Abstract: The invention provides processes for manufacturing cell-binding agent-cytotoxic agent conjugates of improved stability in the presence of exogenous NHS. In some embodiments, the inventive process comprises the addition of a molar ratio of exogenous NHS with respect to the amount of NHS generated during the modification reaction as a result of hydrolysis/aminolysis of the bifunctional linker.

Abstract: Provided is a method for producing synthetic amylospheroids efficiently, the method including agitating a liquid containing amyloid ?-peptides in the presence of a plasticizer. Amylospheroid refers to an assembly of amyloid ?-peptides that selectively can induce cell death of functionally mature neurons. Amylospheroid is considered to play a central role in the development of Alzheimer's disease and dementia with Lewy bodies.

Abstract: The present invention relates to a multi-functional nucleic acid-based anti-cancer drug in which the anti-cancer drug is physically bound to a linear nucleic acid having a thiol group at 5? terminal thereof and then gold nanoparticles and aptamers are chemically bound. The present invention also relates to a method for preparing the anti-cancer drug and to an anti-cancer composition comprising the anti-cancer drug. The multi-functional nucleic acid-based anti-cancer drug according to the present invention uses A10 aptamer to achieve high targeting properties, and uses high-concentration anti-cancer drugs and gold nanoparticles to enable dual therapy of thermal therapy/chemical therapy, and may have less side effects and be more effective in anti-cancer therapy compared to existing anti-cancer drugs.

Abstract: The invention relates to methods for making deoxyribofuranose compounds such as compound (2) which are useful intermediates in the preparation of pharmaceutical compounds such as 5-amino-3-(2?-O-acetyl-3?-deoxy-?-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and the like.

Abstract: Provided are an siRNA-polymer conjugate, and a method for preparing the same, and more specifically, to a hybrid conjugate formed by covalently bonding siRNA and a polymeric compound for improving the in vivo stability of siRNA, and to a preparation method of the hybrid conjugate. The conjugate of the present invention can improve the in vivo stability of siRNA, thereby achieving an efficient delivery of therapeutic siRNA into cells and exhibiting the activity of siRNA even with a small dose of a relative low concentration. Therefore, the conjugate can advantageously be used as not only an siRNA treatment tool for cancers and other infectious disease, but also a novel type siRNA delivery system.

Abstract: Provided are an siRNA-polymer conjugate, and a method for preparing the same, and more specifically, to a hybrid conjugate formed by covalently bonding siRNA and a polymeric compound for improving the in vivo stability of siRNA, and to a preparation method of the hybrid conjugate. The conjugate of the present invention can improve the in vivo stability of siRNA, thereby achieving an efficient delivery of therapeutic siRNA into cells and exhibiting the activity of siRNA even with a small dose of a relative low concentration. Therefore, the conjugate can advantageously be used as not only an siRNA treatment tool for cancers and other infectious disease, but also a novel type siRNA delivery system.

Abstract: The present invention is directed to n-alkylated synthetic nucleosides of high regiospecific purity and oligonucleotides that can be utilized for studies on reversal of cytotoxic and mutagenic DNA damage, and as diagnostic tools.

Abstract: A novel method for attaching oligonucleotides to a paramagnetic solid support is disclosed. Conventional methods of attachment require that oligonucleotides be pre-synthesized with specific end modifications, which is laborious and expensive. Instead, we attached oligonucleotides to paramagnetic beads by direct synthesis of the oligonucleotides on the surface of the beads. An external magnet was used to hold the paramagnetic beads in place during solid-phase synthesis. A magnetic force was applied directly to the beads to prevent their loss, in particular, during reagent purge-to-waste steps that involved high-pressure drain or vacuum. This method can be adapted for use in any laboratory working with conventional synthesis automation, and can be employed, for example, with single columns and multi-well titer plates.

Abstract: Disclosed is a method of preparing cationic starch. The method includes preparing a starch suspension containing a cationization agent; performing ultrahigh pressure treatment on the starch suspension; and obtaining cationic starch from the starch suspension subjected to ultrahigh pressure treatment.

