Abstract: The present invention provides a process for the preparation of N-phenoxyisopropyl ethanolamine of Formula (II) and its conversion to Phenoxybenzamine of Formula (I) or pharmaceutically acceptable salts thereof.

Abstract: A composition and a process for straightening hair are disclosed. The process includes coating keratin fibers with a composition comprising a thermally-activated agent and contacting the coated keratin fibers with a heating device at a temperature of at least 185° C. for sufficient time to modify the keratin fibers. The thermally-activated agent comprises a heterocyclic compound containing two heteroatoms selected from nitrogen and oxygen in a 5 or 6-membered ring, such as a cyclic alkylene carbonate.

Abstract: An optically active spirolactone compound is highly enantioselectively produced by using an iodoarene derivative which can be synthesized easily and which is not racemized easily. A hypervalent iodine compound precursor (iodoarene derivative) which was able to be designed flexibly was synthesized from 2,6-dihydroxyiodoarene by using 1,2-aminoalcohol as a chiral source in short steps, a hypervalent iodine compound was prepared in a reaction system (in situ) by using a catalyst quantity of the resulting precursor in the presence of a stoichiometric quantity of m-CPBA, and a spirolactonization reaction of 3-(1-hydroxy-2-naphthyl)propionic acid was induced. As a result, a corresponding spirolactone compound was obtained at a high enantiomeric excess.

Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract: An optically active spirolactone compound is highly enantioselectively produced by using an iodoarene derivative which can be synthesized easily and which is not racemized easily. A hypervalent iodine compound precursor (iodoarene derivative) which was able to be designed flexibly was synthesized from 2,6-dihydroxyiodoarene by using 1,2-aminoalcohol as a chiral source in short steps, a hypervalent iodine compound was prepared in a reaction system (in situ) by using a catalyst quantity of the resulting precursor in the presence of a stoichiometric quantity of m-CPBA, and a spirolactonization reaction of 3-(1-hydroxy-2-naphthyl)propionic acid was induced. As a result, a corresponding spirolactone compound was obtained at a high enantiomeric excess.

Abstract: The present disclosure provides novel oligo phenylene ethynylene (OPE) compounds, methods for synthesizing these compounds, and materials and substances incorporating these compounds. The various OPEs show antibacterial, antiviral and anti-fungal activity.

Abstract: Anion exchange-hydrophobic mixed mode ligands and methods of their use are provided.

Abstract: Provided are compounds according to the following Formula I: The Formula I compounds are activated in the presence of reactive oxygen species (ROS) and are therefore selective anti-cancer therapeutics for cancers associated with elevated ROS. Also provided are methods and pharmaceutical compositions for treating cancers associated with increased ROS.

Abstract: A paste composition comprises a dye containing a novel oligomeric compound with improved dispersion performance. The oligomeric compound comprises a tail structure consisting of hydrophilic and hydrophobic blocks and an amine or imidazole head structure. The paste composition can be used to prepare a semiconductor electrode of a solar cell. A semiconductor electrode produced using the paste composition and a solar cell fabricated using the semiconductor electrode exhibit greatly improved power conversion efficiency and superior processability.

Abstract: The invention provides compounds of formula I F-L-Q (I) where F comprises a fluorophore capable of absorbing energy at an excitation wavelength and, in the absence of a quencher, emitting energy at an emission wavelength, which is different than the excitation wavelength; Q comprises a quencher; L comprises a linker moiety having two ends, one end being covalently bound to F and the other end being covalently bound to Q. The compounds are capable of undergoing a reversible reaction (1), provided below: (1) where Q+ is an oxidized form of Q representing the absence of a quencher, Ox comprises an oxidizing agent, which is capable of oxidizing Q to its oxidized form Q, and Red comprises a reducing agent, which is capable of converting Q back to its reduced form Q. The compounds can undergo photo-induced electron transfer when irradiated with energy and when Q exists in its oxidized form, Q+.

