Abstract: The present invention provides a new and efficient process for the preparation of the dexmethylphenidate hydrochloride with high optical purity, the process comprising: (a) reacting a solution of threo-N-Boc-ritalinic acid with (S)-1-phenylethylamine, separating precipitated solid salt of (R,R)-enriched N-Boc-ritalinic acid with (S)-1-phenylethylamnine from the reaction mixture and recrystallizing, reslurring and/or trituring of said salt; (b) mixing the solid salt of (R,R)-N-Boc-ritalinic acid and (S)-1-phenylethylamine obtained in step (a) with aqueous acid and separating (R,R)-N-Boc-ritalinic acid from the mixture; and (c) reacting the (R,R)-N-Boc-ritalinic acid prepared in step (b) with hydrogen chloride and methanol to give dexmethylphenidate hydrochloride with optical purity of at least 99% ee. The present invention further provides salt of (R,R)-N-Boc-ritalinic acid with (S)-1-phenylethylamine as new intermediate in the preparation of dexmethylphenidate hydrochloride.

Abstract: A process of preparation of optically pure or optically enriched isomers of omeprazole and structurally related sulfoxides is provided. Also provided are an amorphous form of esomeprazole, as well a pharmaceutical composition containing it and a method of using it for treatment of gastric disorders.

Abstract: The invention relates generally to naphthyridine derivatives of the formula wherein one of U, X, Y and Z is nitrogen and the others are C—R, where R is hydrogen or a substituent. More specifically, the invention relates to 1,8-naphthyridine derivatives and pharmaceutical compositions containing such derivatives. Methods of the invention comprise administration of a naphthyridine derivative of the invention for the treatment of diabetes and related disorders.

Abstract: Novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl; X2 is —CHO, —CN, optionally substituted amino, alkyl, or aryl; or X1 is optionally substituted benzofused heterocyclyl and X2 is hydrogen; or X1 and X2 together form an optionally benzofused spiro heterocyclyl group R1, R2, R3 and R4 are independently H and alkyl, or (R1 and R4) or (R2 and R3) or (R1 and R3) or (R2 and R4) together can form an alkylene bridge of 1 to 3 carbon atoms; Z1 is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or —CO2(alkyl or substituted amino) or CN ; Z2 is H or Z1; Z3 is H oralkyl; or Z1, Z2 and Z3, together with the carbon to which they are attached, form bicyclic saturated or unsaturated rings; pharmaceutical compositions therefore, and the use of said compounds as nociceptin receptor inhibitors useful in the

Abstract: Compounds of the formula (I) below, or pharmacologically acceptable salts, esters or other derivatives thereof: wherein A is furan, thiophene, pyrazole, imidazole, isoxazole or isothiazole; R1 is a substituted or unsubstituted aryl or a substituted or unsubstituted heteroaryl; R2 is a substituted or unsubstituted heteroaryl; and R3 is a bicyclic amino group; provided that the substituents R1 and R2 are bonded to the two atoms of the cyclic group A which are adjacent to the atom of the cyclic group A to which the substituent R2 is bonded. The compounds inhibit the production of inflammatory cytokines.

Abstract: The present invention relates to bottom antireflective coating compositions and polymers useful in making such compositions.

Abstract: The present invention provides a process for the preparation of threo-methylphenidate hydrochloride. According to a preferred embodiment, the process comprises the following steps: (a) contacting 1-(phenylglyoxylyl)piperidine arenesulfonylhydrazone of the formula wherein Ar denotes an aryl group, where the aryl group may be substituted by a C1–C6 alkyl, halo or nitro group; with an inorganic base in the presence of a water immiscible organic solvent and a phase transfer catalyst to obtain (R*,R*)-enriched 7-phenyl-1-azabicyclo [4.2.0]octan-8-one of the formula: (b) reacting the (R*,R*)-enriched 7-phenyl-1-azabicyclo[4.2.0]octan-8-one prepared in step (a) with a solution of hydrogen chloride in methanol to obtain threo-enriched methylphenidate hydrochloride; (c) crystallizing the threo-enriched methylphenidate hydrochloride prepared in step (b) to give the desired threo-methylphenidate hydrochloride.

Abstract: The present invention relates to a blue light-emitting compound for organic polymer EL devices and organic EL devices having superior color purity and light-emitting efficiency by providing a blue light-emitting compound for organic EL devices represented by Chemical Formula 1 and an organic EL device using the blue light-emitting compound: wherein R1 to R8 each independently represents a functional group selected from the group consisting of hydrogen alkyl groups, alkoxy groups, carbon rings, aryl groups, hetero rings and fused aromatic compounds having from 1 to 30 carbon atoms; to of R1 to R3 may additionally be connected by a ring; and two of R4 to R8 may additionally be connected by a ring.

