Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of fibromyalgia pain may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of injury, post-operative pain, osteoarthritis, rheumatoid arthritis, multiple sclerosis, spinal cord injury, migraine, HIV related neuropathic pain, post herpetic neuralgia, diabetic neuropathy, bipolar depression, stress, cancer pain, and lower back pain.

Abstract: The present invention relates to fungicidal N-cycloalkyl-N-[(cycloalkenylphenyl)methylene]carboxamide derivatives and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.

Abstract: The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.

Abstract: A novel process of preparing a Grignard reagent is disclosed. The process is effected by electrochemically reacting a Grignard precursor with an electrode which comprises a metal for forming the Grignard reagent, in the presence an electrolyte solution that comprises a room temperature ionic liquid (RTIL). Electrochemical cells and systems for performing the process, and uses thereof in various applications are also disclosed.

Abstract: The present invention provides an oral pharmaceutical composition for the treatment of premature ejaculation, and the composition provides the effective and excellent treatment of premature ejaculation as well as reduced side effects like nausea, vomiting, drowsiness, sedation effect, awakening effect, and weight-loss etc.

Abstract: The present invention relates to novel tetralin ER-? agonist compounds, pharmaceutical compositions thereof, and use of these compounds to treat a ER-? mediated disease such as nocturia, obstructive uropathy, benign prostatic hypertrophy, obesity, dementia, hypertension, incontinence, colon cancer, prostate cancer, infertility, depression, leukemia, inflammatory bowel disease, and arthritis.

Abstract: Benzocycloheptyl analogs that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs, which, after phosphorylation, can behave as agonists at S1P receptors.

Abstract: A process for preparing cycloaliphatic amines by hydrogenating the corresponding aromatic compounds with hydrogen-comprising gas at a temperature of from 30 to 280° C. and a pressure of 50-350 bar, in the presence of ruthenium catalysts. The hydrogenation is performed in the presence of from 1% by weight to 500% by weight, based on the catalyst calculated as elemental ruthenium (Ru), of suspended inorganic additives, and to the use of the cycloaliphatic amines as a synthesis unit.

Abstract: Benzocycloheptyl analogs that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs, which, after phosphorylation, can behave as agonists at S1P receptors.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.

Abstract: The present invention relates to novel organic electroluminescent compounds having an indenofluorene or a difluorene skeletal, and a display employing the same as an electroluminescent material. The organic electroluminescent compounds according to the invention exhibit good electroluminescent efficiency and excellent life property, so that an OLED device having very good operative lifetime can be advantageously prepared.

Abstract: The invention provides novel ?2 adrenergic receptor agonist compounds of formula (I): wherein R1-R13 and w have any of the values described in the specification. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with ?2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: (wherein n is an integer of 0 to 10; R1 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, substituted or unsubstituted cycloalkyl, substituted or unsubstituted lower alkoxycarbonyl, substituted or unsubstituted heterocyclic-alkyl, substituted or unsubstituted aryl, —CONR7R8, —NR9R10, etc.; R2 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, etc.; R3 and R5 may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, etc.; R4 and R6 may be the same or different, each represent a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, etc.) Provided are an Hsp90 family protein inhibitor comprising, as an active ingredient, a benzene derivative of formula (I) or a prodrug thereof or a pharmaceutically-acceptable salt thereof, etc.

Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, and q have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.

Abstract: This invention relates to a process for preparing R-gossypol L-phenylalaninol dienamine using non-chromatographic purification methods. In particular, the invention is directed to resolution of R- and S-gossypol L-phenylalaninol dienamine by crystallization. R-gossypol L-phenylalaninol dienamine is a useful intermediate for the preparation of R-(?)-gossypol and R-(?)-gossypol acetic acid co-crystal. R-(?)-Gossypol acetic acid and its co-crystal is useful for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death.

Abstract: Compounds of the formula (I) wherein R is phenyl, or phenyl substituted by Cl, Br, C1-C4alkyl or CF3; R1 is H or methyl or ethyl; R2 is H or methyl or acyl; R3 is H or methyl; R?4 is —CH3 or ?CH2; may be obtained in high enantiopurity by hydrogenation of a compound of the formula (II) wherein R and R3 are as in formula (I); A is acyl; and R4 is —CH3 or ?CH2; in the presence of a chiral Rhodium or Ruthenium catalyst. Residues R1 as methyl or ethyl and/or R2 as H or methyl may subsequently be introduced without racemization by deacylation and optional alkylation.