Abstract: This invention refers to photo-crosslinked hydrogel materials based in gellan gum suitable for tissue engineering and regenerative medicine applications or as drug delivery systems. Formulations of gellan gum with different degrees of acylation serve as precursor material for insertion of a polymerizable moiety. The materials are capable of free radical polymerization with a photo-initiator at mild temperatures and exposure to ultraviolet light, enabling control of reticulation and withstanding the encapsulation of human and animal cells and/or drugs, and any combination thereof. The physicochemical and biological properties can be adjusted by combining different formulations of gellan gum and reaction conditions.

Abstract: Aspects of the invention provide compositions for use in the treatment galectin-dependent diseases. In particular, compositions comprising a selectively depolymerized, branched galactoarabino-rhamnogalacturonate whose backbone is predominantly comprised of 1,4-linked galacturonic acid (GalA) moieties, with a lesser backbone composition of alternating 1,4-linked GalA and 1,2-linked rhamnose (Rha), which in-turn is linked to any number of side chains, including predominantly 1,4-b-D-galactose (Gal) and 1,5-a-L-arabinose (Ara) residues.

Abstract: The present invention relates to a pharmaceutical composition for relieving pain in a joint disease, including a hyaluronic acid and a pharmaceutically acceptable carrier, in which the hyaluronic acid is cross-linked by cyclizing a double bond in the moiety of a cinnamic acid in a partially amidated hyaluronic acid represented by Formula (1): [Ar—CH?CH—COO—(CH2)n-NH-]m-HA, to form a cycloubutane ring, in which Ar represents an optionally substituted phenyl group, n represents an integer of 2 or 3, HA represents a carboxy residue of the hyaluronic acid, and m represents an amidation ratio of the hyaluronic acid to the total carboxyl group and is in the range of 3 to 50% relative to the total carboxyl group. The pharmaceutical composition of the present invention is an intra-articular formulation that exerts rapid analgesic effects after administration, and shows extremely long durable effects for a human joint disease with only a single administration rather than multiple administrations of a conventional way.

Abstract: The present invention relates to a process for the preparation of ceftaroline salts or hydrates thereof.

Abstract: Provided herein are ruthenium complexes of Formula I, and processes of preparation thereof. Also provided are methods of their use as a metathesis catalyst.

Abstract: A pseudorotaxane, a rotaxane and a catenane are provided. The pseudorotaxane includes at least a macrocyclic host molecule, a guest molecule, and a metal ion. The host molecule contains at least a binding unit and an aromatic linking spacer. The guest molecule has at least a recognition unit. The metal ion is used to template the threading of the guest molecule through the macrocycle host molecule by coordinating to a binding pocket formed from the binding unit of the macrocycle and the recognition moiety of the guest molecule. Rotaxanes or catenanes can be synthesized from the pseudorotaxane complexes, with or without the metal template ion in their molecular structures.

Abstract: The present invention relates to compounds of the formula (1) which are suitable for use in electronic devices, in particular organic electroluminescent devices.

Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.

Abstract: The present invention provides a compound of Formula I: wherein R is H or F; and A is: or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to 7-membered nitrogen-containing heterocyclic compounds and methods of making the same. Using a novel aza-[4+3] cycloaddition reaction, the 7-membered heterocyclic compounds are synthesized by reacting a first reactant and a second reactant. Exemplary first reactants and second reactants include ?-halohydroxamates and dienes, respectively.

Abstract: An aryl amine derivative and an organic electroluminescent device using the aryl amine derivative as a hole transport material, the aryl amine derivative being represented by the following Chemical Formula 1.

Abstract: Certain chemical entities that modulate PI3 kinase activity, and chemical entities, pharmaceutical compositions, and methods of treatments of diseases and conditions associated with PB kinase activity are described.

