Abstract: Stilbene analogs and pharmaceutical compositions that are useful for the treatment of various cancers, including without limitation, colorectal cancer (CRC) and breast cancer are disclosed. The halogenated stilbene analogs include nitrogen heteroaryl groups and/or amino groups on the stilbene ring.

Abstract: The present disclosure includes compounds of Formula I: wherein R1-R3, Ar, and n are as defined herein, and methods for the quantification of carboxylic acids in samples, specifically biological samples, using the compounds of Formula I. The compounds of Formula I are novel stable isotopic reagents that are useful in differential isotopic labeling methods.

Abstract: Compositions capable of simultaneous two-photon absorption and higher order absorptivities are provided. Compounds having a donor-pi-donor or acceptor-pi-acceptor structure are of particular interest, where the donor is an electron donating group, acceptor is an electron accepting group, and pi is a pi bridge linking the donor and/or acceptor groups. The pi bridge may additionally be substituted with electron donating or withdrawing groups to alter the absorptive wavelength of the structure. Also disclosed are methods of generating an excited state of such compounds through optical stimulation with light using simultaneous absorption of photons of energies individually insufficient to achieve an excited state of the compound, but capable of doing so upon simultaneous absorption of two or more such photons. Applications employing such methods are also provided, including controlled polymerization achieved through focusing of the light source(s) used.

Abstract: The present invention is concerned with novel processes for the preparation of (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and (?)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof. These compounds have pharmaceutical utility and are known to be useful for treating e.g., depression, anxiety disorders, eating disorders and urinary incontinence.

Abstract: Fluorinated compounds and methods of making fluorinated compounds are described herein.

Abstract: The present invention relates to processes for preparing enantiomerically pure cyclopropyl amine derivatives and salts thereof; the chiral intermediates such as the chiral salts are useful for the preparation of such chiral compounds and salts; pharmaceutical compositions comprising the compounds and salts; and method of using such compositions. The chiral cyclopropyl amine derivatives are useful for binding to histamine H3 receptor sites and for providing therapeutic agents for histamine H3 mediated disease.

Abstract: In one aspect, the present invention provides a hyperpolarizable organic chromophore. The chromophore is a nonlinear optically active compound that includes a ?-donor conjugated to a ?-acceptor through a ?-electron conjugated bridge. In other aspects of the invention, donor structures and acceptor structures are provided. In another aspect of the invention, a chromophore-containing polymer is provided. In one embodiment, the chromophore is physically incorporated into the polymer to provide a composite. In another embodiment, the chromophore is covalently bonded to the polymer, either as a side chain polymer or through crosslinking into the polymer. In other aspects, the present invention also provides a method for making the chromophore, a method for making the chromophore-containing polymer, and methods for using the chromophore and chromophore-containing polymer.

Abstract: A process for the preparation of the compound of formula

Abstract: A new ionic compound is provided that is derived from N,N-dimethylaniline and pentafluorophenol in amounts such that there are at least 2 equivalents of pentafluorophenol per equivalent of the N,N-dimethylaniline.

Abstract: The present invention is concerned with novel processes for the preparation of (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and (?)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof. These compounds have pharmaceutical utility and are known to be useful for treating e.g., depression, anxiety disorders, eating disorders and urinary incontinence.

Abstract: Disclosed are highly convergent processes for preparing compounds of formula (I), which compounds are potent active agents for the treatment of hepatitis C virus (HCV) infection: The disclosed processes use SNAr-type coupling reactions between peptidic compounds having a hydroxyproline moiety of the following formula: and halogenated or sulfonated bromoquinoline compounds.

Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 and Ar are as defined in description and in claims, can be used as a medicament.

Abstract: A process for the preparation of the compound of formula

Abstract: A process for preparing substituted biphenyls of the formula I where R1=nitro or amino, R2=cyano, halogen, C1-C4-haloalkyl, C1-C4-haloalkoxy or C1-C4-haloalkylthio, n=from 0 to 3, and R3=hydrogen, cyano or halogen, which comprises reacting a halobenzene of the formula II in which Hal is chlorine or bromine, in the presence of a base and of a palladium catalyst which consists of palladium and a bidentate phosphorus ligand of the formula III where Ar is phenyl which is substituted if desired and R4 and R5 are each C1-C8-alkyl or C3-C6-cycloalkyl or together form a 2- to 7-membered bridge which may, if desired, bear a C1-C6-alkyl substituent, in a solvent or diluent, with a phenylboronic acid IVa a diphenylborinic acid IVb or a mixture of IVa and IVb.

