Abstract: Amphiphilic oligo(p-phenylene vinylene) compounds and methods of use en route to self-assembled composites and device fabrication.

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: Substituted propane-1,3-diamine derivatives, methods for producing such derivatives, and medicaments and pharmaceutical compositions containing such derivatives useful for the treatment or prophylaxis of pain, urinary incontinence, itching, tinitus aurium, or diarrhea are provided.

Abstract: The present invention relates to pharmaceutically acceptable compounds, including acylguanidine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.

Abstract: The present invention provides a new fluorine-containing acetophenone derivative useful as a photo initiator, and a surface layer material containing the fluorine-containing acetophenone derivative. The present invention provides inexpensively an article with a hard coat excellent in anti-staining property, lubricity, scratch resistance and abrasion resistance, and provides a method for forming the hard coat. A fluorine-containing acetophenone derivative represented by the following general formula (I): wherein R1, R2 and R3 each independently represent an organic group other than aryl group, a hydrogen atom, a halogen atom or a hydroxyl group, provided that the following case does not take place: all of R1, R2 and R3 are simultaneously hydrogen atoms; and any two of R1, R2 and R3 may be linked to each other to form a ring, and R4 represents a fluorine-containing organic group.

Abstract: A compound of the formula: wherein Ar is optionally substituted phenyl, etc.; n is 0, 1 or 2; R1 is hydogen atom, optionally substituted alkyl, etc.; R2 and R3 are independently optionally substituted alkyl, etc.; R4 and R5 are independently hydrogen atom or optionally substituted alkyl; R6 is hydrogen atom, hydroxy or alkyl; or a pharmaceutically acceptable salt thereof is useful as a medicament for treating retinal degenerative disorders and the like.

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. In formula (I) D represents CH2 or CH2CH2, E represents C(O)NH or NHC(O) and R3 represents a group of formula (I).

Abstract: Combinatorial libraries are disclosed which are represented by Formula I: (T′—L)q—Ŝ—C(O)—L′—II′  I wherein: Ŝ is a solid support; T′—L— is an identifier residue; and —L′—II′ is a ligand/linker residue. These libraries contain dihydrobenzopyrans of the formula: which interact (i.e., as agonists or antagonists) with &agr; adrenergic receptors, dopamine receptors, &dgr;-opiate receptors, and K+ channels and are inhibitors of carbonic anhydrase isozymes. They are useful in the treatement of ocular diseases such as glaucoma.

Abstract: There is provided a process for the preparation of 2-aryl-5-(perfluoroalkyl)pyrrole compounds from N-[1-chloro-1-(perfluoroalkyl)methyl]arylimidoyl chloride compounds. The 2-aryl-5-(perfluoroalkyl)pyrrole compounds are useful for the control of insect and acarid pests, and may also be used to prepare other pesticidal arylpyrrole compounds. In addition, the present invention provides compounds which are useful as intermediates in the preparation of arylpyrrole compounds.

Abstract: This invention relates to new compositions comprising predominantly one enantiomer of an N-acetonylbenzamide fungicide, methods of preparing N-acetonylbenzamides, and their use as fungicides.

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: Compounds of the formula: are provided, and are useful as cysteine protease inhibitors, particularly in the treatment of diseases such as osteoporosis or autoimmune disorders in which cathepsins K or S contribute to the pathology or symptomatolgy of the disease.

Abstract: Disclosed are methods for treating or preventing inflammatory bowel disease (IBD) using amide and related compounds. Pharmaceutical compositions containing amide compounds which are useful for the treatment or prophylaxis of IBD are also disclosed.

Abstract: A compound of the formula: 1

Abstract: A process for the preparation of primary aromatic carboxamides by the carbonylation of an aromatic compound, which contains at least one leaving group, with carbon monoxide, in the presence of a homogeneous or heterogeneous Pd catalyst and at least stoichiometric amounts of an amidation agent at elevated temperatures, which is characterized in that a primary carboxamide or a primary urethane is used as the amidation agent, and the reaction is carried out in the presence of an acylation catalyst.