Abstract: Functionalized nitrogen heterocyclic compounds, including benzodiazepines and azasugars, and synthetic methods for preparing such compounds. Nitrogen-containing heterocycles are prepared by reacting amino-carbonyl compounds that contain an amine moiety connected via a linker to a carbonyl moiety with an organoboron derivative.

Abstract: A compound of formula (I) (wherein all symbols are as defined in the specification) and salt thereof, and peroxisome proliferator activated receptor regulator comprising thereof as active ingredient. Because a compound of formula (I) have an activity of regulating peroxisome proliferator activated receptor regulator, the compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or treatment agent for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diabetes or syndrome X.

Abstract: The invention relates generally to naphthyridine derivatives of the formula wherein one of U, X, Y and Z is nitrogen and the others are C—R, where R is hydrogen or a substituent. More specifically, the invention relates to 1,8-naphthyridine derivatives and pharmaceutical compositions containing such derivatives. Methods of the invention comprise administration of a naphthyridine derivative of the invention for the treatment of diabetes and related disorders.

Abstract: A method for stereochemically controlled production of azacyclic compounds of general formula (I) in which the substituents have the meanings given in the specification. The invention also relates to intermediate products of this method and to novel azacyclenes.

Abstract: The present application describes novel bicyclic lactam derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein A, B, C, D, R1, and R2 are defined in the present specification, which are useful as metalloprotease, TNF-?, and/or aggrecanase inhibitors.

Abstract: The invention relates to a novel process for producing a the intermediary compound ?,??,dicyano-?,?-pentamethyleneglutarimide. The process includes the steps of reacting a ketone such as cyclohexanone with ethylcyanoacetate in the presence of ammonium hydroxide.

Abstract: The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immunune diseases, to pharmaceutical compositions containing these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.

Abstract: The present invention discloses novel cholinergic receptor ligands. The present invention also relates to the synthesis of substituted derivatives of aza-bridged bicyclic amines for use as muscarinic receptor ligands as well as methods of regulating function of certain cholinergic receptors, and hence acting as antagonists, agonists and partial agonists at certain specific cholinergic receptor subtypes. The present invention also relates to methods for treating disorders associated with cholinergic receptors.

Abstract: Substituted quinolone derivatives in which an oxazolidinone, isoxazolinone, or isoxazoline is covalently bonded to a quinolone, methods of using the quinolone derivatives, and pharmaceutical compositions containing the quinolone derivatives are disclosed. Methods of synthesizing these substituted quinolone derivatives are also disclosed, and in particular a method of manufacturing a 7-(2-oxo-1,3-oxazolidin-3-yl)aryl-3-quinolinecarboxylic acid by condensing a 4-(2-oxo-1,3-oxazolidin-5-yl)aryl boronic acid with a 7-halo-quinolone derivative. The quinolone derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.

Abstract: The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immune diseases and cerebral vasospasm, to pharmaceutical compositions containing these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.

Abstract: This invention relates to cycloalkylpyrrole-3-carboxylic acid derivatives and heterocycloalkylpyrrole-3-carboxylic acid derivatives that bind with high selectively and/or high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in the treatment of central nervous system (CNS) diseases. This invention also relates to the use of these cycloalkylpyrrole-3-carboxylic acid derivatives and heterocycloalkylpyrrole-3-carboxylic acid derivatives in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the detection of GABAA receptors in tissue samples.

Abstract: The invention relates to photoisomerizable compounds of formula I wherein A, Z, L, R, R1, k, m and r are defined herein.

Abstract: 2,3-Dihydro-isoindol-1-one derivatives, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them, for the prevention and treatment of diseases which are mediated by monoamine oxidase B.

Abstract: Novel pyridinones and their derivatives which are effective in treating or preventing Gram-negative bacterial infections are provided. The pyridinones are stable and easily derivatized; the methods by which these derivatizations occur is described. Two regioselective and functional group tolerant methods for the synthesis of the novel pyridinones are also provided. One such synthetic method involves reacting an imine and a Meldrum's acid derivative in solution. The other synthetic method is a solid phase synthesis of the pyridinones in which an imine is prepared bound to a solid support and a Meldrum's acid derivative is reacted with the imine. Novel imine intermediates useful in the solid phase and solution methods of synthesizing the pyridionones are also described.

Abstract: The present invention relates to an organic light emitting diode (OLED) device, comprising an anode disposed on a substrate, an organic EL layer disposed on the anode and a cathode disposed on the organic EL layer.

