Abstract: The process of the present invention can be briefly summarized as depicted in the following scheme: R1 is C1-Calkyl, R2 is C1-C6alkyl and Hal is a halogen atom.

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

Abstract: The invention provides a process for producing a compound of formula (I), wherein Y is selected from the group consisting of CH3, CH2OH, CH2CH2OH, CH2Br and Br; comprising the steps of: (i) reacting a compound of formula (II), wherein OX represents hydroxy or O?M+, in which M+ is a cation selected from Li+, Na+ and K+, and Y is as defined above; with trans-cinnamaldehyde (III), in the presence of a secondary amine compound; then (ii) treating the product of the preceding step with acid to afford the compound of formula (I). The above process may also be used in the production of tolterodine and fesoterodine, which are useful in the treatment of overactive bladder.

Abstract: Crosslinkable compounds useful for making hole-transporting materials for organic light-emitting devices, hole-transporting layers made from the crosslinkable compounds, and light-emitting devices that include the hole-transporting layers.

Abstract: The invention provides a xetine or salt thereof composition having a dissolution in a phosphate buffer at pH 6.8, using USP basket 10 Mesh at 75 rpm, of at least 15% at 60 minutes, of at least 40% at 120 minutes, of at least 70% at 300 minutes.

Abstract: A process for producing 6-dimethylaminomethyl-1-(3-hydroxy- or 3-C1-C4 alkoxyphenyl)-cyclohexane-1,3-diols from 6-dimethylaminomethyl-1-hydroxy-1-(3-hydroxy- or 3-C1-C4 alkoxyphenyl)-cyclohexane-3-ones by catalytic hydrogenation in the presence of heterogeneous or homogeneous catalysts, or by using metal hydrides.

Abstract: The present invention relates to novel base stable ionic liquids and uses thereof as solvents in chemical reactions, especially base catalysed chemical reactions and reactions comprising the use of strong basis.

Abstract: The present invention provides compositions and methods for synthesizing labeled drugs. The present invention further provides methods for preventing or stopping prescription drug abuse for all agents registered as a Drug Enforcement Agency (DEA) schedule II through schedule V medications. According to the present invention, methods are provided for monitoring patient compliance with prescribed drug treatment. The present invention also provides methods for facilitating a replacement prescription when a patient is left without access to their prescribed drug. Furthermore, the present invention provides a method to improve employee compliance with an employer's drug policies via either a voluntary or compulsory system for enhanced drug testing.

Abstract: The present invention provides a reversible thermosensitive recording medium including a support and a thermosensitive recording layer thereon, in which the thermosensitive recording layer contains an electron-donating coloring compound and an electron-accepting compound, and the thermosensitive recording layer is capable of forming a relatively developed condition and a relatively erased condition depending on at least one of the difference of heating temperatures and the difference of cooling rates following to heating, and in which the electron-accepting compound contains a phenol compound expressed by General Formula (1): where, in the General Formula (1), “l” represents an integer of 1 to 3 and “m” represents an integer of 23 or more.

Abstract: This invention provides new compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, prostate cancer, muscle wasting diseases and/or disorders or a bone-related diseases and/or disorders.

Abstract: L-(?)-moprolol L-(+)-tartrate salt (2:1), method for preparing it and pharmaceutical composition comprising it.

Abstract: The substituted pyrazolecarboxanilide derivatives represented by of the formula (I) wherein R1 is H, alkyl, alkylcarbonyl, alkenylcarbonyl, cycloalkyl, phenylalkyl, phenylcarbonyl and the like; R2 is H, halogen, alkyl, CN, OH, alkoxy, phenoxy, phenylthio, phenylsulfonyl and the like; G is alkyl, alkenyl, alkynyl, cycloalkyl, C3-C10 cycloalkenyl and the like; Z is O or S; X is H, halogen, CN, NO2, alkyl and the like; Y1 is H, alkyl, alkenyl, phenyl, alkoxyalkyl and the like; Y2 is H, halogen, CN, NO2, OH, mercapto, amino, carboxyl, C1-C6 alkyl, phenyl, phenoxy, heterocycle and the like, m is 1 or 2; and n is 1-3, and salts thereof exhibit a superior effect as agrohorticultural insecticides or acaricides.

Abstract: The invention relates to a dosage form for controlled release of the active ingredient 3-(2-dimethylaminomethylcyclohexyl)phenol, preferably (1R,2R)-3-(2-dimethylamino-methylcyclohexyl)phenol, or one of the pharmaceutically acceptable salts thereof, which (i) in vivo achieves the peak plasma level of the active ingredient after 2 to 10 h, and/or (ii) in vitro, measured in accordance with the European Pharmacopoeia with a paddle stirrer apparatus in buffer at a pH value of 6.8 (preferably 900 ml), a temperature of 37° C. and 75 rpm releases after 0.5 hours 3.0 to 37 wt. %, after 1 hour 5.0 to 56 wt. %, after 2 hours 10 to 77 wt. %, after 3 hours 15 to 88 wt. %, after 6 hours at least 30 wt. %, after 12 hours at least 50 wt. %, after 18 hours at least 70 wt. % and after 24 hours at least 80 wt. % of the active ingredient originally contained in the dosage form.