Abstract: The present invention describes a series of therapeutically active compounds of formula I, X—Y—Z??(I) that are useful for treating a disorder in a mammal. In the formula I, X and Z, which may be same or different, are independently selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted heterocyclic group or substituted or unsubstituted heterocyclylalkyl; and Y is a linker selected from —O—, —S—, —NH—, —(CH2)n—, —CO—, —CONRa—, —NRaCO—, —NRaCOO—, —COO—, —CONRaCO—, —CONRaCOO— and —COOCOO—.

Abstract: The subject of the invention is a group of new derivatives of aminoalka?ols, more specifically [(phenoxy)alkyl]aminoalkanols and [(phenoxy)acyl)aminoalkanols, their method of obtaining and their use for production of a medicine which is used in the prophylaxis, prevention and/or treatment of diseases or symptoms having neurological background and for production of a medicine with anticonvulsant activity, which is used in seizures of various origin, also in the limbic system, in myoclonic or sound-induced seizures, in psychomotor epilepsy, as well as in relieving neuropathic or inflammatory pain.

Abstract: This invention relates to benzonitryl and nitrobenzyl derivatives that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds. These compounds are useful, for example, in the treatment or prophylaxis of conditions or disorders that respond to selective androgen receptor modulation.

Abstract: The present invention relates to new aminopropanol modulators of beta-1 adrenergic receptor activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present application describes deuterium-enriched atomoxetine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: The present invention discloses a process for the preparation of atomoxetine hydrochloride in a pure crystalline form, characterised by an XRPD spectrum as in FIG. 1. It is also object of the present invention to provide methods to obtain pure atomoxetine hydrochloride without the use of methylene chloride.

Abstract: Thyronamine derivatives and analogs, methods of using such compounds, and pharmaceutical compositions containing them are disclosed.

Abstract: The invention relates to the use of copper-catalyzed nucleophilic aromatic substitution reaction for preparing 3-aryloxy-3-arylpropylamines and more specifically to a method of preparing certain 3-aryloxy-3-arylpropylamines and the pharmaceutically acceptable addition salts thereof, comprising reacting an amino alcohol with a haloaromatic compound in the presence of a base and a catalytic copper source, and in the absence of a separate ligand.

Abstract: The present application describes deuterium-enriched atomoxetine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: Stable Atomoxetine hydrochloride, a process for the manufacture thereof, the use of stable Atomoxetine Hydrochloride for making a pharmaceutical formulation, a process for the preparation of any form of Atomoxetine Hydrochloride, and an analytical method for analyzing the stability of Atomoxetine Hydrochloride are provided.

Abstract: Provided are processes for preparing tomoxetine comprising reacting N-methyl-3-hydroxy-3-phenylpropylamine with dimethylsulfoxide (DMSO) and 2-fluorotoluene in the presence of an alkali base to form tomoxetine. Also provided is the conversion of said tomoxetine into atomoxetine or a pharmaceutically acceptable salt thereof.

Abstract: This invention provides a compound, or its possible salt, having the formula, wherein: Re and ?Re are OH, optionally independently etherified or esterified; Z is —CH2CH2— or —C(R4,R5)—, wherein R4 and R5 are independently H, (1C-2C)alkyl or form together a spiro(3C-5C)cycloalkyl; R1 is H, halogen, CF3, or (1C-4C)alkyl; R2 and R3 are independently H, halogen, —CF3, —OCF3, (1C-8C)alkyl, hydroxy, (1C-8C)alkyloxy, aryloxy, aryl(1C-8C)alkyl, halo(1C-8C)alkyl, —O(CH2)mX, wherein X is halogen or phenyl and m=2-4; —O(CH2)mNRaRb, —S(CH2)mNRaRb or —(CH2)mNRaRb, wherein m=2-4 and wherein Ra, Rb are independently (1C-8C)alkyl, (2C-8C)alkenyl, (2C-8C)alkynyl, or aryl, which alkyl, alkenyl and aryl can optionally be substituted with halogen, —CF3, —OCF3, —CN, —NO2, —OH, (1C-8C)alkoxy, aryloxy, carboxyl, (1C-8C)alkylthio, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl or halo(1C-8C)alkyl; or Ra and Rb form a 3-8 membered ring structure, optionally substituted with halogen, —CF3, —OCF3, —CN, —NO2, hydroxy, hydroxy(1C-

Abstract: Phenoxy amine compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract: The invention provides sodium channel modulating compounds of formula I: wherein X, Y, Q, R1, w, and R2 have any of the values defined in the specification, and salts thereof, which are useful for treating diseases or conditions associated with sodium channel activity, such as neuropathic pain. The invention also provides pharmaceutical compositions comprising a compound of formula (I) or a salt thereof, as well as therapeutic methods comprising administering such a compound or salt to a mammal (e.g. a human).

