Polyperylenes

Dense Nanoscale Logic Circuitry

One embodiment of the present invention is directed to hybrid-nanoscale/microscale device comprising a microscale layer that includes microscale and/or submicroscale circuit components and that provides an array of microscale or submicroscale pins across an interface surface; and at least two nanoscale-layer sub-layers within a nanoscale layer that interfaces to the microscale layer, each nanoscale-layer sub-layer containing regularly spaced, parallel nanowires, each nanowire of the at least two nanoscale-layer sub-layers in electrical contact with at most one pin provided by the microscale layer, the parallel nanowires of successive nanoscale-layer sub-layers having different directions, with the nanowires of successive nanoscale-layer sub-layers intersecting to form programmable crosspoints.

Nanoelectronic differential amplifiers and related circuits implemented on a segment of a graphene nanoribbon

A multiple transistor differential amplifier is implemented on a segment of a single graphene nanoribbon. Differential amplifier field effect transistors are formed on the graphene nanoribbon from a first group of electrical conductors in contact with the graphene nanoribbon and a second group of electrical conductors insulated from, but exerting electric fields on, the graphene nanoribbon thereby forming the gates of the field effect transistors. A transistor in one portion of the graphene nanoribbon and a transistor in another portion of the graphene nanoribbon are responsive to respective incoming electrical signals. A current source, also formed on the graphene nanoribbon, is connected with the differential amplifier, and the current source and the differential amplifier operating together generate an outgoing signal responsive to the incoming electrical signal. In an example application, the resulting circuit can be used to interface with electrical signals of nanoscale sensors and actuators,

Biological control of nanoparticle nucleation, shape and crystal phase

The present invention includes compositions and methods for selective binding of amino acid oligomers to semiconductor and elemental carbon-containing materials. One form of the present invention is a method for controlling the particle size of the semiconductor or elemental carbon-containing material by interacting an amino acid oligomer that specifically binds the material with solutions that can result in the formation of the material. The same method can be used to control the aspect ratio of the nanocrystal particles of the semiconductor material. Another form of the present invention is a method to create nanowires from the semiconductor or elemental carbon-containing material. Yet another form of the present invention is a biologic scaffold comprising a substrate capable of binding one or more biologic materials, one or more biologic materials attached to the substrate, and one or more elemental carbon-containing molecules attached to one or more biologic materials.

Projection Exposure System, Beam Delivery System and Method of Generating a Beam of Light

A beam delivery system of a projection exposure system comprises a laser generating a beam of laser light from a plurality of longitudinal laser modes in a cavity, wherein light generated by a single longitudinal laser mode has an average line width λ lat , wherein the laser light of the beam has, at each of respective lateral positions of the beam, a second line width λ lat corresponding to lateral laser modes, and wherein the laser light of the beam has, when averaged over a whole cross section thereof, a line width λ b corresponding to plural lateral laser modes, and wherein λ m <λ lat <λ b , and wherein an optical delay apparatus disposed in the beam provides an optical path difference Δl, wherein 0.8 · λ 0 2 ( 2 · Δ   λ l ) < Δ   l < 1.8 · λ 0 2 ( 2 · Δλ l ) , wherein λ 0 is an average wavelength of the light of the first beam of laser light, and Δλ lat represents the second line width.

Bridged compounds as hiv integrase inhibitors

Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: the asterisk * in Q denotes the point of attachment to the rest of the compound; and n, L1, L2, X1, X2, χ3, Y, Z, R1, R2 and R3 are defined herein. The N compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

pH MODULATION METHOD TO DETECT LIGAND-RECEPTOR BINDING

The present disclosure relates to detecting receptor-ligand binding by measuring local pH modulation using a pH-sensitive fluorophore.

Modified graphene structures and methods of manufacture thereof

The present invention is directed to a modified graphene structure comprising at least one graphene sheet ( 1 ) and a self-assembled monolayer ( 2 ) of functional organic molecules ( 3 ) non-covalently bonded to the top and/or bottom basal planes of the graphene sheet and methods of manufacture thereof. The present invention is also directed to devices comprising the modified graphene structures, including but not limited to field-effect devices and biosensors, and to methods using the modified graphene structures.

Organic photoelectric conversion element

A high photoelectric conversion efficiency is provided by an organic photoelectric conversion element comprising a first electrode, a second electrode and an active layer, wherein the active layer is located between the first electrode and the second electrode and contains an electron-donating compound and an electron-accepting compound, and the active layer side of the first electrode surface is treated with a coupling agent followed by a lyophilic treatment.

Nonvolatile semiconductor memory

According to one embodiment, in a nonvolatile semiconductor memory in which a charge store layer is formed on a tunnel insulating film formed on a channel region of a semiconductor substrate, a first nanoparticle layer containing first conductive nanoparticles is formed on the channel side, and a second nanoparticle layer containing a plurality of second conductive nanoparticles having an average particle size larger than the first conductive nanoparticles is formed on the charge store layer side. An average energy value ΔE 1 required for charging one electron in the first conductive nanoparticle is smaller than an average energy value ΔE required for charging one electron in the second conductive nanoparticle, and a difference between ΔE 1 and ΔE is larger than a heat fluctuation energy (k B T).

Quantum dot-encoded bead set for calibration and quantification of multiplexed assays, and methods for their use

Control beads are disclosed that allow for improved quantitation of analytes in multiplexed bead assays. The control beads have a range of concentrations of calibration moieties that provide for the preparation of a titration curve. The titration curve can be used to quantify the concentration of the analytes. The titration curve can be used to correlate the signal obtained from a bead with the concentration (or absolute number of molecules) of the analyte bound to the bead.

Artificial retina device

The present technology provides an organic based artificial retina device that includes a substrate and an array of micro-electrodes formed on the substrate. The illustrative artificial retina device further includes a photoconducting polymer blend deposited on the array of micro-electrodes. The photoconducting polymer blend is configured to produce a photoelectric signal in response to receiving light.

Method of forming lutetium and lanthanum dielectric structures

Methods of forming dielectric structures are shown. Methods of forming dielectric structures are shown that include lutetium oxide and lanthanum aluminum oxide crystals embedded within the lutetium oxide. Specific methods shown include monolayer deposition which yields process improvements such as chemistry control, step coverage, crystallinity/microstructure control.

Device

According to one embodiment, a device includes an insulating layer with a first trench, a first interconnect layer in the first trench, the first interconnect layer including copper and includes a concave portion, and a first graphene sheet on an inner surface of the concave portion.

Organic light-emitting device and method of manufacturing the same

An organic solar cell and a method of manufacturing the same.

Tunnel field effect transistor

A tunnel field effect transistor and a method of making the same. The transistor includes a semiconductor substrate. The transistor also includes a gate located on a major surface of the substrate. The transistor further includes a drain of a first conductivity type. The transistor also includes a source of a second conductivity type extending beneath the gate. The source is separated from the gate by a channel region and a gate dielectric. The transistor is operable to allow charge carrier tunnelling from an inversion layer through an upper surface of the source.

Semiconductor device and structure

A method of manufacturing a semiconductor wafer, the method comprising: providing a base wafer comprising a semiconductor substrate; preparing a first monocrystalline layer comprising semiconductor regions; preparing a second monocrystalline layer comprising semiconductor regions overlying the first monocrystalline layer; and etching portions of said first monocrystalline layer and portions of said second monocrystalline layer as part of forming at least one transistor on said first monocrystalline layer.

Two silicon-containing precursors for gapfill enhancing dielectric liner

Aspects of the disclosure pertain to methods of depositing silicon oxide layers on substrates. In embodiments, silicon oxide layers are deposited by flowing a silicon-containing precursor having a Si—O bond, an oxygen-containing precursor and a second silicon-containing precursor, having both a Si—C bond and a Si—N bond, into a semiconductor processing chamber to form a conformal liner layer. Upon completion of the liner layer, a gap fill layer is formed by flowing a silicon-containing precursor having a Si—O bond, an oxygen-containing precursor into the semiconductor processing chamber. The presence of the conformal liner layer improves the ability of the gap fill layer to grow more smoothly, fill trenches and produce a reduced quantity and/or size of voids within the silicon oxide filler material.

Photoelectric conversion device and solid-state imaging device

A photoelectric conversion device having: a pair of electrodes; a photoelectric conversion layer sandwiched between the pair of electrodes; and at least one electron blocking layer provided between one electrode of the pair of electrodes and the photoelectric conversion layer, wherein the photoelectric conversion layer contains at least one organic material, and the at least one electron blocking layer has a mixed layer containing fullerene or fullerene derivatives.

Fused piperidine compound and pharmaceutical containing same

The present invention provides a low molecular weight compound having EPO production-promoting action and/or hemoglobin production-promoting action. The present invention relates to a fused piperidine compound represented by the following general formula (1): (wherein, ring A represents a C 10-14 aryl group or 5- to 10-membered heterocyclic group, X represents N—R 7 , a sulfur atom or an oxygen atom, R 1 , R 2 , R 2′ , R 3 and R 3′ independently represent a hydrogen atom, C 1-6 alkyl group or C 3-6 cycloalkyl group, and R 4 , R 5 and R 6 independently represent a hydrogen atom or halogen atom), or a salt thereof, or a solvate thereof.

Radiolabeled cgrp antagonists

The present invention is directed to radiolabeled CGRP receptor antagonists which are useful for the quantitative imaging of CGRP receptors in mammals.

Inhibitors of syk and jak protein kinases

The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

Multilayer transparent light-receiving device and electronic device

A multilayer transparent light-receiving device with significantly high photoresponsive speed that is easily manufactured, and a high-performance electronic device using the multilayer transparent light-receiving device are provided. The multilayer transparent light-receiving device is composed by laminating a plurality of protein transparent light-receiving elements using an electron transfer protein. The protein transparent light-receiving element has a structure in which a transparent substrate, a transparent electrode, an electron transfer protein layer, an electrolyte layer, and a transparent counter electrode are sequentially laminated. The multilayer transparent light-receiving device is used as a light-receiving device for a camera, an optical disc system and the like.

Programmable metallization memory cell with planarized silver electrode

Programmable metallization memory cells having a planarized silver electrode and methods of forming the same are disclosed. The programmable metallization memory cells include a first metal contact and a second metal contact, an ion conductor solid electrolyte material is between the first metal contact and the second metal contact, and either a silver alloy doping electrode separates the ion conductor solid electrolyte material from the first metal contact or the second metal contact, or a silver doping electrode separates the ion conductor solid electrolyte material from the first metal contact. The silver electrode includes a silver layer and a metal seed layer separating the silver layer from the first metal contact.

Method of manufacturing printed circuit board

A method of manufacturing a printed circuit board, including: applying a conductive paste including carbon nanotubes and a photosensitive binder on a bump-forming area of a circuit substrate having a circuit layer for transferring electrical signals; and patterning the conductive paste, thus forming bumps.

Hydrate of sulfonylurea compound, process for producing the same and suspension formulation containing the same

The present invention relates to a hydrate of sulfonylurea compound represented by formula (I): having herbicidal activity, a process for producing the same, a suspension formulation containing the same, and the like.

Modulators of cell cycle checkpoints and their use in combination with checkpoint kinase inhibitors

In its many embodiments, the present invention provides a novel class of pyrimidine analogs as targeted mechanism-based modulators of cell cycle checkpoints. Cancers and/or malignancies can be treated by administration of a cell cycle checkpoint modulator of the invention. Also discussed are suitable combinations of the cell cycle checkpoint modulator with a checkpoint kinase inhibitor to produce synergistic apoptosis in cancer cells. The invention also includes methods of treating cancers by administering the combination of the cell cycle checkpoint modulator and the checkpoint kinase inhibitor, pharmaceutical compositions comprising the cell cycle checkpoint modulator as well as combinations and pharmaceutical kits. An example cell cycle checkpoint modulator is shown below: formula (I).

Dual small molecule inhibitors of cancer and angiogenesis

The present invention provides analogs and derivatives of thalidomide which inhibit cancer and angiogenesis. The present invention further provides compounds which disrupt microtubule polymerization. The present further provides methods of treating cancers comprising mutant p53.

Organic photovoltaic cell

An organic photovoltaic cell ( 10 ) of the present invention includes an active layer ( 40 ) containing an organic compound and being provided between a pair of electrodes of a first electrode ( 32 ) and a second electrode ( 34 ), and because the active layer contains metallic oxide nano-particles wearing a carbon material on its surface, the organic photovoltaic cell can be manufactured from an inexpensive material.

