Abstract: Provided are two-photon fluorescent probes for imaging acidic vesicles in live cells and tissue. The probes are represented by The probes can selectively bind to vesicles in cytosol to emit two-photon excited fluorescence with high intensity. Therefore, the use of the probes enables effective imaging of acidic vesicles. Further provided is a method for imaging acidic vesicles in live cells and tissue using the probes.

Abstract: The present invention is directed to a 2-deoxyribose-5-phosphate aldolase (DERA) chemoenzymatic process for making chiral compounds.

Abstract: Provided herein are hepatitis C virus entry inhibitor oxoacetamide compounds, pharmaceutical compositions thereof, and methods for their use in treatment or prevention of hepatitis C virus infection in a subject in need thereof.

Abstract: The present invention provides a pharmaceutical which possesses an excellent inhibitory effect on NHE3 (Na+/H+ exchanger type 3) and effectively improves diseases or conditions of organs in which NHE3 is expressed.

Abstract: The present invention is related to a precursor for no-carrier-added fluorine-18 labeled ethacrynic acid, N-(4-[18F]fluorobutyl)-Ethacrynic amide([18F]FBuEA) and the preparation method for HPLC non-radioactive standards. Its chemical structure is shown in the following: In the precursor, R1 represents a protective group for the amide functional group; R2 represents leaving group; or R1 represents carboxyl group, R2 represents p-tosyloxy, methane sulfonyloxy group or trifluoromethane sulfonyloxy group or bromine (Br). For the HPLC non-radioactive standards, R1 represents a protective group for the amide functional group and hydrogen, R2 represents fluorine.

Abstract: The present invention relates to methods of identifying small molecule candidate agents capable of modulating transcription factor function such that the function/expression of a target transcription factor and/or proteins downstream of this target protein comprises the screening of small molecule libraries using in silico high throughput docking for candidate small molecules/agents that are selectively identified for their ability to target and disrupt the transcription factor-DNA interface through unique transcription factor and/or DNA descriptors that are defined within a pharmacophore, and then testing/evaluating the candidate agents identified above through one or more in vitro assays for their ability to modulate transcription factor function including expression of this target protein and/or proteins that are downstream of the target transcription factor. The present invention also relates to various compounds described herein (e.g.

Abstract: A method for the preparation of 4-fluoro-?-[2-methyl-1-oxopropyl]-?-oxo-N-?-diphenylbenzenebutanamide also known as 2-[2-(4-fluorophenyl)-2-oxo-1-phenylethyl]-4-methyl-3-oxo-pentanoic acid phenylamide of the formula I containing about 0.1% or less of ?-[2-methyl-1-oxopropyl]-?-oxo-N-?-diphenylbenzene butanamide, about 0.05% or less of difluoro-?-[2-methyl-1-oxopropyl]-?-oxo-N-?-diphenylbenzene butanamide and about 0.1% or less of 3-[2-(4-Fluorophenyl)-2-oxo-1-phenyl-ethoxy]-4-methyl-pent-2-enoic acid phenylamide.

Abstract: A method for the preparation of 4-fluoro-?-[2-methyl-1-oxopropyl]-?-oxo-N-?-diphenylbenzenebutanamide also known as 2-[2-(4-fluorophenyl)-2-oxo-1-phenylethyl]-4-methyl-3-oxo-pentanoic acid phenylamide of the formula I containing about 0.1% or less of ?-[2-methyl-1-oxopropyl]-?-oxo-N-p-diphenylbenzene butanamide, about 0.05% or less of difluoro-?-[2-methyl-1-oxopropyl]-?-oxo-N-?-diphenylbenzene butanamide and about 0.1% or less of 3-[2-(4-Fluorophenyl)-2-oxo-1-phenyl-ethoxy]-4-methyl-pent-2-enoic acid phenylamide.

Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water.

Abstract: A novel palladium-mediated carbon-carbon bond forming reaction has been discovered using DNA-templated chemistry. The inventive reaction involves the palladium-mediated coupling of a terminal alkyne with an alkene to form an enone. A catalytic amount of palladium may be used in the reaction if an oxidant is present. The reactions is also compatible with a variety of organic solvent as well as aqueous solution. Both intermolecular and intramolecular reactions have been demonstrated. This novel carbon-carbon bond forming reaction is particularly useful in the synthesis of macrocycles. Kits, reagents, catalysts, solvents, oxidants, salts, acids, instructions, and other materials useful in the practice of the inventive reaction are also provided.

Abstract: A process for synthesis of a compound of Formula (X) wherein: R1 is an aryl group substituted with one to three substituent groups, wherein each substituent group of R1 is independently C1-C5 alkyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, halogen, carboxy, cyano, or trifluoromethyl, wherein each substituent group of R1 is optionally independently substituted with one to three substituents selected from C1-C3 alkyl, C1-C3 alkoxy, phenyl, and alkoxyphenyl; and R2 and R3 are each independently C1-C5 alkyl.

