Abstract: The present invention relates to new derivatives of amino acids and their use as medicaments.

Abstract: A compound of Formula (Ih) The compounds may be used, inter alia, for preparing beta aryl-alpha-oxy substituted alkylcarboxylic acids.

Abstract: The present invention relates to an improved process for the preparation of novel antidiabetic compounds having formula (1) where R1 represents hydrogen or lower alkyl group and X represents hydrogen or halogen atom.

Abstract: Compounds represented by general formula (I): and salts thereof, exhibiting excellent adenosine A3 receptor antagonism: wherein A is an optionally substituted benzene ring; B may be further substituted; and R1 is an optionally substituted cyclic group.

Abstract: The invention provides compounds of Formula I: 1

Abstract: A compound of Formula (Ig) The compounds may be used, inter alia, for preparing beta aryl-alpha-oxy substituted alkylcarboxylic acids.

Abstract: The present invention relates to an improved process for the preparation of novel antidiabetic compounds having formula (1) where R1 represents hydrogen or lower alkyl group and X represents hydrogen or halogen atom.

Abstract: This invention relates to novel polymorphic/pseudopolymorphic forms of arginine salt of 3-[4-[2-(phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid, having the formula I shown below. The invention also relates to a pharmaceutical composition comprising the novel polymorphic form or their mixture and a pharmaceutically acceptable carrier. The polymorphic forms of the present invention are more active, as antidiabetic and hypolipidemic agent, than the novel 3-[4-[2-(phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid.

Abstract: The present invention relates to crystalline R-guanidines of (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate, its preparations and its use as therapeutic agents. More specifically the present invention relates to crystalline Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate, preferably (L)-Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate, its preparation and its use as therapeutic agent.

Abstract: This invention relates to novel polymorphic/pseudopolymorphic forms of arginine salt of 3-[4-[2-(phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid, having the formula I shown below. The invention also relates to a pharmaceutical composition comprising the novel polymorphic form or their mixture and a pharmaceutically acceptable carrier. The polymorphic forms of the present invention are more active, as antidiabetic and hypolipidemic agent, than the novel 3-[4-[2-(phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid.

Abstract: The present invention relates to pharmaceutically acceptable salts of compound of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.

Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: Disclosed are compounds of the Formula I 1

Abstract: A compound of formula (1) it derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts, or its pharmaceutically acceptable solvates, processes for its preparation and methods of use thereof.

Abstract: A phenothiazine, acridan, acridone oxime, acridone hydrazone and dibenzodiazepine derivative represented by formula (I) 1

Abstract: The present invention relates-to compounds of the general formula (I) 1

Abstract: The process for chemically modifying metal-free, colored anthraquinone or condensed anthraquinone compounds or the compounds prepared by said process for improving one or more properties thereof such as water dispersibility, compatibility with other organics, or increased chemical reactivity, wherein the process includes providing material with from 1-6 sulfonylhalide groups or sulfonate ester groups or mixtures thereof, and contacting the material under sulfonamido forming conditions with one or more reactants containing one or more poly(oxyalkylene) moieties, each of the reactants having from 1 to 4 functional amino groups, and each of the poly(oxyalkylene) moieties being comprised of from about 4 to about 200 epoxide reactant residues at least about 50 mole percent of which residues contain 2-4 carbons and wherein the total of said epoxide reactant residues is from about 4 to about 600.

Abstract: The invention provides a compound, useful as an optical probe or sensor of the activity of at least one cytochrome P450 enzyme, and methods of using the compound to screen candidate drugs, and candidate drugs identified by these methods.

Abstract: The present invention relates to compounds of the general formula (I) 1

Abstract: The present invention relates to compounds of the general formula (I) 1

Abstract: Therapeutically active compositions of matter are described which are useful for treating or preventing diseases and conditions comprising inflammatory diseases including joint inflammation, Crohn's disease, and inflammatory bowel disease; respiratory diseases such as chronic obstructive pulmonary disease (COPD) including asthma, chronic bronchitis, and pulmonary emphysema; infectious diseases including endotoxic shock and toxic shock syndrome; immune diseases including systemic lupus erythematosis and psoriasis; and other diseases including bone resorption diseases and reperfusion injury; wherein said composition of matter comprises a compound which is an inhibitor of phosphodiesterase isozyme 4 (PDE4) and wherein an indazole is one essential component of said compound's overall chemical structure, and wherein said indazole constitutes a bioisosteric replacement of a catechol component or functional derivative thereof in a known compound having the same said therapeutic activity and the same remaining said c

Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: A process for preparation of alkylated diphenylamine antioxidant which comprises alkylating diphenylamine with a polyisobutylene in the presence of a clay catalyst, wherein the polyisobutylene has an average molecular weight in the range of 120 to 600 and wherein the polyisobutylene contains at least 25% methylvinylidene isomer.

