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The present invention relates to a compound of formula A, wherein R is alkyl. Compound A may be used as an intermediate in the preparation of O-desmethyl venlafaxine or a salt thereof, and the present invention provides such a preparation, as well as a process for preparing the compound of formula A.

Disclosed herein is a method for producing an alcohol and an amine from an amide under an atmosphere of hydrogen with the use of, as a catalyst, a ruthenium complex that is easily prepared, easy to handle, and relatively cheaply obtained. Specifically, the method is a method for producing an alcohol and/or an amine from an amide compound under an atmosphere of hydrogen with the use of as a catalyst, a ruthenium carbonyl complex represented by the following general formula (1): RuXY(CO)(L) (1) wherein X and Y may be the same or different from each other and each represents an anionic ligand and L represents a tridentate aminodiphosphine ligand containing two phosphino groups and a —NH— group.

The invention concerns a new process for the preparation of crystalline form of agomelatine from a solution of agomelatine in a solvent, characterized in that the agomelatine is crystallized by instantaneous precipitation from said solution, at a temperature equal to or below −10° C.

Provided is a method for stably and economically producing xylylenediamine with a high yield and long catalyst service life by hydrogenating dicyanobenzene that is obtained by ammoxidating xylene. By bringing an aqueous basic solution into contact with a dicyanobenzene-absorbed liquid, which is obtained by bringing an ammoxidation reaction gas into contact with an organic solvent, under specified temperature conditions, and subjecting a base and a carboxylic acid in the dicyanobenzene-absorbed liquid to a neutralization reaction so as to form an aqueous phase that contains a water-soluble salt, and then subjecting an organic phase and the aqueous phase to liquid-liquid separation so as to remove the aqueous phase, it is possible to remove the carboxylic acid contained in the dicyanobenzene-absorbed liquid with high selectivity while inhibiting loss of the dicyanobenzene. By subjecting the raw material dicyanobenzene, which is obtained by separating low boiling point compounds from the post liquid-liquid separation organic phase by distillation under reduced pressure, to hydrogenation, xylylenediamine is produced with a high yield and the service life of the hydrogenation catalyst is extended.

A process for reductive amination of aliphatic cyanoaldehydes to aliphatic diamines comprising (1) providing a mixture of 1,3-cyanocyclohexane carboxaldehyde and/or 1,4-cyanocyclohexane carboxaldehyde; (2) contacting said mixture with a metal carbonate based solid bed or a weak base anion exchange resin bed at a temperature from 15 to 40 ° C. for a period of at least 1 minute; (3) thereby treating said mixture, wherein said treated mixture has a pH in the range of 6 to 9; (4) feeding said treated mixture, hydrogen, and ammonia into a continuous reductive amination reactor system; (6) contacting said treated mixture, hydrogen, and ammonia with each other in the presence of one or more heterogeneous metal based catalyst systems at a temperature from 80 ° C. to 160 ° C. and a pressure from 700 to 3500 psig; (7) thereby producing one or more cycloaliphatic diamines is provided.

A process for preparing alkylated p-phenylenediamine having the steps of reacting aniline and nitrobenzene in presence of a complex base catalyst to obtain 4-aminodiphenylamine intermediates, hydrogenating the 4-aminodiphenylamine intermediates to 4-aminodiphenylamine in presence of a hydrogenation catalyst, and reductively alkylating the 4-aminodiphenylamine to alkylated p-phenylenediamine.

Disclosed is a process for preparing an aryloxyalkylene amine compound via an aminoethylation reaction comprising: a) reacting an aromatic hydroxyl compound in the presence of a basic catalyst with a 2-oxazolidinone compound of the formula II to form an intermediate reaction product; wherein R3 is selected from the group consisting of hydrogen or lower alkyl having 1 to 6 carbon atoms, R4 is selected from the group consisting of hydrogen, straight or branched chain alkyl having from one to six carbon atoms, phenyl, alkaryl, or arylalkyl; and b) reacting the intermediate product of step a) with a polyalkylene polyamine.

