91225-41-1Relevant academic research and scientific papers
JAK kinase inhibitor, preparation method thereof, and application in the field of medicines
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Paragraph 0194; 0197; 0200; 0201, (2019/04/10)
The application relates to a JAK kinase inhibitor, a preparation method thereof, and an application in the field of medicines and belongs to the field of medical chemistry. In the application, a series of novel small-molecular JAK inhibitors are provided and are represented as the general formula (II). The compounds have better effects and higher safety in prevention or treatment on JAK-related adaptation diseases.
Imidazo-pyrazine medical intermediate preparation method
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Paragraph 0010; 0013, (2018/09/08)
The invention relates to an imidazo-pyrazine medical intermediate preparation method which comprises the following steps: (a) adding 2-amino-3,5-dibromo pyrazine and ammonium hydroxide into a high pressure kettle, heating to 110 to 150 DEG C under the nitrogen protection, reacting, performing suction filtration after cooling to obtain filter cake and drying to obtain compound II; (b) dissolving the compound II into N,N-dimethyl formamide, dropwise adding triethyl orthoformate and formic acid, heating and refluxing under the nitrogen protection and purifying to obtain compound III; (c) adding the compound III, N-methyl pyrrolidone, ammonium hydroxide and copper sulfate pentahydrate into the other high pressure kettle, heating to 130 to 170 DEG C under the nitrogen protection and purifying to obtain imidazo-pyrazine medical intermediate. Therefore, synthesizing steps of a final product can be reduced, and a yield and a purity are improved.
Preparation method of imidazo-pyrazine medical intermediate
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Paragraph 0012, (2018/11/22)
The invention relates to a preparation method of an imidazo-pyrazine medical intermediate. The preparation method comprises the following steps that (a) 2-amino-3,5-dibromo pyrazine and ammonia waterare added into an autoclave, heating is performed under nitrogen protection to reach 110-150 DEG C, reaction is performed, suction filtration is performed to obtain a filter cake after cooling, and drying is performed to obtain a compound II; (b) the compound II is dissolved in N,N-dimethyl formamide, triethyl orthoformate and formic acid are added dropwise, heating reflux is performed under nitrogen protection, and a compound III is obtained through purification; (c) the compound II, N-methyl pyrrolidone, ammonia water and copper sulfate pentahydrate are added into the autoclave, heating is performed under nitrogen protection to reach 130-170 DEG C, reaction is performed, and a compound IV is obtained through purification; (d) 1,4-dioxane and the compound IV are dissolved in an acetic acid solution, a NaNO2 water solution is dropwise added under the condition of ice-water bath, heating is performed to 40-50 DEG C after adding, reaction is performed to separate out solid, and suction filtration and washing are performed. Therefore, the synthesis steps of a final product can be decreased, and accordingly the yield and purify of the product are improved.
BCR-ABL kinase inhibitor and its application (by machine translation)
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Paragraph 0079, (2017/03/28)
The present invention relates to the field of chemical medicines, in particular to compounds as represented by formula I having BCR-ABL kinase inhibitory activity, or pharmaceutically acceptable salt, isomer, solvate, crystal or prodrug thereof, and pharmaceutical composition containing the compounds, and application of the compounds or compositions in drug preparation. The compounds of the present invention have strong inhibitory effect on BCR-ABL kinase, and can be used to treat diseases such as tumors.
FLAP MODULATORS
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Paragraph 0542; 0543, (2015/11/02)
The present invention relates to compounds of Formula (I), or a form thereof, wherein ring A, R1, L and R2 are as defined herein, useful as FLAP modulators. The invention also relates 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.
FLAP MODULATORS
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Paragraph 0536; 0537, (2015/05/06)
The present invention relates to compounds of Formula (I), or a form thereof, wherein ring A, R1, L and R2 are as defined herein, useful as FLAP modulators. The invention also relates 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.
INHIBITORS OF JAK
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Page/Page column 81-82, (2011/04/18)
The present invention relates to the use of novel compounds of Formula I, wherein the variables m, n, p, q, Q, r, R, R′, X, X′, Y, Z1, Z2, and Z3 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.
