Abstract: The present invention is directed to a method for demethylating 14-hydroxy substituted alkaloid derivatives, in particular of 14-hydroxy-17-methyl-4,5-epoxymorphinane-6-on-derivatives. This is achieved by reacting a starting compound with a compound of general formula R1OOC—N?N—COOR2 in a suitable solvent.

Abstract: This invention is directed generally to substituted pyridinone and pyrimidinone compounds that generally inhibit p38 kinase, TNF, and/or cyclooxyge?ase activity. Such substituted pyridinone and pyrimidinone compounds include compounds generally corresponding in structure to the following formula: wherein Z, n, R1, R2a, R2b, R2c, R2d, R2e, R3a, R3b, R3c, R3d, R4, R5, R6, R7a, R7b, R7c, R7d and R7e are as defined in this specification. This invention also is directed to compositions of such substituted pyridinones and pyrimidinones (particularly pharmaceutical compositions), and methods for treating disorders (typically pathological disorders) associated with p38 kinase activity, TNF activity, and/or cyclooxygenase-2 activity.

Abstract: The invention relates to a method for producing onium salts comprising alkyl anions or aryl sulfonate anions or alkyl carboxylate anions or acryl carboxylate anions by reacting an onium halide with an alkyl silyl ester or trialkyl silyl ester of an alkyl sulfonic acid or aryl sulfonic acid or an alkyl carboxylic acid or aryl carboxylic acid or the anhydrides thereof.

Abstract: An electrochromic compound represented by the following General Formula (1). A-(CX2)n—B ??General Formula (1) In the formula, A is a monovalent binding group, B is a redox chromophore, X is a halogen atom, and n is an integer of 1 or more.

Abstract: An organic electroluminescence device comprising a compound having a specific structure having a heteroatom and an organic electroluminescence device which comprises a cathode, an anode and an organic thin film layer which comprises at least one layer comprising at least a light emitting layer and is disposed between the cathode and the anode, wherein at least one layer in the organic thin film layer comprises the above compound. The device provides excellent efficiency of light emission, forms no defects in pixels, exhibits excellent heat resistance and has a long life.

Abstract: Substituted 4-aminocyclohexane derivatives having the formula I: wherein R1-R4 are as described herein, methods for their preparation, medicinal products and pharmaceutical compositions containing these compounds and the use of substituted 4-aminocyclohexane derivatives for treating pain.

Abstract: A compound having the formula in racemic form, enantiomerically enriched form or enantiomerically pure form, and pharmaceutically acceptable salts thereof.

Abstract: Methods of synthesizing nicotine analogs and derivatives are described. In some embodiments the methods utilize an alkyl or aryl silyl-substituted nicotine analog intermediate. Intermediates useful for the synthesis of nicotine and nicotine analogs are also described.

Abstract: The present invention is directed to compounds having the formula I or II: including salts thereof, and methods for using them for the treatment of cancer.

Abstract: An organic electroluminescence device includes an anode; a cathode; and at least one organic layer, wherein the at least one organic layer includes a first organic layer which is a light-emitting layer being provided between the anode and the cathode and containing at least one light-emitting material, and the at least one organic layer contains at least one compound represented by formula (I): wherein Q1 represents an aromatic heterocyclic ring; each of R1, R2, R3 and R4 independently represents a hydrogen atom or a substituent; and each of R11, R12 and R13 independently represents an alkyl group, an aryl group, or an aromatic heterocyclic group, provided that at least one of R11, R12 and R13 represents an aryl group or an aromatic heterocyclic group.

Abstract: The present invention discloses a bis-triphenylsilyl compound and its applications as a host material, electron transport material, or hole transport material in an organic electronic device. The general structure of the bis-triphenylsilyl compound is as follows: where G represents any atomic moiety or single bond of the functional group selected from the group consisting of the following: aryl group, cyclene group, and heterocyclic ring group; and R1˜R32 represent substituents on aryl groups.

Abstract: The invention relates to a new process for preparing tiotropium salts of general formula 1 wherein X? may have the meanings given in the claims and in the specification.

Abstract: Silicon-containing compounds having selective COX-2 inhibitory activity, as well as compositions thereof are provided. The subject compounds find use in a variety of applications, including therapeutic applications. Also provided are kits containing the subject compounds and pharmaceutical preparations thereof.

Abstract: The novel C10-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells in vitro; (ii) are potent inhibition of Topoisomerase I; (iii) lack of susceptibility to MDR/MRP drug resistance; (iv) require no metabolic drug activation: (v) lack glucuronidation of the A-ring or B-ring; (vi) reduce drug-binding affinity to plasma proteins; (vii) maintain lactone stability; (viii) maintain drug potency; and (ix) possess a low molecular weight (e.g., MW<600).

