Abstract: A compound which is selected from those of formula (I) : ##STR1## in which A, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined in the description, its optical isomers, and its addition salts thereof with a pharmaceutically-acceptable acid or base,and medicinal products containing the same which are useful for treating a disorder of the melatoninergic system.

Abstract: Certain N-acyl-cycloalkylamine derivatives are useful as melatonergic agents.

Abstract: Novel o-phenylenediamines of the formula containing fluoroalkyl(ene) groups ##STR1## in which the symbols used have the meaning given in the description, processes for their preparation and their use as intermediates.

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

Abstract: The invention describes N-fluorosulfonimides which are useful as fluorinating agents. The N-fluorosulfonimides are stable, easily synthesized, and allow the introduction of fluorine into organic compounds under mild conditions.

Abstract: An anilide derivative useful as an atherosclerosis treating drug, represented by the following formula (I): ##STR1## wherein X is an alkyl group having 1 to 4 carbon atoms or an alkoxy group having 1 to 4 carbon atoms; Y is a hydrogen atom or an alkoxy group having 1 to 4 carbon atoms; Z is an alkyl group having 1 to 4 carbon atoms or an alkoxy group having 1 to 4 carbon atoms; A is an alkylene group having 1 to 4 carbon atoms; R is an alkyl group having 6 to 20 carbon atoms, an alkanoyl group having 2 to 20 carbon atoms or a benzyl group which may be substituted with an alkyl group having 1 to 4 carbon atoms; and n is 0, 1 or 2.

Abstract: The compound of the formula (I) or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants ##STR1##

Abstract: A compound which is selected from those of formula (I): ##STR1## in which A, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined in the description, its optical isomers, and its addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful for treating a disorder of the melatoninergic system.

Abstract: The compound of the formula (I) or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.

Abstract: The invention provides the substantially geometrically pure cis-stereoisomeric form of a compound of formula (I) and the substantially geometrically and optically pure cis-stereoisomeric form of a compound of formula (II): ##STR1## wherein R.sup.1 is H or C.sub.1 -C.sub.4 alkyl, together with processes for their preparation. The compounds are intermediates for the preparation of the antidepressant agent known as sertraline.

Abstract: A process for preparing compounds of the formula ##STR1## where a, b, c, R.sub.1, R.sub.2, and R.sub.3 are as defined herein including the step of alkylating a phenol of formula ##STR2## with an acetylene of formula ##STR3## where X is chlorine; bromine; --OC(O)--R.sub.5, where R.sub.5 is alkyl, aryl or substituted aryl; or --OCO.sub.2 R.sub.6, where R.sub.6 is alkyl or ##STR4## in the presence of a catalytic amount of a cuprous or cupric salt. The compounds of formula I are intermediates useful in the preparation of pyranyl cyanoguanidine derivatives.

Abstract: The invention provides the substantially geometrically and optically pure trans-stereoisomeric form of a compound of formula (I): ##STR1## wherein R.sup.1 is H or C.sub.1 -C.sub.4 alkyl, together with processes for its preparation. The compounds are intermediates for the preparation of the antidepressant agent known as sertraline.

Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising an iodoaniline derivative as the x-ray producing agent in combination with a pharmaceutically acceptable clay in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.

Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising an x-ray producing agent of the formula or a pharmaceutically acceptable salt thereof ##STR1## and methods for their use in diagnostic radiology of the gastrointestinal tract, whereinZ is H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.25 alkyl, cycloalkyl, acetyl or halo-lower-alkyl, wherein said C.sub.1 -C.sub.

Abstract: Novel bicyclic amides of the formula ##STR1## wherein Ar.sup.1 and Ar.sup.2 are phenyl, R.sup.2 -substituted phenyl, heteroaryl or R.sup.2 -substituted heteroaryl, wherein R.sup.2 is 1 to 3 substituents independently selected from the group consisting of halogeno, hydroxy, lower alkyl, lower alkoxy, nitro, amino, lower alkylamino and lower dialkylamino;X, Y and Z are --CH.sub.2 --, --CH(alkyl)--, --C(alkyl).sub.2 --, --NH--, --N(alkyl)--, --O-- or --SO.sub.r, wherein r is 0, 1 or 2, and m, n and p are 0 or 1;R.sup.1 is an alkyl chain of 1 to 25 carbon atoms; an alkyl chain substituted by one or more optionally substituted phenyl or heteroaryl groups; an alkyl chain --O--, --SO.sub.r, phenylene, R.sup.2 -substituted phenylene, heteroarylene or R.sup.

