- Discovery of 8-Methyl-pyrrolo[1,2-a]pyrazin-1(2 H)-one Derivatives as Highly Potent and Selective Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitors
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The bromodomain and extra-terminal (BET) family proteins have recently emerged as promising drug targets for cancer therapy. In this study, identification of an 8-methyl-pyrrolo[1,2-a]pyrazin-1(2H)-one fragment (47) as a new binder to the BET bromodomains
- Li, Zizhou,Xiao, Senhao,Yang, Yaxi,Chen, Chao,Lu, Tian,Chen, Zhifeng,Jiang, Hualiang,Chen, Shijie,Luo, Cheng,Zhou, Bing
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p. 3956 - 3975
(2020/05/27)
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- Synthesis process method of 3-substituted-1H-pyrrole
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The invention provides a synthetic process method of a 3-substituted-1H-pyrrole compound. The process method comprises the following steps: by taking diethylamine hydrochloride and glycine ethyl esterhydrochloride as initial raw materials, respectively carrying out Mannich reaction and sulfamide reaction, and carrying out cyclization reaction, dehydration thinning reaction, aromatization reactionand hydrolysis decarboxylation reaction to obtain a 3-substituted-1H-pyrrole compound. According to the synthesis process method of the 3-substituted-1H-pyrrole compound, the whole synthesis route isgood in step repeatability, mild in operation condition and high in safety, and large-scale production and industrial popularization are facilitated; post-treatment energy consumption is low, a largeamount of toxic wastewater is not generated, no pollution is caused to the environment, the production safety level and the production cost are reduced, application of green and environment-friendlyindustrial production is facilitated, and wide application prospects are achieved.
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Paragraph 0155-0157
(2020/05/30)
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- Bromine structural domain inhibitor compound and application thereof
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The invention relates to a bromine structural domain inhibitor and provides a compound shown in a general formula I, pharmaceutical salt, an enantiomer, a diastereoisomer, an atropisomer, racemate, apolymorphic substance and solvate of the compound or an isotope labelled compound (including a deuterium substituted compound), a preparation method of the compound, pharmaceutical composition containing the compound and an application of the above components in pharmaceuticals.
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Paragraph 0117-0120
(2019/08/02)
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- PYRROLOTRIAZINONE DERIVATIVES AS PI3K INHIBITORS
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New pyrrolotriazinone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).
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Page/Page column 101-102
(2014/05/07)
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- PYRROLOTRIAZINONE DERIVATIVES AS PI3K INHIBITORS
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New pyrrolotriazinone derivatives having the chemical structure of formula (I), are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks)
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Page/Page column 122; 123
(2014/05/07)
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- PYRROLOTRIAZINONE DERIVATIVES AS PI3K INHIBITORS
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New pyrrolotriazinone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).
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Page/Page column 105
(2012/11/13)
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- Pyrrolotriazinone derivatives as PI3K inhibitors
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New pyrrolotriazinone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks)
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Page/Page column 44
(2012/11/13)
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