Abstract: The present invention is related to a compound of formula (I), salts and pro-drugs of the compound (I) and methods for treating and/or preventing partial or total ischemia, methods for treating and/or preventing pathologies associated with ischemia or with mitochondrial deficiencies.

Abstract: The invention relates to heterocyclic derivatives of formula (I), or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.

Abstract: The present invention relates compounds of the formula (I): wherein X represents hydrogen, C1-4alkyl optionally substituted by a hydroxy, methoxy or benzyloxy group, or CO2(C1-2alkyl); Z is —CR9R10CH2— or —CH2CR9R10—; and R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.

Abstract: Inhibitors of glucosidase, especially those related to castanospermine, are effective in preventing or ameliorating conditions such as liver damage and emphysema that are present in individuals who produce a mutant form of antitrypsin, &agr;1-ATZ. Also effective in the method of the invention are imino sugars and their reduced forms in general as well as phenylbutyric acid. These compounds enhance the secretion of the mutant form, which retains substantial biological activity, and do not impair its degradation in the endoplasmic reticulum.

Abstract: The present invention relates to novel biphenyl-substituted cyclic ketoenols of the formula (I) in which W represents hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, Z represents hydrogen, halogen, alkyl, alkoxy, halogenoalkyl or halogenoalkoxy, CKE represents one of the groups  in which A, B, D, L, M, Q1, Q2, Q3, Q4, Q5 and Q6 are as defined in the description, to preparation and to their use as pesticides and herbicides.

Abstract: A lactam-aldehyde compound represented by the formula (I) shown in the specification. The lactam-aldehyde compound may be prepared by subjecting a lactone-imine compound represented by formula (III) shown in the specification to an isomerization reaction. The precursor lactone-imine compound may be prepared by rearrangement of a 3,5-dioxa-12-azawurtzitane compound.

Abstract: This invention relates to 6 or 7 substituted swainsonine analogues, processes for their preparation and use as therapeutic agents. The invention also relates to pharmaceutical compositions containing the compounds and their use as therapeutics.

Abstract: The invention relates to a novel process for producing a the intermediary compound &agr;,&agr;′,dicyano-&bgr;,&bgr;-pentamethyleneglutarimide. The process includes the steps of reacting a ketone such as cyclohexanone with ethylcyanoacetate in the presence of ammonium hydroxide.

Abstract: Described herein are compounds selective for a 5-HT1D receptor, which have the general formula:

Abstract: The present invention relates to muscarinic receptor modulators, specifically, 7-oxo-2-azabicyclo[2.2.1]heptanes of formula (I) which are useful for the treatment of various diseases and conditions, for example, Alzheimer's disease, glaucoma, psychosis, particularly schizophrenia or schizophreniform conditions, mania, pain, bipolar disorder, depression, sleeping disorders, epilepsy, gastrointestinal motility disorders, urinary incontinence, and cognition enhancement.

Abstract: Oligomeric compounds and methods of making the compounds having the formula: T&Parenopenst;M—F&Parenclosest;i&Parenopenst;M—F′&Parenclosest;jM  (III) wherein i and j are integers from about 0 to 300 and the sum of i and j is greater than 2, wherein the units F, F′ and T are derived from one or more multi-functional carbonyl compounds of general structure DO—CO—CRaRb—(—CRcRd—)n—NH—(Y)m—CO—OD  (IV) wherein n is an integer from 1 to 15, m is either 0 or 1; Ra, Rb, Rc, and Rd, are each a hydrogen or a hydrocarbyl group; Y is CO—(CReRf)p, wherein Re and Rf are each a hydrogen or hydrocarbyl group and p is zero or an integer from 1 to 20 or CO—C6H4—, D is a hydrocarbyl group, and M is a moiety derived from one or more diamino or dihydroxy compounds that contain a 4-aminopiperidine radical.

Abstract: The present application relates to novel opioid receptor antagonists and agonists, methods of making these compounds, and methods of use thereof.

Abstract: It is to provide a cyclic imide derivative which is useful as an active ingredient of a pharmaceutical composition. A pharmaceutical composition which comprises, a cyclic imide derivative represented by the general formula (I): wherein Q1 is a single bond, —CH2—, —O—, —S— or —NH—, each of Q2 and Q3 is —C(O)—, —C(S)— or —CH2—, provided that at least one of Q2 and Q3 is —C(O)— or —C(S)—, Z is a single bond or a lower alkanediyl group, R is an aryl group which may be substituted or a cycloalkyl group which may be substituted, X is a nitro group, an amino group which may be acylated, a cyano group, a trifluoromethyl group, a hydroxyl group, a halogen atom, an alkyl group, an alkoxy group or an alkylthio group, m is an integer of from 0 to 4, and when m is 2 or above, X may be the same or different, or its salt.

