Abstract: The present invention relates to a process for preparing (R)-5-(2-(benzylamino)ethyl)-1-(6,8-difluorochroman-3-yl)-1H-imidazole-2(3H)-thione, and pharmaceutically acceptable salts thereof, especially the hydrochloride salt. The invention also relates to a process for making intermediates useful in the formation of said compound, and to the intermediates, per se.

Abstract: Compounds which modulate quorum sensing in quorum sensing bacteria. Compounds of the invention inhibit quorum sensing and/or activate quorum sensing in various bacteria. Compounds that inhibit quorum sensing are particularly useful for inhibition of detrimental bacterial biofilm formation. Compounds that activate quorum sensing are particularly useful for promoting growth and biofilm formation of beneficial bacterial.

Abstract: Compounds which modulate quorum sensing in quorum sensing bacteria. Compounds of the invention inhibit quorum sensing and/or activate quorum sensing in various bacteria. Compounds that inhibit quorum sensing are particularly useful for inhibition of detrimental bacterial biofilm formation. Compounds that activate quorum sensing are particularly useful for promoting growth and biofilm formation of beneficial bacterial.

Abstract: Methods and compositions for pest control, and more particularly for control of ants, e.g., of the subfamily Myrmicinae, using tyramides.

Abstract: The invention relates to a class of novel surfactants that have utility in the recovery and/or extraction of oil.

Abstract: Provided is a method for modifying a surface of a cyclic olefin copolymer, comprising: coating a compound of the following Chemical Formula 1 on the surface of a cyclic olefin copolymer substrate, irradiating UV light on the cyclic olefin copolymer substrate, and polymerizing a monomer on the cyclic olefin where X is H or F, and n is an integer of 1 to 6.

Abstract: The present invention provides a process for preparing Teriflunomide of formula (I).

Abstract: Acetoacetic acid arylamides are continuously produced from diketene and primary or secondary aromatic amines under the conditions of a reactive distillation in the presence of water. The continuous method provides a high purity of the products, nearly quantitative yields and a high rate of throughput.

Abstract: Process for the synthesis of ivabradine of formula (I): and addition salts thereof with a pharmaceutically acceptable acid.

Abstract: The present invention provides a process for preparing Teriflunomide of formula (I).

Abstract: The invention is directed to 5-(hetero)aryl-4,5-dihydro-(1H)-pyrazole (pyrazoline) derivatives as cannabinoid CB1 receptor agonists, to pharmaceutical compositions comprising these compounds, to methods for their syntheses, methods for preparing novel intermediates useful for their syntheses, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, administered to patients to achieve a therapeutic effect in disorders in which CB1 receptors are involved, or that can be treated via manipulation of those receptors. Compounds of the present invention include compounds of formula (I): wherein the substituents have the definitions given in the specification.

Abstract: Novel pyruvate derivatives exhibiting outstanding neuroprotective effect, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions for prevention and treatment of brain disease including them as effective ingredient are provided.

Abstract: The present invention relates to the use of compounds of the general Formula (XIII): wherein A7 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; A8 is C(R14)2, O, S, or NR12; A9 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; m is 0, or 1 q is 0, or 1 r is 0, or 1 R12 is H, CH3, CH2—CH3, C6H5, OCH3, OCH2—CH3, OH, or SH; R13 is H, CH3, or CH2—CH3; R14 is H, alkyl, alkoxy, OH, or SH;

Abstract: Process for the preparation of compounds of the formula (I) in which X has the meaning indicated in Patent Claim 1, and precursors thereof.

Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, ?-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

Abstract: The invention concerns amide derivatives of the Formula (I) wherein R3 is (1-6C)alkyl or halogeno; Q is aryl or heteroaryl which optionally bears 1, 2, 3 or 4 substituents such as hydroxy, halogeno, trifluoromethyl, cyano, (1-6C)alkyl, (1-6C)alkoxy, halogeno-(1-6C)alkyl, hydroxyl-(1-6C)alkyl, di-[(1-6C)akly]amino-(1-6C)alkyl, hydroxy-(2-6C)alkoxy, (1-6C)alkoxy-(2-6C)alkoxy, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, amino(2-6C)alkylamino, N-(1-6C)alkyl-(1-6C)alkylamino-(2-6C)alkylamino, aryl, aryl-(1-6C)alkoxy, heteroaryl, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyl-(1-6C)alkyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; p is 0-2 and R2 is a substituent such as hydroxy and halogeno; q is 0-4; and R4 includes optionally substituted aryl, cycloalkyl, heteroaryl and heterocyclyl; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cyt

Abstract: A method for the preparation of 4-fluoro-?-[2-methyl-1-oxopropyl]-y-oxo-N-?-diphenylbenzenebutanamide also known as 2-[2-(4-fluorophenyl)-2-oxo-1-phenylethyl]-4-methyl-3-oxo-pentanoic acid phenylamide of the formula I containing about 0.1% or less of ?-[2-methyl-1-oxopropyl]-?-oxo-N-p-diphenylbenzene butanamide, about 0.05% or less of difluoro-?-[2-methyl-1-oxopropyl]-y-oxo-N-?-diphenylbenzene butanamide and about 0.1% or less of 3-[2-(4-Fluorophenyl)-2-oxo-1-phenyl-ethoxy]-4-methyl-pent-2-enoic acid phenylamide.

Abstract: Acetoacetic acid arylamides are produced from deketene and primary or secondary aromatic amines under the conditions of a reactive distillation in the presence of water. The continuous method provides a high purity of the products, nearly quantitative yields and a high rate of throughput.

Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, ?-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

Abstract: A dye of the formula (2) and a process for preparing the same, wherein the radicals are as defined in the specification

Abstract: The present invention relates to a process for the preparation of a compound of the general formula (I), which comprises converting a compound of the general formula (II), in an aprotic organic solvent in the presence of a catalytically active amount of a strong acid (catalyst) or of an agent that liberates a strong acid or of an ammonium salt of a strong acid, it also being possible for the catalyst to be part of the starting material/product, into a compound of formula I, wherein R5, R6 and R8 are each independently of the others a hydrogen atom, a nitro group, a sulfo group, a halogen atom, a pseudohalogen, a group COOR1 or CONHR2 or a C1-8 alkyl, C1-8 alkoxy or aryloxy radical, an amide group, a thioalkyl or thioaryl radical, an alkyl- or aryl-sulfonyl radical, an alkyl- or aryl-sulfinyl radical, a trifluoromethyl group or a phosphono group, R1 and R2 being a hydrogen atom or a C1-8 alkyl radical or an aryl or aralkyl radical, R10 is a group —C(O)CH2C(O)CH3 and R11 is a hydrogen atom or an acyl radical, o

Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.

Abstract: A compound of Formula (I) wherein R1, R2, R3, R4, R5, and R6 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof, pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Abstract: Compounds of the general Formula: in which R1 and R2 are at each occurrence independently hydroxyl, C1-6-alkyl, C1-6-alkoxy, halogen, phenyl or phenoxy; R2 is hydroxyl, C1-6-alkyl, C1-6-alkoxy, halogen, phenyl or phenoxy; R3 is C1-6-alkyl; m is an integer from 0 to 4; and n is an integer from 0 to 5.

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: 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: The invention relates to a method for producing compounds of general formula (I), wherein R1 and R2, each time they occur and independently of each other, mean hydroxy, 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 said method, diketene is reacted with a N-phenyl-p-phenylenediamine of general formula (II), wherein R1, R2, R3, m and n have the meanings given above, in the presence of 3-40% acetic acid and at temperatures of 20 to 100° C., preferably 60 to 70° C. The invention also relates to the compounds (I) with R3=C1,6-alkyl and the enamines that can be obtained from these by reaction with ammonia, and their hydration products.

