15833-63-3Relevant academic research and scientific papers
SSAO INHIBITORS AND USE THEREOF
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Paragraph 00396, (2021/05/07)
Provided are a compound of formula (I') or (I), a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of SSAO, a pharmaceutical composition comprising a compound of formula (I') or (I), and a method of treating or preventing a disease in which SSAO plays a role.
Discovery and optimization of novel N-benzyl-3,6-dimethylbenzo[d]isoxazol-5-amine derivatives as potent and selective TRIM24 bromodomain inhibitors with potential anti-cancer activities
Hu, Qingqing,Wang, Chao,Xiang, Qiuping,Wang, Rui,Zhang, Cheng,Zhang, Maofeng,Xue, Xiaoqian,Luo, Guolong,Liu, Xiaomin,Wu, Xishan,Zhang, Yan,Wu, Donghai,Xu, Yong
, (2019/12/26)
Tripartite motif-containing protein 24 (TRIM24), recognized as an epigenetic reader for acetylated H3K23 (H3K23ac) via its bromodomain, has been closely involved in tumorigenesis or tumor progression of several cancers. Developing inhibitors of TRIM24 is significant for functional studies and drug discovery. Herein, we report the identification, optimization and evaluation of N-benzyl-3,6-dimethylbenzo[d]isoxazol-5-amines as TRIM24 bromodomain inhibitors starting from an in house library screening. Structure-based optimization leads to two potent and selective compounds 11d and 11h in an Alphascreen assay with IC50 values of 1.88 μM and 2.53 μM, respectively. The viability assay demonstrates the great potential of this series of compounds as inhibitors of proliferation of prostate cancer (PC) cells LNCaP, C4-2B. A colony formation assay further supports this inhibitory activity. Compounds 11d and 11h inhibit cell proliferation of other cancer types such as non-small cell lung cancer (NSCLC) cells A549 with IC50 values of 1.08 μM and 0.75 μM, respectively. These data suggests that compounds 11d and 11h are promising lead compounds for further research.
4,5,6-TRI-SUBSTITUTED INDAZOLES DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF IN MEDICINES
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Paragraph 0127-0128, (2019/02/19)
Provided are 4,5,6-tri-substituted indazoles derivatives, a preparation method therefor, and a use thereof in medicines. Specifically, provided are compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates, or prodrugs thereof
DIHYDROQUINOLIZINONES AS ANTIVIRALS
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Paragraph 00431; 00435; 00436, (2018/09/19)
Compounds, specifically hepatitis B virus and/or hepatitis D virus inhibitors, more specifically compounds that inhibit HBe antigen and HBs antigen in a subject, for the treatment of viral infections, and methods of preparing and using such compounds. Formula (I):
Method for producing dinotefuran
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Paragraph 0019; 0020; 0021; 0022; 0023, (2018/01/03)
The invention discloses a method for producing dinotefuran, which comprises the following steps of stirring tetrahydrofurfuryl alcoholl, toluene and triethylamine, adding p-toluenesulfonyl chloride, heating by steam for refluxing, adding water, stirring, standing, delaminating, distilling to remove toluene, and then performing cut fraction to obtain an intermediate A; adding methyl nitroguanidine, ethanol, and methylamine aqueous solutions into a reactor, then dropwise adding a formaldehyde aqueous solution, heating and reacting, cooling for crystallization, performing suction filtration and drying to obtain an intermediate B; putting the intermediate A, the intermediate B and DMF into the reactor, stirring, mixing and dropwise adding liquid caustic soda, heating and stirring, then cooling to room temperature, adding hydrochloric acid, heating, stirring, then extracting by using methylene dichloride, concentrating, cooling for crystallization, performing suction filtration, and drying to obtain an intermediate C; adding the intermediate C and urea into the reactor, adding isobutanol, heating and keeping temperature, then cooling, filtering, washing with water and drying to obtain the dinotefuran. The method disclosed by the invention has the advantages of simple operation, high total yield, low cost, environmental protection and no pollution, and is suitable for industrialized production.
NOVEL INDOLE DERIVATIVES AND THEIR USE IN NEURODEGENERATIVE DISEASES
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Paragraph 0709-0710, (2016/11/24)
The present invention relates to indole compounds, and pharmaceutically acceptable compositions thereof, useful as antagonists of P2X7, and for the treatment of P2X7-related disorders.
2,4-DIOXO-QUINAZOLINE-6-SULFONAMIDE DERIVATIVES AS INHIBITORS OF PARG
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Paragraph 00835, (2016/07/05)
The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity wherein R1a, R1b, R1c, R1d, R1e, W, X1, X2, X3, X4, X5, X6, X7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated.
TETRAHYDROPYRIDOPYRIMIDINES AND TETRAHYDROPYRIDOPYRIDINES AS INHIBITORS OF HBSAG (HBV SURFACE ANTIGEN) AND HBV DNA PRODUCTION FOR THE TREATMENT OF HEPATITIS B VIRUS INFECTIONS
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Page/Page column 128, (2016/11/21)
The present invention provides tetrahydropyridopyrimidines and tetrahydropyridopyridines having the general formula (I) wherein R1, R2, U, W, X, Y and Z are as described herein, as inhibitors of HBsAg (HBV surface antigen) and HBV DNA production for the treatment and prophylaxis of hepatitis B virus infections.
2- PYRIDONE COMPOUND
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Paragraph 0252; 0253, (2016/10/08)
PROBLEM TO BE SOLVED: To provide a compound that has excellent glucokinase (GK) activating action and is useful as a pharmaceutical. SOLUTION: The present invention provides a 2-pyridone compound represented by formula [1], and a tautomer or stereoisomer of the compound, or their pharmacologically acceptable salts, or their solvates (where R1 is RA-ZA-; RA is any of a carboxy group, a sulfo group or formula [5]). COPYRIGHT: (C)2016,JPOandINPIT
AMIDE COMPOUND AND USE THEREOF FOR PEST CONTROL
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Paragraph 0665; 0666, (2015/01/18)
An amide compound represented by formula (I) has an excellent pest control effect. (In the formula, Y represents a 3-7 membered saturated heterocyclic ring which contains, as ring-forming component(s), one or more atoms or groups that are selected from th
