863504-84-1Relevant articles and documents
4-((1H-pyrazol-3-yl)amino)phthalazin-1(2H)-one derivatives and pharmaceutical composition for use in preventing or treating cancer containing the same as an active ingredient
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Paragraph 0203-0209, (2020/12/01)
The present invention relates to a 4-((1H-pyrazol-3-yl)amino)phthalazine-1(2H)-one derivative and a pharmaceutical composition for preventing or treating cancer containing the same as an active component. The derivative exhibits high inhibitory activity on various protein kinases, and in particular, has excellent inhibitory ability on RET proto-oncogene enzymes, and also has an excellent inhibitory effect on proliferation of medullary thyroid cancer cells and lung cancer cells expressing RET fusion genes, thereby being able to be usefully used for treating medullary thyroid cancer or lung cancer, and in particular, being able to be usefully used for treating cancer in which RET fusion genes are expressed.
Design, Synthesis, and SAR Studies of Heteroarylpyrimidines and Heteroaryltriazines as CB2R Ligands
Qian, Hai-Yan,Wang, Zhi-Long,Chen, Li-Li,Pan, You-Lu,Xie, Xiao-Yu,Xie, Xin,Chen, Jian-Zhong
supporting information, p. 2455 - 2463 (2018/11/23)
Herein we describe the design and synthesis of a new series of heteroarylpyrimidine/heteroaryltriazine derivatives on the basis of quinazoline-2,4(1H,3H)-diones as CB2R-selective ligands using a bioisosterism strategy. An acetamide group was explored to displace the enamine linker of the lead compound for the purpose of stereoisomerism elimination and hydrophilicity increase. As a result, some of the synthesized compounds showed high bioactivity and selectivity for CB2R in calcium mobilization assays, and four displayed CB2R agonist activity, with EC50 values below 30 nm. The compound exhibiting the highest agonist activity toward CB2R (EC50=7.53±3.15 nm) had a selectivity over CB1R of more than 1328-fold. Moreover, structure–activity relationship (SAR) studies indicated that the substituents on the nucleus play key roles in the functionality of a ligand, with one such example demonstrating CB2R antagonist activity. Additionally, molecular docking simulations were conducted with the aim of better understanding of these new derivatives in relation to the structural requirements for agonists/antagonists binding to CB2R.
PYRAZOLE COMPOUNDS AND METHODS OF MAKING AND USING SAME
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, (2017/06/12)
Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL and/or ABHD6. Furthermore, the subject compounds and compositions are useful for the treatment of, for example, pain.