Abstract: A compound containing an alkylene selenocyanate or an alkylene isoselenocyanate moiety effective to prevent the occurrence or progression of cancer or a precancerous condition. The compound can be provided and administered in the form of a pharmaceutical composition, a cosmetic, a food additive, supplement, or the like. Methods for synthesis and use of the chemopreventive compound of the invention are also provided.

Abstract: Substituted C-furan-2-yl-methylamine and C-thiophen-2-yl-methylamine compounds, processes for their preparation, medicaments and pharmaceutical compositions containing them, and their use in treatment methods and in the preparation of analgesics, in the preparation of a local anaesthetic, an antiarrhythmic, an antiemetic, a nootropic agent and/or a medicament for the treatment and/or prophylaxis of cardiovascular diseases, urinary incontinence, diarrhea, pruritus and/or inflammations, and/or a medicament for the treatment of depression and/or alcohol and/or drug and/or medicament abuse, and/or a medicament for increasing vigilance.

Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where J, M, Q, T, W, X, Z, R1, R2, R3, R4, R4′, R5, R6, R6′, R7, m, and n have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also disclosed are pharmaceutical compositions comprising these compounds, and methods of treating or preventing metalloprotease-related maladies using the compounds or the pharmaceutical compositions.

Abstract: Bis-aryl diamidoxime compounds, such as 2,5-bis[4-hydroxy and 4-O-alkylamidinophenyl]furans, can be prepared from 2,5-bis tri-alkylstannanes via a one step palladium-catalyzed cross reaction. Bis-aryl diamidoxime compounds, such as 2,5-bis[4-hydroxy and 4-O-alkylamidinophenyl]furans, are useful as therapeutic compounds. The disclosed process is scalable, simpler, more economic and more feasible than other presently known methods of preparing 2,5-bis[4-hydroxy and 4-O-alkylamidinophenyl]furans and other bis-aryl diamidoxime compounds.

Abstract: The present invention describes novel compounds of Formula I which inhibit HIV integrase. The invention also describes compositions and treatments of AIDS or ARC by using these compounds.

Abstract: The present invention relates to novel 2,5-bis {[alkyl(or aryl)imino]aminophenyl}furans and thiophenes of the general formula in which R1, R2, R3 and R4 are each independently selected from the group consisting of H, alkyl, alkoxy, halide, and alkylhalide groups; R5 is H, alkyl or aryl; R6 is H, alkyl, aryl, or NR7R8, in which R7 and R8 are each independently selected from the group consisting of H, alkyl and aryl; and X is O, S or NR9, in which R9 is H or alkyl, and to the use of such compounds.

Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII): useful in treating Alzheimer's disease and other similar diseases.

Abstract: Disclosed is a method of preparing chiral amine. The method includes reacting ketoxime, palladium, lipase, acyl-donating compound, and tertiary amine to prepare amide, and amide is hydrolyzed.

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-benzyl-N-phenyl aminoalcohols.

Abstract: The present application describes oxygen and sulfur containing heteroaromatics and derivatives thereof of formula I: 1

Abstract: Allomorph of Z isomer of N-[2-[[[5-(dimethylamino)methyl-2-furanyl]methyl]thio]ethyl]-N′-methyl-2-nitro-1,1-ethenediamine hydrochloride, with two carbon atoms linked by a rigid ethylenic bond, marked by an asterisk (*), characterized by the following structural formula: 1

Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts thereof, 1

Abstract: Derivatives of sphingolipids of the formula: 1

Abstract: The present invention generally relates to novel compounds HNP-98701A (epi-manassantin A), HNP-98701B and HNP-98701C (manassantin A), or mixture thereof (HNP-98701) as carcinostatis substance, preparation method thereof and carcinostatis pharmaceutical composition containing them as effective constituents and, more specifically, to novel compounds HNP-98701A and HNP-98701B, known compounds HNP-98701C, or mixture thereof and derivatives thereof obtained by extracting saururus with methanol, fractionating this with various organic solvents, separating ethyl acetate fraction with highest anticancer activity through thin-layer chromatography or column chromatography and purifying it, preparation method thereof and carcinostatis pharmaceutical composition containing them as effective constituents. The carcinostatis substances HNP-98701A, HNP-98701B and HNP-98701C of the present invention selectively affect cancer cell line cells and cause apoptosis-type cell death.

Abstract: There is provided a production method for producing a biarylalanine compound of formula (4): 1

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.

Abstract: The invention relates to polycyclic aryl and heteroaryl substituted benzene compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.

Abstract: 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a polar ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.

Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 1,4-quinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.