Abstract: The present invention relates to the treatment of metabolic syndrome or disorders associated with metabolic syndrome comprising administering a compound of the invention.

Abstract: A compound represented by the following general formula (I): [R1 to R5 represent hydrogen atom, an alkyl group, or a trialkylsilyl group, X represents —NH—CO—, —CO—NH—, —N(COR6)—CO—, —CO—N(COR7)— (R6 and R7 represent a lower alkoxy group, or a carboxy-substituted phenyl group) etc.; and Z represents —Y—CH(R12)—COOH, —CHO, —CH?CH—COOH, or —COOR13 (Y represents a single bond, —CH2—, —CH(OH)—, —CO—, —CO—NH—, or —CO—NH—CH2—CO—NH—, R12 represents hydrogen atom or a lower alkyl group, and R13 represents hydrogen atom, —CH(R14)—COOH(R14 represents hydrogen atom, a lower alkyl group, or hydroxy group), —[CH2CH2—O]n—CH2—CH2—OH, —CH2—O—[CH2CH2—O]m—CH2—OH, or —[CH(CH3)—CO—O]p—CH(CH3)—COOH (m, n and p represent an integer of 1 to 100))], a salt thereof or an ester thereof, which has a property of being converted into a retinoid after absorption in vivo.

Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein R1 is CHX2, CX3, CX2CHX2 or CX2CX3; each X is independently Cl or F; Z is optionally substituted phenyl; and Q is phenyl or 1-naphthalenyl, each optionally substituted as defined in the disclosure; comprising contacting a compound of Formula 2 with hydroxylamine in the presence of a base. The present invention also relates to novel compounds of Formula 2, useful as starting materials for the aforedescribed method.

Abstract: Derivatives of dicarbonyl compounds having antitumor and antibiotic activity which can be used as anticancer agents.

Abstract: Compounds and compositions for modulating the activity of p38 kinases are provided, including p38?, and p38? kinase. Methods for treating, preventing or ameliorating one or more symptoms of a p38 kinase mediated disease or disorder are also provided.

Abstract: A novel process for producing a 2-halogenobenzamide compound useful as a raw material or active ingredient for medicines and agricultural chemicals. The process, which is for producing a 2-halogenobenzamide compound represented by the general formula (I): (wherein R1, R2, R3, R4, and R6 may be the same or different and each represents hydrogen or C1-6 alkyl; R5 represents C1-6 alkyl; k is 1 or 2; Y1, Y2, Y3, and Y4 may be the same or different and each represents hydrogen, halogeno, etc.; and X represents chlorine, bromine, or iodine), is characterized by reacting an benzamide compound with a halogenating agent in the presence of a palladium catalyst to obtain a substituted benzamide compound and then reacting the resultant substituted benzamide compound with an oxidizing agent after or without isolating the substituted benzamide compound.

Abstract: There is provided a compound having Formula I R1—Z—R2 ??Formula I wherein R1 is a group selected from optionally substituted fused polycyclic groups, substituted alkyl groups, branched alkyl groups, and optionally substituted cycloalkyl groups Z is a linker which is or comprises a carbonyl group or a isostere of a carbonyl group R2 is selected from optionally substituted aromatic rings and optionally substituted heterocyclic rings wherein (a) R2 is a 2-substituted thiophene group, and/or (b) Z is a group of the formula —C(?O)—CR3R4—X—(CR5R6)n-, wherein X is selected from NR7, S, O, S?O, and S(?O)2, wherein n is 0 or 1 and/or (c) R1 is an adamantyl group and Z is or comprises an amide group, and/or (d) R1 is an adamantyl group and Z is or comprises a group of the formula —(CR8R9)p- NR10—S(?O)2—(CR11R12)q-, wherein p is 0 or 1 and q is 0 or 1 and/or (e) R1 is an adamantyl group and Z is or comprises a group of the formula —(CR13R14)v-Y—(CR15R16)w- where Y is a heteroaryl group in which a bond in the hetero

Abstract: The invention provide a new class of silicone-containing prepolymers containing ethylenically unsaturated groups and latent UV-activated free radical generating moieties. This class of silicone-containing prepolymer is capable of being actinically crosslinked in the presence of one or more hydrophilic vinylic monomers to form a silicone hydrogel material with a hydrophilic surface without post curing surface treatment. The present invention is also related to silicone hydrogel contact lenses made from this class of silicone-containing prepolymers and a vinylic monomer having a latent UV-activated free radical generating moiety.