Abstract: Benzamides of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: R1—C1-C6-alkyl, branched or unbranched, where one of the C atoms in this chain may be substituted by a phenyl ring, cyclohexyl ring, indolyl ring and an SCH3 group, and the phenyl ring in turn is substituted by by [sic] a maximum of two R4 radicals, where R4 [lacuna] hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, NHCO—C1-C4-alkyl, and R2 can be NR5CO—R6 and NHR5SO2—R6, and R3 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl, CN, COOH, CONH2, COO—C1-C4-alkyl, SO2—C1-C4-alkyl, —SO2Ph, SO2NH—C1-C4-alkyl, iodine, SO2NH2 and NH2, and A can be arom

Abstract: The invention concerns compounds of formula (I) in which: A forms a tricyclic system of formula A1, A2, A3 or A4; R1 represents a hydrogen atom, an alkyl, hydroxy, alkoxy or oxo group; (R2)m and (R3)m′ are such as defined in the description; n represents an integer such that 0≦n≦3; p represents an integer such as defined in the description; B represents a group (a) or (b). The invention is useful for preparing medicines.

Abstract: The invention relates to benzamidoxim derivatives of formula (I) wherein the substituents have the following meanings: R1 represents difluoromethyl or trifluoromethyl, R2 represents hydrogen or fluorine, R3 represents C1-C4 alkyl optionally substituted with cyano, C1-C4 halogenalkyl, C1-C4 alkoxy-C1-C4 alkyl, C3-C6 alkenyl, C3-C6 halogenalkenyl, C3-C6 alkinyl, C3-C8 cycloalkyl-C1-C4 alkyl, R4 represents phenyl-C1-C6 alkyl, which can carry one or more substituents selected from the group composed of halogen, C1-C4 alkyl, C1-C4 halogenalkyl, C1-C4 alkoxy or C1-C4 halogenalkoxy on the phenyl ring, or thienyl-C1-C4 alkyl, which can carry one or more substituents selected from the group composed of halogen, C1-C4 alkyl, C1-C4 halogenalkyl, C1-C4 halogenalkoxy on the thienyl ring, or pyrazol-C1-C4 alkyl, which can carry one or more substituents selected from the group composed of halogen, C1-C4 alkyl, C1-C4 halogenalkyl, C1-C4 alkoxy or C1-C4 halogenalkoxy on the pyrazol ring.

Abstract: The invention pertains to a novel ionophore having the general structure: wherein R1, R2, R3 and R4 are independently straight or branched chain alkyl having 4 to 12 carbon atoms or the alkyl groups may optionally contain a cycloalkyl group having 3 to 8 carbon atoms or R1 and R2 or R3 and R4 together with N to which they are attached, can form a ring having 5 to 8 carbon atoms. This ionophore has increased selectivity for carbonate ions over other ions, especially salicylate. The invention includes membranes containing effective amounts of the novel ionophores and -sensors containing these membranes.

Abstract: Aldehydes are catalytically combined with amines to form carboxamides in one step using an oxidant and a metal-ligand complex or metal/ligand composition.

Abstract: A method of producing benzamides represented by the following general formula (1): where R is trifluoromethyl group, trifluoromethyloxy group, halogen (fluorine, chlorine, bromine or iodine), nitro group, acetyl group, cyano group, alkyl group having 1 to 4 carbon atoms, alkoxy group having 1 to 4 carbon atoms, or a alkoxycarbonyl group having 2 to 5 carbon atoms; and n is 0 or an integer ranging from 1 to 3.

Abstract: The present invention provides compounds of the formula where R1-R5 are each, independently, a hydrogen atom or a normal or branched C1-C6-alkyl group; A is a methionyl, phenylalanyl or phenylglycyl residue; n is 0 or 1; R6 is a hydrogen atom; and R7 is a carbocylic group, an aromatic group, a C1-C4-alkyl group, a pyridylalkyl group or a heterocyclic group. In another embodiment, R6 is benzyl or —C(O)OR8, where R8 is a C1-C6-alkyl group, and R7 is a heteroaromatic group, such as a 2-thiazolyl group.

Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, or hydroxy; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, or pyridyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine. These compounds are useful as kappa agonists.