Novel organic electroluminescent compounds and organic electroluminescent device using the same

Provided are a novel organic electroluminescent compound and an organic electroluminescent device using the same. When used as a host material of an organic electroluminescent material of an OLED device, the organic electroluminescent compound disclosed herein exhibits good luminous efficiency and excellent life property as compared to the existing host material. Therefore, it may be used to manufacture OLEDs having very superior operation life.

Bi-layer pseudo-spin field-effect transistor

A bi-layer pseudo-spin field-effect transistor (BiSFET) is disclosed. The BiSFET includes a first and second conduction layers separated by a tunnel dielectric. The BiSFET transistor also includes a first gate separated from the first conduction layer by an insulating dielectric layer, and a second gate separated from the second conduction layer by an insulating layer. These conduction layers may be composed of graphene. The voltages applied to the first and/or second gates can control the peak current and associated voltage value for current flow between top and bottom conduction channels, and interlayer current voltage characteristic exhibiting negative differential resistance. BiSFETs may be used to make a variety of logic gates. A clocked power supply scheme may be used to facilitate BiSFET-based logic.

Electroforming-free nanoscale switching device

A nanoscale switching device is constructed such that an electroforming process is not needed to condition the device for normal switching operations. The switching device has an active region disposed between two electrodes. The active region has at least one switching layer formed of a switching material capable of transporting dopants under an electric field, and at least one conductive layer formed of a dopant source material containing dopants that can drift into the switching layer under an electric field. The switching layer has a thickness about 6 nm or less.

Quantum dot-fullerene junction based photodetectors

A photodetector includes one or more photodiodes and a signal processing circuit. Each photodiode includes a transparent first electrode, a second electrode, and a heterojunction interposed between the first electrode and the second electrode. Each heterojunction includes a quantum dot layer and a fullerene layer disposed directly on the quantum dot layer. The signal processing circuit is in signal communication each the second electrode. The photodetector may be responsive to wavelengths in the infrared, visible, and/or ultraviolet ranges. The quantum dot layer may be treated with a chemistry that increases the charge carrier mobility of the quantum dot layer.

Spin filter device, method for its manufacture and its use

The present invention relates to a method and a device for providing a current of spin-polarised electrons. More particularly, the present invention is suited for use in spin electronics or detection of spin-polarised electrons.

Methods for increasing bottom electrode performance in carbon-based memory devices

In some aspects, a method of forming a reversible resistance-switching metal-insulator-metal (“MIM”) stack is provided, the method including: forming a first conducting layer comprising a titanium nitride material having between about 50% Ti and about 95% Ti, forming a carbon nano-tube (CNT) material above the first conducting layer, forming a second conducting layer above the CNT material, and etching the first conducting layer, CNT material and second conducting layer to form the MIM stack. Numerous other aspects are provided.

High Performance Field-Effect Transistors

A high performance field-effect transistor includes a substrate, a nanomaterial thin film disposed on the substrate, a source electrode and a drain electrode formed on the nanomaterial thin film, and a channel area defined between the source electrode and the drain electrode. A unitary self-aligned gate electrode extends from the nanomaterial thin film in the channel area between the source electrode and the drain electrode, the gate electrode having an outer dielectric layer and including a foot region and a head region, the foot region in contact with a portion of the nanomaterial thin film in the channel area. A metal layer is disposed over the source electrode, the drain electrode, the head region of the gate electrode, and portions of the nanomaterial thin film proximate the source electrode and the drain electrode in the channel area.

Novel Process for the Preparation of Paliperidone

The present invention relates to a novel process for the preparation of paliperidone by hydrolysis of 9 -O-acylated paliperidone. In a preferred embodiment of the present invention, Paliperidone Form (II) of purity of about 98 % or more was obtained by basic hydrolysis of 9-O-Acetyl Paliperidone.

Nanowire Tunnel Field Effect Transistors

A nanowire tunnel field effect transistor (FET) device includes a channel region including a silicon portion having a first distal end and a second distal end, the silicon portion is surrounded by a gate structure disposed circumferentially around the silicon portion, a drain region including an doped silicon portion extending from the first distal end, a portion of the doped silicon portion arranged in the channel region, a cavity defined by the second distal end of the silicon portion and an inner diameter of the gate structure, and a source region including a doped epi-silicon portion epitaxially extending from the second distal end of the silicon portion in the cavity, a first pad region, and a portion of a silicon substrate.

Charge transport layers and organic electron devices comprising same

Provided are organic n-doped electron transport layers comprising at least one electron transport material and at least one electron rich dopant material and organic p-doped hole transport layers comprising at least one hole transport material and at least one electron deficient dopant material.

Method of Fabricating Thin Film Transistor and Top-gate Type Thin Film Transistor

A method of fabricating a thin film transistor (TFT) and a top-gate type thin film transistor are disclosed, the method of fabricating a TFT of the present invention comprises steps: (A) providing a substrate; (B) forming a source electrode, a drain electrode, and SWCNT (singled-walled carbon nanotubes) layer on the substrate, in which the source electrode and the drain electrode are spaced in a distance and the SWCNT layer is located between the source electrode and the drain electrode; (C) forming a gate oxide layer on the SWCNT layer; (D) annealing the gate oxide layer with oxygen or nitrogen gas; and (E) forming a gate electrode on the gate oxide layer; wherein the temperature used in the step (D) for annealing is a 500° C. to 600° C.

Circuit structure and manufacturing method thereof

A manufacturing method of a circuit structure is provided. A metal layer having an upper surface is provided. A surface passivation layer is formed on the metal layer. The surface passivation layer exposes a portion of the upper surface of the metal layer, and a material of the metal layer is different from a material of the surface passivation layer. The metal layer and the surface passivation layer are dipped into a modifier, and the modifier is selectively absorbed and attached to the surface passivation layer, so as to form a covering layer. The covering layer has a plurality of nanoparticles and covers the surface passivation layer.

Photoproducts of Tryptophan, Their Synthesis and Uses Thereof

We have found that exposure of an aqueous tryptophan solution to window sunlight results in the production of multiple tryptophan photoproducts that have the capability of activating the aryl hydrocarbon receptor and increasing the production of AhR target genes and proteins in hepatocytes. We have isolated three of those photoproducts not previously identified as AhR activators, their chemical identification and synthesis and the demonstration that all three have biologic activities as novel AhR activators. Further, one of the three is a completely novel, not previously described, chemical compound.

Nanowire pin tunnel field effect devices

A nanowire tunnel device includes a nanowire suspended above a semiconductor substrate by a first pad region and a second pad region, the nanowire having a channel portion surrounded by a gate structure disposed circumferentially around the nanowire, an n-type doped region including a first portion of the nanowire adjacent to the channel portion, and a p-type doped region including a second portion of the nanowire adjacent to the channel portion.

Heterocyclic oxime compounds

The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).

Material for photoelectric conversion device and photoelectric conversion device

The present invention provides a photoelectric conversion device that is durable, lightweight, and inexpensive, and has a network structure of organic semiconductor nanowires that has high durability and is suitable for charge transport. In addition, to provide the photoelectric conversion device, the present invention provides, as an electron-donating material, a material for a photoelectric conversion device, the material including phthalocyanine nanowires having a breadth of 50 nm or less and a ratio (length/breadth) of a length to the breadth, the ratio being 10 or more. According to the present invention, a photoelectric conversion device having a long life due to high light resistance of phthalocyanine can be provided at a low cost. Use of such photoelectric conversion devices can constitute a solar-cell module having a long life due to the feature of the photoelectric conversion devices and being manufactured at a low cost.

Double gate planar field effect transistors

A stacked planar device and method for forming the same is shown that includes forming, on a substrate, a stack of layers having alternating sacrificial and channel layers, patterning the stack such that sides of the stack include exposed surfaces of the sacrificial and channel layers, forming a dummy gate structure over a region of the stack to establish a planar area, forming a dielectric layer around the dummy gate structure to cover areas adjacent to the planar area, removing the dummy gate structure to expose the stack, selectively etching the stack to remove the sacrificial layers from the channel layers in the planar area, and forming a gate conductor over and in between the channel layers to form a transistor device.

Ionic liquid containing sulfonate ions

Embodiments are related to ionic liquids and more specifically to ionic liquids used in electrochemical metal-air cells in which the ionic liquid includes sulfonate ions as the anion.

Heterocyclic compound and organic light-emitting diode and flat display device including the heterocyclic compound

A heterocyclic compound, an organic light-emitting diode, and a flat display device, the heterocyclic compound being represented by Formula 1, below:

Inhibitors of hepatitis c virus ns5b polymerase

Disclosed are compounds of formula (I) that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

Method for manufacturing a magnetoresistive sensor using simultaneously formed hard bias and electrical lapping guide

A method for manufacturing a magnetic sensor using an electrical lapping guide deposited and patterned simultaneously with a hard bias structure of the sensor material. The method includes depositing a sensor material, and patterning and ion milling the sensor material to define a track width of the sensor. A magnetic, hard bias material is then deposited and a second patterning and ion milling process is performed to simultaneously define the back edge of an electrical lapping guide and a back edge of the sensor.

Process for producing an organic photoelectric conversion element

Disclosed is an organic photoelectric conversion element including an anode, a cathode, an active layer, and a functional layer, wherein the anode contains a metal, the anode and the functional layer are adjacent to each other, and the functional layer is formed using a solution having a pH value of 5 to 9. Examples of the metal include aluminum, magnesium, titanium, chromium, iron, nickel, copper, zinc, gallium, zirconium, molybdenum, silver, indium, and tin. Preferably, the active layer contains a conjugated polymer compound and a fullerene derivative.

Triode-type field emission device and method of manufacturing the same

A triode-type field emission device and method of manufacturing the same, suitable for use in screen print process of curved or planar substrate, comprising the following steps: firstly, form a cathode and a gate on a cathode substrate at the same time by means of screen printing, and a gap is located between gate and cathode, to avoid short circuit or interference; next, form a hedgehog-shape field emission layer on at least said cathode; then, form a transparent conductive layer and a light emitting layer sequentially on an anode substrate; and finally, dispose cathode substrate and anode substrate in parallel and spaced apart, and package them into a triode-type field emission device. Bias of cathode and gate can be controlled to achieve local adjustment of light. Also, gate may serve as an emitter, to increase field emission efficiency and its service life.

Method for making schottky barrier diode

A method for making a Schottky barrier diode includes the following steps. A first metal layer, a second metal layer and a carbon nanotube composite material are provided. The carbon nanotube composite material is applied on the first metal layer and the second metal layer to form a semiconductor layer. The carbon nanotube composite material includes an insulated polymer and a number of carbon nanotubes dispersed in the insulated polymer. The semiconductor layer is in Schottky contact with the first metal layer and in ohmic contact with the second metal layer.

Process for the preparation of varenicline

It is disclosed a process for the preparation of a compound of formula (I) or a salt thereof, comprising: nitrating a compound of formula (II) or a salt thereof, to obtain a compound of formula (IV) or a salt thereof, reducing it, to obtain a compound of formula (V) or a salt thereof, and subsequently cyclizing it to obtain a compound of formula (I) or a salt thereof and, if desired, converting a compound of formula (I) to a salt thereof, or vice versa, characterized in that: the nitration of a compound of formula (II) or a salt thereof is carried out with concentrated nitric acid in the presence of a strong inorganic acid and that the amino group in the compound of formula (II) is not protected.

Field-effect transistor and method for manufacturing the same

A field-effect transistor includes a semiconductor layer containing carbon nanomaterials; a first electrode and a second electrode formed in contact with the semiconductor layer; a third electrode for controlling current flowing between the first electrode and the second electrode; and an insulating layer formed between the semiconductor layer and the third electrode. The insulating layer contains an aromatic polyamide comprising a substituent containing 1 to 20 carbon atoms.

Raf kinase inhibitors

Described herein are compounds, pharmaceutical compositions and methods for the inhibition of RAF kinae mediated signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human disease and disorders.

Method for Enhancing Optoelectronic Properties of Conjugated Polymers

The present invention provides a method for enhancing optoelectronic properties of polymers that contain conjugated moieties in their molecular structures (hereby denoted as “conjugated polymers”), to be used in lighting, photovoltaics, other various optoelectronic devices and applications. The method of the present invention includes preparing a conjugated polymer layer or multiple conjugated polymer layers and imprinting the conjugated polymer layer or layers through the application of a mold or multiple molds.