Abstract: A light emitting device material comprising a compound represented by the following formula (I): wherein R1, R2 and R3, which may be the same or different, each represents an aryl group, a heterocyclic group or an aliphatic hydrocarbon group, provided that at least one of R1, R2 and R3 represents an aryl group or a heterocyclic group, containing a group represented by the following formula (II): wherein R4, R5 and R6, which may be the same or different, each represents a hydrogen atom or a substituent; X1 represents an oxygen atom, a sulfur atom, N—RX1 or CRX2RX3; RX1, RX2, RX3, which may be the same or different, each represents a hydrogen atom or a substituent; R4, R5, R6 and X1 may be linked to each other to form a ring; Y represents an oxygen atom, a sulfur atom, or N—RY1; and RY1 represents a hydrogen atom or a substituent.

Abstract: Compounds of the formula: where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the picornaviral 3C protease. Also disclosed are compounds of the formula: where the formula variables are as defined herein that advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as rhinovirus 3C proteases. Intermediates and synthetic methods for preparing such compounds are also described.

Abstract: The present invention relates to pharmaceutical compositions comprising and methods of using an N-linked urea or carbamate of a heterocyclic thioester for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance.

Abstract: Methods for performing ring-opening cross-metathesis reactions on solid support are disclosed. Substituted cyclic compounds, libraries of the compounds, and methods of using the compounds to treat bacterial infections are also disclosed.

Abstract: New photoacid generator compounds (“PAGs”) are provided and photoresist compositions that comprise such compounds. In particular, non-ionic PAGs are provided that contain an oxime sulfonate group, and/or an N-oxyimidosulfonate group. PAGs of the invention are particularly useful as photoactive components of photoresists imaged at short wavelengths such as 248 nm, 193 nm and 157 nm.

Abstract: Disclosed are compounds of the Formula: or the pharmaceutically acceptable non-toxic salts thereof wherein: the C ring is a(n) (un)substituted carbocycle; X is hydrogen, hydroxyl or lower alkyl; and W is (un)substituted alkyl, aryl, arylalkyl, or heteroaryl, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.

Abstract: This invention relates to an improved process for preparing (+) (1S,2R,3S)-3-[2-(2-hydroxyeth-1-yloxy)-4-methoxyphenyl]-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof, preferably the ethylene diamine 2:1 salt. This invention relates to novel intermediates useful in preparing (+) (1S,2R,3S)-3-[2-(2-hydroxyeth-1-yloxy)-4-methoxyphenyl]-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid. This invention relates to an improved process for preparing (+) (1S,2R,3S)-3-(2-carboxymethoxy-4-methoxyphenyl)-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof, preferably the disodium salt. This invention relates to novel intermediates useful in preparing (+) (1S,2R,3S)-3-(2-carboxymethoxy-4-methoxyphenyl)-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid.

Abstract: It is to provide a cyclic imide derivative which is useful as an active ingredient of a pharmaceutical composition. A pharmaceutical composition which comprises, a cyclic imide derivative represented by the general formula (I): wherein Q1 is a single bond, —CH2—, —O—, —S— or —NH—, each of Q2 and Q3 is —C(O)—, —C(S)— or —CH2—, provided that at least one of Q2 and Q3 is —C(O)— or —C(S)—, Z is a single bond or a lower alkanediyl group, R is an aryl group which may be substituted or a cycloalkyl group which may be substituted, X is a nitro group, an amino group which may be acylated, a cyano group, a trifluoromethyl group, a hydroxyl group, a halogen atom, an alkyl group, an alkoxy group or an alkylthio group, m is an integer of from 0 to 4, and when m is 2 or above, X may be the same or different, or its salt.

Abstract: Crystalline salts of swainsonine, and methods using same.

Abstract: Bicyclic amino alcohols, whose amino group and hydroxy group are bonded in positions 1,3 adjacent to the bridge, for example 1

Abstract: Described is a process for the preparation of Compound (7) in accordance with the following reaction scheme by reacting Compound (5) with ethylene glycol in a solvent in the presence of a Lewis acid, thereby obtaining Compound (6), and then reacting the resulting compound with a carbonate diester in a solvent in the presence of a metal alkoxide (R1, R6 each represents a C1-6 alkyl group or the like and R5 represents H or C1-5 alkyl group). Compound (7) so obtained is useful as an intermediate for camptothecins useful as antitumor agents.

Abstract: The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.