Abstract: Heterocyclic arylsulfonamidobenzylic compounds are provided which are useful in treating lipid disorders, metabolic disorders and cell-proliferative diseases.

Abstract: The present application describes modulators of MCP-1 of formula (I): 1

Abstract: The present invention is directed in part towards methods of modulating the function of protein kinases with phenol- and hydroxynaphthalene-based compounds. The methods incorporate cells that express a protein kinase. In addition, the invention describes methods of preventing and treating protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to phenol- and hydroxynaphthalene-based compounds and pharmaceutical compositions comprising these compounds.

Abstract: This invention provides estrogen receptor modulators of formula I, having the structure 1

Abstract: The present invention is directed to C2-disubstituted indan-1-ol systems of the Formula I, 1

Abstract: The present invention provides compounds and compound libraries that are useful as protease modulators. The compounds and compound libraries are preferably made using the methods of the present invention which utilize peptide synthesis and combinatorial chemistry methods on a solid phase.

Abstract: The present invention refers to a new procedure for obtaining and purifying 2-bromo-5-(2-bromo-2-nitrovinyl)-furan in one reaction step starting with 2-nitrovinylfuran, and maintains high indexes of purity and an appropriate yield. The process involves the direct bromination of 2-nitrovinylfuran using charcoal from the beginning of the reaction, followed by the neutralization and dehydrobromination using pyridine, and finally crystallizing and purifying the product obtained with ethanol and charcoal. With the new procedure it is possible to reduce the time of obtaining the final product, the reaction becomes endothermic instead of exothermic, which facilitates the work of the operators and allows for the scaling up of the reaction to superior levels. The process significantly decreases the amount of chemicals in the reaction, some of them with toxic properties.

Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.

Abstract: The present invention provides a novel protein that regulates degranulation of mast cells (degranulation regulator), a gene encoding it, a protein (conjugate factor) that interacts with the regulator, a gene encoding it, a screening method of an inhibitor of the degranulation, which uses this degranulation regulator and the conjugate factor, an inhibitor obtained by the screening method and the like.

Abstract: A process is provided for preparing chirally pure S-enantiomers of &agr;-amino acids comprising the steps of: a) preparing an organometallic reagent from an alkyl halide of the formula (R)2CH(CH2)nCH2X; b) adding the organometallic reagent to carbon dioxide to afford a carboxylic acid; c) activating the carboxylic acid with an acid chloride, phosphorus trichloride, acid anhydride, or thionyl chloride in the presence of a tertiary amine base; d) reacting the product of step c) with an alkali metal salt of S-4-benzyl-2-oxazolidinone; e) treating the product of step d) with a strong non-nucleophilic base to form an enolate anion; f) trapping the enolate anion with 2,4,6-triisopropylbenzenesulfonyl azide to afford an oxazolidinone azide; g) hydrolyzing the oxazolidinone azide with an aqueous base to afford an &agr;-azido acid; h) reducing the &agr;-azido acid to the &agr;-amino acid; and i) recrystallizing the &agr;-amino acid to the chirally pure &agr;-amino acid.

Abstract: Sulfones of formula I are useful as antiproliferative agents, including, for example, anticancer agents: wherein: Q1 is selected from the group consisting of (a) a phenyl radical according to formula II  wherein R1, R2, R3, R4 and R5 are independently selected from the group consisting of hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, amino, C1-C6 trifluoroalkoxy and trifluoromethyl; (b) an aromatic radical selected from the group consisting of 1-naphthyl, 2-naphthyl and 9-anthryl; and (c) an aromatic radical according to formula III  wherein n1 is 1 or 2, Y1 and Y2 are independently selected from the group consisting of hydrogen, halogen, and nitro, and X1 is selected from the group consisting of oxygen, nitrogen, sulfur and and Q2 is selected from the group consisting of (d) a phenyl radical according to formula II, as defined above; (e) an aromatic radical selected from the group co

Abstract: The invention relates to novel 2-hetaryl-3,4-dihydro-2H-pyrrole derivatives of the formula (I) in which Hetaryl represents substituted heterocyclyls and Ar represents substituted phenyl, to a plurality of processes for their preparation and to their use as pesticides.

Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes.

Abstract: The present invention relates to 2-amino-6-fluorobicyclo[3.1.

Abstract: The present invention refers to a new procedure for obtaining and purifying 2-bromo-5-(2-bromo-2-nitrovinyl)-furan in one reaction step starting with 2-nitrovinylfuran, and maintains high indexes of purity and an appropriate yield.