Abstract: Novel acetoacetarylamides in the form of a solidified melt which are in a form which can be used in industry and is easy to handle and which has a water content of from 3 to 15 percent by weight. These novel acetoacetarylamides have been used for the preparation of colored pigments or agrochemical active ingredients.

Abstract: The invention relates to compositions that can be isolated from Lepidium plant material and to methods for their isolation. The compositions are useful for treating and preventing cancer and sexual dysfunction.

Abstract: The present invention is a process, including intermediates, to produce (2S)-2-dipropylamino)-6-ethoxy-2,3-dihydro-1H-indene-5-carboxamide which is a useful pharmaceutical agent.

Abstract: A process for the preparation of an N,N-disubstituted-2-fluoro-1,3-ketoamide having the formula RCO.CFR′CONR2″ comprises treating an N,N-disubstituted-1,3-ketoamide having the formula RCO.CHR′CONR2″ with elemental fluorine. The groups R, R′ and R″ are independently selected from alkyl, aryl, substituted aryl, cycloalkyl, and substituted cycloalkyl. The group R′ may also be nitro or chlorine.

Abstract: The present invention provides an inexpensive one-step method for preparing an aromatic carboxamide, such as a phenyl substituted carboxamide) by reacting an aromatic amine (e.g. a phenylamine) and a carboxylic acid (e.g. an alkanoic acid or ester thereof) in the presence of a boron containing compound (e.g. boronic acid or boric acid) and, optionally, a chelating agent (e.g. a 2-pyridinylamine).

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: 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 subject invention concerns mercaptoalkylacyl compounds of formula (I): ##STR1## The compounds of the subject invention can be used to inhibit matrix metalloproteinases and/or TNF.alpha.- and L-selectin sheddase-mediated diseases including degenerative diseases and cancers. The subject invention also concerns methods of using the compounds of the invention to treat or prevent conditions associated with matrix metalloproteinases or that are mediated by TNF.alpha. or L-selectin sheddase.

Abstract: Novel tricyclic compounds of formula I as defined in the specification, a process for their preparation and their use for the preparation of optically active or racemic colchicine and thiocolchicine derivatives.

Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or an optionally substituted hydrocarbon group; R.sup.3 represents an optionally substituted hydrocarbon group; R.sup.4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C.sub.2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.

Abstract: Compounds of formula (I): ##STR1## wherein R represents a CR.sub.4 R.sub.5, CHR.sub.6, or C.dbd.R.sub.7 radical and R.sub.3 represents an oxygen atom, salts thereof, the preparation thereof and drugs containing same. The compounds of formula (I) have valuable pharmacological properties and are alpha-amino-3-hydroxy-5-methyl-4-osoxaziepropionic acid (AMPA) receptor antagonists, said receptor also being known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive N-methyl-D-aspartate (NMDA) receptor antagonists, and particularly NMDA receptor glycine modulation site ligands.

Abstract: There is provided a process for the preparation of substituted .beta.-ketoanilide compounds having the structural formula I ##STR1## The substituted .beta.-ketoanilide compounds are useful for the control of insect pests.

Abstract: The present invention provides a process for converting N-(4-fluorophenyl)-2-hydroxy-N-(1-methylethyl)acetamide acetate to N-(4-fluorophenyl)-2-hydroxy-N-(1-methylethyl)acetamide. The process includes the step of hydrolyzing N-(4-fluorophenyl)-2-hydroxy-N-(1-methylethyl)acetamide acetate with water or an aqueous alkali in the presence of an aprotic, aromatic solvent.