Abstract: The present invention provides processes and intermediates for the preparation of aminoethoxybenzyl alcohols of Formula I useful in the production of pharmaceutically useful compounds

Abstract: The present invention relates to novel dihydronaphthalene compounds, compositions, methods for using the same, and processes for preparing the same. The present invention also relates to novel total synthesis approaches for preparing these compounds. In addition, the present invention relates to methods of producing quantities of isomers of these compounds and separating and purifying them using chiral separation techniques. The present invention also relates to methods of producing quantities of a single isometric compound without the need for chiral separation techniques.

Abstract: The present invention relates to a process for converting a tertiary OH group of an organic compound into a tertiary Cl group of the organic compound by using a solvent selected from the group comprising toluene, o-xylene, m-xylene, p-xylene and mixtures thereof, and thionyl chloride as the chlorinating agent.

Abstract: The present invention provides novel phenol derivatives represented by the formula: wherein the carbon atom marked with (S) represents a carbon atom in S configuration; Z represents the group represented by the formula: or the formula: wherein the carbon atoms marked with (R) represents a carbon atom in R configuration, and a method to produce a phenol derivative represented by the formula (A): (wherein the carbon atom marked with (R) and (S) have the same meanings as defined above) which comprises using any of those derivatives as an intermediate therefore.

Abstract: This invention provides a method of preparing amine stereoisomers, which comprises stereoselectively reducing a sulfinylimine that bears on the sulfinyl group a residue of an alcohol, thiol or amine, or reacting a sulfinylimine stereoisomer that bears on the sulfinyl group a residue of an alcohol, thiol or amine with a source of a nucleophile, to afford a sulfinylamine stereoisomer, followed by contacting the sulfinylamine stereoisomer with a reagent suitable for the cleavage of a sulfur-nitrogen bond, to afford an amine stereoisomer. It also provides novel intermediates useful in the method, and the use of certain of the intermediates in the preparation of sulfoxide and sulfinylamine stereoisomers.

Abstract: Methods and compositions of antidepressants and analogs thereof for inducing local long-lasting anesthesia and analgesia are provided. The methods and compositions are useful for alleviating acute and chronic pain, particularly useful for treating a localized pain.

Abstract: Disclosed are compounds of the formula (I) wherein R1, R2 R3 R4 R5, R6 and N are as disclosed herein. The compounds are useful for the treatment of chronic and acute pain.

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

Abstract: This invention encompasses novel methods of preparing sibutramine and sibutramine derivatives, and stereomerically pure sibutramine derivatives in particular. Examples of sibutramine derivatives include, but are not limited to, sibutramine metabolites such as desmethylsibutramine and didesmethylsibutramine. The invention further encompasses novel compounds useful in the synthesis of sibutramine derivatives.

Abstract: Cytotoxic polyamine analogues are provided that are useful for treating diseases where it is desired to inhibit cell growth and/or proliferation, for example cancer and post-angioplasty injury.

Abstract: The invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 is H, chlorine, or bromine; R2 is electron attractive groups selected from the group consisting of CF3, CN, fluorine, CH3SO3, CF3SO3, and NO2; R3 is linear or branched alkyl having 1 to 10 carbon atoms, linear or branched alkoxyalkyl having 2 to 10 carbon atoms, aliphatic alcohol having 1 to 10 carbon atoms, or cycloalkyl having 3 to 6 carbon atoms. The invention also relates to methods for preparing the said compounds and the composition comprising the same. The compounds of the present invention have the effect of &bgr;2-receptor agonist and can be used for the treatment of asthma and bronchitis.

Abstract: The present invention relates to smooth muscle spasmolytic agents, pharmaceutical compositions containing them and method of using said compounds and compositions for the treatment of urinary incontinence, and other smooth muscle contractility conditions. More particularly, the present invention relates to certain metabolically stabilized secondary amines having smooth muscle relaxing properties while avoiding, on administration to a mammal, adverse side effects such as prominent antimuscarinic, arrhythmogenic and cardiodepressive effects.