Abstract: Provided are a process for preparing terbinafine or its HCl salt, which comprises: (a) reacting a furan derivative with a base; (b) performing a reductive alkylation of the resulting compound obtained in the step (a) with N-methyl-1-naphthalenemethylamine or its HCl salt; and (c) purifying the resulting compound obtained in the step (b).

Abstract: Sulfones of formula I are useful as antiproliferative agents, including, for example, anticancer agents: 1

Abstract: A class of styryl amidine derivatives which are antagonists of the hum NMDA receptor, being selective for those containing the NR2B subunit, are active in the treatment and/or prevention of neurological and neurodegenerative disorders, in particular neuropathic pain and headache, specifically migraine, whils displaying fewer ataxic and related side-effects associated with other classes of NMDA receptor antagonists.

Abstract: Derivatives of C2-substituted indan-1-ol compounds, processes for their preparation and their use are disclosed.

Abstract: Heterocyclic substituted compounds having the general structure: which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes.

Abstract: The present invention relates to novel 2,5-bis {[alkyl (or aryl) imino] aminophenyl} furans and thiophenes of the general formula 1

Abstract: The invention describes novel nitrosated and/or nitrosylated H2 receptor antagonist compounds, and novel compositions comprising at least one H2 receptor antagonist compound that is optionally substituted with at least one NO and/or NO2 group, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase and/or at least one nonsteroidal antiinflammatory drug, antacid, bismuth-containing reagent or anti-viral agent.

Abstract: A process for the production of a compound of formula (I) wherein R1 is hydrogen or C1-C4-alkyl; R2 is hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkinyl, C3-C6-cycloalkyl or a radical —CH2B; A is selected from the group consisiting of 2-chloropyrid-5-yl, tetrahydrofuran-3 -yl, 5-methyl-tetrahydrofuran-3-yl or 2-chlorothiazol-5-yl; and B is phenyl, 3-pyridyl or thiazolyl, which are optionally substituted by one to three substituents selected from the group consisting of C1-C3-alkyl, C1-C3-halogenalkyl, cyclopropyl, halogencyclopropyl, C2-C3-alkenyl, C2-C3-alkinyl, C1-C3-alkoxy, C2-C3-halogenalkenyl, C2-C3-halogenalkinyl, C1-C3-halogenalkoxy, C1-C3-alkylthio, C1-C3-halogenalkylthio, allyloxy, propargyloxy, allylthio, propargylthio, halogenallyloxy, halogenallylthio, halogen, cyano or nitro; and optionally the possible E/Z isomers, E/Z isomeric mixtures and/or tautomers thereof, respectively in free form or in salt form; characterised in that a compound of formula (II)

Abstract: A class of 3,4-diaryl substituted thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders.

Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.

Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.

Abstract: &agr;-Sulfenimino acid derivatives of formula I including the optical isomers thereof and mixtures of such isomers, wherein A is cycloalkyl, cycloalkenyl, aryl or heteroaryl, each optionally substituted, B is a direct bond or optionally substituted alkylene, E is hydrogen or optionally substituted aryl, R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, each optionally substituted, and T is NH or oxygen, have been found to be useful for controlling or preventing the infestation of plants by phytopathogenic microorganisms, especially fungi. The invention relates the novel compounds and also to the preparation thereof and to the use of the compounds for plant protection, and to compositions suitable for applying the novel compounds in agricultural techniques.

Abstract: Compounds represented by the formula: wherein R1 and R2 are hydrogen atom, a hydrocarbon group or a heterocyclic group, or R1 and R2 may form, together with the adjacent carbon atom, a 3- to 8-membered homocyclic or heterocyclic ring, W indicates (i) a group represented by the formula:  wherein ring B indicates a 5- to 7-membered ring, or (ii) a group represented by the formula:  wherein R4 indicates (1) an aliphatic hydrocarbon group, which may be substituted with an aromatic group, or (2) an acyl group containing an aromatic group, R5 is hydrogen atom, a C1-6 alkyl, or an acyl group, provided that, when W is Wa, R3 is hydrogen atom, a hydrocarbon group or a heterocyclic group, when W is Wb, R3 indicates a C6-14 aryl group, or salts thereof or prodrugs thereof have an excellent action to inhibit neurodegeneration and the like as well as an excellent brain penetrability and are low in the toxicity, thereby being useful as prophylactic or thera

Abstract: A compound containing an alkylene selenocyanate or an alkylene isoselenocyanate moiety effective to prevent the occurrence or progression of cancer or a precancerous condition. The compound can be provided and administered in the form of a pharmaceutical composition, a cosmetic, a food additive, supplement, or the like. Methods for synthesis and use of the chemopreventive compound of the invention are also provided.

Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) 1