Abstract: Polymers made by polymerization or cyclization condensation of a fluorine-containing polymerizable monomer represented by the formula [1] wherein “a” represents an integer from 1 to 4. The monomer contains a plurality of polymerizable amines in the molecule and at the same time one or more hexafluoroisopropyl group(s). With this structure it can be used as an effective polymerizable monomer, which can exhibit water repellency, oil repellency, low water absorptive property, heat resistance, weather resistance, corrosion resistance, transparency, photosensitivity, low refractive index property, low dielectric property, etc., and it can be used for advanced polymer material fields.

Abstract: Disclosed are processes for preparing tetrahydroisoquinolines, intermediates useful in the preparation of tetrahydroisoquinolines, processes for preparing such intermediates, and a crystalline form of 6-[(4S)-2-methyl-4-(naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine. Also disclosed are pharmaceutical compositions comprising tetrahydroisoquinolines, methods of using tetrahydroisoquinolines in the treatment of depression and other conditions and methods for obtaining the crystalline form.

Abstract: A process for preparing a compound of formula (V) or its enantiomer, which comprises: (a) reacting racemic aminoindan of formula (II) or its enantiomer with allylhalide in presence of a base and an organic solvent at a temperature ranging from 25 C to the reflux temperature of the solvent to give compound of formula (III); Where R is H or (b) reacting the compound (III) with halogenating agent in a suitable organic solvent to give a dihalo compound of formula (IV). (c) treating the dihalo compound (IV) with a suitable base to give compound (V).

Abstract: 2-(3-Aminobenzoyl)-3-cyclopropyl-3-oxopropanenitriles of the formula (I) are described as herbicides. In this formula (I), X and Y are organic radicals such as alkyl and other radicals such as halogen, nitro and cyano.

Abstract: The invention provides synthetic methods that utilize bromo or chloro substituents as blocking groups during the functionalization of aromatic rings, as well as compounds that are prepared from such methods.

Abstract: The present invention relates to new cyclobutanemethanamine inhibitors of monoamine reuptake, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Substituted pyrazinecarboxylic acid anilide derivatives represented by the general formula (I) or salts thereof; intermediates of them; pesticides (such as insecticides and acaricides) for agricultural and horticultural use, containing the compounds as the active ingredient; and usage thereof: wherein R1 is H, C1-6 alkyl, halo C1-6 alkyl, or the like; R2 is halogeno, C1-6 alkyl, or the like; G is C2-10 alkyl or the like; Z is oxygen or sulfur; X's are each independently H, halogeno, or the like; Y's are each independently H, halogeno, cyano, or the like; and m and n are each an integer of 1 to 3.

Abstract: A process of preparing a radioactive compound containing a fluorine-18 isotope is provided. In one embodiment, the process may comprise forming a [18F] fluoroalkyl triflate by triflating a [18F] fluoroalkyl compound with AgOTf, and forming a [18F] fluoroalkylated radioactive compound through alkylation between the [18F] fluoroalkyl triflate and a radioactive compound precursor having at least one group selected from NH, OH and SH.

Abstract: An efficient method to induce the enantioselectivity in procarbonyl compounds using chiral organometallic complexes. The present invention is also described a method for producing organo metallic complexes using a base and a metal halide.

Abstract: There is provided a composition comprising a compound represented by general formula (I), wherein Rl represents a 5-iodothiophen-2-yl group or the like, and R2 represents a 4-dimethylaminophenyl group or the like. This composition is useful for diagnosis of an amyloid-related disease such as Alzheimer's disease because the compound has high binding specificity to amyloid ? protein, high permeability through the blood-brain barrier, and a property of being rapidly eliminated from sites other than senile plaques in the brain.

Abstract: The present invention relates to a fluorine-containing polymerizable monomer represented by the formula [1], [Chem. 31] wherein “a” represents an integer of 1-4. This monomer has a plurality of polymerizable amines in the molecule and at the same time a hexafluoroisopropyl group(s). With this, it can be used as an effective polymerizable monomer, which can exhibit water repellency, oil repellency, low water absorptive property, heat resistance, weather resistance, corrosion resistance, transparency, photosensitivity, low refractive index property, low dielectric property, etc., and can be used for advanced polymer material fields.

