y

Wheat variety W030377L1

A wheat variety designated W030377L1, the plants and seeds of wheat variety W030377L1, methods for producing a wheat plant produced by crossing the variety W030377L1 with another wheat plant, and hybrid wheat seeds and plants produced by crossing the variety W030377L1 with another wheat line or plant, and the creation of variants by mutagenesis or transformation of variety W030377L1. This invention also relates to methods for producing other wheat varieties or breeding lines derived from wheat variety W030377L1 and to wheat varieties or breeding lines produced by those methods.




y

Osteospermum and Dimorphoteca plants having an altered flower phenotype

The present invention relates to an Osteospermum and Dimorphoteca plant, seed, variety, and hybrid. Another aspect of the present invention relates to an Osteospermum and Dimorphoteca plant having a mutant allele designated KLEDF which results in an altered flower phenotype. The invention also relates to crossing Osteospermum and Dimorphoteca plants containing the KLEDF mutant allele with other Osteospermum and Dimorphoteca plants lacking the KLEDF mutant allele to produce intergeneric and interspecific hybrids. This invention further relates to specific lines of Osteospermum varieties exhibiting the altered-flowering phenotype. Furthermore, the invention relates to pollen, seed, and sexual, as well as asexual progeny of such plants with altered flowers. In addition, the invention relates to methods for propagating said plants and to uses of said plants.




y

Herbicide tolerant soybean plants and methods for identifying same

The invention provides specific transgenic soybean plants, plant material and seeds, characterized in that these products harbor a stack of specific transformation events at specific locations in the soybean genome (elite event EE-GM3 and elite event EE-GM2, or elite event EE-GM3 and elite event EE-GM1). The invention also provides for methods of producing soybean plants and seeds having elite event EE-GM3 and elite event EE-GM2, or elite event EE-GM3 and elite event EE-GM1.




y

Non-glycosylated transferrin expressed in monocots

Disclosed are compositions and methods of making non-glycosylated transferrin protein in transgenic monocot plants.




y

Genetically modified mice that produce hybrid antibodies

A method for engineering and utilizing large DNA vectors to target, via homologous recombination, and modify, in any desirable fashion, endogenous genes and chromosomal loci in eukaryotic cells. These large DNA targeting vectors for eukaryotic cells, termed LTVECs, are derived from fragments of cloned genomic DNA larger than those typically used by other approaches intended to perform homologous targeting in eukaryotic cells. Also provided is a rapid and convenient method of detecting eukaryotic cells in which the LTVEC has correctly targeted and modified the desired endogenous gene(s) or chromosomal locus (loci) as well as the use of these cells to generate organisms bearing the genetic modification.




y

Method and apparatus for conveying a cellulosic feedstock

A method and apparatus for conveying a cellulosic feedstock are disclosed. The apparatus, such as a holding tank, has a passage. At the outlet to the passage, a conveyance member is provided to convey the cellulosic feedstock laterally across the outlet. The conveyance member, e.g., at least one screw conveyor, may have a variable pitch along its length. The method comprises passing the cellulosic feedstock through an impregnation chamber to an outlet of the impregnation chamber; passing the cellulosic feedstock from the outlet of the impregnation chamber to an inlet of a holding tank; passing the cellulosic feedstock downwardly through the holding tank; maintaining a generally constant residence time in the holding tank; and subsequently subjecting the cellulosic feedstock to a hydrolysis process.




y

Mixing device for creating an output mixture by mixing a first material and a second material

A mixing device for mixing a first and second material together to create an output mixture. The device includes a first chamber containing the first material coupled to a mixing chamber defined between a rotor and a stator. The rotor is disposed inside the stator and rotates therein about an axis of rotation. The first chamber houses an internal pump configured to pump the first material from the first chamber into the mixing chamber. The pump may be configured to impart a circumferential velocity into the first material before it enters the mixing chamber. At least one of the rotor and stator have a plurality of through-holes through which the second material is provided to the mixing chamber. Optionally, a second chamber is coupled to the mixing chamber. The second chamber may house an internal pump configured to pump the output material from the mixing chamber into the second chamber.