Abstract: The present invention relates to nonlinear-optically active copolymers which are composed of a chromophore acrylate, a glycidyl-functional acrylate, and a further acrylate unit, and to polyadducts produced from them by crosslinking with a carboxyl-functional polyester. The nonlinear-optical copolymers of the present invention, and the polyadducts prepared from them, possess an orientation stability in the crosslinked state, and a thermal stability, which makes them highly suitable for producing electrooptical and photonic components.

Abstract: The present invention provides novel compounds, and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsey, irritable bowl syndrome, immune supression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: wherein R1, R3, R5, Q, Z, Y, V, X and X′ are as defined herein.

Abstract: Novel heterocyclic compounds which generate chemiluminescence on reaction with a phosphatase enzyme are provided as well as a process for their preparation and intermediates useful therein. The compounds comprise a nitrogen, oxygen or sulfur-containing heterocyclic ring system bearing an exocyclic carbon-carbon double bond. The double bond is further substituted at the distal carbon with a phosphate group and an oxygen or sulfur atom-containing group. Novel compositions further comprising a cationic aromatic compound (CAC) in addition to the heterocyclic phosphate compound are provided. The addition of the CAC in the composition greatly increases the production of chemiluminescence and provides improved detection sensitivity. Compositions further comprising an anionic surfactant and a non-ionic surfactant provide additional improvements in detection sensitivity.

Abstract: 3-piperidyl-4-oxoquinazoline derivatives are provided, which is represented by the formula (I): wherein R represents an amino group or a cyclic amino group such as dibenzoazepine, each of which is substituted with a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, or the like, n is an integer of 1 to 3, R3 and R4 independently represents a hydrogen atom, a lower alkyl group, or the like, or a pharmaceutically acceptable salt thereof. Compounds (I) of the present invention have excellent MTP-inhibitory activity. Thus, these compounds not only inhibit formation of LDL that is a cause of arteriosclerotic diseases but also regulate TG, cholesterol, and lipoproteins such as LDL in the blood and regulate cellular lipids through regulation of MTP activity. They can also be used as a new type of preventive or therapeutic agents for hyperlipemia or arteriosclerotic diseases.

Abstract: A pyridobenzoxazine derivative having a bicyclic amine derivative as its substituent, represented by the formula (I): exhibiting antimcrobial activity, and useful in treating infectious diseases and preserving food and agricultural products.

Abstract: A pharmaceutical compound of the formula in which R1 is C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-10 cycloalkyl, C3-10 cycloalkyl-C1-10 alkyl, C3-10 cycloalkyl-C2-10 alkenyl, C3-10 cycloalky-C2-10 alkynyl, optionally substituted phenyl-C1-10 alkyl, optionally substituted phenyl-C2-10 alkenyl, optionally substituted phenyl-C2-10 alkynyl, optionally substituted naphthyl, optionally substituted naphthyl-C1-10 alkyl, C1-10 alkoxy-C1-10 alkyl, C3-10 cycloalkoxy-C1-10 alkyl, optionally substituted heterocyclyl, optionally substituted heterocyclyl-C1-10 alkyl, optionally substituted phenyl fused to C5-10 cycloalkyl, optionally substituted tricyclic, optionally substituted tricyclic-C1-10 alkyl, or [optionally substituted phenyl(CH2)n]2-C1-10 alkyl, where n is 0 or 1 to 4, and R2 is hydrogen or one of the values for R1; or a salt or ester thereof.

Abstract: A compound of formula (I) ##STR1## its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates, wherein R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are the same or different; R.sup.1 and R.sup.2 together represent along with carbon atoms to which they are attached an aromatic cyclic structure containing 5-6 ring atoms which may optionally be substituted; X represents a heteroatom selected from oxygen or sulfur; R.sup.7 represents hydrogen atom, hydroxy, alkoxy, halogen, lower alkyl group or optionally substituted aralkyl group or forms a bond together with R.sup.8 ; R.sup.8 represents hydrogen atom, hydroxy, alkoxy, halogen, lower alkyl group or optionally substituted aralkyl or R.sup.8 forms a bond together with R.sup.

Abstract: Novel heterocyclic compounds which generate chemiluminescence on reaction with a phosphatase enzyme are provided as well as a process for their preparation and intermediates useful therein. The compounds comprise a nitrogen, oxygen or sulfur-containing heterocyclic ring system bearing an exocyclic carbon-carbon double bond. The double bond is further substituted at the distal carbon with a phosphate group and an oxygen or sulfur atom-containing group.Novel compositions further comprising a cationic aromatic compound (CAC) in addition to the heterocyclic phosphate compound are provided. The addition of the CAC in the composition greatly increases the production of chemiluminescence and provides improved detection sensitivity. Compositions further comprising an anionic surfactant and a non-ionic surfactant provide additional improvements in detection sensitivity.

Abstract: Thienopyrimidine derivatives are disclosed. Also disclosed are methods for the production and use of these compounds.