Abstract: Compounds of the formula ##STR1## wherein m is zero or 1; n is zero, 1 or 2; p is zero or 1 to 6 provided that m and p are not both zero; R.sub.3 is hydrogen, acyl, or benzyl; and R.sub.1 is hydrogen, alkyl, phenyl, substituted phenyl, phenyl-alkylene, heterocyclic-alkylene, etc. These compounds are useful as cardiovascular agents.

Abstract: Fiber-reactive formazan dyes are prepared by diazotizing a protectively formylated hydroxyphenylenediamine, coupling with a hydrazone compound, metallizing, eliminating the protective group, and reacting with a halotriazine and optionally thereafter with an amine or a hydroxy compound via novel aminophenol intermediates.

Abstract: Reactive dyestuffs which, in the form of the free acid, have the following formula ##STR1## in which X denotes fluorine, chlorine or bromine andSO.sub.2 -Z denotes a specific reactive radical,the remaining substituents having the meaning given in the description, and show improved fixation yield in dyeing.

Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, independently, hydrogen, straight or branched chain alkyl or mono- or bi-cyclic alkyl;A is a substituted phenyl group containing one or two substituents selected from cyano, nitro, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, alkylcarboxamido, arylcarboxamido, alkylsulfone, perfluoroalkylsulfone, arylsulfone, chloro, bromo, fluoro, iodo, 1-imidazolyl or carboxyl; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.

Abstract: The present invention relates to N-carbonyl anilines which are intermediates for the preparation of pesticidal 1-aryl imidazoles and to processes for making them.

Abstract: The present invention is a novel compound which is a 3,5-di-t-butyl-4-hydroxyphenylmethylhydroxylamine or derivative thereof and a pharmaceutically acceptable acid addition or base salt thereof, pharmaceutical composition and methods of use therefor. The invention compounds are now found to have activity as inhibitors of one or both of cyclooxygenase and 5-lipoxygenase providing treatment of conditions advantageously affected by such inhibition including inflammation, arthritis, pain, fever, and the like.

Abstract: This invention relates to structurally novel acyclic tocotrienol analogs, which are useful for cholesterol/lipid lowering in cases of hypercholesterolemia and hyperlipidemia, and for atherosclerosis. Also provided are pharmaceutical compositions and a method of use employing those compositions.

Abstract: Acylamides or amine acylate salts of arylalkanolamines are prepared by reacting an arylisonitrosoalkanone with hydrogen and a carboxylic acid, carboxylic acid anhydride or carboxylic acid ester or mixture thereof in the presence of a transition metal catalyst; optionally the product is converted to the corresponding arylalkanolamine hydrochloride salt by reaction of the acylamide or amine acylate salt of the arylalkanolamine with hydrogen chloride in a C.sub.1 -C.sub.3 alkyl alcohol.

Abstract: A keratinous fiber dye composition comprising a developer and a coupler, wherein the coupler is a 2-substituted amino-5-alkylphenol derivative represented by the following formula (1): ##STR1## wherein the all symbols are defined in the disclosure, is disclosed. The keratinous fiber dye composition imparts a color tone of a high chroma and is excellent in coloring power and fastness.

Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a polymeric material capable of forming a coating on the gastrointestinal tract and an x-ray producing agent of the formula ##STR1## and methods for their use in diagnostic radiology of the gastrointestinal tract whereinZ=H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.25 alkyl, cycloalkyl acetyl, or halo-lower-alkyl, wherein said C.sub.1 -C.sub.25 alkyl, cycloalkyl, acetyl and halo-lower-alkyl are optionally substituted with, fiuoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy;n is 1-5;y is 1-4; andx is 1 or 2in a pharmaceutically acceptable carrier.

Abstract: Disclosed are contrast agents of the formula ##STR1## contained in aqueous compositions and methods for their use in diagnostic radiology of the gastrointestinal tract whereinZ=H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.25 alkyl, cycloalkyl, acetyl or halo-lower-alkyl, wherein said C.sub.1 -C.sub.25 alkyl, cycloalkyl, acetyl and halo-lower-alkyl are optionally substituted with fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy,n is 1-4;y is 1-4; andx is 1 or 2.

Abstract: Disclosed is a process for producing 2-fluoro-4-(trifluoromethyl) acetanilide which comprises reacting 3,4-difluorobenzotrifluoride with acetamide in the presence of a base in an aprotic polar solvent or in a mixture of an aprotic polar solvent and an aprotic non-polar solvent.