Abstract: Compounds of formula (1): wherein R1, R2, R3, R4, R5 and R6 are independently selected from hydrogen, alkyl, aryl and non-aromatic heterocyclic groups, or each of one or more pair(s) of the substituent groups R1 to R6 may together form a 3,4,5,6,7 or 8-membered ring containing 0,1 or 2 heteroatom(s); R7 is selected from alkyl, aryl and non-aromatic heterocyclic groups; and R8 is selected from hydrogen, halogen, alkyl, aryl and non-aromatic heterocyclic groups; and pharmaceutically acceptable salts and prodrugs thereof, are useful for treating conditions generally associated with abnormalities in glutamatergic transmission.

Abstract: The present invention is directed to forms II, III, V, VI, VII, VIII, IX and X of sertraline hydrochloride and novel methods for their preparation. According to the present invention, sertraline hydrochloride polymorph II may be produced by slurrying sertraline hydrochloride polymorph VI in aprotic organic solvent. Sertraline hydrochloride polymorphic form III may be produced by heating sertraline hydrochloride polymorphs V and VI. Sertraline hydrochloride forms V and VI may be produced from either sertraline hydrochloride or sertraline base by crystallization. Sertraline hydrochloride Form VII may be produced by suspending sertraline chloride polymorph V in water, followed by filtration. Sertraline hydrochloride Forms VIII and IX may be produced by suspending sertraline base in water followed by acidification and filtration. Sertraline hydrochloride Form X may be produced by suspending sertraline hydrochloride in benzyl alcohol with heating, followed by filtration.

Abstract: The present invention is directed to Form II of sertraline hydrochloride and novel methods for its preparation. According to the present invention, sertraline hydrochloride Form II may be produced directly form sertraline base or sertraline mandelate. It may also be produced from sertraline hydrochloride solvate and hydrate forms, and crystallized from new solvent systems. Pharmaceutical compositions containing sertraline hydrochloride Form II and methods of treatment using such pharmaceutical compositions are also disclosed.

Abstract: The present invention provides an efficient method of making O-desmethylvenlafaxine.

Abstract: A NK1 antagonist having the formula (I), with the variables defined herein, which is useful for treating a number of disorders, including emesis, depression, anxiety and cough: 1

Abstract: One aspect of the present invention relates to amines. A second aspect of the present invention relates to the use of the amines as inhibitors of a mammalian anandamide transporter. The compounds of the present invention will also find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to asthma, neuropathic pain, persistent pain, inflammatory pain, hyperactivity, hypertension, brain ischemia, Parkinson's disease, spasticity, Tourette's syndrome, schizophrenia, hemorrhagic shock, septic shock, cardiac shock, migrane, Horton's headache, multiple sclerosis, anorexia, AIDS wasting syndrome, organ rejection, autoimmune diseases, allergy, arthritis, Crohn's disease, malignant gliomas, neurodegenerative diseases, Huntington's chorea, glaucoma, nausea, anxiety, psychosis, attention deficit hyperactivity disorder, premature ejaculation, and stroke.

Abstract: Provided are processes for preparation of crystalline sertraline hydrochloride Form II substantilly free of other polymorphic forms of sertraline hydrochloride, preferably on an industrial scale.

Abstract: Described are compounds of Formula I and Formula II and their pharmaceutically acceptable salts. The compounds of Formulas I and II are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease.

Abstract: Described are cyclohexylamine derivatives of Formula (I), Formula (II) or Formula (III) and their pharmaceutically acceptable salts thereof. The compounds are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease. The substituents are described in the specification.

Abstract: The invention relates to high purity (1R,2S,4R)-(−)-2-[(2′-{N,N-dimethylamino}-ethoxy)]-2-[phenyl]-1,7,7-tri-[methyl]-bicyclo[2.2.1]heptane and pharmaceutically acceptable acid addition salts thereof containing not more than 0.2% of (1R,3S,4R)-3-[(2′-{N,N-dimethylamino}-ethyl)]-1,7,7-tri-[methyl]-bicyclo[2.2.1]heptane-2-one and/or of a pharmaceutically acceptable acid addition salt thereof. Furthermore the invention is concerned with a process for the preparation of these compounds. Moreover the invention relates to medicaments containing 1 or more of these compounds and their use.

Abstract: Compounds of formula I are effective in treating disorders modulated by opiate receptor activity and/or monoamine activity.