Cpp-gmr sensor with corrosion resistent spacer layer and higher signal/noise ratio

A method and apparatus for increasing the electrical resistivity and corrosion resistance of the material forming a spacer layer in current-perpendicular-to-the-plane (CPP) giant magnetoresistive (GMR) sensors. The increased resistivity of the spacer layer, and thus, the CPP-GMR sensor permits a larger voltage across the sensor and a higher signal-to-noise ratio. The increased corrosion resistance of the spacer layer minimizes the effects of exposing the spacer layer to corrosive materials during fabrication. For example, adding tin to silver to form a metallic alloy spacer layer increases the corrosion resistance of the spacer layer and the electrical resisitivity of the CPP-GMR sensor relative to a spacer layer consisting solely of silver. The Ag—Sn alloy permits a larger current to flow through the sensor, which increases the signal-to-noise ratio.

Ultrasensitive biosensors

The present invention is a biosensor apparatus that includes a substrate, a source on one side of the substrate, a drain spaced from the source, a conducting channel between the source and the drain, an insulator region, and receptors on a gate region for receiving target material. The receptors are contacted for changing current flow between the source and the drain. The source and the drain are relatively wide compared to length between the source and the drain through the conducting channel.

Quantum computing circuits

A system for performing digital operations, including a first device configured to transform a digital input into one or more signals, at least one AB ring, the at least one AB ring irreducibly-coupled and configured to include at least three terminals, a second device configured to read a portion of a signal expressed upon two or more of the at least three terminals, and a third device configured to transform the portion of the signal expressed upon two or more of the at least three terminals into a digital output, the third device operationally connected to the second device.

Efficient organic solar cell using core/shell metal oxide nanoparticles, and method for manufacturing same

The present invention relates to a photoactive layer solution for an efficient organic solar cell including core/shell metal oxide nano-particles, to a method for manufacturing same, and to an organic solar cell including the photoactive layer solution and to a method for manufacturing same. Uniform coating of a substrate having a large area is difficult using the existing PEDOT:PSS. However, using the photoactive layer solution according to the present invention enables P-type metal oxide nano-particles to be directly dispersed on the photoactive layer, thereby having efficiency similar to the existing layer-by-layer (LbL)-type organic solar cell, and enabling a reduction in costs, since there is no need to deposit a separate p buffer layer such as PEDOT:PSS, and the organic solar cell to be manufactured by means of just a simple wet process. Also, application products can be selected through various types of coating methods.

ORGANIC NANOFIBER STRUCTURE BASED ON SELF-ASSEMBLED ORGANOGEL, ORGANIC NANOFIBER TRANSISTOR USING THE SAME, AND METHOD OF MANUFACTURING THE ORGANIC NANOFIBER TRANSISTOR

An organic nanofiber including a gelled organic semiconductor compound. Also disclosed is an organic semiconductor transistor and a method of manufacturing an organic semiconductor transistor. 1. An organic semiconductor transistor comprising:a substrate;a gate electrode;a source electrode and a drain electrode, each of which are insulated from the gate electrode;an organic semiconductor layer, which is insulated from the gate electrode and electrically connected to the source and drain electrodes; andan insulating layer, which insulates the gate electrode from the source and drain electrodes and the organic semiconductor layer,wherein an organic nanofiber comprising a gelated organic semiconductor compound is disposed on the organic semiconductor layer.2. The organic semiconductor transistor of claim 1 , formed by self-assembly of the gelated organic semiconductor compound in an organic solvent.3. The organic semiconductor transistor of claim 1 , wherein the organic semiconductor layer is formed using bottom contact geometry and the channel layer is formed on the source and drain electrodes claim 1 , or wherein the organic semiconductor layer is formed using top contact geometry and the source and drain electrodes are formed on the channel layer.6. The organic semiconductor transistor of claim 5 , wherein the organic solvent comprises dimethyl sulfoxide. This application is a divisional of U.S. application Ser. No. 12/499,310, filed on Jul. 8, 2009, which claims priority to Korean Patent Application No. 10-2008-0066471, filed on Jul. 9, 2008, and all the benefits accruing therefrom under 35 U.S.C. §119, the contents of which in their entirety are incorporated herein by reference.The patent or application file contains at least one drawing executed in color. Copies of this patent or patent application publication with color drawings will be provided by the Office upon request and payment of the necessary fee.BACKGROUND1. FieldOne or more embodiments relate to an ...

SUBSTITUTED HYDROXYETHYL AMINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE

The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I 3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 1a', '1b', '7, 'Rand Rtaken together with the carbon atom to which they are attached form a partially or fully saturated 4-, 5- or 6-membered ring of carbon atoms optionally including 1-2 heteroatoms selected from O, N, or S, the ring optionally substituted independently with 1-3 substituents of R; and'}{'sup': '1c', 'Ris H.'}4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein m is 1 and Ris a ring selected from phenyl claim 1 , pyridyl claim 1 , pyrimidyl claim 1 , pyridazinyl claim 1 , pyrazinyl claim 1 , triazinyl claim 1 , thiophenyl claim 1 , furyl claim 1 , pyrrolyl claim 1 , pyrazolyl claim 1 , imidazolyl claim 1 , triazolyl claim 1 , tetrazolyl claim 1 , thiazolyl claim 1 , oxazolyl claim 1 , isoxazolyl claim 1 , isothiazolyl claim 1 , thiadiazolyl claim 1 , oxadiazolyl claim 1 , pyrrolidinyl claim 1 , oxazolinyl claim 1 , isoxazolinyl claim 1 , thiazolinyl claim 1 , pyrazolinyl claim 1 , morpholinyl claim 1 , piperidinyl claim 1 , piperazinyl and pyranyl claim 1 , said ring optionally substituted with 1-5 substituents of R.6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': '1', 'Ais CH;'}{'sup': 2', '6, 'Ais CR;'}{'sup': 3', '4', '6', '3', '4, 'each of Aand A, independently, is CH or CRor N, provided no more than one of Aand Ais N;'}{'sup': 1a', '7, 'sub': 1-6', '2-6', '2-6', '1-6', '1-3', '1-6', '1-3', '1-6', '2', '1-3', '1-6', '1-3', '1-3', '1-3', '2-4', '1-3', '2-4', '1-3', '2-4', '1-3', '2-4', '1-3, 'Ris C-alkyl, Calkenyl, C-alkynyl, Calkyl-O—C-alkyl-, C-alkyl-S—C-alkyl-, C-alkyl ...

Soluble mtor complexes and modulators thereof

The present invention relates to small molecule modulators of mTORC1 and mTORC2, syntheses thereof, and intermediates thereto. Such small molecule modulators are useful in the treatment of proliferative diseases (e.g., benign neoplasms, cancers, inflammatory diseases, autoimmune diseases, diabetic retinopathy) and metabolic diseases. Novel small molecules are provided that inhibit one or more of mTORC1, mTORC2, and PI3K-related proteins. Novel methods of providing soluble mTORC1 and mTORC2 complexes are discussed, as well as methods of using the soluble complexes in a high-throughput manner to screen for inhibitory compounds.

INHIBITORS OF JUN N-TERMINAL KINASE

The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: 3. The compound of claim 1 , wherein ring A is chosen from thiophene claim 1 , thiazole claim 1 , and pyrazole claim 1 , wherein the thiophene claim 1 , the thiazole claim 1 , or the pyrazole is optionally substituted with 1 or 2 substituents chosen from C-C-alkyl claim 1 , C-C-alkenyl claim 1 , C-C-alkynyl claim 1 , C-C-haloalkyl claim 1 , 2- to 4-membered heteroalkyl claim 1 , C-C-cycloalkyl claim 1 , 3- to 6-membered heterocycloalkyl claim 1 , CN claim 1 , and halogen.6. The compound of claim 1 , wherein W is methylene (—CH—).7. The compound of claim 1 , wherein Ris H.8. The compound of claim 1 , wherein Cy is chosen from phenyl claim 1 , naphthyl claim 1 , quinoline claim 1 , isoquinoline claim 1 , quinoxaline claim 1 , quinazoline claim 1 , 3 claim 1 ,4-dihydroquinolin-2-one claim 1 , and 3 claim 1 ,4-dihydro-1 claim 1 ,6-naphthyridin-2-one claim 1 , each optionally substituted with 1-6 substituents independently chosen from C-C-alkyl claim 1 , C-C-alkenyl claim 1 , C-C-alkynyl claim 1 , C-C-haloalkyl claim 1 , 2- to 6-membered heteroalkyl claim 1 , C-C-cycloalkyl claim 1 , 3- to 8-membered heterocycloalkyl claim 1 , aryl claim 1 , 5- or 6-membered heteroaryl claim 1 , CN claim 1 , halogen claim 1 , OR claim 1 , SR claim 1 , NRR claim 1 , C(O)R claim 1 , C(O)NRR claim 1 , OC(O)NRR claim 1 , C(O)OR claim 1 , NRC(O)R claim 1 , NRC(O)OR claim 1 , NRC(O)NRR claim 1 , NRC(S)NRR claim 1 , NRS(O)R claim 1 , S(O)NRR claim 1 , S(O)Rand S(O)R claim 1 ,wherein{'sup': 52', '53', '55', '52', '53, 'sub': 1', '6', '3', '8, 'R, Rand Rare independently chosen from H, acyl, C-C-alkyl, 2- to 6-membered heteroalkyl, aryl, 5- or 6-membered heteroaryl, C-Ccycloalkyl and 3- to 8-membered heterocycloalkyl, wherein Rand R, together with the nitrogen atom to which they are bound are optionally joined to form a 5- to 7-membered heterocyclic ring; and'}{'sup ...

PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS

The present invention provides compounds of Formula I including tautomers, resolved enantiomers, resolved diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. 2. The method of claim 1 , wherein Ris H claim 1 , CH claim 1 , CHCH claim 1 , CH═CH claim 1 , CHOH claim 1 , CF claim 1 , CHFor CHF.3. The method of claim 1 , wherein m is 2 and n is 1.4. The method of claim 1 , wherein m is 2 and n is 2.5. The method of claim 1 , wherein m is 3 and n is 1.6. The method of claim 1 , wherein m is 3 and n is 2.7. The method of claim 1 , wherein m is 4 and n is 1.8. The method of claim 1 , wherein m and n are independently 1 or 2 claim 1 , provided that m and n taken together are 3.9. The method of claim 1 , wherein m and n are independently 1 claim 1 , 2 or 3 claim 1 , provided that m and n taken together are 4.10. The method of claim 1 , wherein p is 1 or 2 and Ris F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , (CH)NRRor (CH)OR.15. The method of claim 1 , wherein Ris (CRR)C-Caryl claim 1 , wherein said aryl is optionally substituted by F claim 1 , Cl claim 1 , Br or I.18. The method of claim 1 , wherein Ris O(CRR)C-Caryl claim 1 , wherein said aryl is optionally substituted by F claim 1 , Cl claim 1 , Br or I.19. The method of claim 18 , wherein t is 0 claim 18 , 1 claim 18 , 2 or 3; Ris independently selected from H claim 18 , OH claim 18 , O(C-Calkyl) or (CH)NRR claim 18 , or two Rare taken together to form oxo;{'sup': 11', '11, 'sub': 1', '3', '3', '6, 'and Ris independently selected from H or C-Calkyl, or two Rare taken together to form a C-Cheterocyclyl, optionally substituted by methyl or ethyl.'}21. The method of claim 1 , wherein Ris C-Calkyl or (CRR)C-Ccycloalkyl claim 1 , wherein said alkyl and cycloalkyl are optionally substituted by F.22. The method of claim 21 , wherein Ris methyl claim 21 , ethyl claim 21 , n-propyl claim 21 , iso-propyl claim 21 , cyclopropyl claim 21 , cyclobutyl claim 21 , cyclopentyl ...

Process for preparing varenicline, varenicline intermediates, and pharmaceutically acceptable salts thereof

Provided herein is an improved, convenient, commercially viable and environmentally friendly process for the preparation of varenicline or a pharmaceutically acceptable salt thereof comprising reacting 1-(4 ,5-diamino-10-aza-tricyclo[6.3.1.0 2.7 ]dodeca-2(7),3,5-trien-10-yl)-2,2,2-trifluoro-ethanone with chloroacetaldehyde in the presence of an oxygen source. Provided further herein is an improved and industrially advantageous process for the preparation of 1-(4,5-diamino-10-aza-tricyclo[6.3.1.0 2.7 ]dodeca-2(7),3,5-trien-10-yl)-2,2,2-trifluoro-ethanone.