Abstract: A compound of the formula wherein R1 and R2 are H, a hydrocarbon group or a heterocyclic group, or R1 and R2 are combinedly a spiro ring; R3 is a hydrocarbon group, a substituted amino group, a substituted hydroxyl group or a heterocyclic group; R4 is H or alkyl; ring A is a substituted benzene ring; m and n denote 1 to 4; {overscore (.........)} means a single or double bond or a salt, a process of producing thereof and a composition having a binding affinity for melatonin receptor.

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

Abstract: The invention relates to new oxime derivatives, to a plurality of processes for their preparation, and to their use as pesticides.

Abstract: A process is provided for increasing the fluorine content of benzene or pyridine rings which are optionally substituted with from 1 to 3 inert substituents. The process involves (a) contacting the ring with a metal fluoride composition comprising cupric fluoride (CuF.sub.2) at a temperature above 250.degree. C. sufficient to transfer F from cupric fluoride to the optionally substituted ring, thereby chemically reducing the metal fluoride composition; (b) oxidizing the reduced metal fluoride composition from (a) in the presence of HF to regenerate a metal fluoride composition comprising cupric fluoride; and (c) employing regenerated metal fluoride composition of (b) in (a).

Abstract: A phenylenediamine derivative or a salt thereof in accordance with the present invention is expressed by the following formula 1: ##STR1## wherein A represents a group expressed by --CO--, --CH.sub.2 CO--, --CS--, or --SO.sub.2 --; Y represents a carbon atom or nitrogen atom; R.sub.1 represents a lower alkyl group; R.sub.2 represents a hydrogen, lower alkyl, alkenyl, benzyl, or benzoyl group; and each of R.sub.3 and R.sub.4 represents an alkyl group having 1-10 carbon atoms. The phenylenediamine derivative above mentioned, as a radical scavenger, has antioxidant effect and lipid peroxidation inhibitory activity so as to be available for inhibiting brain infarction or brain edema.

Abstract: 4-Chlorobiphenyls are prepared by reacting a haloaromatic with an aryl Grignard compound, where halogen is chlorine, bromine or iodine, in the presence of a palladium catalyst of the formula (IV) ##STR1##

Abstract: An alkylenediamine derivative or a salt thereof expressed by the following formula 1: ##STR1## wherein each of R.sub.1 and R.sub.2 represents a lower alkyl group, and W represents a group expressed by any of the following formulas 2 and 3; ##STR2## wherein all variables are as defined in the specification The alkylenediamine derivative has an anti- ulcer effect or an antibacterial activity against Helicobacter pyroli, and has also high safety to be available for prevention or cure of ulcers.

Abstract: A method for binding albumin by contacting an aqueous liquid containing an albumin with an albumin-binding compound is selected from albumin-binding compounds containing the scaffold --CO--NH--C(.dbd.C--)--CO--, and conjugates that are capable of binding albumin and exhibiting the scaffold --CO--NH--C(.dbd.C--)--CO--.

Abstract: The present invention relates to ortho-substituted benzoylguanidines of the formula I, defined in the specification. The invention also embraces processes for making these compounds, as well as compositions and methods of using them. The compounds of the invention exhibit very good antiarrhythmic properties, making them useful in treating or preventing infarction, angina pectoris, and pathophysiological processes associated with ischemically induced damage.

Abstract: This invention relates to a process for the preparation of an .alpha.-chloroketone compound comprising the steps of(i) cyclizing an alkynyl amide to form a 5-methyleneoxazoline ##STR1## (ii) chlorinating the 5-methyleneoxazoline using trichloroisocyanuric acid to produce a chlorinated oxazoline intermediate ##STR2## and (iii) hydrolyzing the chlorinated oxazoline intermediate with an aqueous acid top produce the desired monochloroketone ##STR3## wherein Z is alkyl or substituted alkyl, aryl or substituted aryl, heteroaryl or substituted heteroaryl or phenylene,R is a hydrogen atom or alkyl, andR.sup.1 and R.sup.2 are each independently an alkyl or substituted alkyl group, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form a cyclic structure.Additionally, when R is a hydrogen atom, a dichioroketone can be conveniently formed through adjustment of reaction conditions.

Abstract: Disclosed are 4-(2'-trifluoromethylethyl)benzoylguanidine and 3-methylsulfonyl-4-(2'-trifluoromethylethyl)benzoylguanidine. Also disclosed are pharmaceutical compositions and the use of the compounds in the treatment of disorders induced by ischemia.