A process for conversion of aliphatic bicyclic amines to aliphatic diamines including contacting one or more bicyclic amines selected from the group consisting of 3-azabicyclo[3.3.1]nonane and azabicyclo[3.3.1]non-2-ene with ammonia and hydrogen, and alcohols in the presence of heterogeneous metal based catalyst systems, a metal selected from the group consisting of Co, Ni, Ru, Fe, Cu, Re, Pd, and their oxides at a temperature from 140° C. to 200° C. and a pressure from 1540 to 1735 psig for at least one hour reactor systems; forming a product mixture comprising aliphatic diamine(s), bicyclic amine(s), ammonia, hydrogen, and alcohol(s); removing said product mixture from the reactor system; removing at least some of the ammonia, hydrogen, water, alcohols, bicyclic amines from said product mixture; thereby separating the aliphatic diamines from said product mixture.

An improved process for making ethoxylated amine compounds such as ethanolamines. The improvement comprises the addition of an acid to the amine compound prior to the addition of ethylene oxide to a reactor wherein the ethoxylated amine compound is prepared. The improvement reduces the concentration of undesirable glycol ether and/or vinyl ether ethoxylate byproducts which may contribute to undesirable properties, such as color and foaming, of the ethoxylated amine compounds.

Borazine derivatives are used in the manufacture of electronic devices, in particular electroluminescent and semiconductor devices. More specifically, stable borazine derivatives include boron atoms substituted by aryl groups used in one or more layers of an electroluminescent or a semiconductor device, in particular in the emissive layer of organic light-emitting devices (OLED).

The invention relates to a method for preparing ring-halogenated N,N-dialkylbenzylamines and intermediates obtainable therefrom for preparing agrochemicals and pharmaceutically active ingredients.

A system and method that facilitates urban traffic state detection based on support vector machine (SVM) and multilayer perceptron (MLP) classifiers is provided. Moreover, the SVM and MLP classifiers are fused into a cascaded two-tier classifier that improves the accuracy of the traffic state classification. To further improve the accuracy, the cascaded two-tier classifier (e.g., MLP-SVM), a single SVM classifier and a single MLP classifier are fused to determine a final decision for a traffic state. In addition, fusion strategies are employed during training and implementation phases to compensate for data acquisition and classification errors caused by noise and/or outliers.

The present disclosure involves systems, software, and computer-implemented methods for providing process intelligence by correlating events from multiple business process systems to a single business scenario using configurable correlation strategies. An example method includes identifying a raw event associated with a sending business process and a receiving business process, identifying a sending business process attribute associated with the sending business process and a receiving business process attribute associated with the receiving business process, determining a correlation strategy for associating the raw event with a business scenario instance, the determination based at least in part on the sending business process attribute and the receiving business process attribute, and generating a visibility scenario event from the raw event according to the correlation strategy, the visibility scenario event associated with the business scenario instance.

Various embodiments provide lossless compression of an enumeration space for genetic founder lines. In one embodiment, an input comprising a set of genetic founder lines and a maximum number of generations G is obtained. A set of genetic crossing templates of a height h is generated. A determination is made if at least a first genetic crossing template in the set of genetic crossing templates is redundant with respect to a second genetic crossing template in the set of genetic crossing templates. Based on the at least first genetic crossing template being redundant is redundant with respect to the second genetic crossing template, the at least first genetic crossing template is removed from the set of genetic crossing templates. This process of removing the at least first genetic crossing template from the set of genetic crossing templates the redundant creates an updated set of genetic crossing templates.

Systems and methods are disclosed that may be implemented for network management system (NMS) configuration management support for network devices using a learning and natural language processing application to capture the usage and behavior of the Command Line Interface (CLI) of a network device with the aid of a CLI knowledge model, which in one example may be ontology-based.