y

Method and apparatus for conveying a cellulosic feedstock

An apparatus for conveying a cellulosic feedstock is disclosed. The apparatus comprises an enclosed volume having a lower surface comprising a plurality of longitudinally extending portions. Each longitudinally extending portion has an inner surface that is arcuate in transverse section. A plurality of conveyance members are provided within the enclosed volume. Each conveyance member is associated with one of the inner surfaces and configured to sweep the one of the inner surfaces. Additionally, a method for treating a cellulosic feedstock is disclosed. The method comprises providing a cellulosic feedstock being less than 100% saturated moisture. The cellulosic feedstock is introduced into a longitudinally extending enclosed volume, and conveyed longitudinally through the enclosed volume while being mixed.




y

Container system

A method and system for providing a homogenized slurry output comprises a container body defining an interior portion, a discharge for supplying the slurry from the container body to a downstream source and at least one inlet in fluid communication with a pressurized supply of slurry for introducing the slurry into the interior portion of the container body in a circulation pattern that creates a homogenized mixture of slurry in the interior portion of the body.




y

Apparatus, system and method for mixing and dispensing dental impression materials

An apparatus, system and method for mixing and dispensing dental impression materials is described. A dental impression material mixing machine comprises a water dispenser fluidly coupled to a hollow mixing axle, the mixing axle extending through a pulley, wherein an inner circumference of the hollow mixing axle forms a water conduit and an outer circumference of the hollow mixing axle forms a hub connector, a closeable valve inserted at a water entrance to the water conduit and electronically coupled to a water pump, an electronically commutated motor rotatably coupled to the pulley, wherein the hub connector receives a tubular rotatable hub of a disposable mixing vessel comprising dry dental impression powder, and wherein water is dispensed from the water dispenser into the disposable mixing vessel through the water conduit and hub orifice.




y

Machine for continuous casting of pre-mortared masonry panels

A machine for continuous casting of pre-mortared masonry panels includes a rotatable continuous mold for continuously forming pre-mortared masonry panels and an application system for applying polymeric material to the continuous mold as the continuous mold rotates. The machine also includes a brick setter system for setting bricks onto the polymeric material as the continuous mold rotates. The machine further includes a cutting device for cutting the bricks and polymeric material into panels to form the pre-mortared masonry panels.




y

Lug type extruder screw

An extruder screw that enables mixing of viscous materials, such as rubber mixtures and thermoplastic materials, is disclosed. The screw includes a core extending from a sealing end to a nose cone end. At least one flight extends radially from the core in a quasi-helical pattern, wherein flights adjacent one another form channels therebetween. A plurality of elongate lugs extend radially from the core and are disposed in the channels. The shape as well as the number of lugs can be varied to ensure the requirements for a thorough and turbulent deflection and mixing of the material stream.




y

Method and devices for sonicating liquids with low-frequency high energy ultrasound

A method and devices comprise a low frequency high energy ultrasound system having at least one sonotrode projecting into a reactor vessel through which the liquid passes via at least one inlet orifice and at least one outlet orifice. To avoid cavitation at the sonotrode, in a close region of the oscillation-transducing sonotrode surface a pressure/amplitude combination close to or above the pressure-amplitude characteristic line is generated at which considerably reduced or no cavitation occurs and in the adjacent region in the vessel at least in a region and at least at times a pressure/amplitude combination is maintained below the pressure-amplitude characteristic line at which cavitation is generated. A device has an inlet orifice arranged such that the liquid impacts directly onto the oscillation-transducing sonotrode surface, and is shaped that in the close region of the oscillation-transducing sonotrode surface a pressure close to or above the pressure-amplitude characteristic line prevails.




y

Clay mixing apparatus

A clay mixing apparatus includes a mixing chamber, a rotor arranged within the mixing chamber, a drive unit arranged to rotate the rotor, an ejecting unit, a pressure reducing unit; and an exhaust flow path. The rotor includes a shaft rotated by the drive unit, an extruding member and a mixing member. The mixing member includes a plurality of arms and a plurality of blades arranged at tip ends of the arms. The exhaust opening is opposed, in a radial direction about the center axis, to a portion of the mixing member lying near the extruding member and/or a portion of the extruding member lying near the mixing member.




