5775-89-3Relevant academic research and scientific papers
MACROCYCLES AND THEIR USE
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Paragraph 0731; 0753; 0754, (2022/02/06)
The present disclosure relates to macrocyclic compounds, pharmaceutical compositions containing macrocyclic compounds, and methods of using macrocyclic compounds to treat disease, such as cancer.
Synthesis method of glatianide intermediate
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, (2021/08/25)
The invention provides a synthesis method of a strain facitinib intermediate, which takes acetone oxalate as a starting raw material in a simple and easy manner and is cyclized in sequence. The bromo, propionamide, bromination, amidation, deprotection and dehydration 7 steps give (4 - bromo -5 - cyano -1 - methyl - 1H - pyraz -3 -yl) methyl tert-butyl carbamate. The synthesis method of the Litinib intermediate disclosed by the invention has the characteristics of easily available raw materials, simple operation, low cost, short steps and high yield.
MACROCYCLIC CHLORINE SUBSTITUTED INDOLE DERIVATIVES
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Page/Page column 259; 260, (2019/06/13)
The present invention relates to macrocyclic indole derivatives of general formula (I) : (I), in which R1, R2, R3, R4, R5, R6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active 10 ingredients.
ARYL ANNULATED MACROCYCLIC INDOLE DERIVATIVES
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Page/Page column 141, (2019/06/05)
The present invention relates to aryl annulated macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
MACROCYCLIC CHLORINE SUBSTITUTED INDOLE DERIVATIVES
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Page/Page column 190-191, (2019/06/09)
The present invention relates to macrocyclic indole derivatives of general formula (I) : in which R1, R2, R3, R4, R5, R6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
MACROCYCLIC FLUORINE SUBSTITUTED INDOLE DERIVATIVES AS MCL-1 INHIBITORS, FOR USE IN THE TREATMENT OF CANCER
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Page/Page column 150, (2019/06/09)
The present invention relates to macrocyclic indole derivatives of general formula (I) : in which R1, R2, R3, R4, R5, R6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
MACROCYCLIC INDOLE DERIVATIVES
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Page/Page column 275, (2017/12/15)
The present invention relates to macrocyclic indole derivatives of general formula (I) : (I), in which R1, R2, R3, R4, R5, R6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
Synthesis and anti-TMV activity of novel N-(3-alkyl-1H-pyrazol-4-yl)-3- alkyl-4-substituted-1H-pyrazole-5-carboxamides
Zhang, Da Qiang,Xu, Gao Fei,Fan, Zhi Jin,Wang, Dao Quan,Yang, Xin Ling,Yuan, De Kai
scheme or table, p. 669 - 672 (2012/07/17)
In order to investigate the biological activity of novel bis-pyrazole compounds, a series of N-(3-alkyl-5-(N-methylcarbamyl)-1H-pyrazol-4-yl)-3-alkyl- 4-substituted-1H-pyrazole-5-carboxamides were designed and synthesized with ethyl 3-alkyl-1H-pyrazole-5-