Abstract: The novel C7-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells in vitro; (ii) are potent inhibition of Topoisomerase I; (iii) lack of susceptibility to MDR/MRP drug resistance; (iv) require no metabolic drug activation: (v) lack glucuronidation of the A-ring or B-ring; (vi) reduce drug-binding affinity to plasma proteins; (vii) maintain lactone stability; (viii) maintain drug potency; and (ix) possess a low molecular weight (e.g., MW<600).

Abstract: Provided is a bridged organosilane, which has a large complex organic group, and which is useful in the synthesis of a mesoporous silica and a light-emitting material, and a production method of the bridged organosilane. The bridged organosilane is expressed by the following general formula (1): [in the formula (1), q represents an integer in a range from 2 to 4, X1— represents a substituent selected from the group consisting of substituents expressed by the following general formulae (2) to (5): (in the formulae (2) to (5), R1 represents alkyl group having 1 to 5 carbon atoms, R2 represents an allyl group, and n represents an integer in a range from 0 to 3, and m represents an integer in a range from 0 to 6), and A1 represents an organic group expressed by, for example, the following general formula (6): (in the formula (6), Y1< represents a substituent expressed by, for example, O?C<)].

Abstract: The present invention relates to a new method of cross-coupling aryl moieties comprising reacting an arylhalide with an arylboronic acid in the presence of a palladium compound and a compound comprising a di-alkylphosphine moiety.

Abstract: It is intended to provide water-soluble derivative of camptothecins which are excellent in therapeutic effect and suitable for chemotherapy for cancer. Namely, a water-soluble high-molecular weight derivative of camptothencins being excellent in sustained-release which is obtained by ester-bonding a carboxylic acid group of a polyethylene glycol-polycarboxylic acid polymer to a phenolic hydroxyl group of phenolic camptothencins.

Abstract: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.

Abstract: Diaminoalkanes of Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.

Abstract: The present invention relates to heterocyclic compounds of the formula (I) or a pharmaceutically acceptable salt, a solvate or hydrate thereof wherein the heterocycle comprises two double bonds which may be present at several positions, and which are represented by the dashed lines (---); the heterocycle contains two heteroatoms, W is N or NH; Y is CH, O or NH, wherein if Y is O, X1 is CH and X2 is C-Z-R2 or C—R3, wherein Z is NH, O, or S; and if Y is CH or NH, one of X1 and X2 is CH or N, wherein if X1 is CH or N, X2 is C-Z-R2 or C—R3, and if X2 is CH or N, X1 is C-Z-R2 or C—R3, wherein Z is NH or S; R1 is chosen from structures (a), (b) and (c): R2 is chosen from (C1-C10)alkyl, (C2-C10)alkenyl and (C2-C10)alkynyl, optionally independently substituted with one or more substituents chosen from halogen, hydroxy, cyano, oxo, (C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkenyloxy, (C1-C6)alkenylthio, (C1-C4)alkoxy(C1-C4)alkoxy, (C5-C7)cycloalkyl, a 5-membered unsaturated heterocycle (optionally s

Abstract: In one aspect, the invention relates to silicon-based prepolymers. The disclosed prepolymers exhibit satisfactory solubility in aqueous solutions or hydrophilic solutions and can overcome undesirable shrinkage, expansion, and related problems possessed by conventional silicone monomers and related conventional polymerization techniques by producing hydrogels from a crosslinkable prepolymer. Also disclosed are polymers and molded articles produced from the disclosed prepolymers, which attain a satisfactory oxygen permeability. Also disclosed are methods for producing the disclosed prepolymers. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: The present invention relates to anthracene derivatives, to the use thereof in organic electroluminescent devices, and to organic electroluminescent devices comprising these compounds.

Abstract: The invention relates to azinylimidazoazines of structure (I) and their salts and N-oxides, whereby the symbols have the meanings given in the description, as well as to methods for their preparation and new intermediates. The invention further relates to the use of the compounds of structure (I) and the intermediates for the control of zoopests and undesirable micro-organisms.

Abstract: A Grignard process for preparing phenyl-containing chlorosilane products, in particular diphenylchlorosilanes, is carried out in three embodiments. In the first embodiment, the reactants of the Grignard process are a phenyl Grignard reagent, an ether solvent, a trichlorosilane, and an aromatic hydrocarbon coupling solvent. In the second embodiment, the reactants of the Grignard process are a phenyl Grignard reagent, an ether solvent, a phenylchlorosilane, and an aromatic hydrocarbon coupling solvent. In the third embodiment, the reactants of the Grignard process are a phenyl Grignard reagent, an ether solvent, a trichlorosilane, a phenylchlorosilane, and an aromatic hydrocarbon coupling solvent. In each embodiment, the reactants are present in a particular mole ratio.