y

Eddy current minimizing flow plug for use in flow conditioning and flow metering

An eddy-current-minimizing flow plug has an outer radial wall with open flow channels formed between the plug's inlet and outlet. The plug has a central region coupled to the inner surface of the outer radial wall. Each open flow channel includes (i) a first portion originating at the inlet and converging to a location in the plug where convergence is contributed to by changes in thickness of the outer radial wall and divergence of the central region, and (ii) a second portion originating in the plug and diverging to the outlet where divergence is contributed to by changes in thickness of the outer radial wall and convergence of the central region. For at least a portion of the open flow channels, a central axis passing through the first and second portions is non-parallel with respect to the given direction of the flow.




y

Apparatus for mixing and controlling the temperature of laboratory vessel contents

The present invention relates to an apparatus for mixing and controlling the temperature of laboratory vessel contents with an accommodating device in detachable connection with an exchangeable block for accommodating and controlling the temperature of laboratory vessels and with a drive by which the accommodating device can be set in a mixing motion, and with a temperature control device with a heat source or sink in heat-conducting connection with the exchangeable block at least through in each case at least one adjoining contact face firstly on the accommodating device and secondly on the exchangeable block, which is characterized in that the detachable connection is maintained by a spring element which, by virtue of its spring force, horizontally clamps together a first undercut between the accommodating device and the exchangeable block in at least one first direction.




y

Tank agitation system with moveable shaft support

An apparatus for containing and mixing a load of liquids and solids is disclosed. The apparatus includes an elongated tank, which includes a lower portion and an upper portion. The apparatus further includes an elongated rotatable shaft within the tank. At least one blade is connected to the shaft and is configured to mix the liquids and solids when the shaft is rotated. The apparatus also includes a shaft support configured for maintaining the shaft in a rotatable manner within the tank. The shaft support is selectively moveable in a manner permitting the shaft to move in an upward direction from the lower portion toward the upper portion, and in a downward direction from the upper portion toward the lower portion. An is contained with the tank for moving the shaft support in the upward direction and in the downward direction.




y

Multi-component mixing system having a rotatable container and container therefor

A container (10, 30, 50) is provided for single- or multi-component molding materials. The container has a container body (12, 32, 52) having a constant outer contour in a longitudinal extent of the container (10, 30, 50), a piston (17, 37) movable in the longitudinal direction, and a cover (11, 31) having an outlet opening (13, 33, 53). A volume for a molding material is defined between the piston (17, 37) and the cover (11, 31), the volume being variable in the direction of the longitudinal extent of the container (10, 30, 50). The container distinguishes itself in that the container body (12, 32, 52) is rotatable relative to the outlet opening (13, 33, 53), and the piston (17, 37) thereby pushes out the content of the container (10, 30, 50).




y

Mixing and kneading machine for continual compounding and method of implementing continual compounding by means of a mixing and kneading machine

A mixing and kneading machine (1) for continual compounding comprises a screw shaft (3) rotating in a casing (2) and simultaneously moving axially translationally. To sustainably enhance the efficiency of the machine as regards its material thruput per unit of time the screw shaft (3) comprises at least four groups of radial screw vanes (4a, 4b, 4c, 4d) evenly distributed circumferentially, each group consisting of a plurality of screw vanes in axial sequence. The outer diameter (Da) of the screw shaft ranges from 400 to 800 millimeters. The rotary speed of the screw shaft (3) ranges from 30 to 80 rpm. A mixing and kneading machine (1) engineered as such is particularly suitable for compounding an anodic mass in the production of electrodes—anodes—for the aluminum industry.




y

Dissolution generator, method of dissolving powder, and mixing system

A dissolution generator includes: an upright housing; a screen assembly extending across an interior of the housing, and configured to support a column of powder thereabove; a spray nozzle disposed below the screen assembly and directed towards the screen assembly; and a pressure mechanism disposed above the screen assembly, and configured to apply a substantially constant downward pressure.