Abstract: The present invention provides a process for [18F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular 18F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [18F]-labelled prosthetic groups. [18F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided.

Abstract: A process for the production of a color-stable composition containing cardanol, including (a) subjecting crude, cashew nutshell liquid to distillation to obtain a distillate; (b) reacting the distillate with acetic anhydride to obtain a reaction mixture; and (c) subjecting the reaction mixture to fractional distillation is provided. A method for the production of color-stable phenalkamines, including (a) subjecting crude, cashew nutshell liquid to distillation to obtain a distillate; (b) reacting the distillate with acetic anhydride to obtain a reaction mixture; (c) subjecting the reaction mixture to fractional distillation to obtain a cardanol-containing fractional distillate; and (d) reacting the fractional distillate with an aliphatic amine and formaldehyde to form a color-stable phenalkamine is also provided.

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

Abstract: The present invention relates to amphiphilic squaraine dyes of the general formula (1) as shown below Formula (1) wherein, R1=—(CH2—CH2—O)n—CH3, n=4-8, or —(CH2)n—CO2X, n=3-6, X=H, succinamide and R2=—CH3 or —(CH2—CH2—O)n—CH3, n=4-8 and pharmaceutically acceptable derivatives thereof, for use as near infrared fluorescence probes in photodynamic diagnostic and biological, biochemical and industrial applications.

Abstract: Disclosed herein are substituted cyclohexanol opioid receptor modulators and/or neurotransmitter reuptake modulators of Formula I or Formula II, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention is directed to novel, potent, and selective agents, which are agonists or antagonists of the one or more of the individual receptors of the S1P receptor family. The compounds of the invention are useful as therapeutics for treating medical conditions associated with agonism or antagonism of the individual receptors of the S1P receptor family.

Abstract: Solid forms comprising a compound useful in the treatment, prevention and management of various conditions and diseases are provided herein. In particular, the invention provides solid forms comprising (?)—O-desmethylvenlafaxine, including salts thereof, having utility for the treatment, prevention and management of conditions and disorders including, but not limited to, affective disorders such as depression, bipolar and manic disorders, attention deficit disorder, attention deficit disorder with hyperactivity, Parkinson's disease, epilepsy, cerebral function disorders, obesity and weight gain, incontinence, dementia and related disorders.

Abstract: The process of the present invention can be briefly summarized as depicted in the following scheme: R1 is C1-Calkyl, R2 is C1-C6alkyl and Hal is a halogen atom.

Abstract: Disclosed is a process for preparing substituted anisidines of formula I starting from substituted cyclic hydroxy-ketones II via aromatization through a substituted oxime intermediate IV in which R is C1-C6 alkyl or halogen, and Alk is C1-C6 alkyl. The substituted anisidines of formula I have been found to be useful as intermediates in the preparation of agents for the treatment of hepatitis C viral (HCV) infections.

Abstract: A fragment-based strategy, involving “multicomponent reaction chemistry” (MCR), can identify novel chemotypes that disrupt the p53/MDM2 or p53/MDM4 complex employs. This approach uses high resolution structural information to delineate the region of a first protein or a ligand that is nestled within the binding pocket of a second target protein. The identified region is imported into a database containing MCR scaffolds to generate a virtual library of compounds, which subsequently are docked into the binding pocket of the target protein. Results from docking then are used to select compounds for synthesis and screening. A complementary, NMR-based methodology allows for screening the ability of compounds, selected using MCR, to disrupt the p53/MDM2 or p53/MDM4 complex.

Abstract: The invention relates to new compounds, namely capsaicin derivates, a new method for their production, and their use as micro-organism-repellent agents in paints and coatings, in particular for marine installations and ships, but also for land-based structures.

Abstract: This invention provides a blend which comprises (i) at least one aromatic primary diamine, with which has been blended a color-minimizing amount of at least one N,N-dmydrocarbylhydroxylamine, wherein the aromatic primary diamine is in the form of one benzene ring having two primary amino groups on the ling, which amino groups are meta or para relative to each other, and in which each position ortho to a primary amino group bears an alkyl group, and (ii) at least one aromatic secondary diamine having a Gardner color number no more than about 7, wherein said aromatic secondary diamine either is in the form of one benzene ring having two secondary amino groups on the ring, or is in the form of two benzene rings connected by an alkylene bridge and having one secondary amino group on each ring. Optionally, at least one N,N-dihydrocarbylhydroxylamine has been blended with the aromatic secondary diamine.