Abstract: The present disclosure relates to polycationic monochromophoric hydrazone compounds of following formula (I): wherein W1 is a heteroaromatic radical comprising 5 or 6 ring members, optionally condensed with an aromatic ring comprising 6 ring members, comprising a quaternized nitrogen atom and optionally another heteroatom which may or may not be identical to nitrogen; X, which may or may not be identical, is a nitrogen atom or a CR2 group; Z is a cationic group comprising at least one quaternized nitrogen atom. The present disclosure also relates to a composition for dyeing human keratin fibers comprising the polycationic compounds disclosed herein, and to a dyeing process using the composition of the present disclosure, and even further to multicompartment device.

Abstract: A method of administering a topoisomerase inhibiting agent to a mammal includes administering a pharmaceutically effective amount of a compound having the following formula or a pharmaceutically acceptable salt thereof:

Abstract: Provision of a novel platinum complex which is useful as a material for a light-emitting device of good light emission characteristic and light emission efficiency, and a novel light-emitting material that may be utilized in various fields. A platinum complex represented by the following general formula (1): (in which two rings of ring A, ring B, ring C, and ring D represent nitrogen-containing heterocyclic rings which may have a substituent and the remaining two rings of them represent aryl rings or hetero aryl rings which may have a substituent, the ring A and the ring B, the ring A and the ring C or/and the ring B and the rind D may form condensed rings. Two of X1, X2, X3, and X4 represent nitrogen atoms coordination bonded to a platinum atom and the remaining two of them represent carbon atoms or nitrogen atoms.

Abstract: The present invention discloses: (i) a novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof; (ii) methods of synthesis of said novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof; (iii) pharmaceutically-acceptable formulations comprising said novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more additional chemotherapeutic agents; (iv) methods of administration of said novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more additional chemotherapeutic agents, to subjects in need thereof; and (v) devices for the administration of said novel, lactone-stable, “flipped” E-ring camptothecin, pharmaceutically-acceptable salts, and/or analogs thereof, and, optionally, one or more chemotherapeutic agents, to subjects in need ther

Abstract: The present application relates to a novel tetrahydroquinoline derivative, to a process for its preparation, to its use on its own or in combination for treating and/or preventing diseases and to its use for preparing medicaments, in particular as an inhibitor of the cholesterol ester transfer protein (CETP) for the treatment and/or prevention of cardiovascular disorders, in particular hypolipoproteinaemias, dyslipidaemias, hypertriglyceridaemias, hyperlipidaemias, hypercholesterolaemias and arteriosclerosis.

Abstract: Provided is an organosilane compound expressed by any one of the following general formulae (1) to (7): (wherein: Ar represents a phenylene group or the like; R1 represents a hydrogen atom or the like; R2 to R8 each represent a methyl group or the like; n represents an integer in a range from 0 to 2; m represents an integer of 1 or 2; L represents a single bond or the like; X represents a hydrogen atom or the like; and Y represents a hydrogen atom or the like).

Abstract: The present invention relates to a method for preparing ?-hydroxy, ?-substituted methylenebisphosphonates and phosphonoacetates via addition of Grignard or organoindium reagents to tetraalkyl carbonylbisphosphonates and trialkyl carbonylphosphonoacetates. Also disclosed are compounds so synthesized.

Abstract: This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.

Abstract: The present invention relates to a novel silane coupling agent represented by Formula 1 below and a method for manufacturing the same. Because the compound has urethane and pyridine functional groups, it has superior storage stability and good adhesion property to a matrix resin having hydroxy groups, and thus can be used in a variety of applications. where each of R1 and R2 is hydrogen or C1-C3 alkyl, a is an integer from 0 to 3, each of R3, R4, R5 and R6 is hydrogen, C1-C10 alkyl, halogen, trifluoroalkyl or alkoxyalkyl and n is an integer from 1 to 3.

Abstract: Provided is an organic light emitting device capable of emitting light with high efficiency by incorporating a silyl compound in which a silyl group is directly bonded to an anthracene ring particularly into its light emitting layer.

Abstract: Methods of synthesizing nicotine analogs and derivatives are described. In some embodiments the methods utilize an alkyl or aryl silyl-substituted nicotine analog intermediate. Intermediates useful for the synthesis of nicotine and nicotine analogs are also described.

Abstract: This invention provides 6H-[1]benzopyrano[4,3-b]quinoline compounds having the formula I: The invention further provides compositions including the compounds, methods for the use of the compounds, and methods of preparation of the compounds.

