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The present invention relates to Brexpiprazole having a purity of about 99.5% or more by area percentage of HPLC, having total impurities not more than 0.5% relative to brexpiprazole as measured by area percentage of HPLC, and having less than 0.1% 1-(benzo[b]thiophen-4-yl)piperazine or a salt thereof relative to brexpiprazole by area percentage of HPLC. The present invention also provides a composition comprising brexpiprazole having 1-(benzo[b]thiophen-4-yl)-piperazine or a salt thereof in an amount less than about 0.1% relative to brexpiprazole by area percentage of HPLC and process for the preparation of brexpiprazole.

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The invention discloses a kind of type (1) a compound represented by the method for preparing brexpiprazole, particularly in 4–aminobenzene and [b] thiophene as the starting material for synthesizing ethylene, to avoid heavy metal palladium-catalyzed reaction, synthesis step and impurities is reduced, reducing the cost of the preparation method. (by machine translation)

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The invention provides a piripiprazole derivative and a preparation method, wherein the chemical structural formula of the epiprazole derivative is expressed by a chemical structural formula. The epiprazole derivative is composed of epiconazole, (HCHO). m N – hydroxymethyl according to the first basic catalyst is prepared; and then N – hydroxymethyl-piripiprazole and an alkylformylchloride compound are reacted under second basic catalyst to prepare. The half-life of the epiprazole derivative is prolonged, the drug delivery frequency can be reduced; and the epiprazole derivative prepared by the preparation method is low in impurity, and low in cost. (by machine translation)

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Processes for preparation of Brexpiprazole, intermediates used during preparation, and polymorphs of Brexpiprazole are provided.

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Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP 17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.

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Provided are a pyrimidinyl amino compound having protein kinase inhibitor activity, and a pharmaceutical composition containing said compound; also provided are a use and application of said compound. What is provided is selected from a group consisting of the compound represented by formula (I), a stereoisomer thereof, a tautomer thereof, a pharmacologically acceptable salt thereof, a solvate thereof, and a prodrug thereof. The described compound has good inhibitory activity against the JAK family of kinases and the SYK family of kinases, and therefore may serve as a JAK inhibitor and SYK inhibitor, and is effective in use for the prevention or treatment of diseases related to the JAK and SYK families of kinases.

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The present invention provides a new method for preparing according to […], which belongs to the technical field of pharmaceutical and chemical synthesis. It solves the problem that the existing according to[…] of the preparation method of the impurity is high, the yield is low, the problem of serious pollution. This method, in order to 4-hydroxybenzene and thiophene as the starting material 4 is prepared by the step of reaction intermediates V, to 7-hydroxy-2-quinolone by 2 VII is prepared by the step of reaction intermediates, intermediate V and intermediates prepared by condensation VII clinical medicine […]according to. The raw materials of this invention is easy to obtain, the price is low, the operation is simple, mild reaction conditions, has excellent industrial application value. (by machine translation)

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Disclosed are compounds having the formula: or a salt thereof, wherein A, n, R1, R1A, and R2 are as defined herein, and methods of making and using the same

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PROCESS FOR THE PREPARATION OF BREXPIPRAZOLE AND INTERMEDIATES THEREOF

The present invention relates to Brexpiprazole having a purity of about 99.5% or more by area percentage of HPLC, having total impurities not more than 0.5% relative to brexpiprazole as measured by area percentage of HPLC, and having less than 0.1% 1-(benzo[b]thiophen-4-yl)piperazine or a salt thereof relative to brexpiprazole by area percentage of HPLC. The present invention also provides a composition comprising brexpiprazole having 1-(benzo[b]thiophen-4-yl)-piperazine or a salt thereof in an amount less than about 0.1% relative to brexpiprazole by area percentage of HPLC and process for the preparation of brexpiprazole.

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Herbicides

The invention provides certain herbicidal thiazolotriazole sulphonamides, processes for their preparation, and compositions containing them, the compounds being of the formula: STR1 where: R1 and R2, which may be the same or different, each represent hydrogen, hydroxy, halo, cyano, substituted or unsubstituted alkyl, alkoxy, alkenyloxy, alkynyloxy, aryl, aralkyl, heteroaryl or carbamoyl, or a group –CORa or –CO2 Ra or where Ra is hydrogen or alkyl; or R1 and R2 together represent an alkylene chain of 3 or 4 carbon atoms; R3 represents a substituted or unsubstituted aryl, heterocyclyl or benzheterocyclyl group; and R4 represents hydrogen, an alkali-metal atom, an ammonium group, a substituted or unsubstituted alkyl, alkenyl, alkynyl, acyl, alkoxycarbonyl or aralkyl group, a heterocyclic group, or a group of the formula: STR2 where R1 and R2 are as defined hereinbefore.

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