Abstract: The present invention is directed to compositions comprising lysophosphatidic acid analogs and methods of using such analogs as agonist or antagonists of LPA receptor activity. In addition the invention is directed to LPA receptor agonists that vary in the degree of selectivity at individual LPA receptors (i.e. LPA1, LPA2 and LPA3). More particularly the present invention is directed to LPA analogs wherein the glycerol is replaced with ethanolamine and a variety of substitutions have been linked at the second carbon atom.

Abstract: A novel calcium receptor active compound having the formula is provided: Ar1—[CR1R2]p—X—[CR3R4]q—[CR5R6]—NR7—[CR8R9]—Ar2 wherein: Ar1 is selected from the group consisting of aryl, heteroaryl, bis(arylmethyl)amino, bis(heteroarylmethyl)amino and arylmethyl(heteroarylmethyl)amino; X is selected from the group consisting of oxygen, sulfur, sulfinyl, sulfonyl, carbonyl and amino; R1, R2, R3, R4, R5, R6, R7, R8 and R9 are, for example, hydrogen or alkyl; Ar2 is selected from the group consisting of aryl and heteroaryl; p is an integer of from 0 to 6, inclusive; and, q is an integer of from 0 to 14, inclusive.

Abstract: The present invention relates to new cinnamic acid salts of salmeterol, processes for the preparation thereof as well as the use thereof as pharmaceutical compositions.

Abstract: A novel calcium receptor active compound having the formula is provided: Ar1—[CR1R2]p—X—[CR3R4]q—[CR5R6]—NR7—[CR8R9]—Ar2 wherein: Ar1 is selected from the group consisting of aryl, heteroaryl, bis(arylmethyl)amino, bis(heteroarylmethyl)amino and arylmethyl(heteroarylmethyl)amino; X is selected from the group consisting of oxygen, sulfur, sulfinyl, sulfonyl, carbonyl and amino; R1, R2, R3, R4, R5, R6, R7, R8 and R9 are, for example, hydrogen or alkyl; Ar2 is selected from the group consisting of aryl and heteroaryl; p is an integer of from 0 to 6, inclusive; and, q is an integer of from 0 to 14, inclusive.

Abstract: An improved process for the preparation of polyalkylphenoxyaminoalkanes which comprises the aminoethylation of a polyalkylphenol compound in the presence of a basic catalyst with 2-oxazolidinone or a derivative thereof having the following formula: wherein R1 and R2 are independently hydrogen or lower alkyl having 1 to about 6 carbon atoms and wherein the polyalkyl group of said polyalkylphenol has an average molecular weight in the range of about 600 to 5,000 and wherein the process is carried out in the presence of an alcohol.

Abstract: A process for the preparation of polyalkylphenoxyaminoalkanes which comprises the aminoethylation of a polyalkylphenol compound in the presence of a basic catalyst with &bgr;-amino alcohol or derivative thereof having the following structure: R1NH—CHR2—CH2—OH and a dialkyl carbonate having the following formula: (R3O)2CO wherein R1 and R2 are independently hydrogen or lower alkyl having 1 to about 6 carbon atoms, hydroxylalkylene, phenyl, alkaryl, or aralkyl, R3 is lower alkyl having 1 to about 6 carbon atoms, and wherein the polyalkyl group of said polyalkylphenol has an average molecular weight in the range of about 600 to 5,000. Optionally, an alcohol co-solvent having the structure R4—OH wherein R4 is an alkyl group of about 4 to 10 carbon atoms may be used.