Abstract: The present invention provides a novel therapeutic drug for cerebral infarction, which contains a piperazine compound as an active ingredient. The compound of the present invention can be provided as a novel therapeutic drug for cerebral infarction having an effect of suppressing brain injury volume or improving neurological deficit, since it suppresses production of plural inflammatory cytokines and chemokines present in the brain such as TNF-?, IL-1?, IL-6 and MCP-1 and the like.

Abstract: The present invention provides a novel therapeutic drug for cerebral infarction, which contains a piperazine compound as an active ingredient. The compound of the present invention can be provided as a novel therapeutic drug for cerebral infarction having an effect of suppressing brain injury volume or improving neurological deficit, since it suppresses production of plural inflammatory cytokines and chemokines present in the brain such as TNF-?, IL-1?, IL-6 and MCP-1 and the like.

Abstract: Compounds of Formula I, and their N-oxides and agriculturally suitable salts, are disclosed which are useful for controlling undesired vegetation wherein R1 is cyclopropyl optionally substituted with 1-5 R5, isopropyl optionally substituted with 1-5 R6, or phenyl optionally substituted with 1-3 R7; R2 is ((O)jC(R15)(R16))kR; R is CO2H or a herbicidally effective derivative of CO2H; R3 is halogen, cyano, nitro, OR20, SR21 or N(R22)R23; R4 is —N(R24)R25 or —NO2; j is 0 or 1; and k is 0 or 1; provided that when k is 0, then j is 0; and R5, R6, R7, R15, R16, R20, R21, R22, R23, R24 and R25 are as defined in the disclosure. Also disclosed are compositions comprising the compounds of Formula I and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula I.

Abstract: The present invention relates to an improved stereoselective process for the preparation of (2R,3S/2S,3R)-3-(4-chloro-5-fluoropyrimidin-6-yl)-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol intermediate compound. This intermediate compound is further used to prepare voriconazole—a triazole antifungal agent.

Abstract: The discovery of distinct modes of asymmetric catalysis has the potential to rapidly advance chemists' ability to build enantioenriched molecules. As an example, the use of chiral cation salts as phase-transfer catalysts for anionic reagents has enabled a vast set of enantioselective transformations. A largely overlooked analogous mechanism wherein a chiral anionic catalyst brings a cationic species into solution is itself a powerful method. The concept is broadly applicable to a number of different reaction pathways, including to the enantioselective fluorocyclization of olefins, and dearomatization of aromatic systems with a cationic electrophile-transferring (e.g., fluorinating) agent and a chiral phosphate catalyst. The reactions proceed in high yield and stereoselectivity. The compounds and methods of the invention are of particular value, especially considering the scarcity of alternative approaches.

Abstract: Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.

Abstract: The present invention relates to a process for the preparation of vilazodone or its pharmaceutically acceptable salts. The present invention further provides a crystalline form of vilazodone free base.

Abstract: The present invention relates to iron and manganese complexes based on hexadentate ligand systems containing one carboxylato donor and five nitrogen donor atoms and to their use in methods for the catalysis of the oxidation of organic substrates. The manganese complexes of the invention also may be used as (pro)-catalysts in methods for the catalysis of water.

Abstract: The present invention is concerned with an improved process for the preparation of pyrido[2,1-a]isoquinoline derivatives of formula I wherein R1, R2 and R3 are each independently hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy or lower alkenyl, wherein lower alkyl, lower alkoxy and lower alkenyl may optionally be substituted by lower alkoxycarbonyl, aryl or heterocyclyl, and the pharmaceutically acceptable salts thereof. The invention also relates to two crystalline forms of (2S,3S,11bS)-1-(2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl)-4(S)-fluoromethyl-pyrrolidin-2-one dihydrochloride, which are form A and form B and to an amorphous form of said compound.

Abstract: Novel alpha-hydrogen substituted nitroxyl compounds and their corresponding oxidized (oxoammonium cations) and reduced (hydroxylamine) forms, and the use of such compounds, inter alia, for oxidation of primary and secondary alcohols to aldehydes and ketones, respectively; resolution of racemic alcohols; desymmetrization of meso-alcohol; as radicals and spin trapping reagents; and as polymerization agents. Processes for preparing the novel nitroxyl/oxoammonium/hydroxylamine compounds from the corresponding amines, and certain novel amine derivatives and their uses. The compounds and amine precursors are useful as ligands for transition metals and as organocatalysts in e.g., aldol reactions.