Abstract: Triphenylethylene compounds of formula (I) are provided. The compounds are particularly useful for selective estrogen receptor modulation.

Abstract: Compounds of formula (IIa): are provided where: X is a group capable of being cleaved from the ?-carbon atom to form an ion of formula (I?) C is a carbon atom bearing a single positive charge or a single negative charge; The invention further provides compounds of formula (IIb): where: X is a counter-ion to C. The compounds of formula (IIa) and (IIb) may form ions of formula (I?) by either cleaving the C—X bond between X and the ?-carbon atoms in the case of the compounds of formula (IIa) or dissociating X in the case of compounds of formula (IIb).

Abstract: A 1-amino-phthalazine derivative of general formula (I) wherein the substituents are as defined herein. Also disclosed are a method for preparing such compounds, intermediates for use in such method and medical treatments using the compounds of formula (I).

Abstract: The present invention is directed to compounds of formula (I): or a pharmaceutically acceptable salt thereof; wherein A is (II); X is selected from CH, CF and N, R8 is selected from H, C1-C6 alkyl, aryl, heteroaryl, C1-C6 alkylaryl, C1-C6 alkylheteroaryl, C2-C6 alkyl-O—C1-C6 alkyl, C1-C6 haloalkyl, hydroxy C2-C6 alkyl, —C(O)R9 and —SO2R9, or R7 and R8 combine to form (III), (IV); W is selected from CR1O and CR15, R1O is selected from H, halo, —C(O)NR13R14, C1-C6 alkyl, aryl, heteroaryl, C1-C6 alkylaryl, C1-C6 alkylheteroaryl, C1-C6 alkyl-O—C1-C6 alkyl and hydroxy C1-C6 alkyl; Het is a N-linked 5-membered heteroaryl ring optionally substituted with 1-3 substituents selected from methoxy, Cl, F, CH3, CF3, aryl, heteroaryl, C1-C4 alkylaryl or C1-C4 alkylheteroaryl, for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.

Abstract: A photosensitive compound has two or more structural units, in a molecule, represented by the following general formula (1): wherein R1 to R10 are selected from the group consisting of hydrogen atom, halogen atom, alkyl group, alkoxy group, phenyl group, naphthyl group, and alkyl group in which a part or all of hydrogen atoms are substituted with fluorine atom; and X is a substituted or unsubstituted phenylene group or a substituted or unsubstituted naphthylene group.

Abstract: Provided are processes and intermediates for the synthesis of O-desmethylvenlafaxine.

Abstract: The present invention relates to novel essentially pure venlafaxine and the process of preparation thereof. The present invention also relates to novel solvate forms of venlafaxine hydrochloride and the process of preparation thereof. Furthermore, the present invention provides a novel process for preparing venlafaxine hydrochloride from venlafaxine; the process comprises the steps of: i) preparing a mixture of venlafaxine with acetone; and ii) exposing the mixture in gaseous hydrochloric acid.

Abstract: A method of making an amino-alkylenediol and intermediate compounds useful in the method is disclosed. The method includes preparing a first intermediate compound comprising an aminoalkylene diol wherein a protecting group is linked to the amino functionality, and optionally, preparing a second intermediate compound comprising a salt of the first intermediate compound. The first intermediate compound has the structure wherein R is a divalent alkylene radical having from 2 to 20 carbon atoms, X and Y are independently a divalent linking moiety or a single bond, and Z is a protecting group. The second intermediate compound has the structure wherein R is a divalent alkylene radical having from 2 to 20 carbon atoms, X and Y are independently a divalent linking moiety or a single bond, TsO? is toluene sulfonate, and Z is a protecting group.

Abstract: The present invention relates to the use of compounds of the formula (I), with radicals defined in the description, as antioxidants, to corresponding novel compounds and compositions, and to corresponding processes for the preparation of compounds and compositions.

Abstract: The present invention provides a surface-independent surface-modifying multifunctional biocoating and methods of application thereof. The method comprises contacting at least a portion of a substrate with an alkaline solution comprising a surface-modifying agent (SMA) such as dopamine so as to modify the substrate surface to include at least one reactive moiety. In another version of the invention, a secondary reactive moiety is applied to the SMA-treated substrate to yield a surface-modified substrate having a specific functionality.

Abstract: A process for preparing a 3-aminophenylacetylene compound of formula (5), including: a) reacting a 3-haloaniline compound of formula (1) with an acetylene compound of formula (2) in the presence of a palladium compound, a copper compound, and an amine compound of formula (3) to form an aniline compound of formula (4); b) precipitating the aniline compound of formula (4) in the form of a crystal, and isolating it by solid/liquid separation; and c) reacting the aniline compound of formula (4) with a base to obtain 3-aminophenylacetylene.

