82031-32-1Relevant academic research and scientific papers
Copper-Catalyzed Divergent C-H Functionalization Reaction of Quinoxalin-2(1H)-ones and Alkynes Controlled by N1-Substituents for the Synthesis of (Z)-Enaminones and Furo[2,3-b]quinoxalines
Feng, Qiong,He, Meiqin,Huang, Huabin,Ji, Fanghua,Jiang, Guangbin,Li, Xuan,Nie, Hongsheng,Wang, Shoucai,Xiong, Zhicheng,Yang, Guang
supporting information, p. 1859 - 1864 (2022/03/16)
With control by N1-substituents, the switchable divergent C-H functionalization reaction of quinoxalin-2(1H)-ones is achieved for the synthesis of (Z)-enaminones and furo[2,3-b]quinoxalines using the combination of a copper catalyst and an oxidant. This new protocol features mild reaction conditions, readily available materials, and a broad substrate scope. Gram-scale and mechanistic studies were also investigated. Furthermore, the desired products exhibited excellent antitumor activity against A549, HepG-2, MCF-7, and HeLa cells, which were tested by MTT assay.
Double-target inhibitor targeting FGFR (fibroblast growth factor receptor) and HDAC (histone deacetylase) as well as preparation method and application thereof, pharmaceutical composition and medicament
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Paragraph 0131-0133, (2021/06/09)
The invention discloses a double-target inhibitor targeting FGFR (fibroblast growth factor receptor) and HDAC (histone deacetylase) as well as a preparation method and application thereof, a pharmaceutical composition and a medicament, and belongs to the
SUBSTITUTED IMIDAZOQUINOXALINE COMPOUNDS AND USES THEREOF
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Page/Page column 32, (2021/03/19)
The disclosure provides substituted imidazo [1, 5-a] quinoxaline and related compounds as kinase inhibitors, and their uses. Specifically, the disclosure provides compounds of Formula I, or pharmaceutically acceptable salts thereof or prodrugs thereof, wherein, A 1-A 3, Cy and R 1-R 2 are defined herein. The compounds of Formula I are kinase inhibitors. Therefore, the compounds of the disclosure can be used to treat clinical conditions caused by DDR function defects, such as cancers. (I)
Synthesis of (E)-Quinoxalinone Oximes through a Multicomponent Reaction under Mild Conditions
Xu, Jun,Yang, Huiyong,He, Lei,Huang, Lin,Shen, Jiabin,Li, Wanmei,Zhang, Pengfei
supporting information, p. 195 - 201 (2021/01/13)
Herein, a novel method for the gram-scale synthesis of (E)-quinoxalinone oximes through a multicomponent reaction under mild conditions is described. Such a transformation was performed under transition-metal-free conditions, affording (E)-oximes in a moderate-to-good yield through recrystallization. Our methodology demonstrates a successful combination of a Mannich-type reaction and radical coupling, providing a green and practical approach for the synthesis of potentially bioactive quinoxalinone-containing molecules.
Electrochemically C-H/S-H Oxidative Cross-Coupling between Quinoxalin-2(1 H)-ones and Thiols for the Synthesis of 3-Thioquinoxalinones
Zhou, Jiadi,Li, Zhonghui,Sun, Zexu,Ren, Quanlei,Zhang, Qiwei,Li, Hu,Li, Jianjun
, p. 4365 - 4372 (2020/04/10)
An electrochemical method for the C(sp2)-H thioetherification of quinoxalin-2(1H)-ones with primary, secondary, and tertiary thiols has been reported. Various quinoxalin-2(1H)-ones underwent this thioetherification smoothly under metal- A nd chemical oxidant-free conditions, affording 3-alkylthiol-substituted quinoxalin-2(1H)-ones in moderate to good yields.
TRI-SUBSTITUTED IMIDAZOLES FOR THE INHIBITION OF TGF BETA AND METHODS OF TREATMENT
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Paragraph 0093, (2019/01/17)
Pharmaceutical compounds, their methods of manufacture, and methods of treatment of mammals with pharmaceutical compounds are provided.
SUBSTITUTED FUSED HETEROARYL COMPOUND SERVING AS A KINASE INHIBITOR, AND APPLICATIONS THEREOF
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Paragraph 0169, (2019/11/21)
The disclosure relates to substituted fused heteroaromatic compounds and the use thereof. Specifically, the disclosure provides compounds of the following Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein A1-A4, B1-B3, D1-D4 and R1-R3 are defined herein. Compounds having Formula I are kinalse inhibitors. Therefore, compounds of the disclosure may be used to treat clinical conditions caused by DDR functional defects, such as cancer.
NOVEL 6-6 BICYCLIC AROMATIC RING SUBSTITUTED NUCLEOSIDE ANALOGUES FOR USE AS PRMT5 INHIBITORS
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Page/Page column 280, (2017/03/14)
The present invention relates novel 6-6 bicyclic aromatic ring substituted nucleoside analogues of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PRMT5 inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
PYRIMIDINE AND TRIAZINE DERIVATIVES AND THEIR USE AS AXL INHIBITORS
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Page/Page column 73, (2016/07/05)
Compounds of the general formula(I): (I) processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
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, (2016/04/26)
The present invention provides for a method for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth.