GYRASE INHIBITORS

Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth. Compounds of Formula (I), are disclosed: Formula (I), wherein Y is N or CH; Z is N or CR; Ris H, a substituted or unsubstituted hydrocarbyl residue (1-3C) containing 0-2 heteroatoms selected from O, S and N, or is an inorganic residue; L is O, S, NR, or CRR; Ris H or Calkyl; Rand Rare each independently H or Calkyl; Ris H, a hydrocarbyl residue (1-40C) containing 0-10 heteroatoms selected from O, S and N optionally substituted with an inorganic residue; Ris H, an inorganic residue, or a hydrocarbyl residue (1-30C) containing 0-12 heteroatoms selected from O, S and N and containing 0-10 inorganic residues, wherein Rand Rtogether may join to form a fused ring; and Ris selected from the group consisting of H, Calkyl, Calkenyl, Calkynyl, halo Calkyl, halo Calkenyl, halo Calkynyl, Chydroxyalkyl, Calkyl chloride, Calkenyl chloride, and Calkynyl chloride; or a pharmaceutically-acceptable salt, ester, or prodrug thereof. 2. The compound of claim 1 , whereinY is N; and{'sub': '2', 'L is O, S, NH, or CH.'}3. The compound of claim 1 , wherein Z is CR claim 1 , wherein Ris selected from the group consisting of hydrogen claim 1 , halo claim 1 , unsubstituted Calkyl claim 1 , and Calkyl substituted with one or more substituents selected from the group consisting of ═O claim 1 , halo claim 1 , NH claim 1 , NHCH claim 1 , ≡N claim 1 , and Calkenyl claim 1 , wherein Rand Rtogether may join to form a fused ring.4. The compound of claim 1 , wherein Ris methyl claim 1 , C(O)CH claim 1 , C(O)NH claim 1 , CHOH claim 1 , CF claim 1 , CN claim 1 , CHF claim 1 , CHO claim 1 , acetyl claim 1 , Cl or Br.5. The compound of claim 1 , wherein Rcomprises at least one aryl or heteroaryl moiety.6. The compound of claim 1 , wherein the at least one aryl or a heteraryl moiety of Ris directly linked to L.7. The compound of claim 1 , wherein the at least one aryl or heteraryl moiety of Ris substituted ...

PYRIDO[3,4-B]INDOLES AND METHODS OF USE

This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. 2. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris unsubstituted C-Calkyl.3. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein Q is phenyl or substituted phenyl.4. The compound according to claim 1 , wherein any one or more of (i)-(xi) apply claim 1 , provided that provisions (iv) and (v) are not combined claim 1 , provisions (ii) and (xi) are not combined and (iii) and (xi) are not combined:(i) q and m are both 0;{'sup': '11', '(ii) Ris H;'}{'sup': '12', 'sub': 1', '8, '(iii) Ris an unsubstituted C-Calkyl;'}{'sup': 3a', '3b, '(iv) one of Rand Ris methyl, ethyl or phenyl and the other is H;'}{'sup': 3a', '3b, '(v) Rand Rare both H;'}{'sup': '1', 'sub': 1', '8, '(vi) Ris an unsubstituted C-Calkyl;'}{'sup': 9', '4', '4, 'sub': 1', '8, '(vii) Xis CRwhere Ris unsubstituted C-Calkyl or halo;'}{'sup': 7', '8', '10', '4', '4, '(viii) X, Xand Xare each CRwhere Ris H;'}{'sup': 2a', '2b, '(ix) Rand Rare both H;'}{'sup': 10a', '10b, '(x) Rand Rare both H; and'}{'sup': 11', '12, '(xi) Rand Rare taken together to form a bond.'}6. The compound of claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein any one or more of (i)-(viii) apply claim 5 , provided that if any of provisions (ii) claim 5 , (iii) or (iv) applies claim 5 , only one of (ii) claim 5 , (iii) and (iv) applies:(i) q is 0;{'sup': 8c', '8d', '8e', '8f, '(ii) Rand Rare both H and Rand Rare independently H, hydroxyl or methyl;'}{'sup': 8c', '8e', '8d', '8f, '(iii) Ris taken together with Rto form a bond and ...

6-(4-Hydroxy-phenyl)-3-alkyl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors

The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, 10. A pharmaceutical composition comprising the compound of .11. A method of treating a disease associated with diabetes or a diabetic complication claim 1 , comprising administering to a human in need thereof a therapeutically effective amount of the compound of .12. A method of preventing or treating a neuropathy claim 1 , a retinopathy claim 1 , an ischemia claim 1 , inflammation claim 1 , a central nervous system disorder claim 1 , a cardiovascular disease claim 1 , a dermatological disease claim 1 , an autoimmune disease claim 1 , or cancer claim 1 , the method comprising administering to a human in need thereof a therapeutically effective amount of the compound of .13. A method of treating a disease associated with the PKC receptor claim 1 , the method comprising administering to a human in need thereof a therapeutically effective amount of the compound of .14. A method of treating a disease associated with diabetes or a diabetic complication claim 9 , comprising administering to a human in need thereof a therapeutically effective amount of the pharmaceutical composition of .15. A method of preventing or treating a neuropathy claim 9 , a retinopathy claim 9 , an ischemia claim 9 , inflammation claim 9 , a central nervous system disorder claim 9 , a cardiovascular disease claim 9 , a dermatological disease claim 9 , an autoimmune disease claim 9 , or cancer claim 9 , the method comprising administering to a human in need thereof a therapeutically effective amount of the pharmaceutical composition of .16. A method of treating a disease associated with the PKC receptor claim 9 , the method comprising administering to a human in need thereof a therapeutically effective amount of the pharmaceutical composition of . Protein kinase C (PKC) comprises a family of several related isoenzymes that function as serine/threonine kinases. PKC plays an important role in intercellular and ...

ANTI-VIRAL TREATMENT AND ASSAY TO SCREENFOR ANTI-VIRAL AGENT

The present disclosure relates to novel compounds of formulas (1) through (19) and to a method for treating humans infected with a virus including various respiratory viruses such as members of the Paramyxoviridae family (respiratory syncytial virus (RSV), human metapneumovirus (HMPV), human parainfluenza virus (HPIV), measles virus, and mumps virus) with a compound of formulas (1) through (19). The present disclosure also relates to a cytopathic effect (CPE)-based assay that will assess virus-induced CPE for screening of compounds for treating viral diseases or inhibiting a virus. 2. The method of wherein the virus is a respiratory virus.3. The method of wherein the virus is selected from the group consisting of the families Paramyxoviridae claim 1 , human metapneumovirus claim 1 , human parainfluenza virus claim 1 , measles virus claim 1 , and mumps virus.4. The method of wherein the virus is respiratory syncytial virus.6. The method of wherein the virus is a respiratory virus.7. The method of wherein the virus is selected from the group consisting of the families Paramyxoviridae claim 5 , human metapneumovirus claim 5 , human parainfluenza virus claim 5 , measles virus claim 5 , and mumps virus.8. The method of wherein the virus is respiratory syncytial virus.9. A method for screening for compounds for use as an anti-viral agent against a virus which comprises obtaining frozen cells infected with said virus claim 5 , thawing said infected cells and mixing said infected cells with uninfected cells of the same type as the infected cells claim 5 , contacting the mixture of said infected cells and uninfected cells with a compound to be screened and determining the viability of said cells.10. The method of wherein the virus is a respiratory virus.11. The method of wherein the virus is selected from the group consisting of the families Paramyxoviridae claim 9 , human metapneumovirus claim 9 , human parainfluenza virus claim 9 , measles virus claim 9 , and mumps virus. ...

DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE AS MEDICAMENT

The present invention relates to a compound of following formula (I): 122-. (canceled)24. The compound according to claim 23 , wherein:{'sub': 1', '4, 'Yand/or Y═N,'}{'sub': '2', 'Y═CH or C—X—Ar, and'}{'sub': '3', 'Y=═C—W or C—X—Ar.'}25. The compound according to claim 23 , wherein X represents a divalent group selected from S claim 23 , S(O) claim 23 , S(O) claim 23 , NR claim 23 , CH claim 23 , CHS claim 23 , CHS(O) claim 23 , CHS(O) claim 23 , CHO claim 23 , CHNR claim 23 , NHS(O) claim 23 , SCH claim 23 , S(O)CH claim 23 , S(O)CH claim 23 , S(O)NH claim 23 , OCH claim 23 , NRCH claim 23 , CHCH claim 23 , CH═CH claim 23 , and C≡C claim 23 , wherein the first atom of these groups is bound to atom of chain —X—Ar.26. The compound according to claim 25 , wherein X represents a divalent group selected from S claim 25 , S(O) claim 25 , S(O) claim 25 , NR claim 25 , CH claim 25 , SCH claim 25 , S(O)CH claim 25 , S(O)CH claim 25 , S(O)NH claim 25 , CHCH claim 25 , C≡C claim 25 , OCH claim 25 , and NRCH claim 25 , wherein the first atom of these groups is bound to atom of chain —X—Ar.27. The compound according to claim 26 , wherein X represents a divalent group selected from S claim 26 , S(O) claim 26 , CH claim 26 , SCH claim 26 , S(O)CH claim 26 , S(O)NH claim 26 , CHCH claim 26 , and C≡C claim 26 , wherein the first atom of these groups is bound to atom of chain —X—Ar.28. The compound according to claim 23 , wherein Ar represents an aryl group optionally substituted by one or more groups selected from a halogen atom claim 23 , (C-C)alkyl claim 23 , (C-C)haloalkyl claim 23 , (C-C)haloalkoxy claim 23 , (C-C)halothioalkoxy claim 23 , CN claim 23 , NO claim 23 , OR claim 23 , SR claim 23 , NRR claim 23 , COR claim 23 , CONRR claim 23 , SOR claim 23 , SONRR claim 23 , COR claim 23 , NRCORand NRSOR; or a pyridine group.29. The compound according to claim 28 , wherein Ar represents a phenyl group optionally substituted by one or more groups selected from a halogen atom claim ...

NOVEL 2-PYRIDINECARBOXAMIDE DERIVATIVES

The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): 138-. (canceled)40. The compound according to claim 39 , or a pharmaceutically acceptable salt thereof claim 39 , wherein D is S.41. The compound according to claim 39 , or a pharmaceutically acceptable salt thereof claim 39 , wherein both of Rand Rare hydrogen atoms.42. The compound according to claim 39 , or a pharmaceutically acceptable salt thereof claim 39 , wherein Xis selected from the group consisting of: a nitrogen atom claim 39 , sulfur atom claim 39 , oxygen atom claim 39 , —CH— claim 39 , —N—CH— claim 39 , —S—CH— claim 39 , —O—CH— claim 39 , —CH—N— claim 39 , —CH—O— claim 39 , and —CH—S—.43. The compound according to claim 39 , or a pharmaceutically acceptable salt thereof claim 39 , wherein the substituent on ring A is a hydrogen atom claim 39 , lower alkyl group claim 39 , lower alkoxy group claim 39 , hydroxy group claim 39 , or hydroxy lower alkyl group (the hydrogen atom of the hydroxy group of the hydroxy lower alkyl group may further be substituted by a lower alkyl group).44. The compound of claim 39 , or a pharmaceutically acceptable salt thereof claim 39 , wherein the substituent on ring B is a hydrogen atom claim 39 , lower alkyl group claim 39 , halogen atom claim 39 , hydroxyalkyl group claim 39 , aminoalkyl group claim 39 , or alkanoyl group.45. The compound according to claim 39 , or a pharmaceutically acceptable salt thereof claim 39 , wherein Rrepresents a pyridyl group.46. The compound according to claim 39 , or a pharmaceutically acceptable salt thereof claim 39 , wherein the substituent in Ris hydrogen atom claim 39 , hydroxyalkyl group claim 39 , lower alkyl group claim 39 , lower alkoxy group claim 39 , carbamoyl group claim 39 , alkylcarbamoyl group claim 39 , dialkylcarbamoyl group claim 39 , cyano group claim 39 , trifluoromethyl group claim 39 , ...

Electron donating polymer and organic solar cell including the same

A polymer, and an organic solar cell including the polymer, include a repeating unit A represented by Chemical Formula 1, and a repeating unit B represented by Chemical Formula 2.