y

Method and apparatus for high intensity ultrasonic treatment of baking materials

The present invention discloses a high intensity ultrasonic treatment method and apparatus that is used in conjunction with an existing commercial dough or batter mixer to enhance the rheological, aeration and textural properties of the dough or batter. This change in properties is a result of the phenomenon of acoustic cavitation induced in the dough or batter by treatment with high intensity ultrasonic waves. The present invention discloses a mixing bowl (20) of an existing mixer system that is preloaded with dough or batter, the bowl (20) is located at the center of an ultrasonic bath tank (101) filled with a working fluid. The effect of ultra-sonic waves with power levels above 1 kW can be observed over the entire or partial mixing period of the dough or batter. The ultra-sonic waves of the present invention are generated by a plurality of ultrasonic wave generators (104A, 104B) and piezoelectric transducers (1) mounted on a stainless steel tank (101). The electrical energy received in each transducer (1) will be converted into appropriate mechanical expansion and contractions in the piezoelectric ceramics of the transducer (1) thus leading to pressure waves being transmitted to the dough or batter to be mixed. The generation and transmission of high intensity ultrasonic waves to the dough or batter affects its rheological, aeration and textural properties.




y

Changing and measuring consistency

A measuring device comprising at least one mixer structure to receive a fiber suspension sample from at least one process part. Each mixer structure is provided with a measuring unit, a feeding valve for feeding feed liquid into a sample line for pushing the sample in the sample line towards the measuring unit, a mixing valve structure for feeding dilution liquid into the mixer structure The mixer structure mixes the flowing sample and the dilution liquid with one another in order to reduce the consistency of the sample. The measuring device measures from the first part of the mixed sample one property of the fiber suspension and the measuring device measures from the second part of the mixed sample a further property.




y

Compact, portable blender system

A compact portable blender system features a base unit. A base unit top surface features a recess having an “L” shaped locking slot and a motor with a drive gear. A base unit bottom surface features a removable power supply. The base unit features a power charger, a removable cord, a cord storage cavity, a power switch, and a power indicator. The system features a blending container. A blending blade unit is located on a container bottom. A blade drive gear located on a blending blade unit bottom and a blending blade is located on a blending blade unit top. The blending blade unit features a locking tab located on a blending blade unit side wall. The system features a container lid having an aperture. The container lid features a cover located over the aperture on a container lid top.




y

Dinitroxide-type biradical compounds optimized for dynamic nuclear polarization (DNP)

The present invention relates to the field of organic chemistry and in particular to organic free radicals used as polarizing agents in the technique of Dynamic Nuclear Polarization (DNP), which involves transferring the polarization of electron spins to the nuclei of a compound whose Nuclear Magnetic Resonance (NMR) is being observed. It concerns Dinitroxide-type Biradical polarizing agents characterized by a rigid linkage between the aminoxyl groups of said nitroxide units. This particular structure enables, at low temperatures and high fields, optimal transfer of polarization and optimal enhancement of NMR/MAS signals of the polarized nuclei of the compound studied.




y

Pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives and methods of use

This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are 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. The compounds may bind to and antagonize receptor α2B, α1B or α2A. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption, or to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. The compounds may also be used to treat diseases or conditions that are expected to be responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular, renal disorders or type 2 diabetes is particularly described.




y

Dihydroethidine analogues and uses thereof

Tracers for imaging distribution of reactive oxygen species (ROS) are disclosed. The tracers include radiolabeled dihydroethidine (DHE) analogues. Further disclosed are uses of the compounds, including methods of imaging tissue distribution of ROS in vivo by positron emission tomography (PET). Methods of synthesizing the compounds are also disclosed.




y

Synthesis of MSE-framework type molecular sieves

A method of synthesizing a crystalline molecular sieve having an MSE framework type comprises crystallizing a reaction mixture comprising a source of water, a source of an oxide of a tetravalent element, Y, selected from at least one of silicon, tin, titanium, vanadium, and germanium, optionally a source of a trivalent element, X, a source of an alkali or alkaline earth metal, M, and a source of organic dications, Q, such as 3-hydroxy-1-(4-(1-methylpiperidin-1-ium-1-yl)butyl)quinuclidin-1-ium, 3-hydroxy-1-(5-(1-methylpiperidin-1-ium-1-yl)pentyl)quinuclidin-1-ium, 1,1'-(butane-1,4-diyl)bis(1-methylpiperidin-1-ium), 1,1'-(pentane-1,5-diyl)bis(1-methylpiperidin-1-ium), 1,1'-(hexane-1,6-diyl)bis(1-methylpiperidin-1-ium), and 1,1'-((3as,6as)-octahydropentalene-2,5-diyl)bis(1-methylpiperidin-1-ium).