Abstract: Diacylpiperazines of general structure ##STR1## are: angiotensin II (A-II) antagonists selective for the type 2 (AT.sub.2) subtype useful in the treatment of cerebrovascular, cognitive, and CNS disorders; tachykinin receptor antagonists useful in the treatment of inflammatory diseases and pain or migraine; and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.

Abstract: The present invention relates to novel substituted pyrimidobenzimidazole derivatives of the formula ##STR1## wherein the substituents are as described in the specification, and pharmaceutically acceptable salts thereof.The products have an inhibitory action on the DNA-gyrase activity in bacteria. They can accordingly be used for the prevention or control of bacterial infections.

Abstract: A process for preparing phenoxyethanamines from phenols and 2-oxazolines in quantitative yields was discovered. Phosphoric acid hydrolyzes the amide intermediate from the phenol/2-oxazoline reaction without cleaving the amide at the ether linkage and without undesired aromatic ring substitution. Thus, yield to the desired phenoxyethanamines is often 98% or better, requiring no subsequent purification. In contrast, sulfuric and hydrochloric acids give these undesired side reactions. Phenoxyethanamines are useful in thermosetting resins, pharmaceuticals and as surfactants.

Abstract: The present invention provides methods for inhibiting protein kinase C which comprise contacting protein kinase C with an inhibitory amount of a compound having the formula ##STR1## wherein R.sub.1 is C.sub.8 through C.sub.15 alkyl; R.sub.2 is H, C.sub.1 through C.sub.10 alkyl, or benzyl; R.sub.3 is N-heterocyclic, N-alkylheterocyclic, quaternized N-heterocyclic, NR.sub.4 R.sub.5 or N.sup.+ R.sub.4 R.sub.5 R.sub.6 X.sup.- ; R.sub.4, R.sub.5 and R.sub.6 are independently C.sub.1 through C.sub.10 alkyl; n is 2, 3, 4, or 5; and X is an anion. The invention also provides novel compounds having the formula ##STR2## wherein R.sub.1 is C.sub.8 through C.sub.15 alkyl; R.sub.2 is H, C.sub.1 through C.sub.10 alkyl, or benzyl; R.sub.3 is N-heterocyclic, N-alkylheterocyclic or quaternized N-heterocyclic; and n is 2, 3, 4, or 5.

Abstract: Methods of producing N-aryl amides comprise reacting an aromatic isocyanate compound with substantially anhydrous carboxylic acid and recovering the resulting N-aryl amide. Additionally, or alternatively, methods of forming N-aryl amides comprise reacting an aromatic isocyanate compound with substantially anhydrous carboxylic acid in the presence of an anhydrous hydrogen halide or hydrolytically unstable halide compound and recovering the resulting N-aryl amide. These reactions may occur in the presence of an aprotic solvent.

Abstract: A process for producing an amide which comprises subjecting an oxime to liquid phase rearrangement in the presence of phosphorus pentoxide and at least one compound selected from the group consisting of N,N-dialkyl amides, N-alkyl cyclic amides and dialkyl sulfoxides and optionally a fluorine-containing strong said or its derivative. Said process can rearrange an oxime to a corresponding amide in a good yield under mild reaction conditions in the presence of a less stoichiometric amount of a catalyst.

Abstract: Substituted anilino-nicotinic acid derivatives are readily prepared from the condensation of two intermediates, 2-alkyl-3-perfluoroalkyl-anilines and alkyl 2-chloronicotinates. The 2-alkyl-3-perfluoroalkyl-aniline intermediate can be prepared via a novel three step synthesis. 3-Perfluoroalkyl-anilines are reacted with an amine directing protecting group reagent to protect the amine. The protected amine is then alkylated, and finally, the directing group is removed to form the 2-alkyl-3-perfluoroalkyl-aniline intermediate. The 2-alkyl-3-perfluoroalkyl-aniline intermediate is condensed with the alkyl 2-chloronicotinate to form the anilino-nicotinic acid derivative.

Abstract: The present invention relates to a process for producing an aromatic nitro compound by introducing a nitrogen oxide gas and ozone-containing oxygen or air into a halogenated organic solvent dissolving or suspending therein an aromatic compound, thereby subjecting the aromatic compound to nitration. By the use of a system comprising the nitrogen oxide and ozone-containing oxygen or air as the nitrating agent, the aromatic nitro compound can be produced under mild conditions without using any mineral acid. In addition, the various disadvantages due to the use of mineral acid in the conventional process can be avoided by the process of the present invention.