Abstract: The invention provides a novel compound 4-(p-methoxy-phenyl)-2-aminobutane exhibiting growth inhibition and antifeedant activity and represented by the structural formula. C11H17ON=4-(p-methoxy phenyl)-2-amino butane and an insecticidal composition comprising an effective amount of the novel compound and appropriate adjuvant.

Abstract: The compounds of this invention comprise 2-10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Na+ channel, thereby modulating the biological activities thereof.

Abstract: A process for the preparation of polyalkylphenoxyaminoalkanes which comprises the aminoethylation of a polyalkylphenol compound in the presence of a basic catalyst with 2-oxazolidinone or a derivative thereof having the following formula: wherein R1 and R2 are independently hydrogen or lower alkyl having 1 to about 6 carbon atoms and wherein the polyalkyl group of said polyalkylphenol has an average molecular weight in the range of about 600 to 5,000.

Abstract: The present invention relates to novel 3-alkoxybenzylamine derivatives of general formula (1): which are useful as medicinal products and in particular as antipsychotic agents.

Abstract: The present invention provides novel processes for the preparation of Form A of fluoxetine hydrochloride.

Abstract: The present invention provides novel amorphous fluoxetine hydrochloride as a useful intermediate for the preparation of Form A of fluoxetine hydrochloride.

Abstract: The present invention provides novel processes for the preparation of Form A of fluoxetine hydrochloride.

Abstract: The present invention relates to novel, antiarrhythmically active phenoxyalkylamine derivatives possessing a double point of attack. More particularly, the present invention relates to new phenoxyalkylamine derivatives of the formula (1) wherein R1 and R2, independently from each other, mean hydrogen, halogen or C1-4 alkyl group; R3, R4 and R5, independently from each other, stand for hydrogen or C1-4 alkyl group; R6 represents hydrogen, C1-4 alkyl or benzyl group; R7 means nitro group or amino group optionally monosubstituted by C1-4 alkyl, benzoyl, C1-4 alkylcarbonyl, C1-4 alkylsulfonyl, C1-4 alkylcarbamoyl or C1-4 alkylthiocarbamoyl group; both n and m are 0 or 1, with the proviso that R2 is different from hydrogen, when R1 is hydrogen, as well as stereoisomers or mixtures of stereoisomers thereof, acid addition salts thereof and hydrates, prodrugs and metabolites of all these compounds.

Abstract: The invention relates to methods for the treatment of central nervous system disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising an effective amount of certain sigma receptor ligands to a patient in need of such treatment. The invention further relates to novel sigma receptor ligands having high binding to the sigma receptor and pharmaceutical compositions thereof. Unexpectedly, certain of the sigma receptor ligands of the present invention have selectivity for the sigma receptor over the DA, PCP and 5-HT.sub.1A receptors.

Abstract: Novel amine derivatives of the following general formula (I): ##STR1## (wherein) A may denote --(CH.sub.2)--O--, --(CH.sub.2).sub.2 --O--, or --(CH.sub.2).sub.2 --NH--;B may denote --(CH.sub.2).sub.2 --;R.sub.1 may denote a hydrogen atom, a halogen atom, a nitro group, a 1-pyrrolyl group, an acetamido group, an amino group or a dimethylamino group;R.sub.2 may denote a hydrogen atom or a nitro group;R.sub.3 and R.sub.4 may denote a hydrogen atom;R.sub.8a and R.sub.8b which are the same may denote a chlorine atom or a methoxy group;R.sub.9 may denote a hydrogen atom or an amino group;R may denote a methyl group; andX may denote a methanesulfonamido group, a 1-imidazolyl group or a nitro group or a salts thereof are useful as antiarrhythmic drugs.

Abstract: Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hypoxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequently occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).

Abstract: The invention provides a compound of formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical compositions containing a compound of formula I, and methods of using a compound of formula I for inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia, and estrogen dependent cancer.

Abstract: The invention provides naphthofluorene compounds, intermediates, formulations, processes, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, cardiovascular-related pathological conditions, including hyperlipidemia, and estrogen-dependent cancer.