The disclosed embodiments describe a method, an apparatus, an application specific integrated circuit, and a server that provides a fast and efficient look up for data analysis. The apparatus and server may be configured to obtain data segments from a plurality of input devices. The data segments may be individual unique subsets of the entire data set obtained by a plurality input devices. A hash function may be applied to an aggregated set of the data segments. A result of the hash function may be stored in a data structure. A codebook may be generated from the hash function results.

A method for manufacturing a refined fat or oil, including: carrying out a first steam treatment of bringing a fat or oil into contact with water vapor; and subsequently carrying out a second steam treatment of bringing the fat or oil having a temperature lower by 10° C. or more than a temperature of the fat or oil in the first steam treatment into contact with water vapor in the presence of an organic acid.

The invention relates to the use of a composition of A) at least one quaternary ammonia compound comprising at least one organic radical bonded to the ammonia nitrogen atom and optionally comprising heteroatoms and having 1 to 36 carbon atoms, and B) at least one amine alkoxylate ester of formula (1) or a salt thereof, where A, B are, independently of each other, a C2- through C5-alkylene radical R1, a C8- through C24-alkyl radical or alkenyl radical R2, R3, R4 independent of each other, H, or a C8- through C24-acyl radical, with the stipulation that at least one of the radicals R2, R3 or R4 stands for a C8- through C24-acyl radical, and x, y, z, independently of each other, stand for a whole number from 0 through 50, with the stipulation that x+y+z is a whole number from 1 through 100, in quantities of 10 through 5000 g/tonne of ore as a collector in silicate floation.

The present application describes modulators of MCP-1 or CCR-2 of formula or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, n, W, X, R1 and R6, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.

Disclosed embodiments provide pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating diseases associated with kinase activity, in particular enhanced PLK1 catalytic activity, such as diseases associated with abnormal cell proliferation, including neoplastic disorders.

The invention relates compounds of general formula (I) and pharmaceutically acceptable salts and solvates thereof wherein R1 is halogen, vinylene-aryl, substituted aryl, heteroaryl or a benzo[1,3]dioxolil group,W is a group of formula —NH—SO2—R2 or heteroaryl group or NHR3 group where R3 is hydrogen or heteroaryl; and n is 1, 2, 3 or 4. Furthermore, the present invention is directed to pharmaceutical composition containing at least one compound of general formula (I) and/or pharmaceutically acceptable salts or solvates thereof and for the use of them for the preparation of pharmaceutical compositions for the prophylaxis and/or the treatment of protein kinase related, especially CDK9-related diseases e.g. cell proliferative disease, infectious disease, pain, cardiovascular disease and inflammation.

Provided are triazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.

The invention discloses quinoxaline derivatives or salts thereof having PDE9-inhibiting activity and being useful as treating agent of dysuria and the like, which are represented by the formula (I) in the formula, R1 and R2 each independently stands for hydrogen, halogen, alkyl, alkoxy, acyl, amino and the like,R3 stands for alkyl, aryl, saturated carbocyclic group, saturated heterocyclic group, acyl and the like,R4 stands for hydrogen, hydroxy, alkyl or amino,R5 and R8 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkoxy, cyano or nitro,R6 and R7 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, cyano, amino, carbocyclic group, heterocyclic group, COR9 or SO2R9,R9 stands for hydrogen, hydroxy, alkyl, amino, pyrrolidin-1-yl, piperidin-1-yl, pyperazin-1-yl or the like,X stands for S or O, andA1, A2 and A3 each independently stands for N or C.

