1222174-93-7Relevant academic research and scientific papers
Synthesis method of 5-bromine-1-methyl-1H-pyrazole-3-amine
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Paragraph 0015, (2020/12/30)
The invention discloses a synthesis method of 5-bromine-1-methyl-1H-pyrazole-3-amine. The method comprises the steps of condensing diethyl butynedioate serving as a raw material with methylhydrazine to obtain 5-hydroxyl-1-methyl-1H-pyrazole-3-carboxylic acid ethyl ester, and reacting the 5-hydroxyl-1-methyl-1H-pyrazole-3-carboxylic acid ethyl ester with phosphorus oxybromide to obtain 5-bromine-1-methyl-1H-pyrazole-3-carboxylic acid ethyl ester; hydrolyzing in a sodium hydroxide alcohol solution to obtain 5-bromine-1-methyl-1H-pyrazole-3-carboxylic acid, reacting the 5-bromine-1-methyl-1H-pyrazole-3-carboxylic acid with dimethyl azide phosphate and tert-butyl alcohol to obtain tert-butyl (5-bromine-1-methyl-1H-pyrazole-3-yl) carbamate, and hydrolyzing in trifluoroacetic acid to obtain the5-bromine-1-methyl-1H-pyrazole-3-amine. The method has the advantages of simple synthesis route, reasonable process selection, low raw material cost, simple and easily available raw materials, convenient operation and post-treatment, and no use of highly toxic reagents, and overcomes the defects of expensive and unavailable raw materials, unsafe operation, difficult amplification and the like in the existing synthesis process.
PYRAZOLYL-BASED CARBOXAMIDES USEFUL AS CALCIUM RELEASE ACTIVATED CALCIUM CHANNEL (ICRAC) INHIBITORS
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Page/Page column 30, (2015/07/07)
The invention relates to pyrazolyl-based carboxamide compounds useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to these compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders, in pa
PYRAZOLYL-BASED CARBOXAMIDES V
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Page/Page column 27, (2016/04/20)
The invention relates to pyrazolyl-based carboxamlde compounds of formula (I) useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to these compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders.
PYRIDINYL-SUBSTITUTED PYRAZOLYL CARBOXAMIDES
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Paragraph 0290; 0294; 0295; 0296, (2015/06/24)
The invention relates to pyrazolyl-based carboxamide compounds useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to methods of using these compounds for the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders.
Pyrazolyl-Based Carboxamides II
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Paragraph 0356-0358, (2014/07/22)
The invention relates to pyrazolyl-based carboxamide compounds useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to these compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders.
PYRAZOLYL-BASED CARBOXAMIDES II AS CRAC CHANNEL INHIBITORS
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Page/Page column 48; 49, (2014/07/23)
The invention relates to pyrazolyl-based carboxamide compounds of formula (I) useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to these compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders.
SUBSTITUTED-1,4-DIHYDROPYRAZOLO[4,3-b]INDOLES
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Paragraph 0179-0180, (2014/03/26)
Disclosed are compounds of Formula (1), and pharmaceutically acceptable salts thereof, wherein L, R1, R2, R3, R4, R5, R6, and R7 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating obesity and related diseases, disorders, and conditions associated with MetAP2.
Fragment-based discovery of indole inhibitors of matrix metalloproteinase-13
Taylor, Steven J.,Abeywardane, Asitha,Liang, Shuang,Muegge, Ingo,Padyana, Anil K.,Xiong, Zhaoming,Hill-Drzewi, Melissa,Farmer, Bennett,Li, Xiang,Collins, Brandon,Li, John Xiang,Heim-Riether, Alexander,Proudfoot, John,Zhang, Qiang,Goldberg, Daniel,Zuvela-Jelaska, Ljiljana,Zaher, Hani,Li, Jun,Farrow, Neil A.
experimental part, p. 8174 - 8187 (2012/01/13)
Matrix metalloproteases (MMPs) play an important role in cartilage homeostasis under both normal and inflamed disease states and, thus, have become attractive targets for the treatment of arthritic diseases. Herein, we describe the identification of a pot
HETEROARYL SUBSTITUTED INDOLE COMPOUNDS USEFUL AS MMP-13 INHIBITORS
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Page/Page column 50, (2010/04/30)
Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.