Abstract: Compounds of formula I, and their pharmaceutically acceptable salts, ##STR1## in which R.sup.1 and R.sup.2 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, phenylalkyl or alkenyl; or NR.sup.1 R.sup.2 is a heterocyclic group; A is trimethylene optionally substituted by alkyl and the phenyl ring is optionally substituted by substituents such as halogeno, alkenyl, amino, cyano, ureido, alkyl, carbamoylalkyl, alkanoylamino, alkoxycarbonyl, N-alkyl-alkanoylamino, alkanoyl and amines thereof; are inhibitors of squalene synthese and hence useful in treating diseases in which a lowering of cholesterol is desirable. As well as the use of these compounds in medicine, novel compounds, processes for their preparation and pharmaceutical compositions are also referred to.

Abstract: The invention provides dihydronaphthofluorene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions.

Abstract: The invention relates to diaryl antimicrobial compounds of the general formula: ##STR1## where G, E L, J, q, m, X, Ar, W, p, n and A are as described herein, pharmaceutical compositions containing the compounds, methods for their production and their use in treating bacterial infections.

Abstract: Compounds of the formula I ##STR1## including pharmaceutically acceptable salts thereof are disclosed in which R.sub.1, R.sub.2, R.sub.3, and R.sub.4 independently represent hydrogen, hydroxy, halo, halogenated alkyl, halogenated alkoxy, alkyl, alkoxy, cyano, a carbamoyl group, carbonyl group, or R.sub.1 and R.sub.2 together with the phenyl ring represent a naphthalene ring (optionally substituted); L.sub.1 represents C.sub.2-6 alkylene; R.sub.5 represents hydrogen or alkyl, R.sub.6 represents hydrogen or alkyl, phenylalkyl (optionally substituted) or R.sub.5 and R.sub.6 together with the nitrogen atom to which they are attached represent a saturated 3-7 membered heterocyclic ring; L.sub.2 represents a C.sub.1-6 alkylene chain; and R.sub.7 and R.sub.8 independently represent hydrogen or alkyl or R.sub.7 and R.sub.8 together with the nitrogen atom to which they are attached represent a saturated 3-7 membered heterocyclic ring.

Abstract: This invention relates to a compound of the Formula I: ##STR1## as a racemic mixture and its individual enantiomers, in particular the (R)-enantiomer, and their pharmaceutically acceptable salts. These compounds are useful as sodium channel blockers, and are particularly useful for the alleviation of neuropathic pain.

Abstract: Hydroxylamine ethers I ##STR1## (where X is NO.sub.2, CN, halogen, alkyl or haloalkyl, Y is H, NO.sub.2, CN, halogen, alkyl or haloalkyl, n is 0-2 or 1-4 where Y and all radicals X are halogen and Alk is unsubstituted or substituted alkylene) and their salts with mineral acids or strong organic acids are prepared by reacting either a hydroximino compound II ##STR2## (where R.sup.1 is alkyl, R.sup.2 is alkyl or alkoxy or R.sup.1 +R.sup.2 form an alkylene chain) in the presence of an alkali metal hydroxide, alkali metal alcoholate, alkali metal bicarbonate or alkali metal carbonate as the base, or the corresponding anion II directly, with an alkylating agent III ##STR3## (where R.sup.3 is unsubstituted or substituted alkyl or unsubstituted or substituted phenyl) to give an oximino derivative IV ##STR4## said derivative is cleaved by means of a mineral acid or a strong organic acid to give the salt of I and, if desired, the latter is converted by means of a base into the free compound I.

Abstract: Polyalkylphenoxyaminoalkanes having the formula: ##STR1## wherein R is a polyalkyl group having an average molecular weight in the range of about 600 to 5,000;R.sub.1 and R.sub.2 are independently hydrogen or lower alkyl having 1 to 6 carbon atoms; andA is amino, N-alkyl amino having about 1 to about 20 carbon atoms in the alkyl group, N,N-dialkyl amino having about 1 to about 20 carbon atoms in each alkyl group, or a polyamine moiety having about 2 to about 12 amine nitrogen atoms and about 2 to about 40 carbon atoms.The compounds of formula I are useful as fuel additives for the prevention and control of engine deposits.