The present invention relates to pyridazine compounds of formulae I or II and the salts thereof, the N-oxides thereof and the salts of the N-oxides thereof, where the radical A is of the formula A, wherein # denotes the point of attachment to the remainder of formulae I or II, and wherein A1 is N or C—RA1, A2 is N or C—RA2, A3 is N or C—RA3, A4 is N or C—RA4 and A5 is N or C—RA5, provided that one or two of the variables A1, A2, A3, A4 or A5 is N; RA1, RA5, if present, are H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-haloalkyl and the like; RA2, RA4, if present, are H, halogen, CN, NO2, C1-C10-alkyl, C1-C10-haloalkyl and the like; RA3, if present, is H, halogen, CN, NO2, C1-C10-alkyl, C1-C10-haloalkyl and the like; where W is N or C—RW and V is N or C—RV, provided that one of the variables W or V is N; Rt and Rw, if present, are H, halogen, methyl, C1-haloalkyl and the like; Ru and Rv, if present, are H, halogen, C1-C4-alkyl, C1-C3-haloalkyl and the like; X1 is S, O or NR1a, wherein R1a is H, C1-C10-alkyl and the like; X2 is OR2a, NR2bR2c, S(O)mR2d, wherein m is 0, 1 or 2, R2a is C1-C4-alkyl, C1-C4-haloalkyl and the like, R2b, R2c are H, C1-C4-alkyl, C1-C4-haloalkyl and the like, or R2b and R2c together with the nitrogen atom to which they are bound form a heterocycle, and R2d is C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl and the like; and R1 is H, CN, C1-C10-alkyl and the like. The present invention further relates to a method for controlling invertebrate pests, to a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material, comprising at least one compound according to the present invention, to a method for treating or protecting an animal from infestation or infection by parasites and to an agricultural composition containing at least one compound according to the present invention.

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain pyridyl-amino-pyrazine carbonitrile compounds that, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or thymidylate synthase (TS) inhibitor; (d) a microtubule targeted agent; and (e) ionizing radiation.

The present invention provides 4,6-disubstituted pyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same.

The invention relates to oxazolopyrimidine compounds of formula I, where A, R1 and R2 are defined as stated in the claims. The compounds of formula I are suitable, for example, for wound healing.

The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.

The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, T, V, W, X, Y, Z, ring A, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and m are defined herein. There novel pyrrolopyrimidine and purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.

The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R1 represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C1-5alkylR3, wherein R3 is piperidinyl-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C1-4alkyl, C1-4hydroxyalkyl and C1-4alkoxy; 2) C2-5alkenylR3, wherein R3 is as defined herein; 3) C2-5alkynylR3, wherein R3 is as defined herein; and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof; processes for their preparation; pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.

The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.

This invention relates to novel 5-[(hydroxymethyl)aryl]-substituted pyrrolo[2,1-f][1,2,4]triazin-4-amines of formula (I), to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating angiogenesis-related disorders, in particular angiogenesis-related ocular disorders.

4,6-dichloro-2-methyl-5-(1-acyl-2-imidazolin-2-yl)-aminopyrimidine is reacted with methanol in the presence of a non-ionic organic base, and moxonidine is obtained directly from the reaction mixture.

Disclosed are oil-extended olefin block copolymer compositions with microcrystalline wax. The microcrystalline wax reduces oil-bleed while maintaining composition softness.

A rubber composition for manufacturing tyres is based on one or more diene elastomers, one or more reinforcing fillers, and a vulcanization system. The vulcanization system includes one or more 1,2,4-triazine compounds chosen from compounds of formula I and compounds of formula II: Certain specific 1,2,4-triazine derivatives are described.

Compounds of formula (I) ##STR1## in which R1 is hydrogen, O°, CN, NO, cyanomethyl, C1 -C12 -alkyl, C3 -C12 -alkenyl or C3 -C12 -alkynyl subject to the proviso that the carbon atom attached to the nitrogen atom is a primary carbon atom, C7 -C12 -aralkyl, C1 -C12 -acyl, 2,3-epoxypropyl, OH-monosubstituted C2 -C6 -alkyl or 2,3-dihydroxypropyl, R2 is hydrogen, C1 -C18 -alkyl, C5 -C18 -cycloalkyl, C6 -C18 -aryl or C7 -C18 -aryalkyl, R3 is C6 -C18 -aryl or a group of the formula (II) ##STR2## in which R1 is as defined above, n is an integer from 1 to 4 and R4 is an organic or inorganic radical of a valency equal to n are useful for stabilizing organic material against oxidative, thermal and/or light induced degradation.