- SUBSTITUTED AMINOPYRIMIDINE COMPOUNDS AND METHODS OF USE
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The invention relates to the preparation and use of new aminopyrimidine derivatives as drug candidates in free form or in pharmaceutically acceptable salt form and formulations thereof for the modulation of a disorder or disease which is mediated by the activity of the PI3K enzymes. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of disorders or diseases, such as disorders of immunity and inflammation in which PI3K enzymes play a role in leukocyte function, and hyperproliferative disorders associated with PI3K activity, including but not restricted to leukemias and solid tumors, in mammals, especially humans.
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- Substituted aminopyrimidine compound and usage method and application thereof
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The present invention relates to a substituted aminopyrimidine compound and a usage method and application thereof, and in particular to application of the novel aminopyrimidine compound and free-form salts or pharmaceutically acceptable salts and preparations thereof as the medicaments for the treatment of PI3-kinase abnormality-related disorder or diseases. The invention also relates to the pharmaceutical compositions comprising the compound, and application of the pharmaceutical compositions to the treatment of mammals, particularly for the treatment of PI3-kinase abnormality-related human disorder or diseases, such as treatment of PI3-kinase regulated immune and inflammatory diseases, wherein PI3-kinase plays a major role in leukocyte function, and the treatment of of PI3- kinase-related proliferative diseases including but not limited to leukemia and solid tumors.
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- Copper-catalyzed radical methylation/C-H amination/oxidation cascade for the synthesis of quinazolinones
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A copper-catalyzed radical methylation/sp3 C-H amination/oxidation reaction for the facile synthesis of quinazolinone was developed. In this cascade reaction, dicumyl peroxide acts not only as a useful oxidant but also as an efficient methyl source. Notably, a methyl radical, generated from peroxide, was confirmed by electron paramagnetic resonance for the first time.
- Bao, Yajie,Yan, Yizhe,Xu, Kun,Su, Jihu,Zha, Zhenggen,Wang, Zhiyong
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p. 4736 - 4742
(2015/05/13)
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