Abstract: Three improved Grignard processes are used for preparing phenyl-containing chlorosilane products wherein the yield of diphenylchlorosilanes as a product is maximized, while the yield of phenylchlorosilanes as a product is minimized. In one embodiment, the process involves contacting a phenyl Grignard reagent, an ether solvent, an aromatic halogenated coupling solvent and a trichlorosilane. In another embodiment, the process involves contacting a phenyl Grignard reagent, an ether solvent, an aromatic halogenated coupling solvent, a trichlorosilane, and a phenylchlorosilane. In yet another embodiment, the process involves contacting a phenyl Grignard reagent, an ether solvent, an aromatic halogenated coupling solvent, and a phenylchlorosilane. In each embodiment, the reactants are present in particular mole ratios of the components.

Abstract: The present invention is directed to electroluminescent complexes of iridium(III) with silylated, germanylated and stannylated ligands. The invention is further directed to electronic devices in which the active layer includes an electroluminescent Ir(III) complex with silylated, germanylated and stannylated ligands.

Abstract: N-halamine compounds which contain hindered amine and amide functional groups. Compounds include wherein X, X?, and X? independently are H, Cl, or Br, wherein no more than two of X, X?, and X? are H and wherein R, R?, and R? are independently alkyl groups containing 1 to 4 carbon atoms or hydrogen, and X and X? are independently H, Cl, or Br. Compositions comprising the compounds are also described. The compounds and/or compositions can be used, for example, for the purpose of constructing biocidal coatings and materials. The biocidal activity can inactivate pathogenic microorganisms such as bacteria, fungi, and yeasts, as well as, virus particles.

Abstract: The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them, their use in the treatment and/or prevention of disorders mediated by one or more estrogen receptors and processes for their preparation. The compounds of the invention are useful in the treatment and/or prevention of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.

Abstract: The present invention relates to polymeric compositions useful in the manufacture of biocompatible medical devices. More particularly, the present invention relates to certain cationic monomers capable of polymerization to form polymeric compositions having desirable physical characteristics useful in the manufacture of ophthalmic devices. Such properties include the ability to extract the polymerized medical devices with water. This avoids the use of organic solvents as is typical in the art. The polymer compositions comprise polymerized silicon-containing monomers end-capped with polymerizable cationic hydrophilic groups.

Abstract: Stable carbene ligands are provided having a carbene center flanked by a quaternary carbon and an amino group, and having utility in the preparation of various transition metal complexes.

Abstract: The present invention relates to an acrylic pressure sensitive adhesive composition containing organic functional groups of urethane and pyridine, more precisely an acrylic pressure sensitive adhesive composition which has excellent removability owing to its low initial peel strength on glass and excellent long-term durability since the peel strength of the pressure sensitive adhesive composition onto glass is being increased under high temperature and high humidity. The present invention also relates to an acrylic pressure sensitive adhesive composition for a polarizer having excellent adhesive functions and durability, a polarizer and a LCD containing the same.

Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, m, n, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Abstract: The present invention provides a silane molecule which combines pre-activated and protein-resistant functionalities in one molecule; the molecule has a general formula: A-(CH2)n—(O[CH2]t)m—(CH2)v—Y ??(1) wherein A is a functional group for binding to a substrate and Y is a functional group for binding to biomolecules. The invention furthermore provides a method for the synthesis of such a silane molecule and a method for depositing a monolayer of such silane molecules onto a substrate. Such a monolayer of silane molecules may be used in biosensors, DNA/protein micro-arrays or other sensor applications. For further lowering the protein binding to the surface of the biosensor, the monolayer may furthermore comprise second silane molecules with formula: B—(CH2)o—(OCH2CH2)r—Z.

Abstract: This invention provides the compounds of formula (I): or a pharmaceutically acceptable ester of such compound, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 independently represent a hydrogen atom or the like; R3 represents an aryl group having from 6 to 10 ring atoms or the like; X represents an oxygen atom, or the like; Y represents an oxygen atom or the like; and n represents an integer 0, 1 or 2. These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.

Abstract: The present invention provides active compounds for modulating nicotinic acetylcholine receptors and methods of making the same. The methods of preparing the active compounds utilize different intermediate compounds.

Abstract: Provided is an organic light emitting device capable of emitting light with high efficiency by incorporating a silyl compound in which a silyl group is directly bonded to an anthracene ring particularly into its light emitting layer. In the organic light emitting device including: a pair of electrodes formed of an anode and a cathode, at least one of which being transparent or semi-transparent; and one or more layers containing an organic compound layer interposed between the pair of electrodes, at least one of the layer containing the organic compound contains the following silyl compound, and a layer containing at least one kind of the silyl compound is a light emitting layer.

Abstract: (20S) esters of camptothecin analogs are provided. The compounds are (20S) esters of an oxyalkanoic acid and camptothecin, which is are optionally substituted at the 7, 9, 10, 11, and 12 positions of the camptothecin ring. The compounds are useful for treating cancer.