Semiconductor device and capacitor

The present invention relates to a semiconductor device including nanodots and a capacitor. A semiconductor device includes a channel layer, a tunnel insulating layer formed on the channel layer, a memory layer formed on the tunnel insulating layer and including first nanodots, a charge blocking layer formed on the memory layer, a gate electrode conductive layer formed on the charge blocking layer, and a buffer layer located, at least one of, inside the tunnel insulating layer, inside the charge blocking layer, at an interface between the tunnel insulating layer and the memory layer and at the interface between the charge blocking layer and the memory layer, wherein the buffer layer includes second nanodots.

Antimicrobial Compounds and Methods of Making and Using the Same

The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals. 3. The compound according to claim 1 , wherein Z is —NRCONR—; or a pharmaceutically acceptable salt claim 1 , ester claim 1 , tautomer claim 1 , or prodrug thereof.5. The compound according claim 1 , wherein (a) a 3-14 member saturated, unsaturated, or aromatic heterocycle containing one or more heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur,', '(b) a 3-14 member saturated, unsaturated, or aromatic carbocycle, and', '(c) a single bond,, 'A is selected from'}{'sup': '5', 'wherein (a) or (b) is optionally substituted with one or more Rgroups;'}{'sub': 1-8', '2-8', '2-8, 'claim-text': [{'sub': p', 'p', 'p, 'sup': 6', '6', '6', '6', '6, 'i) 0-4 carbon atoms in any of (a)-(c) immediately above optionally is replaced by a moiety selected from the group consisting of —O—, —S(O)—, —NR—, —(C═O)—, —C(═NR)—, —S(O)NR—, and —NRS(O)NR—,'}, {'sup': '5', 'ii) any of (a)-(c) immediately above optionally is substituted with one or more Rgroups, and'}, {'sub': 1', '8, 'sup': '5', 'iii) any of (a)-(c) immediately above optionally is substituted with —(C-Calkyl)-Rgroups, and'}], 'B is selected from (a) —(Calkyl)-, (b) —(Calkenyl)-, (c) —(Calkynyl)-, (d) a single bond, wherein'}{'sub': 2', '2, 'C is selected from (a) NH, (b) —NHC(═NH)NHand (c) hydrogen;'}or a pharmaceutically acceptable salt, ester, tautomer, or prodrug thereof.6. The compound according to claim 1 , whereinA is selected from azepanyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, phenyl, pyridinyl, cyclohexenyl, cyclohexadienyl, dihydropyridyl, furanyl, tetrahydrofuranyl, tetrahydropyridyl, azetidinyl, pyrrolidinyl, piperidinyl, and piperidenyl;{'sup': '5', 'wherein any of A immediately above optionally is substituted with one or more Rgroups;'} ...

COMPOUNDS FOR ELECTRONIC DEVICES

The present invention relates to compounds of the formula (I), to the use of compounds of the formula (I) in electronic devices, and to electronic devices comprising one or more compounds of the formula (I). The invention furthermore relates to preparation processes for compounds of the formula (I) and to formulations comprising one or more compounds of the formula (I). 114-. (canceled)16. The compound according to claim 15 , wherein X claim 15 , Xand Xare on each occurrence claim 15 , identically or differently claim 15 , from C(R) claim 15 , C═O claim 15 , NR claim 15 , O or S.17. The compound according to claim 15 , wherein one of the two groups Xand Xis equal to CRand the other is equal to N.18. The compound according to claim 15 , wherein all three groups X claim 15 , Xand Xdo not simultaneously represent O.19. The compound according to claim 15 , wherein all three groups X claim 15 , Xand Xdo not simultaneously represent S.21. The compound according to claim 15 , wherein not more than three groups Z per aromatic ring are equal to N and the remaining groups Z are equal to CR.23. An oligomer claim 15 , polymer or dendrimer comprising one or more compounds according to claim 15 , where the bond(s) to the polymer claim 15 , oligomer or dendrimer is optionally localised at any positions in formula (I) substituted by a radical Ror R.24. A formulation comprising at least one compound according to and at least one solvent.25. A formulation comprising at least one polymer claim 23 , oligomer or dendrimer according to and at least one solvent.26. An electronic device which comprises the compound according to .27. An electronic device which comprises the polymer claim 23 , oligomer or dendrimer according to .28. The electronic device according to claim 26 , wherein the device is an organic electroluminescent device (OLED).29. An emitting layer of an electronic device which comprises the compound according to as matrix material in combination with one or more further ...

IMIDAZOQUINOLINE COMPOUNDS

The invention provides novel compositions comprising imidazoquinoline compounds. Also provided are methods of administering the compositions in an effective amount to enhance the immune response of a subject. Further provided are novel compositions and methods of administering the compositions in combination with (an)other agent(s). 2. The compound of claim 1 , wherein Rand Rare each H.3. The compound of claim 2 , wherein Ris —NRR.4. The compound of claim 2 , wherein Ris —S(O)R.5. The compound of claim 2 , wherein Ris —C(O)NRR.6. The compound of claim 2 , wherein Ris —(CH)CH═CH(CH)R.7. The compound of claim 2 , wherein Ris —(CH)C≡C(CH)R.8. The compound of claim 2 , wherein Ris Calkyl.9. The compound of claim 3 , wherein Rand Rwithin Rare independently H claim 3 , Calkyl or —(CH)CH═CH(CH)R.10. The compound of claim 4 , wherein Ris —SR claim 4 , and the Rof the —SRis Calkyl.11. The compound of claim 8 , wherein Ris isobutyl.12. The compound of claim 10 , wherein the Calkyl within Ris selected from methyl claim 10 , ethyl claim 10 , n-butyl claim 10 , or n-pentyl.13. The compound of claim 9 , wherein m is 1 claim 9 , n is 0 claim 9 , and Ris H.14. The compound of claim 2 , wherein Ris —N(CH)CHCHCH.15. The compound of claim 2 , wherein p is 0.16. The compound of claim 2 , wherein Ris substituted Calkyl.17. The compound of claim 16 , wherein Ris —CHC(CH)(OH).18. The compound of claim 2 , wherein Ris —S-cyclopropyl claim 2 , —S—CHCH(CH)or —S—CHCHCH.19. The compound of claim 1 , wherein Ris —S—Ccycloalkyl.20. The compound of claim 1 , wherein Rand Rare taken together to form a substituted or unsubstituted heterocyclyl group.21. The compound of claim 20 , wherein said heterocyclyl group is selected from piperidinyl claim 20 , pyrrolidinyl claim 20 , azetidinyl claim 20 , or aziridinyl.24. A pharmaceutical composition claim 2 , comprising: the compound of and a pharmaceutically acceptable excipient. This application is a Continuation of U.S. patent application Ser. No. 13/ ...

Pyridone derivative having integrase inhibitory activity

An object of the present invention is to provide a novel integrase inhibitor. The present invention relates to a novel compound having an antiviral effect, more specifically, a pyridone derivative having HIV integrase inhibitory activity, and a medicament containing the same, in particular, an anti-HIV agent. The compound of the present invention has integrase inhibitory activity and/or cell proliferation inhibitory activity against viruses, in particular, HIV and drug-resistant strains thereof. Thus, the compound is useful in preventing or treating various diseases, viral infections (for example, AIDS), and the like in which integrase participates.

Pyrazolopyridine, Pyrazolopyrazine, Pyrazolopyrimidine, Pyrazolothiophene and Pyrazolothiazole Compounds as MGLUR4 Allosteric Potentiators, Compositions, and Methods of Treating Neurological Dysfunction

Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction. 2. The method of claim 1 , wherein the mammal is a human.3. The method of claim 1 , wherein the dysfunction is Parkinson's disease.4. The method of claim 1 , wherein the dysfunction is schizophrenia claim 1 , psychosis claim 1 , “schizophrenia-spectrum” disorder claim 1 , depression claim 1 , bipolar disorder claim 1 , cognitive disorder claim 1 , delirium claim 1 , amnestic disorder claim 1 , anxiety disorder claim 1 , attention disorder claim 1 , obesity claim 1 , eating disorder claim 1 , or NMDA receptor-related disorder.5. The method of claim 1 , wherein the dysfunction is Parkinson's disease; anxiety; motor effects after alcohol consumption; neurogenic fate commitment and neuronal survival; epilepsy; or certain cancers claim 1 , for example claim 1 , medulloblastoma claim 1 , inflammation (for example claim 1 , multiple sclerosis) and metabolic disorders (for example claim 1 , diabetes) and taste enhancing associated with glutamatergic dysfunction and diseases in which mGluR4 receptor is involved.6. The method of claim 1 , wherein the mammal has been diagnosed with the dysfunction prior to the administering step.7. The method of claim 1 , further comprising the step of identifying a mammal having a need for treatment of the dysfunction.825-. (canceled)27. The compound of claim 25 , wherein n is 2.28. The compound of claim 25 , wherein X is N claim 25 , S claim 25 , or CR.29. The compound of claim 25 , wherein Y is N claim 25 , or NH.30. The compound of claim 25 , wherein ...

CARBOLINE CARBOXAMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS

Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, formula (I) are useful as kinase modulators, including Btk modulation. 115-. (canceled)20. The compound according to claim 16 , wherein{'sup': 1', '2', '2', '2', '2', '2', '2', '11', '2', '2', '2', '2', '11', '2', '11', '11', '2', '11', '2', '11', '2', '11', '2, 'sub': 2', 'r', '2', '2, 'Dand Dare independently R, —(CH)R, —OR, —C(═O)R, —C(═O)OR, —C(═O)NRR, —S(O)R, —S(O)R, —SR, —NRC(O)R, —NRC(O)NRR, —NRC(═O)OR, —NRS(═O)R, or —NRR;'}{'sup': 2', '2a', '2a', '2a', '2a', '2a', '2a, 'sub': 1-6', '2-6', '3-10', '6-10, 'Ris hydrogen, Calkyl substituted with 0-3 R, Calkenyl substituted with 0-3 R, Ccycloalkyl substituted with 0-4 R, —Caryl substituted with 0-4 R, a 5-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with 0-4 R, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with 0-4 R;'}{'sup': 2a', 'b', 'b', 'b', 'b', 'b', '11', '11', '11', '11', 'b', 'c', 'b', 'c', 'b', '11', '11', '11', '11', 'b', 'c', 'c', 'c', 'a', 'a', 'a, 'sub': 3', '3', '2', '2', 'p', 'p', '2', '1-6', '2', 'r', '2', 'r', 'p, 'Ris hydrogen, ═O, F, Cl, Br, OCF, CF, CHF, CN, NO, OR, SR, —C(O)R, —C(O)OR, —OC(O)R, —NRR, —C(O)NRR, —NRC(O)R, —NRC(O)OR, —NRC(O)NRR, —S(O)NRR, —NRS(O)R, —S(O)R, —S(O)R, Calkyl substituted with 0-2 R, —(CH)-3-14 membered carbocycle substituted with 0-1 R, wherein the carbocycle is cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; or —(CH)-5-7 membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, O, and S(O)substituted with 0-2 R; and'}r is 0, 1, or 2.26. The compound according to claim 25 , wherein{'sup': a', 'b', 'b', 'b', 'b', 'b', '11', '11', '11', '11', 'b', 'c', 'b', 'c', 'b', '11', '11', '11', '11', 'b', 'c', 'c', 'c, 'sub': 3', '3', '2', '2', 'p', 'p', '2', '1-6', '1-6', '2', 'r', '2', 'r', 'p, 'Ris hydrogen, F, Cl, Br, OCF, CF, CHF ...

CGRP Receptor Antagonists

The disclosure generally relates to the novel compounds of formula I, including pharmaceutically acceptable salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD). 6. A compound of where Ris N-piperidinyl and is 4-substituted.8. A compound of where Ris hydrogen claim 1 , Ris hydrogen claim 1 , Ris hydrogen claim 1 , Ris hydrogen claim 1 , Ris hydrogen claim 1 , Ris hydroxy claim 1 , azido claim 1 , or amino claim 1 , and Ris hydrogen; or where Ris hydrogen claim 1 , Ris hydrogen claim 1 , Ris hydrogen claim 1 , Ris hydrogen claim 1 , Ris hydrogen or hydroxy claim 1 , and Rand Rtaken together is oxo; or where Ris hydrogen claim 1 , Ris hydrogen claim 1 , Ris hydrogen claim 1 , Ris hydrogen claim 1 , Ris hydroxy claim 1 , Ris hydrogen or hydroxy claim 1 , and Ris hydrogen; or where Ris hydroxy claim 1 , Ris hydrogen claim 1 , Ris hydrogen claim 1 , Ris hydrogen claim 1 , Ris hydrogen claim 1 , Ris hydrogen claim 1 , and Ris hydrogen.9. A compound of where Aris phenyl substituted with 2 halo substituents.10. A compound of where Aris 2 claim 9 ,3-difluorophenyl.11. A compound of where X is O.12. A compound of selected from the group consisting of(5R,8S,9S)-9-(tert-butoxycarbonylamino)-8-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyrazin-5-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate;(5R,8S,9S)-9-amino-8-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyrazin-5-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate;N-((5R,8S,9S)-9-amino-8-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyrazin-5-yl)-4-(2-oxo-2, ...