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: Novel aromatic compounds of formula (I): wherein A1, A2, A3, A4, R1, R2, R5, G1, G2, Q1, Q2, Y1, Y2, Y3 and Y4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests.

Abstract: Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1 L2Ar2Alk- in which: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted arylene or heteroarylene group; and Alk is a chain —CH2—CH(R)—, —CH?C(R)— or in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; and the salts, solvates, hydrates and N-oxides thereof.

Abstract: Combretastatin derivatives of formula (I), preparation and use thereof are disclosed, wherein: Rf is alkyl with 1-8 carbon atoms and 1-17 fluorine atoms, R is amino, substituted amino, hydroxyl, nitro, halo, alkyloxy, phosphate or amino acid side chain. Said derivatives have a capability to inhibit the polymerization of microtubules and are useful in treatment against tumor and neovascularization.

Abstract: Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of Fesoterodine or a pharmaceutically acceptable salt thereof in high yield and purity. Disclosed also herein is an improved and industrially advantageous optical resolution method of racemic (±)-N,N-Diisopropyl-3-(2-benzyloxy-5-bromophenyl)-3-phenylpropylamine and use thereof for the preparation of Fesoterodine.

Abstract: The present invention provides a new method for preparation and crystallization of hydrochlorides, hydrobromides or hydroiodides of pharmaceutical compounds or their intermediates in which the base or its acid addition salt is reacted in a solvent with a Trialkylsilylhalogenide.

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: The present invention relates to a process for preparing biaryls using catalysts based on palladium compounds with phosphine ligands.

Abstract: A fluorine-substituted amphetamine or amphetamine derivative with the formula (I): where at least one of the residues R1 or R2 is different from H and Ph is a phenyl ring, which is substituted with fluorine in at least one position or the residues R1 and R2 independently of one another are H or are different from H and Ph is a phenyl ring, which is substituted with fluorine in at least three positions or the residues R1 and R2 independently of one another are H or are different from H and Ph is a phenyl ring, which is substituted with fluorine in at least one position and has a substituent different from H in at least one other position.

Abstract: The invention relates to a method for identifying a candidate compound for treating a disorder or condition associated with dysfunction of monoamine neurotransmission in the central nervous system, the method comprising the following steps: (a) providing a compound to be tested; (b) testing the ability of the compound to bind to the cocaine-binding site of a monoamine reuptake transporter; and (c) testing the ability of the compound to modulate the inward or outward transport of monoamine neurotransmitters via the monoamine reuptake transporter, wherein the test compound is identified as a candidate compound for treating a disorder or condition associated’ with dysfunction of monoamine neurotransmission if it is able to bind to the cocaine-binding site of the monoamine reuptake transporter and modulate its activity. The invention further relates to compounds identified using the method of the invention, and uses, compositions and medicaments thereof.

Abstract: The invention is concerned with novel hexafluoroisopropanol derivatives of formula (I) wherein R1 to R6, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.

Abstract: A new ionic compound is provided that is derived from N,N-dimethylaniline and pentafluorophenol in amounts such that there are at least 2 equivalents of pentafluorophenol per equivalent of the N,N-dimethylaniline.

Abstract: A liquid crystal compound represented by formula (1), a liquid crystal composition comprising the compound, and a liquid crystal display device comprising the composition: For example, R1 is alkyl having 1 to 20; ring A1, ring A2, ring A3, ring A4, ring A5, and ring A6 are 1,4-cyclohexylene or 1,4-phenylene; Z1, Z2, Z3, Z4, Z5, and Z6 is a single bond; X1 is hydrogen or halogen; l, m, n, o, p, and q are 0 or 1, and l+m+n+o+p+q is 3.

Abstract: The instant invention relates to compounds of formula I, diagrammed below, wherein R3, E, D and Y are defined in the application, which are useful as reversible inhibitors of monoamine oxidase-B and/or monoamine oxidase-A, and therefore useful to treat or prevent neurological diseases or conditions in mammals, preferably humans.