Abstract: Ortho-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament containing themOrtho-substituted benzoylguanidines of the formula I ##STR1## in which R(2) and R(3) have the meanings given in the claims, are suitable, as antiarrhythmic pharmaceuticals having a cardioprotective component, for the prophylaxis and treatment of infarction and for the treatment of angina pectoris. They also inhibit, in a preventive manner, the pathophysiological processes associated with the development of ischemically induced damage, in particular in association with the triggering of ischemically induced cardiac arrhythmias.

Abstract: The invention provides a process for the production of a 2,3-dihydroxypropylamino compound, said process comprising the reaction steps of:(i) obtaining an allylamino compound;(ii) epoxidizing said allylamino compound to yield an epoxypropylamino compound; and(iii) hydrolysing said epoxypropylamino compound to yield a 2,3-dihydroxypropylamino compound.This process may be used to produce simple 2,3-dihydroxypropylamino compounds such as APD or complex ones such as BAPD (an intermediate in the production of iohexol).

Abstract: Combinatorial libraries are disclosed which are represented by Formula I:(T'--L).sub.q --S--C(O)--L'--II' Iwherein:S is a solid support; T'--L-- is an identifier residue; and --L'--II' is a ligand/linker residue. These libraries contain dihydrobenzopyrans of the formula: ##STR1## which interact (i.e., as agonists or antagonists) with .alpha. adrenergic receptors, dopamine receptors, .sigma.-opiate receptors, and K.sup.+ channels and are inhibitors of carbonic anhydrase isozymes. They are useful in the treatment of ocular diseases such as glaucoma.

Abstract: Novel aryl amides are inhibitors of tumor necrosis factor .alpha. and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is N-benzoyl-3-amino-3-(3',4'-dimethoxyphenyl)propanamide.

Abstract: 2,4,5-Trihalogenobenzene derivatives of the formula ##STR1## in which R is --COOH, --COCl, --COF, --CN, --CONH.sub.2, --CH.sub.2 OH, --CH.sub.2 Cl, --CHCl.sub.2, --CCl.sub.3 or --CHO,R.sup.1 is H, Cl or F, andR.sup.2 is Cl or F,it only being possible for R.sup.1 or R.sup.2 to be F, and processes for their preparation starting from benzonitriles reacted with potassium fluoride. The novel compounds are intermediates for antibacterials such as quinolone carboxylic acids.

Abstract: A range of 3-oxybenzamide compounds and related quinazolinone compounds are disclosed which can act as potent inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase or PARP enzyme (EC 2.4.2.30), and which thereby can provide useful therapeutic compounds for use in conjunction with DNA-damaging cytotoxic drugs or radiotherapy to potentiate the effects of the latter. The compounds disclosed include 3-benzyloxybenzamides, 3-oxybenzamides in which a chain of 5 or more methylene groups terminate in a halogen atom or in a purin-9-yl moiety, certain benzoxazole-4-carboxamide compounds and certain quinazolinone compounds. In formula X and Y together may form a bride --X--Y-- that represents the grouping (a), (b) or (c )wherein R.sup.5 is H, alkyl, aryl or aralkyl.

Abstract: It is known to prepare fluorinated aromatic compounds of the formula I ##STR1## in which X, Y and Z can have the meaning specified in the description, by reacting aromatic compounds of the formula II ##STR2## in which X, Y and Z have the meaning specified for formula I, with fluorine in a reaction medium.According to the invention, the direct fluorination is carried out in a reaction medium containing polyfluoroalkanesulfonic acids of the formula IIICF.sub.n H.sub.3-n (CFY).sub.m --SO.sub.3 H (III)in whichm, n and Y have the meaning specified in the description.By this means, it is possible, particularly advantageously to provide a process, which improves the known processes not only with regard to the selectivity and the yield, but also with respect to the quality of the resulting products of the process in a manner not readily predictable.Fluorinated aromatic compounds of the formula I as intermediates for active compound synthesis.