TRIAZOLOPYRIDINE COMPOUND, AND ACTION THEREOF AS PROLYL HYDROXYLASE INHIBITOR OR ERYTHROPOIETIN PRODUCTION-INDUCING AGENT

The present invention provides a triazolopyridine compound having a prolyl hydroxylase inhibitory action and an erythropoietin production-inducing ability. The present invention relates to a compound represented by the following formula [I]: 2. (canceled)6. The compound according to claim 1 , wherein both Rand Rare hydrogen atoms claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof7. The compound according to claim 1 , wherein Ris a hydrogen atom claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof.8. The compound according to claim 1 , wherein Ris a hydrogen atom claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof.9. The compound according to claim 1 , wherein{'sup': '2', 'Ris'}{'sub': '1-10', '(1) a Calkyl group,'}{'sub': '6-14', '(2) a Caryl group optionally substituted by the same or different 1 to 5 substituents selected from the above-mentioned group B,'}{'sub': 6-14', '1-6', '6-14, '(3) a Caryl-Calkyl group (wherein Caryl is optionally substituted by the same or different 1 to 5 substituents selected from the above-mentioned group B), or'}{'sub': 3-8', '1-6', '3-8, '(4) a Ccycloalkyl-Calkyl group (wherein Ccycloalkyl is optionally substituted by the same or different 1 to 5 substituents selected from the above-mentioned group B), or a pharmaceutically acceptable salt thereof, or a solvate thereof.'}1013.-. (canceled)1525.-. (canceled)26. A pharmaceutical composition comprising the compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof claim 1 , and a pharmaceutically acceptable carrier.2734.-. (canceled)35. A method of inhibiting prolyl hydroxylase claim 1 , comprising administering an effective amount of the compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof to a mammal.36. A method of inducing erythropoietin production claim 1 , comprising ...

DEUTERATED HIV ATTACHMENT INHIBITORS

Deuterated piperazine and piperidine HIV attachment inhibitor compounds are set forth. The present invention provides compounds of Formula I, the pharmaceutically acceptable salts and/or solvates (e.g., hydrates) thereof, their pharmaceutical formulations, and their use in patients suffering from or susceptible to a virus such as HIV. The compounds of Formula I, their pharmaceutically acceptable salts and/or solvates are effective antiviral agents, particularly as inhibitors of HIV. They are useful for the treatment of HIV and AIDS. This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. In particular, the invention herein is directed to deuterated HIV attachment inhibitors that possess unique antiviral activity. More particularly, the present invention relates to deuterated piperazine and piperidine compounds useful for the treatment of HIV and AIDS.HIV-1 (human immunodeficiency virus-1) infection remains a major medical problem, with an estimated 45 million people infected worldwide at the end of 2007. The number of cases of HIV and AIDS (acquired immunodeficiency syndrome) has risen rapidly. In 2005, approximately 5.0 million new infections were reported, and 3.1 million people died from AIDS. Currently available drugs for the treatment of HIV include nucleoside reverse transcriptase (RT) inhibitors or approved single pill combinations: zidovudine (or AZT or RETROVIR®), didanosine (or VIDEX®), stavudine (or ZERIT®), lamivudine (or 3TC or EPIVIR®), zalcitabine (or DDC or HIVID®), abacavir succinate (or ZIAGEN®), tenofovir disoproxil fumarate salt (or VIREAD®), emtricitabine (or FTC-EMTRIVA®), COMBIVIR® (contains −3TC plus AZT), TRIZIVIR® (contains abacavir, lamivudine, and zidovudine), Epzicom (contains abacavir and lamivudine), TRUVADA® (contains VIREAD® and EMTRIVA®); non-nucleoside reverse transcriptase inhibitors: nevirapine (or VIRAMUNE®), delavirdine (or RESCRIPTOR®) and efavirenz (or ...

Light-emitting device and photovoltaic cell, and method for manufacturing the same

Provided are a light-emitting device and a photovoltaic cell having excellent characteristics. A light-emitting device ( 10 ) includes a cathode ( 34 ), an anode ( 32 ), a light-emitting layer ( 50 ) interposed between the cathode ( 34 ) and the anode ( 32 ), and an electron injection layer ( 44 ) provided between the cathode ( 34 ) and the light-emitting layer ( 50 ) and connected to the cathode ( 34 ), in which at least one of the anode ( 32 ) and the cathode ( 34 ) contains a conductive material having an aspect ratio of 1.5 or more, and the electron injection layer ( 44 ) contains an organic compound having at least one of an ionic group and a polar group.

HIGHLY PURE VARENICLINE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF SUBSTANTIALLY FREE OF METHYLVARENICLINE IMPURITY

Provided herein is an impurity of varenicline, methylvarenicline, 6-methyl-5,8,14-triazatetracyclo[10.3.1.0,0]hexadeca-2(11),3,5,7,9-pentaene, and a process for the preparation and isolation thereof. Provided further herein is a highly pure varenicline or a pharmaceutically acceptable salt thereof substantially free of methylvarenicline impurity, processes for the preparation thereof, and pharmaceutical compositions comprising highly pure varenicline or a pharmaceutically acceptable salt thereof substantially free of methylvarenicline impurity. 1. Varenicline or a pharmaceutically acceptable salt thereof comprising a 6-methyl-5 ,8 ,14-triazatetracyclo[10.3.1.0 ,0]hexadeca-2(11) ,3 ,5 ,7 ,9-pentaene impurity (methylvarenicline impurity) in an amount of less than 0.15 area-% as measured by HPLC.2. Varenicline of claim 1 , comprising the methylvarenicline impurity in an amount of about 0.01 area-% to about 0.1 area-%; wherein the varenicline or a pharmaceutically acceptable salt thereof has a purity of about 99.5% to about 99.99% as measured by HPLC; and wherein the pharmaceutically acceptable salt of varenicline is a hydrochloride salt claim 1 , a hydrobromide salt claim 1 , a sulphate salt claim 1 , a phosphate salt claim 1 , a tartrate salt claim 1 , a fumarate salt claim 1 , a maleate salt claim 1 , an oxalate salt claim 1 , an acetate salt claim 1 , a propionate salt claim 1 , a succinate salt claim 1 , a mandelate salt claim 1 , a mesylate salt claim 1 , a besylate salt claim 1 , or a tosylate salt.3. Varenicline of claim 2 , comprising the methylvarenicline impurity in an amount of about 0.01 area-% to about 0.05 area-%; and wherein the pharmaceutically acceptable salt of varenicline is a tartrate salt.4. Varenicline of claim 1 , having a non-detectable amount of the methylvarenicline impurity as measured by HPLC.6. The process of claim 5 , wherein the reaction in step-(a) is carried out in the presence of a solvent selected from the group consisting of water ...

SYSTEMS AND METHODS FOR HIGH-THROUGHPUT DETECTION OF AN ANALYTE IN A SAMPLE

Provided are high-throughput detection systems. The systems include a magnetic sensor device, a magnetic field source and a reservoir plate that includes a plurality of fluid reservoirs. The magnetic sensor device includes a support with two or more elongated regions each having a magnetic sensor array disposed at a distal end. Also provided are methods in which the subject high-throughput detection systems find use. 119-. (canceled)20. A reservoir plate comprising:an addressable array of fluid reservoirs comprising two or more rows of fluid reservoirs and two or more columns of fluid reservoirs, wherein the fluid reservoirs in each row have the same volume and at least two fluid reservoirs in separate columns have different volumes.21. The reservoir plate of claim 20 , wherein the array of fluid reservoirs comprises 24 or more fluid reservoirs.22. The reservoir plate of claim 20 , wherein each fluid reservoir has a volume of 1 mL or less.23. The reservoir plate of claim 20 , wherein the reservoir plate is configured to operatively couple to a reservoir plate actuator configured to move the reservoir plate along an axis of movement.24. The reservoir plate of claim 23 , further comprising an alignment guide configured to align a longitudinal axis of the reservoir plate parallel to the axis of movement.25. A method for determining whether an analyte is present in a sample claim 23 , the method comprising:(a) contacting a magnetic sensor device with a set of samples contained in a set of fluid reservoirs to generate a signal, the magnetic sensor device comprising a support with two or more elongated regions each having a magnetic sensor array disposed at a distal end; and(b) determining whether the analyte is present in each sample based on the signal.26. The method of claim 25 , wherein each magnetic sensor array comprises one or more magnetic sensors having an analyte-specific probe bound to a surface of the magnetic sensor.27. The method of claim 25 , wherein the ...

METHODS OF USING (+)-1,4-DIHYDRO-7-[(3S,4S)-3-METHOXY-4-(METHYLAMINO)-1-PYRROLIDINYL]-4-OXO-1-(2-THIAZOLYL)-1,8-NAPHTHYRIDINE-3-CARBOXYLIC ACID FOR TREATMENT OF ANTECEDENT HEMATOLOGIC DISORDERS

Methods of treating, preventing or managing antecedent hematologic disorders, such as myelodysplastic syndrome, including chronic myelomonocytic leukemia are disclosed. The methods encompass the administration of SNS-595. Also provided are methods of treatment using this compound with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy. In certain embodiments, the method of treatment comprise administering SNS-595 in combination with cytarabine. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods are also disclosed. 1. A method of treating an antecedent hematological disorder comprising administering to a mammal in need thereof a therapeutically effective amount of an enantiomerically pure (+)-1 ,4-dihydro-7-[(3S ,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1 ,8-naphthyridine-3-carboxylic acid.2. The method of claim 1 , wherein the antecedent hematological disorder is a myelodysplastic syndrome.3. The method of claim 1 , wherein the myelodysplastic syndrome is characterized by ineffective blood cell production claim 1 , progressive cytopenia claim 1 , risk of progression to acute leukemia or cellular marrow with impaired morphology.4. The method of claim 2 , wherein the myelodysplastic syndrome is selected from group consisting of refractory anemia claim 2 , refractory anemia with ringed sideroblasts claim 2 , refractory anemia with excess blasts claim 2 , refractory anemia with excess blasts in transformation claim 2 , and chronic myelomonocytic leukemia.5. The method of claim 2 , wherein the myelodysplastic syndrome is chronic myelomonocytic leukemia.6. The method of claim 5 , wherein the chronic myelomonocytic leukemia is relapsed claim 5 , refractory claim 5 , or resistant to conventional therapy.7. The method of claim 1 , further comprising administering a therapeutically effective amount of a second active agent.8. The method of claim 7 , wherein the second active ...

SUBSTITUTED 5-(PYRAZIN-2-YL)-1H-PYRAZOLO [3, 4-B] PYRIDINE AND PYRAZOLO [3, 4-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS

Substituted 5-(pyrazin-2-yl)-1H-pyrazolo[3,4-b]pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson's disease, Alzheimer's disease, Down's Syndrome, Huntington's disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated therewith using compounds and pharmaceutical compositions including the compounds. 4. The invention of wherein R claim 1 , Rand Rat each occurrence is independently —H claim 1 , optionally substituted Calkyl claim 1 , optionally substituted cycloalkyl claim 1 , optionally substituted heterocycloalkyl claim 1 , optionally substituted aryl or optionally substituted heteroaryl.5. The invention of wherein R claim 1 , Rand Rare each independently —NHCOCalkyl claim 1 , —NHCOcycloalkyl claim 1 , —NHCOheterocycloalkyl claim 1 , —CONHCalkyl claim 1 , —CONHcycloalkyl claim 1 , or —CONHheterocycloalkyl.6. The invention of wherein R claim 1 , Rand Rare each independently directly substituted by —H claim 1 , —F claim 1 , —Cl claim 1 , —OCF claim 1 , CF claim 1 , —CH claim 1 , —OCHFor —OCH claim 1 , wherein at least one of RRand Ris not hydrogen.10. The invention of wherein ZRis directly substituted by —H claim 9 , —F claim 9 , —Cl claim 9 , —OCF claim 9 , CF claim 9 , —CH claim 9 , —OCHFor —OCH claim 9 , wherein at least one of Ris not hydrogen;15. A compound according to which is a protein kinase inhibitor.16. A compound according to wherein the compound is an inhibitor of a protein kinase selected from the group consisting of ...