y

Nitrogen-containing condensed heterocyclic compound

There are provided compounds represented by the following general formula (I) or pharmaceutically acceptable salts of thereof, which have a superior monoacylglycerol acyltransferase 2 inhibitory action: wherein Ring A represents a partially saturated heteroaryl group, an aryl group or a heteroaryl group,RB represents a C4-18 alkyl group, a C3-8 cycloalkyl group, a partially saturated aryl group, an aryl group, or the following formula (II): wherein V represents the formula —CR11R12—, —CO—, —CO—O—, or —CO—NH—,W represents a single bond or a C1-3 alkylene group, andRing B represents a C3-8 cycloalkyl group, a C3-8 cycloalkenyl group, a partially saturated heteroaryl group, a saturated heterocyclyl group, an aryl group, or a heteroaryl group,Y represents a nitrogen atom or the formula N+(RF),RF represents a C1-4 alkyl group, andm and n, which may be the same or different, each represent an integer of 0 or 1.




y

Process for preparing a biphenyl-2-ylcarbamic acid

The invention provides a process of preparing an intermediate useful in the synthesis of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and a process of preparing a crystalline freebase of the ester.




y

Process for preparing a compound useful for producing an optically active diazabicyclooctane compound

A process for preparing the compound of the following formula (E): wherein Bn represents a benzyl group, and tBu represents a tert-butyl group, the process including: (a) subjecting the following compound (B) to trifluoroacetylation, wherein tBu represents a tert-butyl group to produce the following compound (C): wherein tBu represents a tert-butyl group, and TFA represents a trifluoroacetyl group; (b) reacting the compound (C) with benzyloxyamine in the presence of a hydroxyl group activating agent to produce the following compound (D): wherein Bn represents a benzyl group, tBu represents a tert-butyl group, and TFA represents a trifluoroacetyl group; and (c) subjecting the compound (D) to detrifluoroacetylation.




y

N-(1,2,5-oxadiazol-3-yl)pyridinecarboxamides and use thereof as herbicides

A description is given of N-(1,2,5-oxadiazol-3-yl)pyridinecarboxamides of the general formula (I) as herbicides. R in this formula (I) stands for radicals such as hydrogen, organic radicals, and other radicals such as halogen. W stands for a substituted pyridyl radical.




y

Compositions of protein receptor tyrosine kinase inhibitors

The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.




y

Aryl and heteroaryl fused lactams

This invention relates to compounds of general formula (I) in which R1, R2, U, V, L, M, R5, m, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.




y

Fused tetracyclic pyrido [4,3-B] indole and pyrido [3,4-B] indole derivatives and methods of use

This disclosure is directed to fused tetracyclic pyrido[4,3-b>]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are 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.




y

Oxime-substituted-quinoxaline-type piperidine compounds as ORL-1 modulators

The present disclosure relates to Oxime-Substituted Quinoxaline-Type Piperidine Compounds, such as those of Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R20, R21, Q, Y1, Z, A, B, and a are as defined herein; compositions comprising an effective amount of an Oxime-Substituted Quinoxaline-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of an Oxime-Substituted Quinoxaline-Type Piperidine Compound.




y

[1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators

The present invention is directed to a compound of Formula (I) and to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.




y

Pyrimidines as novel therapeutic agents

The present invention features compounds having the Formula (Ia) and (Ib) (e.g., a compound of any of Formulas ((Ia-2)-(Ia-21)), including other tautomers, stereoisomers, E/Z stereoisomers, prodrugs, pharmaceutically acceptable salts, and compositions thereof. The invention also features methods for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient by administering an effective amount of a compound of Formula (Ia) or (Ib). The invention also features a method for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient that includes administering to a patient in need thereof an effective amount of a compound of Formula (IIa) or (IIb) (e.g., a compound of any of Formulas ((IIa-2)-(IIa-6)). The compounds described herein (e.g., a compound of Formulas (Ia), (Ib), (IIa), or (IIb)) can also be used as anticonvulsants.




y

Small molecule inhibitors of polynucleotide kinase/phosphatase, poly(ADP-ribose) polymerase and uses thereof