Abstract: A reaction accelerator for rearrangement of an oxime to an amide consisting of an alkylating agent and an N,N-disubstituted formamide or N,N-disubstituted carboxylic acid amide represented by formula (1): ##STR1## wherein R.sup.1 and R.sup.2, which may be the same or different, represent alkyl groups having 1 to 6 carbon atoms or substituted or unsubstituted phenyl groups having 6 to 9 carbon atoms, and R.sup.3 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms. An amide can effectively be produced by rearranging a corresponding oxime in the presence of said reaction accelerator.

Abstract: Sulfonyl compounds of the formula ##STR1## where Ar is the radical of a benzene or naphthalene ring,R.sup.1 and R.sup.2 are each hydrogen, substituted or unsubstituted C.sub.1 -C.sub.4 -alkyl, substituted or unsubstituted phenyl, C.sub.1 -C.sub.4 -alkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, cyano, halogen or hydroxysulfonyl,R.sup.3 is nitro, amino, C.sub.1 -C.sub.4 -alkanoylamino or benzoylamino, andR.sup.4 is a radical of the formula ##STR2## where X.sup.1, X.sup.2 and X.sup.3 are each hydrogen, substituted or unsubstituted C.sub.1 -C.sub.4 -alkyl or substituted or unsubstituted phenyl, andX.sup.4 is a group which is detachable under alkaline conditions,either in the free form or in the form of their salts, are useful for synthesizing reactive dyes.

Abstract: The invention concerns novel pharmaceutical compositions for use in the treatment of certain complications of diabetes and galactosemia and which contain a nitromethane derivative (or its non-toxic salt) as active ingredient. The nitromethane derivatives are inhibitors of the enzyme aldose reductase. Many of the inhibitors are novel and are provided, together with processes for their manufacture and use, as further features of the invention.

Abstract: Disclosed is a method which comprises introducing into a reaction zone a feed which comprises a hydroxyl compound reactant, R"OH at least one amide reactant selected from R--CONH.sub.2 and R--CONHR', and a Lewis base as catalyst, thereby reacting R"OH with said amide reactant to produce a reaction mixture containing at least one disubstituted amide selected from R--CONR".sub.2 and R--CONR'R", whereineach of R, R' and R" contains no acetylenic unsaturation and 1 to 30 carbon atoms;each of R, R' and R" is selected from a hydrocarbyl groups and a hydrocarbyl group that is substituted with a group selected from carbamoyl, hydrocarbylcarbamoyl, dihydrocarbylcarbamoyl, and hydroxyl.

Abstract: The invention relates to a process for the preparation of compounds of formula ##STR1## wherein R is unsubstituted or substituted C.sub.1 -C.sub.4 alkyl or unsubstituted or substituted phenyl, X is hydrogen or unsubstituted or substituted C.sub.1 -C.sub.4 alkyl, and Y is unsubstituted or substituted C.sub.1 -C.sub.4 alkyl, which process comprises subjecting compounds of formula ##STR2## wherein R, X and Y are as defined for formula I, to catalytic hydrogenation in the alkaline pH range.The compounds obtained by the process of this invention are suitable intermediates for the synthesis of dyes.

Abstract: This invention concerns a process for preparing diketones and keto-acids by reacting a dicarboxylic acid and an aromatic compound in the presence of an alkylsulfonic acid such as methanesulfonic acid and an organic anhydride compound such as methanesulfonic anhydride or trifluoroacetic anhydride. The diketones and keto-acids can be used to prepare polyketones which are useful as molding plastics, coatings, films, fibers, and the like.

Abstract: A process to prepare compounds of formula I ##STR1## in which n=0, 1 or 2 comprising the cyclization of compounds of formula II ##STR2## in which n=0, 1 or 2. The cyclization may be effected in the presence of an organic or inorganic base or thermally at a temperature in the range 40.degree.-160.degree. C.Compounds of formula II and certain analogues thereof are disclosed as cardiovascular agents.

Abstract: The present invention relates generally to compounds having melatonin receptor activities and in particular to substituted 2-amidotetralin derivatives; to pharmaceutical preparations comprising such compounds; and to methods for using these compounds as therapeutic and diagnostic reagents.