New Enzyme Inhibitor Compounds

Disclosed are compounds which inhibit SSAO enzyme activity. Also disclosed are pharmaceutical compositions comprising these compounds and the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumour growth. 2. A compound as claimed in in which X has the formula 1 and wherein R , R , Y , Z and W are as defined in .3. A compound as claimed in in which X has the formula 2 and wherein R , R , Y , Z and W are as defined in .4. A compound as claimed in in which X has the formula 3 and wherein R , R , Y , and Z are as defined in .5. A compound as claimed in in which X has the formula 4 and wherein R , R , Y , and W are as defined in .6. A compound as claimed in in which X has the formula 5 and wherein R , R , and Y are as defined in .7. A compound as claimed in in which X has the formula 6 and wherein R , R , Y , and Z are as defined in .8. A compound as claimed in wherein Ris —B-Q-[R].9. A compound as claimed in wherein Ris —B—R.10. A compound as claimed in wherein B is a bond claim 1 , —C(O)— or methylene.11. A compound as claimed in wherein B is a bond.12. A compound as claimed in wherein W is hydrogen.13. A compound as claimed in wherein Y is H claim 1 , OH claim 1 , or NH.14. A compound as claimed in wherein Y is hydrogen15. A compound as claimed in wherein Ris optionally substituted with one or more substituents selected from halogen claim 1 , cyano claim 1 , hydroxyl claim 1 , C-alkyl claim 1 , halo-C-alkyl claim 1 , Calkoxy-Calkyl claim 1 , hydroxy-C-alkyl claim 1 , cyano-C-alkyl claim 1 , amino-C-alkyl claim 1 , C-alkylamino-C-alkyl claim 1 , di(C-alkyl)amino-C-alkyl claim 1 , —NRR.16. A compound as claimed in wherein Ris heteroaryl optionally substituted with one or more substituents selected from as fluoro claim 1 , chloro claim 1 , and C-alkyl.17. A compound as claimed in wherein Ris pyridine-2-yl claim 16 , pyridine ...

IP RECEPTOR AGONIST HETEROCYCLIC COMPOUNDS

The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed. Examples of compounds of the invention include the compounds according to Formula Ia, or a pharmaceutically acceptable salt thereof, and the compounds of the examples. 2. The compound according to claim 1 , wherein{'sup': '1', 'Ris X—Y;'}{'sup': '2', 'sub': 1', '8, 'Ris H, or C-Calkyl optionally substituted by one or more halogen atoms;'}{'sup': '2a', 'Ris hydrogen;'}{'sub': 1', '6', '1', '4, 'X is C-Calkylene optionally substituted by hydroxy, halogens or C-Calkyl;'}{'sup': x', 'x', 'x, 'sub': q', '1', '4, 'Y is —C(O)OH, —C(O)ORor —CONH—S(O)—R, wherein Ris —C-Calkyl;'}q is 2;{'sup': '3', 'sub': 1', '4', '3', '7', '1', '4, 'Ris H, C-Calkoxy, OH, CN, halogen, C-Ccycloalkyl or C-Calkyl optionally substituted by one or more halogen atoms;'}{'sup': '4', 'sub': 1', '4', '3', '7', '1', '4, 'Ris H, C-Calkoxy, OH, CN, halogen, C-Ccycloalkyl or C-Calkyl optionally substituted by one or more halogen atoms.'}3. The compound according to claim 1 , wherein{'sup': 1', '7, 'sub': 2', 'm', '2', 'm', '2', 'n, 'Ris X—Y, wherein X—Y is —(CH)—C(O)OR″, or —(CH)—R—(CH)—C(O)OR″;'}{'sup': '2', 'sub': 1', '4, 'Ris H, C-Calkyl optionally substituted by one or more halogen atoms;'}{'sup': '2a', 'Ris hydrogen;'}{'sup': '3', 'sub': 1', '4', '3', '7', '1', '4, 'Ris H, C-Calkoxy, OH, CN, halogen, C-Ccycloalkyl or C-Calkyl optionally substituted by one or more halogen atoms;'}{'sup': '4', 'sub': 1', '4', '3', '7', '1', '4, 'Ris H, C-Calkoxy, OH, CN, halogen, C-Ccycloalkyl or C-Calkyl optionally substituted by one or more halogen atoms;'}{'sub': 1', '4, 'R″ is H or C-Calkyl optionally substituted by one or more halogen atoms;'}m is 1 ...

PROCESSES AND INTERMEDIATES FOR PRODUCING AZAINDOLES

The present invention relates to processes and intermediates for the preparation of compounds useful as inhibitors of Janus kinases (JAK). 2. The process of claim 1 , wherein the organic solvent of step i) is an aprotic solvent.3. The process of claim 2 , wherein the aprotic solvent is acetonitrile claim 2 , toluene claim 2 , N claim 2 ,N-dimethylformamide claim 2 , N claim 2 ,N-dimethylacetamide claim 2 , acetone claim 2 , methyl tert-butyl ether claim 2 , or any combination thereof.4. The process of claim 1 , wherein the organic solvent of step i) is a protic solvent.5. The process of claim 4 , wherein the protic solvent is an alcohol selected from methanol claim 4 , propanol claim 4 , isopropanol claim 4 , butanol claim 4 , tert-butanol claim 4 , or any combination thereof.6. The process of claim 1 , wherein the base of step i) is an inorganic base.7. The process of claim 6 , wherein the inorganic base comprises tripotassium phosphate claim 6 , dipotassium hydrogen phosphate claim 6 , dipotassium carbonate claim 6 , disodium carbonate claim 6 , trisodium phosphate claim 6 , disodium hydrogen phosphate claim 6 , or any combination thereof.8. The process of claim 7 , wherein the inorganic base comprises an alkali metal hydroxide.9. The process of claim 8 , wherein the alkali metal hydroxide comprises NaOH claim 8 , KOH claim 8 , or any combination thereof.10. The process of claim 1 , wherein the transition metal catalyst of step i) is a palladium catalyst.11. The process of claim 10 , wherein the palladium catalyst of step i) comprises palladium(II)acetate claim 10 , tetrakis(triphenylphosphine)palladium(0) claim 10 , tris(dibenzylideneacetone)dipalladium(0) claim 10 , or any combination thereof.13. The process of claim 1 , wherein the reaction of step i) is performed at a temperature between about 50° C. and about 110° C.14. The process of claim 13 , wherein the reaction of step i) is performed at a temperature between about 60° C. and about 95° C.15. The process ...

METHODS OF TREATING HIV INFECTION: INHIBITION OF DNA DEPENDENT PROTEIN KINASE

Methods of treating HIV-1 infection/AIDS in a patient infected with an HIV-1 virus comprising providing a DNA-PK inhibitor to the patient are provided herein. In one embodiment the DNA-PK inhibitor is compound of the Formula I 1. A method of treating HIV-1 infection in a patient infected with an HIV-1 virus comprising providing a therapeutically effective amount of a DNA-PK inhibitor to the patient.5. The method of claim 2 , wherein Ais N claim 2 , Ais O claim 2 , and Ais O.6. The method of claim 2 , wherein Ris hydrogen claim 2 , halogen claim 2 , C-Calkyl claim 2 , or C-Calkoxy.7. The method of wherein Ais CR claim 2 , Ais CR claim 2 , and Ais CR.8. The method of claim 7 , wherein Rand Rare independently chosen from hydrogen claim 7 , halogen claim 7 , C-Calkyl claim 7 , and C-Calkoxy.9. The method of claim 5 , wherein Rand Rare joined to form an optionally substituted phenyl ring.10. The method of claim 9 , wherein Rand Rare joined to form a phenyl ring that is unsubstituted or substituted with 1 claim 9 , 2 claim 9 , or 3 substituents independently chosen from hydrogen claim 9 , halogen claim 9 , hydroxyl claim 9 , cyano claim 9 , amino claim 9 , thiol claim 9 , C-Calkyl claim 9 , C-Calkoxy claim 9 , mono- or di-C-Calkylamino claim 9 , C-Chaloalkyl claim 9 , and C-Chaloalkoxy.11. The method of claim 9 , wherein Rand Rare joined to form an unsubstituted phenyl ring.13. The method of claim 12 , wherein Xis S.15. The method of claim 1 , wherein the DNA-PK inhibitor is provided together with instructions for treating an HIV-1 infection.16. A method of inhibiting CD4 cell death in a patient infected with HIV-1 comprisingPerforming a count of CD4 cells in the patient's blood; andAdministering an effective amount of a DNA-PK inhibitor to the patient. This application claims priority from U.S. Provisional Patent application No. 61/329,775, filed Apr. 30, 2010, which is hereby incorporated by reference in its entirety.This invention was made in part with government ...

Naphthridine derivatives as PI3K inhibitors for the treatment of cancer and immune-inflammatory disease

Compounds of formulae (I) and (II): or a pharmaceutically acceptable salt thereof, wherein: Ris a nitrogen-containing 5 to 7-membered heteroaryl or heterocycle; Rand Rare each independently (LQ)Y, are described. The compounds are PI3K inhibitors and are useful for the treatment of cancer and immune-inflammatory diseases. 4. The compound according to claim 1 , wherein Ris H.5. The compound according to claim 1 , wherein Ris substituted aryl.6. The compound according to claim 5 , wherein Ris aryl substituted with at least one C-Chydroxyalkyl.7. The compound according to claim 1 , wherein Ris aryl substituted with at least one (NR)group.8. The compound according to claim 1 , wherein Ris (C-Calkylene)-NR-aryl.10. A pharmaceutical composition comprising a compound according to claim 1 , and a pharmaceutically acceptable excipient.11. A method for treating cancer claim 1 , an immune disorder or an inflammatory disorder claim 1 , wherein said method comprises administering claim 1 , to a subject in need of such a treatment claim 1 , a compound according to .12. (canceled)13. The method according to claim 11 , wherein the cancer is a leukaemia or a PTEN-negative solid tumour.14. The method compound or composition according to claim 11 , wherein the immune disorder is organ rejection and the method is used to provide anti-rejection therapy to a subject following an organ transplant.15. Use of a compound as defined in claim 1 , for the manufacture of a medicament for use in therapy.16. (canceled) The present invention relates to 1,6-naphthyridines which act as inhibitors of PI3K, for the treatment of cancer, and immune-inflammatory diseases.The phosphoinositide 3-kinases (PI3Ks) constitute a family of lipid kinases involved in the regulation of a network of signal transduction pathways that control a range of cellular processes. PI3Ks are classified into three distinct subfamilies, named class I, II, and III based upon their substrate specificities. Class IA PI3Ks possess a ...

DERIVATIVES OF PYRIDO [3,2-D] PYRIMIDINE, METHODS FOR PREPARATION THEREOF AND THERAPEUTIC USES THEREOF

The present invention relates to a compound of the following general formula (I): 2. The compound of formula (I) according to claim 1 , wherein Ris selected from the group consisting of:hydrogen,halogens,(hetero)aryls comprising from 5 to 30 carbon atoms.3. The compound of formula (I) according to claim 1 , wherein Rrepresents a phenyl group.4. The compound of formula (I) according to claim 1 , wherein Rrepresents a phenyl group.5. The compound of formula (I) according to claim 1 , wherein Rrepresents a phenyl group substituted with a group OR claim 1 , R representing H or an alkyl group comprising from 1 to 10 carbon atoms.612.-. (canceled)13. The compound of formula (I) according to claim 1 , wherein Rrepresents H.14. The compound of formula (I) according to claim 1 , wherein Rrepresents H claim 1 , Rrepresents a phenyl group and Rrepresents a halogen or a phenyl group.15. The compound of formula (I) according to claim 1 , wherein Rrepresents H claim 1 , Rrepresents a phenyl group substituted with a group OR claim 1 , R representing H or an alkyl group claim 1 , comprising from 1 to 10 carbon atoms claim 1 , and Rrepresents a halogen or a phenyl group substituted with a group OR claim 1 , R representing H or an alkyl group comprising from 1 to 10 carbon atoms.17. The compound according to claim 1 , of the above formula (I-3) claim 1 , wherein Ris selected from the group consisting of the following groups:halogen,furanyl,thiophenyl,pyridyl,phenyl,benzothiazolyl, and{'sub': b', 'b, 'claim-text': phenyl,', 'pyridyl,', 'pyrimidinyl,', 'thiazolyl, and', 'isoxazolyl., 'a group —NHR″, R″being selected from the group consisting of the following groups18. The compound of formula (I) according to claim 1 , wherein Rrepresents NHBn.19. The compound of formula (I) according to claim 1 , wherein Rrepresents a —NH—(CH)—OH group.21. A method for treating or preventing diseases related to a deregulation of CDK1 claim 1 , CDK5 claim 1 , GSK3 and/or DYRK1A kinases comprising a step ...

