Abstract: Process for the preparation of a compound of formula (I) wherein R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification, comprising the step of reacting an acrylic acid chloride compound of formula (II?): wherein R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification, with aqueous hydroxylamine and optionally converting the resulting compound into an acid addition salt thereof.

Abstract: A compound containing carboxylate ester and N2S2 ligand bi-functional groups and a manufacturing method thereof are disclosed. The S in the N2S2 ligand of the compound containing carboxylate ester and N2S2 ligand bi-functional groups includes a protective group so as to avoid to be oxidized and easy storage. In a complex reaction, the protective group is automatically released As to the active carboxylate ester, it is for reacting with compounds having amino groups such as amines, amino acids, peptides, or protein etc while the N2S2 ligand is for bonding with technetium or rhenium so as to form neutral complex. The compound containing carboxylate ester and N2S2 ligand bi-functional groups is applied to radiopharmaceuticals such as contrast agents for tissues and target agents.

Abstract: The invention relates to oxycarbamoyl compounds of Formula I: The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

Abstract: The invention relates to pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula I: and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1, R2, Z and m are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

Abstract: The present invention relates to fluorescent pyrene dyes in general. The present invention provides a wide range of fluorescent dyes and kits containing the same, which are applicable for labeling a variety of biomolecules, cells and microorganisms. The present invention also provides various methods of using the fluorescent dyes for research and development, forensic identification, environmental studies, diagnosis, prognosis, and/or treatment of disease conditions.

Abstract: Compounds isolated from the fruiting body of A. camphorata in a solid culture or pharmaceutically acceptable salts thereof, which exhibit immunostimulatory or anti-inflammatory effects. Also disclosed are methods of stimulating immune responses and/or treating an inflammatory disorder with these compounds or pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising a drug linker conjugate D-L, wherein -D is an amine containing biologically active moiety; and -L is a non-biologically active linker moiety -L1 represented by formula (I), wherein the dashed line indicates the attachment to the amine of the biologically active moiety and wherein R1, R1a, R2, R2a, R3, R3a, X, X1, X2, X3 have the meaning as indicated in the description and the claims and wherein L1 is substituted with one to four groups L2-Z and optionally further substituted, provided that the hydrogen marked with the asterisk in formula (I) is not replaced by a substituent; wherein L2 is a single chemical bond or a spacer; and Z is a carrier group. The invention also relates to A-L, wherein A is a leaving group, pharmaceutical composition comprising said prodrugs and their use as medicaments.

Abstract: A method of manufacturing ruthenium carbene complexes and novel aryl alkylidene ruthenium complexes based on the method, the complexes able to used as catalysts in metathesis reactions.

Abstract: A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof.

Abstract: The invention relates, in particular, to supported transition metal complexes based on a polystyrene matrix comprising structural units of the formula (Ia): or supported transition metal complexes based on a silica gel matrix comprising structural units of the formula (II): where the radicals and indices have the meanings given in the description. The invention also relates to the use of the supported transition metal complexes in catalysis and corresponding processes for the transition metal-catalyzed conversion of starting material(s) into product(s). In particular, the invention relates to the field of olefin metathesis.

Abstract: A compound of the formula (I) where, for example, W, X and Y are each CH; R1 and R6 together with the adjacent nitrogen forms a 3 to 10-membered saturated ring, wherein the ring may contain, in addition to the nitrogen and carbon ring members, 1, 2 or 3 heteroatoms and/or heteroatom groups as ring members, independently of one another, selected from the group consisting of sulfur, CO, SO, SO2 and N—R7 and/or the ring may carry 1, 2 or 3 radicals, independently of one another, each selected, for example, from the group consisting of halogen, cyano, nitro, amino, and C1-C6-alkyl. R2 is, for example, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy or C1-C6-alkoxy-C1-C6-alkoxy, and R7 is for example, R10C(?O), C1-C6 alkyl or C1-C6-haloalkyl; and/or salts thereof; and their use as pesticidal agents.

Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.

Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.

Abstract: The invention generally relates to novel polymers (SMAMPs) and their syntheses and use. The polymers exhibit promising properties of AMPs. In particularly, for example, a ring-opening metathesis polymerization (ROMP) platform was developed that allows syntheses of SMAMPs that employ a minimum number of norbornene-based building blocks and/or enable easy and independent variation of hydrophobic and hydrophilic groups in the monomer units and/or along the polymeric backbone to finetune and select desirable properties of the polymers.

Abstract: Described are various compounds and methods for the treatment of disorders arising from aberrant protein folding, including in particular lysosomal storage diseases. In particular, polyhydroxylated alkaloids and imino sugars which are pharmacoperones of an enzyme and which do not bind to a catalytic site of said enzyme are described.

Abstract: The present invention provides (I) a method of manufacturing a triphenylmethane colorant that can suppress the sub-reactions in conversion to a sulfonamide and is industrially advantageous, (II) a colorant compound that has both excellent spectral characteristics and a high solubility relative to organic solvents or polymers as a coloring agent to be used in color filters and (III) a blue resist composition for use in a color filter that shows a high lightness and an excellent hue particularly for blue color and can be used to display an image that is excellent in terms of spectral characteristics and contrast.

Abstract: The invention relates to compounds comprising a photolabile protecting group and to the use thereof as coupling agents for the functionalisation of solid supports. The invention also relates to the solid supports functionalised by said compounds and to the use of same for the immobilisation of biological molecules of interest, such as nucleic acid molecules.

Abstract: Compounds of the formula I in which the substitutents have the definitions provided in the specification, are novel, effective HDAC inhibitors.

Abstract: The present invention relates to a novel process for the preparation of almotriptan and pharmaceutically acceptable salts thereof, which affords product conveniently and efficiently with commercially acceptable yields and purity. The present invention also relates to a novel synthetic intermediate used in the process.

Abstract: The present invention relates to compounds from mycelium of Antrodia cinnamomea. The present invention also relates to a composition and a method for treating or prophylaxis of hepatitis C virus (HCV) infection.

Abstract: Compounds of a certain formula (I), in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, are novel effective HDAC inhibitors.

Abstract: A multibranched polyoxyalkylene compound represented by the following formula (1): CH2-L1-(OA1)n-L2-X CH(OA2)mOR1 CH(OA2)mOR1 CH(OA2)mOR1 CH2(OA2)mOR1 ??(1) wherein R1 is the same or different and is a hydrocarbon group having 1 to 24 carbon atoms, OA1 and OA2 are the same or different and are an oxyalkylene group having 2 to 4 carbon atoms, n and m are the same or different and are an average number of moles of the oxyalkylene group added, n represents 0 to 1000, m is the same or different and represents 10 to 1000, X represents a functional group capable of reacting with an amino group, a mercapto group, an aldehyde group, a carboxyl group, a triple bond, or an azide group to form a chemical bond, and L1 and L2 are the same or different and are a single bond, an alkylene group, or an alkylene group in which at least one bond selected from an ester bond, a urethane bond, an amide bond, an ether bond, and an amino is interposed.

Abstract: There is provided a hyperbranched polymer having a nitroxyl group. A hyperbranched polymer comprising at least one organic radical structure (nitroxyl group) of Formula (1), Formula (2) or Formula (3): and having a weight average molecular weight measured by gel permeation chromatography in a converted molecular weight as polystyrene of 500 to 5,000,000.

Abstract: New prodrugs are derived from highly water soluble parent drugs that exist as primary or secondary amines in their parent form. Lipophilic carrier groups are bonded to the parent drug via an amide linkage with additional linker elements between the amide group and the carrier group.

Abstract: This invention relates to novel homotopic prodrugs and medicaments and methods for their preparation, testing and use. In one embodiment, the homotopic prodrug has the general formula wherein is a biologically-active moiety comprising a carboxylic acid functional group, and Rb is a homotopically-symmetrical alcohol bonded to the biologically-active moiety through the carboxylic acid functional group to form an ester linkage, as well as optical isomers, enantiomers, pharmaceutically acceptable salts, biohydrolyzable amides, esters, and imides thereof and combinations thereof.