Abstract: 2-Chloro and 2,6-dichloroanilines, optionally substituted in the 3-, 5-, and/or 6-position are prepared from the corresponding anilides by selective bromination, chlorination, reduction and hydrolysis. The selectivity of the process for introducing chlorines ortho to the amino group is very high.

Abstract: A process to prepare compounds of formula I ##STR1## in which n=0, 1 or 2 comprising the cyclisation of compounds of formula II ##STR2## in which n=0, 1 or 2. The cyclisation may be effected in the presence of an organic or inorganic base or thermally at a temperature in the range 40.degree.-160.degree. C.Compounds of formula II and certain analogues thereof are disclosed as cardiovascular agents.

Abstract: The fibre-reactive formazan dyes of the formula ##STR1## where B is an aliphatic or sulfo-free aromatic bridge member, R is .alpha.,.beta.-dihalopropionyl, .alpha.-haloacryloyl or haloacetyl, T.sub.1 is halogen, X is halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, cyano or nitro, Y is --CO-- or --SO.sub.2 --, Z is nitrogen or --C--T.sub.2, T.sub.2 is halogen, hydrogen, C.sub.1 -C.sub.4 alkylthio, cyano, formyl or C.sub.1 -C.sub.4 alkylsulfonyl, m is 1, 2 or 3, n is 0, 1 or 2, qu is 0 or 1 and r and s are each eitehr 0 or 1 but never the same as each other, produce dyeings having good fastness properties on nitrogen-containing or hydroxyl-containing fibre materials.

Abstract: Novel 4'-hydroxybenzylamine derivatives of the formula ##STR1## pharmaceutical compositions and methods of use thereof are the present invention. Utility is for the treatment of arthritis, asthma, Raynaud's disease, inflammatory bowel disorders, trigeminal or herpetic neuralgia, inflammatory eye disorders, psoriasis, dental pain, and headaches, particularly vascular headache, succh as migraine, cluster, mixed vascular syndromes, as well as nonvascular, tension headaches.

Abstract: A compound of the formula: ##STR1## wherein R is a C.sub.1 -C.sub.5 alkyl group, a C.sub.3 -C.sub.5 alkenyl group, a C.sub.3 -C.sub.5 alkynyl group or a C.sub.3 -C.sub.7 cycloalkyl group, which is useful as a herbicide.

Abstract: Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is C.sub.1-12 -alkyl, which may optionally be substituted by hydroxy, formyl, carboxy, carboxylic esters, amides or amines, C.sub.3-8 -cycloalkyl, aryl, aralkyl; and wherein R.sup.6 is, hydrogen, halogen, CN, CF.sub.3, NO.sub.2, or OR', wherein R' is C.sub.1-4 -alkyl and R.sup.5, R.sup.7 and R.sup.8 is hydrogen, provided R.sup.6 is not CF.sub.3, OCH.sub.3, NO.sub.2, C.sup.1 or Br when R.sup.1 is CH.sub.3 ; orR.sup.6 and R.sup.7 independently are NO.sub.2, halogen, CN, CF.sub.3, or OR', wherein R' is C.sub.1-4 -alkyl, and R.sup.5 and R.sup.8 are each hydrogen; orR.sup.5 and R.sup.6 together form a further fused aromatic ring, which may be substituted with halogen, NO.sub.2, CN, CF.sub.3 or OR', wherein R' is C.sub.1-4 -alkyl, and R.sup.7 and R.sup.8 independently are hydrogen, halogen, CN, CF.sub.3, NO.sub.2 or OR', wherein R' is C.sub.1-4 -alkyl; orR.sup.7 and R.sup.

Abstract: The invention concerns compounds of formula I ##STR1## wherein: X and Y are independently selected from the group consisting of hydrogen, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 haloalkyl, and the group wherein X and Y together from a three or four-membered carbon bridge the bridge optionally comprising one or both of a double bond and a carbonyl group;Z is selected from the group consisting of hydrogen, halogen, C.sub.1 to C.sub.4 alkyl and C.sub.1 to C.sub.4 alkanoyl;R.sup.1 is selected from the group consisting of: hydrogen; an acyl group; and an inorganic or organic cation;R.sup.2 is selected from the group consisting of: C.sub.1 to c.sub.6 alkyl; C.sub.2 to C.sub.6 alkenyl; C.sub.2 to C.sub.6 haloakenyl; C.sub.2 to C.sub.6 alkynyl; and substituted C.sub.1 to C.sub.