The present invention generally relates to use of compounds and compositions as a chemosensitizers and/or radiosensitizers and/or inhibitors of PNKP phosphatase activity. The present invention provides pharmaceutical combinations and/or a pharmaceutically acceptable salt thereof, kits containing such compounds and/composition and methods of using such compounds and/or compositions.




y

Phenoxyisobutyric acid compounds and method of synthesis

The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).




y

Substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors

The invention is directed to novel substituted benzylamino quinolines, compounds comprising substituted benzylamino quinolines, methods of making substituted benzylamino quinolines, the use of substituted benzylamino quinolines for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism, and the use of substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors.




y

Amino azaheterocyclic carboxamides

The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.




y

Methine-substituted cyanine dye compounds

Cyanine dye compounds having a substituted methine moiety that are nucleic acid stains, particularly for fluorescent staining of RNA, including compounds having the formula where R1 is a C1-C6 alkyl, sulfoalkyl, carboxyalkyl or C1-C6 alkoxy; each R2 is independently selected from the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy, fused benzo, trifluoromethyl, amino, sulfo, carboxy and halogen, that is optionally further substituted; at least one of R3, R4, and R5 is an alkyl, aryl, heteroaryl, cyclic, or heterocyclic moiety that is optionally substituted by alkyl, amino, aminoalkyl, carboxy, nitro, or halogen; and the remaining R3, R4 or R5 are hydrogen; X is S, O, or Se; and D is a substituted or unsubstituted pyridinium, quinolinium or benzazolium moiety.




y

Dual inhibitors of farnesyltransferase and geranylgeranyltransferase I

Many GTPases such as Ras, Ral and Rho require post-translational farnestylation or geranylgeranylation for mediating malignant transformation. Dual farnesyltransferase (FT) (FTI) and geranylgeranyltransferase-I (GGT-1) inhibitors (GGTI) were developed as anticancer agents from based on an ethylenediamine scaffold. On the basis of a 4-fold substituted ethylenediamine scaffold, the inhibitors are structurally simple and readily derivatized, facilitating extensive structure-activity relationship studies. The most potent inhibitor is compound exhibited an in vitro hFTase IC50 value of 25 nM and a whole cell H-Ras processing IC50 value of 90 nM. Several of the inhibitors proved highly selective for hFTase over the related prenyltransferase enzyme geranylgeranyltransferase-I (GGTase-I). A crystal structure of an inhibitor cocrystallized with farnesyl pyrophosphate in the active site of rat FTase illustrates that the para-benzonitrile moiety is stabilized by a π-π stacking interaction with the Y361β residue, suggesting an importance of this component of the inhibitors.




y

1H-benzimidazole-5-carboxamides as anti-inflammatory agents

There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.




y

Adenosine A1 agonists for the treatment of glaucoma and ocular hypertension

The present invention relates to the use of selective adenosine A1 agonists, in particular the dicyanopyridines of formula (I), for the treatment and/or prophylaxis of glaucoma and ocular hypertension as well as the their use for the production of a medicament for the treatment and/or prophylaxis of glaucoma and ocular hypertension.




y

Substituted pyridine and pyrazine compounds as PDE4 inhibitors

The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.




y

Fluorescent dyes with large stokes shifts

Herein are disclosed fluorescent dyes based around a framework for a ligand comprising a pyridyl group linked to a diaryl anilido unit. A variety of ligands based on this framework are disclosed. The ligands chelate to a BF2 center to produce the fluorescent dye. The disclosed dyes combine longer Stokes shifts (approximately 100 nm) with increased quantum yields. They are also photostable in aqueous and organic solutions for several hours. These dyes may be used in the labeling of biomolecules for bioimaging and assays. Also disclosed are methods for the synthesis of these dyes.




y

Pyrrolidine inhibitors of IAP

The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, Q, X1, X2, Y, R1, R2, R3, R4, R4', R5, R6 and R6' are as described herein.




y

Bicyclic thiazoles as allosteric modulators of mGluR5 receptors

The present invention relates to novel bicyclic thiazoles which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (“mGluR5”) and which are useful for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which mGluR5 is involved.




y

Method for producing pyridazinone compounds and intermediate thereof

The present invention relates to a novel method for producing a pyridazinone compound and an intermediate thereof as shown in the following scheme: wherein the symbols are as defined in the specification.