Abstract: The invention relates to a three-functional pseudo-peptidic reagent, to the various uses thereof, in particular for preparing bioluminescent reagents or optionally luminescent bio-conjugates, to the use of said reagents and bio-conjugates for functionalising solid substrates, and to the use of solid substrates thus functionalised in the detection of molecules of interest.

Abstract: The present invention relates to a compound represented by the following formula I or a pharmaceutically acceptable salt thereof; wherein R1, R2, and y are defined herein. The present invention further relates to compositions that include the compound of the present invention as well as a method of treating a patient from endometreosis or uterine fibroids.

Abstract: Metal chelators of Formula I and Formula II are disclosed: or a pharmaceutically acceptable salt thereof. Also disclosed are metal chelator-targeting moiety complexes, metal chelator-targeting moiety-metal conjugates, kits, and methods of their preparation and use in diagnosis and/or treatment of diseases and conditions, including, inter alia, cancer and thrombosis.

Abstract: The present invention relates to the use of compounds which increase extracellular levels of catecholamines, dopamine and norepinephrine, in cerebral cortical areas of the mammalian brain, and more specifically to the use of 3-disubstituted phenyl-1-pyrrolidinols for the treatment of central nervous system disorders.

Abstract: Novel preparative methods for fluoroalkyl arylsulfinyl compounds are disclosed. Fluorinated compounds as useful fluorinated compounds, intermediates, or building blocks are disclosed. Useful applications of the fluoroalkyl arylsulfinyl compounds are shown.

Abstract: The present invention relates to novel compounds from Antrodia camphorata and the use thereof.

Abstract: The invention relates to novel N-substituted imides and polymerizable compositions comprising these N-substituted imides. The invention further relates to the use of N-substituted imides as polymerization initiators.

Abstract: The present invention provides a short, safe, inexpensive, commercially scalable process for preparing (R)- or (S)-2-methylpyrrolidine from 2-methylpyrroline, which does not require the isolation of synthetic intermediates.

Abstract: The invention provides epoxy and oxetane compositions including the novel acyloxy and N-acyl curing agents described herein. Use of invention curing agents result in cured adhesive compositions with remarkably increased adhesion and reduced hydrophilicity when compared to resins cured with other types of curing agents. Furthermore, the curatives of this invention do not interfere with free-radical cure and are thus suited for use in hybrid cure thermoset compositions.

Abstract: Objects of the present invention are to provide a compound which is useful as a surface modifier for producing a drug carrier or the like, or a salt thereof; a fine particle comprising the same; and the like.

Abstract: The present disclosure relates to methods of synthesizing N-hydroxysuccinimidyl-carbonate intermediates from the corresponding sulfones useful in the preparation of 1-(acyloxy)-alkyl carbamate prodrugs.

Abstract: The present invention is directed to novel compounds. These compounds can be useful in inhibiting the activity of GGTase I. The compounds can also be used as anti-cancer therapeutics including as part of methods for treating cancer, in assays, and in kits.

Abstract: The invention relates to pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula I: and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1, R2, Z and m are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

Abstract: Disclosed are methods of preparing a macromolecular conjugated ligand and a metal complex thereof. The metal complex is targeted for use as a contrast agent, for example, in MRI. The method of preparing a macromolecular conjugated ligand comprises: (a) providing a compound of formula (I) wherein R, A, and Pg are as defined herein, (b) reacting the compound of formula (I) with a macromolecular compound (e.g., dendrimer) in an organic solvent medium which is substantially free of water to obtain a macromolecular conjugated compound, and (c) removing the carboxyl-protecting groups to obtain a carboxyl-deprotected macromolecular conjugated compound. The metal complex can be prepared by reacting the carboxyl-deprotected macromolecular conjugated compound with an ion (e.g., Gd(III)). Also disclosed are two carboxyl-protected 1B4M-DTPA intermediate compounds.