Abstract: The present invention provides innovative strategies for synthesizing pyrazole ring-functionalized benzodiazepinones. Alternative intermediates and high conversion strategies for forming alpha-aminobenzophenone intermediates involve a combination of aromatic acylation, displacement of electronegative leaving groups with amine, and then N-displacement strategies to produce the desired alpha-aminobenzophenone with primary amine functionality. Reaction strategies are then provided for converting alpha-aminobenzophenones to alpha-aminoamidobenzophenone intermediates with high yield and convenient reaction strategies. These alpha-aminoamidobenzophenone intermediates are then converted into benzodiazepinones. These benzodiazepinones are then converted to pyrazole ring functionalized benzodiazepinones through a series of innovative intermediates and/or reaction strategies.

Abstract: The present invention relates to the use of end groups Y, where Y stands for (formula I), where Rf stands for CF3—(CH2)r—, CF3—(CH2)r—O—, CF3—(CH2)r—S—, CF3CF2—S—, SF5—(CH2)r—, [CF3—(CH2)r]2N—, [CF3—(CH2)r]NH— or (CF3)2N—(CH2)r—, B stands for a single bond, O, NH, NR, CH2, C(O)—O, C(O), S, CH2—O, O—C(O), N—C(O), C(O)—N, O—C(O)—N, N—C(O)—N, O—SO2 or SO2—O, R stands for alkyl having 1 to 4 C atoms, b stands for 0 or 1 and c stands for 0 or 1, q stands for 0 or 1, where at least one radical from b and q stands for 1, and r stands for 0, 1, 2, 3, 4 or 5, as end group in surface-active compounds, to corresponding novel compounds, and to processes for the preparation of these compounds.

Abstract: A process for producing an ?,?-difluoroamine which comprises using hydrogen fluoride and a Lewis base in specific amounts in the halogen-fluorine exchange reaction using an ?,?-dihaloamine as the substrate. The process can be industrially applied, enables to obtain the object compound in a short time at a great yield and can be conducted easily with excellent productivity.

Abstract: Process for the preparation of a compound of general formula (I): in which X represents a halogen atom, by reaction of para-trifluoromethylaniline of formula (II): with a dihalogen X2, the two compounds being introduced simultaneously into a polar aprotic solvent in a dihalogen/compound (II) molar ratio ranging from 1.9 to 2.5 and at a temperature ranging from 100 to 300° C.

Abstract: The present invention relates to a production method of an optically active morpholine compound represented by the formula 10, which includes the following steps: wherein each symbol is as defined in the specification. The present invention also relates to a production method of an compound represented by the formula 55, which includes the following steps: wherein each symbol is as defined in the specification. According to the production method of the present invention, an optically active 2-aryl-substituted morpholine compound and 3-oxo-3-(pyrimidin-4-yl)propionate, which are important as starting materials for synthesizing 2-(2-arylmorpholin-4-yl)-1-methyl-1H-[4,4?]bipyrimidinyl-6-one having a tau protein kinase 1 inhibitory activity and useful as a therapeutic drug for Alzheimer's disease and the like, can be produced in a high yield by an industrially advantageous method.

Abstract: Disclosed are highly convergent processes for preparing compounds of formula (I), which compounds are potent active agents for the treatment of hepatitis C virus (HCV) infection: The disclosed processes use SNAr-type coupling reactions between peptidic compounds having a hydroxyproline moiety of the following formula: and halogenated or sulfonated bromoquinoline compounds.

Abstract: Novel optically active phthalamides of the formula (I) in which A, q, R1, R2, E1, E2, X, m, Y, n and Z are as defined in the description, processes for preparing these compounds and their use for controlling pests.

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

Abstract: Disclosed is a fluorine-containing polymerizable monomer represented by the formula [1] below. (In the formula [1], a represents an integer of 1-4.) By having a plurality of polymerizable amines in a molecule while containing a hexafluoroisopropyl group, this fluorine-containing polymerizable monomer exhibiting water repellancy, oil repellency, low water absorbency, heat resistance, weather resistance, corrosion resistance, transparency, photosensitivity, low refractive index, low dielectric properties, and the like, and thus can be applied to the field of advanced polymer materials.

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: Combretastatin derivatives of formula (I), preparation and use thereof are disclosed, wherein: Rf is alkyl with 1-8 carbon atoms and 1-17 fluorine atoms, R is amino, substituted amino, hydroxyl, nitro, halo, alkyloxy, phosphate or amino acid side chain. Said derivatives have a capability to inhibit the polymerization of microtubules and are useful in treatment against tumor and neovascularization.