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: The present invention provides novel compounds, compounds and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsy, irritable bowel syndrome, immune suppression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: ##STR1## wherein R.sup.1, R.sup.3, R.sup.4, R.sup.5, Z, Y, V, X, X', J, K, L, and M are as defined herein.

Abstract: A phenothiazine or phenoxazine derivative represented by the following general formula (1), a charge-transporting material comprising the derivative, and an electrophotographic photoreceptor containing the charge-transporting material are disclosed. The charge-transporting material has good solubility in binder polymers, satisfactory sensitivity, and a low residual potential.

Abstract: Novel .beta.-aryl-.alpha.-oxysubstituted alkylcarboxylic acids of the formula (I) and compositions containing them. ##STR1## The compounds have hypolipidemic, antihyperglycemic uses.

Abstract: A phenothiazine or phenoxazine derivative represented by the following general formula (1), a charge-transporting material comprising the derivative, and an electrophotographic photoreceptor containing the charge-transporting material are disclosed. The charge-transporting material has good solubility in binder polymers, satisfactory sensitivity, and a low residual potential In general formula (1) Ar.sup.1 and Ar.sup.2 may be the same or different and each represents an optionally substituted aryl group; R.sup.1 and R.sup.2 may be the same or different and each represents a hydrogen atom, a lower alkyl group, or an optionally substituted aryl group; R.sup.3 represents a lower alkyl group, an alicyclic hydrocarbon group having 5 to 7 carbon atoms, an optionally substituted aryl group, or an optionally substituted aralkyl group; X represents a sulfur atom or an oxygen atom; and n and m each represents an integer of 0 or 1.

Abstract: A quinuclidine derivative represented by the following general formula (I), a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof, which has strong squalene synthase inhibiting activity and is useful as a cholesterol lowering agent without causing side effects. ##STR1## (Symbols in the formula represent the following meanings; R.sub.1 : a hydrogen atom, a halogen atom or a lower alkyl group,R.sub.2 : a hydrogen atom, a hydroxyl group or a lower alkoxy group,. . : a single bond or a double bond, with the proviso thatR.sub.2 does not exist when . . . is a double bond,X and Y: the same or different from each other and each represents a bond, an oxygen atom (--O--), a carbonyl group (--CO--), a group represented by the formula --S(O).sub.p -- or a group represented by the formula --NR.sub.3 --,p: 0, 1 or 2,R.sub.3 : a hydrogen atom or a lower alkyl group which may have a substituent,A: a saturated or unsaturated lower alkylene group, a group of the formula --(CH.sub.2).sub.m Z(CH.sub.

Abstract: Aliphatic hydrocarbyl-substituted aromatic amines are prepared by reacting an aromatic amine and an aliphatic hydrocarbylating agent, such as an olefin, in the presence of a heteropolyacid catalyst such as Cs.sub.2.5 H.sub.0.5 PW.sub.12 O.sub.40, for a period of time and at a temperature sufficient to permit reaction.

Abstract: There are described compounds of the formula ##STR1## Wherein the variables have been defined herein. The compounds are useful as research tools in the determination of biologically active peptides sequences and also potentially suitable as medicaments, some of them being useful in the prevention or control of the formation of blood platelet thrombi, and some compounds are useful as intermediates.

Abstract: There are described compounds of the formula ##STR1## Wherein the variables have been defined herein. The compounds are useful as research tools in the determination of biologically active peptides sequences and also potentially suitable as medicaments, some of them being useful in the prevention or control of the formation of blood platelet thrombi, and some compounds are useful as intermediates.

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: Novel water soluble dyes of the formula I are provided ##STR1## wherein R.sup.1 and R.sup.4 are alkyl of 1 to 4 carbon atoms or hydrogen; or R.sup.1 -R.sup.2 or R.sup.2 -R.sup.4 form part of aliphatic heterocyclic rings; R.sup.2 is hydrogen or joined with R.sup.1 or R.sup.4 as described above; R.sup.3 is --(CH.sub.2).sub.m --SO.sub.3.sup.-, where m is 1 to 6;X is N, CH or ##STR2## where Y is 2 --SO.sub.3.sup.- ; Z is 3, 4, 5 or 6 --SO.sub.3.sup.-. The novel dyes are particularly useful as the active media in water solution dye lasers.

Abstract: The present invention relates to labelling agents comprising non-proteinaceous boronic acid conjugates having absorption maxima at not less than 600 nm, said label being provided by e.g., an azine, triphenylmethane, cyanine or phthalocyanine dye. The labelling agents are useful in the estimation and quantification of cisdiols such as glycosylated haemoglobin, by virtue of the substantially total absence of overlap with the absorption spectrum of haemoglobin. Oxazine and thiazine dyes exhibiting similar absorption characteristics and containing other activated moieties are similarly useful labelling agents, especially in the presence of haemoglobin.

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: The invention relates to pyrrolidine monomeric units and to oligomers which are joined via phosphate linkages, including phosphorothioate, phosphodiester and phosphoramidate linkages.

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.