Abstract: Compounds of the Formula (I) wherein x is an integer from 1-4; p is an integer from 1-3; q is an integer from 0-3; Ar is phenyl, naphthyl, anthryl or phenanthryl each of which optionally is substituted by one or more Cl, CN, OR5, C3-C5alkenyl or C1-C6alkyl which optionally is substituted by one or more OR6, COOR or halogen; R1 if x is 1, is ORS, O—X+, NR8R9, C1-C20alkyl optionally substituted by one or more COOR10, or is C2-C20alkyl interrupted by one ore more O, or is C2-C5alkenyl or phenyl-C1-C4alkyl; R1 if x is 2, is for example C1-C20alkylene; R1 if x is 3, is for example a tri-valent radical; R1if x is 4, is for example a tetravalent radical; R2and R3are hydrogen or C1-C8alkyl, or R2and R3 together are O, C1-C3alkylene or CH?CH; R4 is C1-C4alkyl; R5, R6, R7, R8, R9 and R10 are for example hydrogen or C1-C4alkyl; and X is a x-valent cationic counter ion; are in particular suitable as photoinitiators for the curing with UV-A light (320-450 nm).

Abstract: There is provided a novel process intermediate represented by the general formula (1) or (2): (where, X represents halogen atom, cyano group or the like, Y represents halogen atom, cyano group or the like, R1 represents C1-C6 haloalkyl group or C3-C8 halocycloalkyl group, R2 represents methyl group, halogen atom, cyano group or the like, m represents an integer of 1 to 5, and n represents an integer of 1 to 4).

Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Abstract: Process for the industrial synthesis of the compound of formula (I)

Abstract: The present invention provides a compound of the formula (I): in which R1, R2, R3, A and n are described and set forth more fully herein. Also provided are their preparation and their application in therapy.

Abstract: A method for the preparation of 4-fluoro-?-[2-methyl-1-oxopropyl]-y-oxo-N-?-diphenylbenzenebutanamide also known as 2-[2-(4-fluorophenyl)-2-oxo-1-phenylethyl]-4-methyl-3-oxo-pentanoic acid phenylamide of the formula I containing about 0.1% or less of ?-[2-methyl-1-oxopropyl]-?-oxo-N-p-diphenylbenzene butanamide, about 0.05% or less of difluoro-?-[2-methyl-1-oxopropyl]-y-oxo-N-?-diphenylbenzene butanamide and about 0.1% or less of 3-[2-(4-Fluorophenyl)-2-oxo-1-phenyl-ethoxy]-4-methyl-pent-2-enoic acid phenylamide.

Abstract: This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.

Abstract: The present invention relates generally to compounds providing antibacterial therapeutic agents and preparations, and related methods of using and making antibacterial compounds. Antibacterial compounds of the present invention include chalcone, alkylpyrimidine, aminopyrimidine and cyanopyridine compounds and derivatives thereof exhibiting minimum inhibitory concentrations (MIC) similar to or less than conventional antibacterial compounds in wide use.

Abstract: Novel compounds useful for inhibiting the 90 kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.

Abstract: The present invention relates to the treatment of metabolic syndrome or disorders associated with metabolic syndrome comprising administering a compound of the invention.

Abstract: The diketone of atorvastatin is prepared by first washing a reaction vessel with a non-ketonic solvent, especially tetrahydrofuran, to remove water.

Abstract: The present invention relates to photo-labile pro-fragrance conjugates comprising: a) a photo-labile unit which upon exposure to electromagnetic radiation is capable of releasing a pro-fragrance unit; and b) a pro-fragrance unit, which when so released is either i) a pro-fragrance compound capable of releasing a fragrance raw material; or ii) a fragrance raw material. The present invention relates to systems for delivering fragrances to a situs, and to laundry detergent compositions, fine fragrances, personal care and hair care compositions comprising said systems.

Abstract: The present invention provides a novel modulator of the TRPV1-receptor function, comprising a compound of the formula; wherein ring A is an optionally substituted carbocycle or heterocycle, ring B is an optionally substituted benzene ring or an optionally substituted 6-membered heteroaromatic ring containing N atom, a dashed line means existence or absence of a bond, n is 1 or 2, R1 and R2 are hydrogen etc., R3 is lower alkyl, R4 is lower alkyl or aryloxy, or R3 and R4 taken together may form optionally substituted 5- or 6-membered non-aromatic heterocycle.

Abstract: Provided are two-photon fluorescent probes for imaging acidic vesicles in live cells and tissue. The probes are represented by The probes can selectively bind to vesicles in cytosol to emit two-photon excited fluorescence with high intensity. Therefore, the use of the probes enables effective imaging of acidic vesicles. Further provided is a method for imaging acidic vesicles in live cells and tissue using the probes.

Abstract: To provide a novel compound having NMDA receptor channel blocking activity, and also a pharmaceutical agent comprising the compound. A pharmaceutical agent for the treatment or prevention of a disease caused by overexcitation of an NMDA receptor, which comprises a compound having NMDA receptor channel blocking activity and represented by the formula (1), a salt thereof, or a hydrate of the compound or the salt.

