or cycloalkyl group,Z represents O or S,R.sup.1, R.sup.2, R.sup.5 and R.sup.9 each independently represent hydrogen or alkyl C.sub.1-6,R.sup.3 and R.sup.4 represent hydrogen, or R.sup.3 and R.sup.4 together form a group --S--, --NR.sup.9 -- or --CH.sub.2 --,R.sup.6 and R.sup.7 independently represent hydrogen, alkyl C.sub.1-6, fluoro, cyano, or CF.sub.3, provided that at least one of R.sup.6 and R.sup.7 is other than hydrogen,R.sup.8 represents hydrogen or alkyl C.sub.1-6, or when X is interrupted or terminated by more than one --NR.sup.8 -- group may together with another R.sup.8 group form the chain --CH.

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

Abstract: Certain N-acyl 2-aryl cyclopropylmethylamine derivatives are useful as melatonergic agents.

Abstract: A compound of the general formula (I) ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.2 and R.sub.3 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a substituted phenyl group of the following formula: ##STR2## wherein R.sub.4 is F, perfluoroalkyl group of 1 to 10 carbon atoms or perfluoroalkoxy of 1 to 10 carbon atoms; or a pharmaceutically acceptable salt thereof relax smooth muscles.

Abstract: The present invention provides a method for preparation of a compound of the formula (I) useful as a fog restrainer for a silver halide light-sensitive material, especially for a heat-developing light-sensitive material and a synthetic intermediate for the fog restrainer. The method makes it possible to obtain the fog restrainer in good yield and in short steps. ##STR1## wherein, R.sup.1 is alkyl, cycloalkyl, or aryl, R.sup.2 and R.sup.3 are hydrogen atom or alkyl, R.sup.4 is hydrogen atom or acyl, and R.sup.1 and R.sup.4 may be bonded together to form 5- or 6-membered ring.

Abstract: A hydroxylamine derivatives of formula (I): ##STR1## wherein R represents ##STR2## in which R.sup.1 and R.sup.2 represents alkyl group, alkenyl group, alkynyl group, cycloalkyl group, haloalkyl group, haloalkynyl group, alkoxy - alkyl group, phenoxy - alkyl group, alkylthio - alkyl group, alkylsulfonyl - alkyl group, alkylamino - alkyl group, phenyl group, benzyl group, phenethyl group, cinnamyl group, pyridyl group, furyl group, thienyl group, X represents CO.sub.2, CO or SO.sub.2, and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 represent a hydrogen atom or a lower alkyl group, and n represents 0 or 1, and fungicides contain said compound as an active ingredient.The compounds of the present invention have excellent effects for controlling wood-rot fungi, plant diseases and fungi of humans and animals, and are useful as industrial, agricultural and medical fungicides.

Abstract: Novel glutamate receptor antagonists represented by the formula ##STR1## or a pharmaceutically acceptable salt thereof, whereinZ is an alicyclic fused ring having 5 to 7 carbon atoms;R.sup.1 is hydrogen, an alkyl or an arylalkyl; andA is O, CH.sub.2, NR.sup.4, CH.sub.2 NR.sup.4, CN, tetrazole or CO wherein R.sup.4 is hydrogen, alkyl, hydroxyalkyl, aminoalkyl or aralkyl, wherein(i) when A is O, CH.sub.2, NR.sup.4 or CH.sub.2 NR.sup.4 then B is hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, hydroxyalkyl, alkoxy, aminoalkyl, heterocyclic, alkylheterocyclic, heterocyclic-methyl, heterocyclic-ethyl, alkylcarbonyl, cycloalkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heterocyclic-carbonyl, alkylheterocyclic-carbonyl, or when A is NR.sup.4 or CH.sub.2 NR.sup.4 then B is a naturally occurring .alpha.-amino acid moiety joined by an amide bond or B joins with R.sup.4 and the nitrogen to form a four to seven membered heterocyclic ring, provided that when Z is a fused cyclohexyl ring and R.sup.

Abstract: Preparation of N-alkenyl carboxamides of the general formula I ##STR1## in which the radicals R.sup.1 to R.sup.4 independently stand for hydrogen or for aliphatic, cycloaliphatic, or aromatic radicals, which optionally carry inert substituents, wherein an amide of the general formula II ##STR2## in which the radical R.sup.1 has the above meaning, and a carbonyl compound of the general formula III ##STR3## in which the radicals R.sup.2 to R.sup.4 have the above meanings, are caused to react in the presence of a base, said reaction being eithera) carried out in the presence of a carboxylic acid derivative of the general formula IV ##STR4## in which the radical R.sup.5 stands for hydrogen or an alkyl or aryl group and X is a halogen, alkoxy, or carboxylalkyl radical, orb) continued in the presence of a carboxylic acid derivative of the formula IV, and the amide of the formula I is isolated.

Abstract: An improved synthesis of a highly potent HIV reverse transcription inhibitor is disclosed, involving an acetylide and a trifluoromethyl ketone which produces a chiral product in the presence of a chiral amino alcohol.

Abstract: The invention relates to a dye composition for keratinic fibers comprising an oxidation colorant precursor of the type ortho and/or para and a sulfured metaphenylenediamine having formula (I) ##STR1## wherein Z is alkyl, aralkyl, monohydroxyalkyl or polyhydroxyalkyl, aryl or aminoalkyl, as well as the acid salts thereof, with the condition that R.sub.1 and R.sub.2 do not represent simultaneously hydrogen when Z is alkyl or hydroxyalkyl, as well as the acid salts corresponding to the compounds of formula (I).

Abstract: A compound selected from those of formula (I): ##STR1## in which A, R, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined in the description,and a medicinal product containing the same useful for treating a disorder of the melatoninergic system.

Abstract: 2-fluoro-cyclopropylamine is prepared in an advantageous manner by reacting an N-vinyl compound with a carbene of type FXC: (where X=chlorine or bromine) to give the corresponding cyclopropylamine derivative, replacing the radical X in this derivative by hydrogen, by reduction, and finally eliminating the other substituents on the hydrogen atom.