Abstract: The present invention relates to polymeric derivatives, which can be conjugated to an amino-containing drug to improve its in vivo properties. The polymeric derivative can subsequently be released to yield the drug in its native form. Methods of preparing and using these polymeric derivatives and drug conjugates are described.

Abstract: Novel dyes, precursors to novel dyes, and conjugates of the novel dyes are disclosed, as well as methods of making and using the same.

Abstract: Compounds of formula I: inhibit the processing of APP by gamma-secretase and hence find use in treatment of Alzheimer's disease.

Abstract: Activated cytotoxic compounds are described for attachment to targeting molecules for the treatment of a mammalian disease condition which comprise, an activator, a spacer linker, a linker (e.g., self-immolative), and a cytotoxic drug selected from the group consisting of AMINO-SUBSTITUTED (E)-2,6-DIALKOXYSTYRYL 4-SUBSTITUTED BENZYLSULFONES, AMINO-AND-HYDROXY SUBSTITUTED STYRYLSULFONANILIDES, and SUBSTITUTED PHENOXY- AND PHENYLTHIO-STYRYLSULFONE DERIVATIVES. Activated cytotoxic compound attached to a targeting molecule are described wherein the targeting molecule is selected from the group consisting essentially of an antibody, a receptor, a ligand, a cytokine, a hormone, and a signal transduction molecule. The invention is further directed to a method of treatment of disease conditions.

Abstract: The invention provides methods for preparing polymers bearing a terminal propionic acid. The method involves first reacting a water soluble and non-peptidic polymer comprising at least one hydroxyl group with a tertiary alkyl acrylate in the presence of a catalyst to form a propionic acid ester of the polymer, wherein the polymer has a weight average molecular weight of at least about 10,000 Da; and then treating the propionic acid ester of the polymer with a strong acid to form a propionic acid of the polymer.

Abstract: Compounds of a certain formula 1, in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, as well as salts thereof are novel effective HDAC inhibitors.

Abstract: A cyclic polycarboxylic acid anhydride, a polycarboxylic acid, or a mixture of them is allowed to react with hydroxylamine or a salt thereof in an organic solvent under dewatering conditions to yield a corresponding cyclic N-hydroxyimide compound. The cyclic polycarboxylic acid anhydride can be, for example, succinic anhydride or glutaric anhydride. The polycarboxylic acid can be, for example, succinic acid, glutaric acid, or adipic acid. In this process, the reaction is preferably carried out using an organic solvent capable of undergoing azeotropy with water as all or part of a reaction solvent while removing water from the reaction system by azeotropy with the organic solvent. This process produces a cyclic N-hydroxyimide compound in a good yield from any of a cyclic polycarboxylic acid anhydride and a polycarboxylic acid.

Abstract: Methods and compounds are provided to improve the desorption and ionization of analyte for mass spectrometry analysis. More specifically, it is for laser desorption/ionization mass spectrometry. The method uses photon energy absorbing molecules that can bind with analyte either temporarily or permanently to improve the desorption and ionization of analyte. The photon energy absorbing molecules can be positively charged or negatively charged.

Abstract: Compounds of a certain formula I, in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, as well as salts thereof are novel effective HDAC inhibitors.

Abstract: The present invention provides compounds and methods for rapid labeling of N-glycans, for example, rapid fluorescent labeling of N-glycans. In one aspect, the present invention provides fluorescent carbamate or thiocarbamate compounds. Upon contacting with N-glycans, the compounds undergo facile reactions with N-glycans to form fluorescent-labeled N-glycans.

Abstract: This invention relates to a novel class of compounds, represented by the formula (I) below, wherein the meanings of R1, R2, R3, R4, R5, R6, R7, X and Y are indicated therein, which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsms K L, S and B These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis, osteoarthritis and rheumatoid arthritis