Abstract: The present invention relates to non-steroidal progesterone receptor modulators of the general formula 1, the use of the progesterone receptor modulators for the manufacture of medicaments, and pharmaceutical compositions which comprise these compounds. The compounds according to the invention are suitable for the therapy and prophylaxis of gynaecological disorders such as endometriosis, leiomyomas of the uterus, dysfunctional bleeding and dysmenorrhoea, and for the therapy and prophylaxis of hormone-dependent tumours and for use for female fertility control and for hormone replacement therapy.

Abstract: The invention is directed to a compound of formula (I) Having VDCC blocking activity. These compounds are useful for the treatment of a series of human diseases and conditions, especially cognitive or neurodegenerative diseases or conditions.

Abstract: The present invention overcomes limitations of the prior art by providing new compounds and methods for the treatment of conditions, such as neurodegenerative diseases (e.g., multiple sclerosis), psychiatric disorders (e.g., psychosis, bipolar disorder, depression, neuropathic pain), conditions involving CNS-mediated chronic pain, spinal cord injuries, and other diseases or injuries.

Abstract: Disclosed herein are novel compositions and methods for treating or preventing a variety of disorders and conditions associated with lipid metabolism. The methods generally include administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition comprising one or more fibric acid or statin derivative compositions alone or in combination with one or more lipid altering agents and/or PDE inhibitors.

Abstract: The present invention relate to a compound represented by the formula (I) or (II) wherein ring A is an optionally substituted ring (the ring should not be pyrrolidine, piperidine and piperazine), ring B is an optionally substituted aromatic ring, ring D is an optionally substituted ring, R1 and R2 are each independently a hydrogen atom or a substituent, R3 is a hydrogen atom or a C1-6 alkyl group, or R3 is bonded to ring A to form a non-aromatic ring, ring Aa is an optionally substituted aromatic hydrocarbon, Y is CH or N, Ra1 is an optionally substituted hydrocarbon group, and Ra2 and Ra3 are each independently a hydrogen atom or a substituent, or a salt thereof. The present invention provides a compound having a DGAT inhibitory activity, which is useful for the treatment or amelioration of diseases or pathologies caused by high expression or high activation of DGAT.

Abstract: There is provided a novel process intermediate represented by the general formula (1) or (2): (where, X represents halogen atom, cyano group or the like, Y represents halogen atom, cyano group or the like, R1 represents C1-C6 haloalkyl group or C3-C8 halocycloalkyl group, R2 represents methyl group, halogen atom, cyano group or the like, m represents an integer of 1 to 5, and n represents an integer of 1 to 4).

Abstract: Novel cyclohexyl-1,4-diamine compounds corresponding to formula I: methods for their production, pharmaceutical formulations containing these compounds, methods of producing such pharmaceutical formulations and related methods of treating or inhibiting certain diseases or conditions.

Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Abstract: Compounds are described that are active on at least one of PPAR?, PPAR?, and PPAR?, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPAR?, PPAR?, and PPAR?.

Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.

Abstract: Disclosed are alpha keto amide and alpha hydroxy amide compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetic-related diseases.

Abstract: Derivatives of dicarbonyl compounds having antitumor and antibiotic activity which can be used as anticancer agents.

Abstract: The present invention provides a branched polyalkylene glycol wherein three or more single-chain polyalkylene glycols and a group having reactivity with an amino acid side chain, the N-terminal amino group or the C-terminal carboxyl group in a polypeptide or a group convertible into the group having reactivity are bound; and a physiologically active polypeptide modified with the branched polyalkylene glycol.

Abstract: The present invention relates to compounds of formula I: wherein A, X, R1, R2 and R3 are as defined herein and pharmaceutically acceptable salts thereof. The invention also relates to methods of using the compounds of formula I and pharmaceutical compositions comprising the compounds of formula I.

Abstract: Disclosed is a process for producing a benzylamine derivative represented by the general formula (3): wherein X1, R1 and R2 are as defined below, which comprises reacting a benzyl derivative represented by the general formula (1): wherein X1 represents a halogen atom and R1 represents an acyl group, with a haloacyl compound represented by the general formula (2): R2—X2??(2) wherein X2 represents a halogen atom and R2 represents an acyl group, in the presence of Lewis acid. According to this method, a benzylamine derivative as an intermediate, which is useful for the preparation of a carbamate-based agricultural or horticultural bactericide, can be preferably prepared.

Abstract: Inhibitors of HIV reverse transcriptase which are useful for the treatment of HIV infection. Exemplars of the invention are compounds of the formula wherein the substituents are as defined in the following table R1 R2 R4 R5 R8a F CF3 Me H —OH F CF3 Cl H —OH F CF3 Me H —O—CH2CO2H Cl CN Cl H —OH.