Abstract: The invention relates to a compound selected from these of formula (I): ##STR1## in which R.sub.7, R.sub.8, Y, n and A are as defined in the description, and medicinal product containing the same useful for treating a disorder of the melatoninergic system.

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: A compound of the following structure: ##STR1## wherein R.sub.8 =H: R.sub.1 =alkyl, cycloalkyl, arylalkyl, aryl;R.sub.2 =cycloalkyl, aryl, C.sub.3 -C.sub.10 alkyl;X,Y=O, S(O).sub.n, NH;Z=CO.sub.2 R.sub.3, C(O)CO.sub.2 R.sub.3, CH(OH)CO.sub.2 R.sub.3, CHFCO.sub.2 R.sub.3, CF.sub.2 CO.sub.2 R.sub.3, CONR.sub.3 R.sub.4, CONR.sub.3 OR.sub.4, CONR.sub.3 NR.sub.4 R.sub.5, 1-tetrazole, C(O)CONR.sub.3 R.sub.4, CH(OH)CONR.sub.3 R.sub.4, CF.sub.2 CONR.sub.3 R.sub.4R.sub.3, R.sub.4, R.sub.5 =hydrogen, alkyl, aryl, aryalkyl, cycloalkyl, or fluoroalkyl;halo=Cl, Br, or I;fluoroalkyl=CF.sub.3, CHF.sub.2, CH.sub.2 F, CH.sub.2 CF.sub.3, C.sub.2 F.sub.5 ;cycloalkyl=C.sub.3 -C.sub.6 cycloalkyl;arylalkyl=C.sub.1 -C.sub.4 alkyl aryl;aryl=phenyl, furanyl, thienyl, or pyridyl; andn=0-2;or pharmaceutically acceptable salts thereof, useful in the treatment of asthma, and allergic and inflammatory diseases, as well as methods of treatment and pharmaceutical compositions utilizing the same.

Abstract: A method for producing an alkylthiobenzamide by carrying out a reaction of a halobenzamide with an alkanethiol in the presence of a base in a heterogeneous solvent; a method for producing an alkylsulfinylbenzamide by carrying out a reaction of an alkylthiobenzamide with a halogen in a heterogeneous solvent; a method for producing an alkylsulfinylbenzamide by carrying out a reaction of a halobenzamide with an alkanethiol in the presence of a base in a heterogeneous solvent and a subsequent reaction with a halogen; and a method for producing a 1,2-benzisothiazol-3-one by carrying out a reaction of a 2-(alkylthio)benzamide with a halogenating agent.

Abstract: Novel aminoalkyloximes of the formula ##STR1## wherein: a. X is hydrogen, loweralkyl, loweralkoxy, halogen, trifluoromethyl, or a group of the formula ##STR2## wherein Y is hydrogen or loweralkyl, and p is 1 or 2; b. A is a group of the formula ##STR3## c. R.sup.1 and R.sup.2 are independently hydrogen or lowerakyl; and d. m is 2 to 6 and n is 0, or 2 to 6, inclusive, serotonin reuptake inhibitors, useful for treating depression and obsessive compulsive disorders are described. Also described are precursors of and processes for the preparation of such aminoakyloximes.

Abstract: The present invention provides a novel synthesis of the compounds of Formula (I): ##STR1## The compounds are produced in high yield and without utilizing expensive chromatographic separations. The synthesis is particularly advantageous because it is stereoselective.

Abstract: N-Alkenylcarboxamides of the formula I ##STR1## where at least one of the radicals R.sup.1 is hydrogen, the second radical R.sup.1 is hydrogen or C.sub.1 -C.sub.4 -alkyl and R.sup.2 is hydrogen or an aliphatic, cycloaliphatic or aromatic radical, are prepared by reacting an alkenyl carboxylate of the formula II ##STR2## where R.sup.1 has the abovementioned meanings and R.sup.3 is hydrogen or an aliphatic, cycloaliphatic or aromatic radical, and a carboxamide of the general formula III ##STR3## where R.sup.2 has the abovementioned meanings, in the presence of a base.

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.

Abstract: The present invention provides a novel synthesis of the compounds of Formula (I): ##STR1## The compounds are produced in high yield and without utilizing expensive chromatographic separations. The synthesis is particularly advantageous because it is stereoselective.