Abstract: The present invention relates to halogenated 4-aminophenols and to halogenated 4-(phenyldiazenyl)phenols, to a process for their preparation and to the use of the halogenated 4-hydroxyphenols for preparing active ingredients, especially in pharmaceuticals and agrochemicals.

Abstract: The present invention describes processes for the preparation of O-desmethylvenlafaxine and tridesmethylvenlafaxine, which may be used as an intermediate in preparing O-desmethylvenlafaxine.

Abstract: Disclosed is a compound having the formula: pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein. The compounds, salts and solvates of this invention are useful as LXR agonists.

Abstract: The present invention provides the diaminophenyladamantane derivatives with antitumor activities and the preparation method therefore. The method includes a step of reacting an aromatic diol with at least one 5-halo-2-nitrophenol in the presence of at least one inorganic base in an organic solvent with a relatively high boiling point.

Abstract: The present invention relates to a novel process for the preparation of compounds of formula (I) wherein X, Q, R1 and R2 are as defined in the specification, the compounds being useful in the preparation of therapeutic agents. The invention further relates to novel intermediates useful in the preparation of the therapeutic agents.

Abstract: L-(?)-moprolol L-(+)-tartrate salt (2:1), method for preparing it and pharmaceutical composition comprising it.

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: An anilide is reacted with an acylating agent by using as a catalyst a tri(perfluoroalkane sulfonate) compound of any of the elements belonging to groups 3 to 5 and groups 13 to 15 in periods 4 to 6 of the periodic table, thereby bonding an acyl group to the benzene ring. Thus, ketoaniline derivatives, which are useful as physiologically active compounds or intermediates in synthesizing the same, are synthesized in high reaction yield by catalytic acylation.

Abstract: Processes for producing antibacterial agents and intermediates useful in producing antibacterial agents are provided and include producing compound (VI-a) in accordance with the following reaction schema, as well as production intermediates thereof

Abstract: Disclosed are colorant precursor compounds of the formula wherein R is an alkyl group, an aryl group, an arylalkyl group, or an alkylaryl group, and wherein R can be joined to the phenyl moiety to form a ring, each R?, independently of the others, is a halogen atom, an alkyl group, an alkoxy group, a nitrile group, a nitro group, an amide group, or a sulfonamide group, z is an integer of 0, 1, 2, 3, or 4, n is an integer representing the number of carbon atoms in each repeat alkylene oxide unit, and x is an integer representing the number of repeat alkylene oxide units, wherein said colorant precursor has no more than one —OH, —SH, or primary or secondary amino group per molecule.

Abstract: A process for preparing 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol with high stereoselectivity and high yield by reacting 2-[(dimethylamino)methyl]-cyclohexanone in a Grignard reaction with a Grignard compound of 3-bromoanisole in a suitable solvent and in the presence of an inorganic lithium salt and an ?,?-dialkoxyalkane.

Abstract: Primary intermediates for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): where R1 and R2 are each individually selected from a hydrogen atom, a C1 to C3 alkyl group, a C1 to C5 mono or dihydroxyalkyl group, phenyl or benzyl optionally substituted with an alkoxy group, or R1 and R2 together with the nitrogen atom to which they are attached form a piperazine, piperidine, imidazole, or morpholine ring.

Abstract: The invention relates to 3,3-diphenylpropylamines of formula (I), wherein R1 signifies hydrogen or methyl, R2 and R3 independently signify hydrogen, methyl, methoxy, hydroxy, carbamoyl, sulphamoyl or halogen, and X represents a tertiary amino group of formula (II), wherein R4 and R5 signify non-aromatic hydrocarbyl groups, which may be the same or different and which together contain at least three carbon atoms, and wherein R4 and R5 may form a ring together with the amine nitrogen, their salts with physiologically acceptable acids and, when the compounds can be in the form of optical isomers, the racemic mixture and the individual enantiomers.

Abstract: The invention relates to 3,3-diphenylpropylamines of formula (I), wherein R1 signifies hydrogen or methyl, R2 and R3 independently signify hydrogen, methyl, methoxy, hydroxy, carbamoyl, sulphamoyl or halogen, and X represents a tertiary amino group of formula (II), wherein R4 and R5 signify non-aromatic hydrocarbyl groups, which may be the same or different and which together contain at least three carbon atoms, and wherein R4 and R5 may form a ring together with the amine nitrogen, their salts with physiologically acceptable acids and, when the compounds can be in the form of optical isomers, the racemic mixture and the individual enantiomers.