Abstract: There is disclosed a process for the preparation of an indanylamine compound of general formula ##STR1## wherein R.sup.1 represents an optionally substituted alkyl group, and R.sup.2, R.sup.3 and R.sup.4 independently represent a hydrogen atom or an optionally substituted alkyl group, the process including the steps of hydrogenating a compound of general formula ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as described above and R.sup.5 and R.sup.6 independently represent a halogen atom, a hydroxyl, nitro or cyano group, or an optionally substituted alkyl, alkoxy, alkoxycarbonyl, alkylcarboxy or alkylamino group provided that R.sup.5 and R.sup.6 represent different atoms or groups, and subsequent rearrangement and derivatisation of the product thereof. Compounds of general formula I may be used to prepare preferred stereoisomers of fungicidal N-indanyl carboxamide compounds.

Abstract: This invention provides a compound having the formula R.sup.1 --Y.sup.1 --CHZ.sup.1 --CH(NY.sup.2 Y.sup.3)--CH.sub.2 --Z.sup.2, wherein: R.sup.1 is a straight-chained alkyl, alkenyl or alkynyl group having from 8 to 19 carbon atoms in the aliphatic chain; Y.sup.1 is --CH.dbd.CH--, --C.tbd.C-- or --CH(OH)CH(OH)--; Z.sup.1 is OH or a conversion-inhibiting group; Z.sup.2 is a conversion-inhibiting group; Y.sup.2 is H, a phenyl group, an alkyl-substituted phenyl group having from 1 to about 6 carbons in the alkyl chain, or an alkyl chain having from 1 to 6 carbons; Y.sup.3 is H or a group having the formula --C(O)R.sup.2 or --S(O).sub.2 R.sup.2 ; R.sup.2 is a straight-chained alkyl, alkenyl or alkynyl group having from 1 to 23 carbon atoms in the chain; and when Z.sup.2 is an amino, R.sup.2 is an aliphatic chain having from 1 to 9 or from 19 to 23 carbon atoms in the aliphatic chain.

Abstract: A process for the preparation of glycoloylanilide of the formula (G) ##STR1## is recited that involves reacting a nitrobenzene with hydrogen and, if desired, with a carbonyl compound, in the presence of a noble metal catalyst and a solvent, reacting the compound produced with chloroacetyl chloride, reacting the resulting product with a benzyl alcohol and with a base, or reacting the resulting compound with an O-benzylglycoloyl chloride, and debenzylating the resulting benzylglycoloylanilide product by reacting with hydrogen in the presence of a noble metal catalyst. The invention also relates to a process for the preparation of O-benzylglycoloylanilide.

Abstract: A process for preparing acetoacetarylamides of the formula I ##STR1## where R.sup.1 and R.sup.2 are identical or different alkyl radicals,l and m are each 0, 1 or 2, andis 0 or 1,by addition of diketene to the appropriate arylamine by continuously reacting the arylamine with diketene in the presence of a mixture of water and of a (C.sub.1 -C.sub.4)-alkanol at temperatures from 60.degree. C. to 100.degree. C. in the course of from 0.1 to 10 min.

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: 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: A process for the preparation of .alpha.-chloroacetoacetanilide compounds (.alpha.-Cl AAA) which comprises the steps of:(a) reacting an acetoacetanilide compound (AAA) with chlorine in the presence of a solvent mixture consisting essentially of an organic solvent and water, wherein the percent water to organic solvent in the solvent mixture is between about 10% and 150% (v/v);(b) isolating the .alpha.-Cl AAA produced in step (a); and(c) optionally hydrogenating any .alpha.,.alpha.-dichloroacetoacetanilide compound (.alpha.,.alpha.-diCl AAA) produced in step (a), with hydrogen in the presence of a catalyst selected from the group consisting of palladium, platinum and Raney nickel, and in the presence of a solvent mixture consisting essentially of water and an organic solvent, wherein the percent of the water to the organic solvent in the solvent mixture is between 10% to 150% (v/v), for a period of time sufficient to produce .alpha.-Cl AAA; and isolating the .alpha.-Cl AAA so produced.

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: 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.

Abstract: The invention relates to compositions that can be isolated from Lepidium plant material and to methods for their isolation. The compositions are useful for treating and preventing cancer and sexual dysfunction.