Abstract: The invention relates to a novel process for the preparation of 2-phenyl-[1,2,4]triazolo[1,5-a]pyridine derivatives of formula I or of a salt thereof wherein R1 stands for hydrogen, a halogen, for an optionally protected hydroxyl group or for an optionally protected amino group and R2 is hydrogen or a halogen. 2-Phenyl-[1,2,4]triazolo[1,5-a]pyridine derivatives of formula I with their 1,2,4-triazole nucleus build the structural core of a great number of functionalized molecules in medicinal chemistry.

Abstract: The present invention provides a heterocycle derivative having a superior amyloid ? production inhibitory activity and/or a superior ?-secretase modulation activity, and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.

Abstract: There is provided a method for catalytic asymmetric synthesis of optically active isoxazoline compound and an optically active isoxazoline compound. A method for catalytic asymmetric synthesis of optically active isoxazoline compound of a formula (6) including reacting an ?,?-unsaturated carbonyl compound of a formula (1) and a hydroxylamine in a solvent in the presence of a base by adding a chiral phase transfer catalyst. An optically active isoxazoline compound of a formula (13) that can be synthesized by the method.

Abstract: The present invention relates to organophosphate-inhibited acetylcholinesterase (AChE) reactivators with central nervous system (CNS) bioavailability and their associated methods of preparation including their use for treatment of exposure to AChE inhibitors such as an organophosphate (OP) insecticides and nerve agents.

Abstract: Reagents comprising MS active, fluorescent molecules with an activated functionality for reaction with amines useful in tagging biomolecules such as N-glycans and uses thereof are taught and described.

Abstract: The invention relates to a process for the preparation of a compound of formula (I) wherein R1 is C1C6 alkyl or benzyl by reacting a compound of formula (II) wherein R1 is as defined for formula (I) with 2-quinoline carboxaldehyde. The process is suitable for use on an industrial scale.

Abstract: The present invention concerns the production of compounds comprising nitrite functions and cyclic imide compounds. More specifically, the invention relates to the production of compounds comprising nitrile functions from compounds comprising carboxylic functions, advantageously of natural and renewable origin, and from methyl-2 glutaronitrile (MGN) or a mixture N of dinitriles comprising methyl-2 glutaronitrile (MGN), ethyl-2 succinonitrile (ESN) and adiponitrile (AdN).

Abstract: A highly energetic, high-oxygen carrier suitable as high-performing green replacement for ammonium perchlorate includes halogen-free ionic salts consisting of fuel cations and over-oxidized anions containing multiple nitro- or nitromethyl-substituted azolyl ligands. The over-oxidized anions include a central atom selected from the group consisting of boron, aluminum, or gallium. Characteristically, the carrier has sufficient amounts of oxygen for complete or near complete combustion of the over-oxidized anions, the fuel cations, metal additives and binders.

Abstract: A process for the preparation of a compound of formula I: wherein, R1 represents hydrogen, cyano, nitro, halogen, or acyl; R2 represents aryl, alkenyl, alkynyl, halogen substituted alkyl, halogen substituted alkenyl, or halogen substituted alkynyl; R3 represents hydrogen or NR6R7 wherein R6 and R7 each independently represent hydrogen, alkyl, alkenylalkyl, alkynylalkyl, formyl, optionally halogen substituted alkanoyl, optionally halogen substituted alkoxycarbonyl, or alkoxymethyleneamino, halogen, or R6 and R7 together with, the N atom attached form a heterocycle; and R4 represents hydrogen, alkyl, aryl, or heteroaryl; the process including oxidizing a compound of formula II:

Abstract: The invention relates to chiral imidodiphosphates and derivatives thereof having the general formula I, The compounds are suitable as chiral Brønsted acid catalysts, phase-transfer catalysts, chiral anions for organic salts, metal salts or metal complexes for catalysis.