TETRAHYDROCARBOLINE DERIVATIVE

An object of the present invention is to provide a drug having the inhibitory activity on ENPP2 which is a different target from that of the existing drug, as a medicament useful in a urinary excretion disorder patient for whom the existing drug has the insufficient effect. 3. The compound according to , wherein Y is a straight C1-3 alkylene group optionally substituted with one or two Rs wherein Ris as defined in .4. The compound according to claim 3 , wherein X is a nitrogen atom.5. The compound according to claim 3 , wherein X is a carbon atom.6. The compound according to claim 4 , wherein Ris a hydrogen atom.8. The compound according to claim 7 , wherein Yis an unsubstituted methylene group claim 7 , and Tis a bond or an unsubstituted methylene group.9. The compound according to claim 7 , wherein the C5-10 bridged carbon ring in the C5-10 bridged carbon ring optionally substituted with one to five Rs is bicyclo[2.2.1]heptane or bicyclo[2.2.2]octane.10. The compound according to claim 7 , wherein the 5- to 7-membered monocycle in the 5- to 7-membered monocycle optionally substituted with one to five Rs is (i) a C5-7 monocyclic carbon ring or (ii) a 5- to 7-membered monocyclic heterocyclic ring containing one to four heteroatoms selected from an oxygen atom claim 7 , a nitrogen atom and a sulfur atom.11. The compound according to claim 10 , wherein the C5-7 monocyclic carbon ring is benzene claim 10 , cyclopentane or cyclohexane.14. The compound according to claim 7 , wherein the ring A is a C5-6 monocyclic carbon ring or a C9-10 bicyclic carbon ring.15. The compound according to claim 7 , wherein the ring A is (i) a 5- to 6-membered monocyclic heterocyclic ring containing one to four heteroatoms selected from an oxygen atom claim 7 , a nitrogen atom and a sulfur atom or (ii) a 9- to 10-membered bicyclic heterocyclic ring containing one to four heteroatoms selected from an oxygen atom claim 7 , a nitrogen atom and a sulfur atom.16. The compound according to claim ...

NOVEL COMPOUNDS

The invention relates to novel spirocyclic derivatives with affinity for Cav2.2 calcium channels and which are capable of interfering with Cav2.2 calcium channels; to processes for their preparation; to pharmaceutical compositions containing them; and to the use of such compounds in therapy for the treatment of pain. 2. A compound as defined in claim 1 , wherein n represents 1.3. A compound as defined in claim 1 , wherein R claim 1 , Rand Reach represent hydrogen and Rrepresents methyl claim 1 , ethoxy claim 1 , trifluoromethyl or trifluoromethoxy claim 1 , such as trifluoromethyl or trifluoromethoxy.4. A compound as defined in claim 1 , wherein R claim 1 , Rand Reach represent hydrogen and Rrepresents difluoromethoxy claim 1 , trifluoromethyl or trifluoromethoxy.5. A compound as defined in claim 1 , wherein Rand Reach represent hydrogen claim 1 , Rrepresents methyl or trifluoromethyl and Rrepresents chlorine claim 1 , bromine claim 1 , methyl claim 1 , trifluoromethyl or trifluoromethoxy.6. A compound as defined in claim 1 , wherein Rand Reach represent hydrogen claim 1 , Rrepresents methyl claim 1 , methoxy or trifluoromethyl and Rrepresents trifluoromethyl.7. A compound as defined in claim 1 , wherein Rand Reach represent hydrogen claim 1 , Rrepresents chlorine or trifluoromethyl and Rrepresents chlorine claim 1 , fluorine claim 1 , methyl or trifluoromethyl.8. A compound as defined in claim 1 , wherein Rand Reach represent hydrogen claim 1 , Rrepresents chlorine or trifluoromethyl and Rrepresents methyl or trifluoromethoxy.9. A compound as defined in claim 1 , wherein X represents—N(H)—, —N(Me)— or —O—, such as —N(H)— or —N(Me)—, in particular, —N(H)—.10. A compound or salt as defined in which is selected from:7-{[4-(Trifluoromethyl)phenyl]sulfonyl}-2,7-diazaspiro[4.5]decan-1-one (E1);2-Methyl-7-{[4-(trifluoromethyl)phenyl]sulfonyl}-2,7-diazaspiro[4.5]decan-1-one (E2);7-{[2-Chloro-4-(trifluoromethyl)phenyl]sulfonyl}-2,7-diazaspiro[4.5]decan-1-one (E3);7-{[2- ...

NEURODEGENERATIVE DISEASE THERAPEUTIC AGENT

Provided is an unprecedented composition that is not a conventional symptomatic treatment, but makes possible the fundamental treatment of current neurodegenerative diseases by inhibiting oxidative-stress induced nerve-cell death. The disclosed neurodegenerative disease therapeutic agent includes a compound, or a salt of said compound, that inhibits oxidative-stress induced nerve-cell death to a high degree and is an agent used in the treatment of neurodegenerative diseases such as Parkinson's disease. 2. (canceled)3. The therapeutic agent for a neurodegenerative disease according to claim 1 , wherein m and n are 0.4. The therapeutic agent for a neurodegenerative disease according to claim 1 , wherein Ato Aare a single bond claim 1 , —O— claim 1 , —CO— claim 1 , —COO— claim 1 , —OCO— claim 1 , —O—CO—O— claim 1 , —NH— claim 1 , or —NH—COO—.5. The therapeutic agent for a neurodegenerative disease according to claim 1 , each independently of one another claim 1 , have a substituent claim 1 , and are Calkyl claim 1 , Calkenyl claim 1 , Calkynyl group claim 1 , Ccycloalkyl claim 1 , Caryl claim 1 , 5- to 10-membered heterocyclyl group comprising claim 1 , in addition to a carbon atom claim 1 , 1 to 4 heteroatoms selected from nitrogen atom claim 1 , oxygen atom claim 1 , and sulfur atom.6. The therapeutic agent for a neurodegenerative disease according to claim 1 , wherein at least one of -A-Rto -A-Ris a hydrogen atom claim 1 , a hydroxyl group claim 1 , or the following group which may have a substituent: a straight or branched chain Calkyl group claim 1 , a straight or branched chain Calkoxy group claim 1 , a straight or branched chain Calkyl-carbonyl group claim 1 , a straight or branched chain Calkoxy-carbonyl group claim 1 , a straight or branched chain Calkyl-carbonyloxy group claim 1 , a straight or branched chain Calkoxy-carbonyloxy group claim 1 , a Caryl group claim 1 , a 5- to 10-membered heterocyclyl group (comprising claim 1 , in addition to a carbon atom ...

PROCESS FOR THE PREPARATION OF PYRIDO[2,1-a] ISOQUINOLINE DERIVATIVES BY CATALYTIC ASYMMETRIC HYDROGENATION OF AN ENAMINE

The invention relates to a process for the preparation of pyrido[2,1-a]isoquinoline derivatives of the formula 2. The process according to claim 1 , characterized in that the asymmetric hydrogenation in step a) is performed with a transition metal catalyst selected from a ruthenium claim 1 , rhodium or iridium complex catalyst containing a diphosphine ligand.3. The process according to claim 1 , characterized in that the asymmetric hydrogenation in step a) is performed with a rhodium complex catalyst containing a diphosphine ligand.6. The process according to claim 1 , characterized in that the asymmetric hydrogenation in step a) is performed with a rhodium complex catalyst containing (S claim 1 ,R)-PPF-P(tBu)as chiral diphosphine ligand.7. The process according to claim 1 , characterized in that the asymmetric hydrogenation is carried out in an inert organic solvent.8. The process according to claim 8 , characterized in that the asymmetric hydrogenation is carried out in 2 claim 8 ,2 claim 8 ,2-trifluoroethanol.9. The process according to claim 1 , characterized in that the asymmetric hydrogenation takes place at a hydrogen pressure in a range from 1 bar to 200 bar.10. The process according to claim 1 , characterized in that the asymmetric hydrogenation takes place at a reaction temperature in a range from 20° C. to 120° C.11. The process according to claim 1 , characterized in that in step b) tert-butoxycarbonyl is introduced as amino protecting group.12. The process according to claim 1 , characterized in that the amidation in step c) is performed with formamide/sodium methoxide claim 1 , formamide/sodium ethoxide claim 1 , acetamide/sodium methoxide and acetamide/sodium ethoxide.13. The process according to claim 1 , characterized in that the amidation in step c) is performed in an organic solvent at temperatures of 10° C. to 70° C.14. A process for the preparation of (S)-1-((2S claim 1 ,3S claim 1 ,11bS)-2-amino-9 claim 1 ,10-dimethoxy-1 claim 1 ,3 claim 1 ,4 ...

HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS

Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X, X, and Xare N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 2. The compound of wherein Xis N.3. The compound of wherein Xis N.4. The compound of wherein Xis N.5. The compound of wherein Xand Xare N claim 1 , Xand Xare N claim 1 , or Xand Xare N.6. The compound of wherein Ris optionally substituted C-Cheteroaryl selected from pyrazolyl claim 1 , pyridinyl claim 1 , pyrimidinyl claim 1 , 5-methyl-4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydropyrazolo[1 claim 1 ,5-a]pyrazin-2-yl claim 1 , 5-acetyl-4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydropyrazolo[1 claim 1 ,5-a]pyrazin-2-yl claim 1 , 6 claim 1 ,7-dihydro-4H-pyrazolo[5 claim 1 ,1-c][1 claim 1 ,4]oxazin-2-yl claim 1 , and 1-methyl-5-(5-(4-methylpiperazin-1-yl)pyridin-2-yl.7. The compound of wherein Ris —(C-Cheteroaryl)-(C-Cheterocyclyl) where heteroaryl is optionally substituted pyridinyl and heterocyclyl is optionally substituted piperazinyl.8. The compound of wherein Ris phenyl claim 1 , optionally substituted with one or more groups selected from F claim 1 , Cl claim 1 , —CH claim 1 , —S(O)CH claim 1 , cyclopropyl claim 1 , azetidinyl claim 1 , oxetanyl claim 1 , and morpholino.11. The compound of wherein Ris CH.12. The compound of wherein Yis CH and Yis N.13. The compound of wherein Yis N and Yis CH.14. The compound of wherein Yand Yare each CH.15. The compound of wherein Yand Yare each CH claim 1 , and Ris CH.16. The compound of selected from Table 1.17. The compound of selected from Table 218. A pharmaceutical composition comprised of a compound of and a pharmaceutically ...

ALKYLATED PIPERAZINE COMPOUNDS

Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 2. The compound of wherein X is CR claim 1 , and Ris H3. The compound of wherein X is N.4. The compound of wherein Ris —CHOH.5. The compound of wherein Ris F.6. The compound of wherein Rand Rare H.7. The compound of wherein Ris CH.8. The compound of selected from Table 1.9. The compound of selected from Table 2.10. A pharmaceutical composition comprised of a compound of and a pharmaceutically acceptable carrier claim 1 , glidant claim 1 , diluent claim 1 , or excipient.11. The pharmaceutical composition according to claim 10 , further comprising a therapeutic agent.12. A process for making a pharmaceutical composition which comprises combining a compound of with a pharmaceutically acceptable carrier.13. A method of treating a disease or disorder which comprises administering a therapeutically effective amount of the pharmaceutical composition of to a patient with a disease or disorder selected from immune disorders claim 10 , cancer claim 10 , cardiovascular disease claim 10 , viral infection claim 10 , inflammation claim 10 , metabolism/endocrine function disorders and neurological disorders claim 10 , and mediated by Bruton's tyrosine kinase.14. The method of wherein the disease or disorder is an immune disorder.15. The method of wherein the immune disorder is rheumatoid arthritis.16. The method of wherein the disease or disorder is systemic and local inflammation claim 13 , arthritis claim 13 , inflammation related to immune suppression claim 13 , organ transplant rejection claim 13 , allergies claim 13 , ulcerative colitis ...