Abstract: This invention encompasses novel methods of preparing sibutramine and sibutramine derivatives, and stereomerically pure sibutramine derivatives in particular. Examples of sibutramine derivatives include, but are not limited to, sibutramine metabolites such as desmethylsibutramine and didesmethylsibutramine. The invention further encompasses novel compounds useful in the synthesis of sibutramine derivatives.

Abstract: Disclosed are a compound of tramadol and a sugar substitute, pharmaceutical compositions and sustained-release formulations comprising the compound, and methods of treatment using the compound. The tramadol compound according to the present invention has reduced bitter taste of tramadol and is more acceptable to the patient.

Abstract: The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a hedgehog agonist, such as the compounds depicted in FIGS. 32 and 33. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal ptc pathway or agonizing smoothened or hedgehog activity.

Abstract: The invention is directed, in part, to racemic and stereomerically pure 2-hydroxy derivatives of sibutramine and its metabolites, and 2-hydroxy derivatives of desmethylsibutramine and didesmethylsibutramine in particular. The invention is further directed to novel methods of preparing these derivatives are also disclosed.

Abstract: A process for the preparation of venlafaxin and/or the physiologically acceptable addition salts thereof that consists of reacting a compound of general formula (II) where R is a C1-C10 alkyl, aryl, aralkyl or cycloalkyl group of 3 to 6 atoms of carbon, with a organomagnesium compound of general formula (III) where X is an atom of halogen and, if desired, a salt of the thus obtained venlafaxin is formed by reaction thereof with a physiologically acceptable acid.

Abstract: This invention encompasses novel methods of preparing sibutramine and sibutramine derivatives, and stereomerically pure sibutramine derivatives in particular. Examples of sibutramine derivatives include, but are not limited to, sibutramine metabolites such as desmethylsibutramine and didesmethylsibutramine. The invention further encompasses novel compounds useful in the synthesis of sibutramine derivatives.

Abstract: The invention concerns compounds of formula (I) wherein A, X, Y, n, R1, R2 and R3 are as defined in claim 1. Said compounds are specifically binding to sigma receptors particularly those of the peripheral nervous system.

Abstract: The invention relates, in part, to making of making and using, and compositions comprising, racemic and stereomerically pure cyclobutylalkylamines, including hydroxylated sibutramine and hydroxylated metabolites of sibutramine. Methods of treating and preventing a variety of diseases and disorders are disclosed, as are pharmaceutical compositions and unit dosage forms that comprise compounds of the invention.

Abstract: The present invention is directed to (+)-cis-sertraline hydrochloride and methods of preparation. The present invention also includes processes for making sertraline having a cis/trans ratio greater than 3:1, greater than or equal to 8:1, or between about 8:1 and about 12:1, from the Schiff base of sertralone, sertraline-1-imine.

Abstract: The invention relates to high purity (1R,2S,4R)-(−)-2-[(2′-{N,N-dimethylamino}-ethoxy)]-2-[phenyl]-1,7,7-tri-[methyl]-bicyclo[2.2.1]heptane and pharmaceutically acceptable acid addition salts thereof containing not more than 0.2% of (1R,3S,4R)-3-[(2′-{N,N-dimethylamino}-ethyl)]-1,7,7-tri-[methyl]-bicyclo[2.2.1]heptane-2-one and/or of a pharmaceutically acceptable acid addition salt thereof. Furthermore the invention is concerned with a process for the preparation of these compounds. Moreover the invention relates to medicaments containing 1 or more of these compounds and their use.

Abstract: The naphthyloxyacetic acid derivatives of the formula (I) wherein A is H, -(alkylene)COOR1, -(alkylene)CONR2R3, -(alkylene)OH, -(alkylene)tetrazole, -(alkylene)CN; E is single bond or alkylene; G is —S—, —SO—, —SO2—, —O— or —NR4—; L is alkylene, —(CH2)m—CH═CH—(CH2)n— or —(CH2)x—CH(OH)—(CH2)y—; M is phenyl, phenyl(thio, oxy, amino), diphenylmethyl, diphenylmethyl(thio, oxy, amino), and pharmaceutical composition comprising them as an active ingradient. The compounds of the formula (I) can combine PGE2 receptor and exhibit the activity to antagonize or agonize for PGE2 receptor. Therefore, they are useful as anti-hyperlipemia, for the prevention of abortion, for analgesics, as antidiarrheals, sleep inducer, diuretic, anti-diabetes, abortient, cathartics, antiulcer, anti-gastritis or antihypertensive etc.