Abstract: It refers to a new group of acetal monoesters and diesters which have in its structure the ester function and cyclic ethers that give these products excellent properties as solvency, plasticity in polymers, solubility in polar and nonpolar means, spreadability, wetting, low volatility, non-toxicity and biodegradability. These properties make these products excellent candidates as solvents in formulations of pesticides, agricultural herbicides, for the paint and leather industry in domestic or industrial hygiene formulations; as plasticizers for polymers such as polyvinyl chloride, nitrocellulose, cellulose, acrylics, polyvinyl vinyl and its copolymers; as lubricants in industrial formulations, textile industry; as emollients agents which donate oiliness for the cosmetic industry; as wetting agents that are commonly used, and as biodiesel additives to reduce the freezing point and to improve its combustion.

Abstract: The present invention relates to a non-solvated crystalline Darunavir, process for its preparation and pharmaceutical composition comprising it. The present invention also relates to a process for the preparation of amorphous Darunavir from a non-solvated crystalline Darunavir.

Abstract: The present invention relates to a process for chemical conversion of cellulose isolated from aromatic spent biomass to hydroxymethyl furfural using an eco-friendly and economical liquids system with recoverable and reusable solid Indion catalysts and zeolite-phosphomolybdic acid hybrid catalysts. The present invention further relates to the preparation of an effective hybrid catalyst i.e. zeolite-phosphomolybdic acid catalyst for synthesis of HMF. The selectivity and yield of HMF is nearly doubled in zeolite-phosphomolybdic acid hybrid catalyst compared to the individual catalysts (zeolite or phosphomolybdic acid) or combination of catalysts viz. zeolite and phosphomolybdic acid.

Abstract: The invention relates to anhydrides, solvates and ethanol hetero-solvates and hydrates of dimethoxy docetaxel or (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenyl-propionate of 4-acetoxy-2?-benzoyloxy-5?,20-epoxy-1-hydroxy-7?, 10?-dimethoxy-9-oxo-tax-11-ene-13?-yle, and to the preparation thereof.

Abstract: The present invention relates to the compound of formula (I): which may be in the form of an anhydrous base, a hydrate or a solvate, for its use for the treatment of pediatric cancers.

Abstract: Embodiments of the present disclosure relate to asymmetric epoxidation of olefinic alcohols, using a chiral alcohol chelated titanium catalyst and an organic peroxide performed in a microreactor flow reactor system that can comprise multiple microreactor modules. Molecular sieves can be used to remove any adventitious water in the reagent feed solutions and ensure an anhydrous reaction solution. The use of a microreactor flow reactor allows for the epoxidation reaction to be run at elevated temperatures of at least 20, 30, or even 50° C., which dramatically accelerates the reaction, but without a large drop in enantioselectivity. The reaction can therefore be performed with short reaction times resulting in a high throughput.

Abstract: Phosphoranimide-metal catalysts are disclosed. The catalysts comprise first row transition metals such as nickel, cobalt or iron. The hydrocarbon-soluble catalysts have a metal to anionic phosphoranimide ratio of 1:1, and have no inactive bulk phase and no dative ancillary ligands. The electronic state of the clusters can be adjusted to optimize catalytic activity for a range of commercially important reductive transformations, including hydrodesulfurization. A method of synthesis of these catalysts by anionic metathesis of a halide substituted precursor followed by oxidation is also disclosed.

Abstract: Disclosed herein is a single step catalytic process for the production of enantiomerically pure ?-Aryloxy-??-Azido/Alkoxy alcohols of formula (A). The invention, in particular discloses phenolytic kinetic resolution of racemic anti and syn azido/alkoxy epoxides to generate two stereocentres of high optical purities of formula (A).

Abstract: This invention relates to hydrolysable silanes useful in the modification of elastomers, and as coupling agents for diene elastomer compositions containing a filler. In particular the invention relates to novel hydrolysable silanes containing a tertiary amine group and an ether or thioether linkage.