5653-21-4Relevant articles and documents
Method for efficiently synthesizing nitroacetonitrile
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Paragraph 0030-0032; 0035-0038, (2021/03/13)
The invention discloses a method for efficiently synthesizing nitroacetonitrile, which comprises the following steps: by using nitromethane as a starting raw material, carrying out Henry reaction under the action of alkali to obtain nitroacetaldehyde oxime, and dehydrating the nitroacetaldehyde oxime under the action of thionyl chloride to obtain nitroacetonitrile. The method is designed by starting from a commercially available low-cost raw material nitromethane, wherein the nitroacetaldehyde oxime is obtained through a Henry reaction under the action of alkali and is dehydrated under the action of thionyl chloride to obtain nitroacetonitrile; therefore, the efficient synthesis of nitroacetonitrile is achieved through two-step reaction, the requirement for temperature in the synthesis process is relatively wide, operation steps are not complex, and the method is suitable for industrial production. Thus, the product with stable yield and stable purity can be obtained, the production cost is low, the period is short, the problems of unstable yield and quality, high production cost, long production period and the like of a traditional preparation method are solved. Excellent technical support can be provided for subsequent application of nitroacetonitrile in the field of high-density energetic materials.
QUINOLINO-PYRROLIDIN-2-ONE DERIVATIVE AND APPLICATION THEREOF
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Paragraph 0076; 0078, (2021/07/08)
Disclosed are a series of quinolino-pyrrolidin-2-one compounds, and application thereof in preparation of drugs for ATM inhibitor-related diseases. The present disclosure specifically relates to a derivative compound represented by formula (I), tautomers thereof or pharmaceutically acceptable compositions thereof.
Nitroacetonitrile and Its Synthetic Equivalents
Iwai, Kento,Nishiwaki, Nagatoshi
, p. 13177 - 13185 (2021/09/02)
Nitroacetonitrile (NAN) serves as a cyano(nitro)methylating agent facilitating the construction of polyfunctionalized compounds; however, its explosive property is a significant drawback in terms of practical handling. Alkali metal salts of NAN are therma
IMIDAZOQUINOLINE-TYPE COMPOUNDS AND USES THEREOF
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Paragraph 0013; 00106; 00107, (2021/10/11)
Provided in the present disclosure are imidazoquinoline-type compounds, methods for their preparation, pharmaceutical compositions thereof and their use, wherein the imidazoquinoline-type compounds, upon local administration, form depots inducing cell mediated immune response while mitigating a systemic proinflammatory immune response.
Design, synthesis, evaluation and molecular modeling study of 4-N-phenylaminoquinolines for Alzheimer disease treatment
Zhu, Jun,Wang, Li-Ning,Cai, Rong,Geng, Shang-Qi,Dong, Ya-Fei,Liu, Yu-Ming
supporting information, p. 1325 - 1329 (2019/04/08)
Dual binding site acetylcholinesterase (AChE) inhibitors and butyrylcholinesterase (BChE) inhibitors have recently emerged as two classes of new anti-Alzheimer agents to positively modify the disease's course. In this work, a new series of 4-N-phenylaminoquinolines was synthesized and evaluated for their abilities to inhibit AChE and BChE. Compound 11b showed significant inhibitory activities on AChE and BChE with IC50 values of 0.86 and 2.65 μM, respectively, a lot better than that of reference drug galanthamine. Furthermore, docking study showed that compound 11b interacted simultaneously not only with active and peripheral sites of AChE, but also with all five regions of BChE active site. These findings suggest that these derivatives could be regarded as promising starting points for further drug discovery developments.
INHIBITORS OF MALT1 AND USES THEREOF
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Paragraph 00339; 00340, (2018/09/28)
Provided herein are compounds that inhibit MALTl, a protein whose activity is responsible for constitutive NF-κΒ signaling in certain cancers (e.g., activated B-cell diffuse large B-cell lymphoma (ABC-DLBCL)). Also provided are pharmaceutical compositions and kits comprising the compounds, and methods of treating MALTl -related diseases and disorders (e.g., cancer) with the compounds in a subject, by administering the compounds and/or compositions described herein.
Discovery of Potent and Selective Inhibitors of Cdc2-Like Kinase 1 (CLK1) as a New Class of Autophagy Inducers
Sun, Qi-Zheng,Lin, Gui-Feng,Li, Lin-Li,Jin, Xi-Ting,Huang, Lu-Yi,Zhang, Guo,Yang, Wei,Chen, Kai,Xiang, Rong,Chen, Chong,Wei, Yu-Quan,Lu, Guang-Wen,Yang, Sheng-Yong
, p. 6337 - 6352 (2017/08/02)
Autophagy inducers represent new promising agents for the treatment of a wide range of medical illnesses. However, safe autophagy inducers for clinical applications are lacking. Inhibition of cdc2-like kinase 1 (CLK1) was recently found to efficiently induce autophagy. Unfortunately, most of the known CLK1 inhibitors have unsatisfactory selectivity. Herein, we report the discovery of a series of new CLK1 inhibitors containing the 1H-[1,2,3]triazolo[4,5-c]quinoline scaffold. Among them, compound 25 was the most potent and selective, with an IC50 value of 2 nM against CLK1. The crystal structure of CLK1 complexed with compound 25 was solved, and the potency and kinase selectivity of compound 25 were interpreted. Compound 25 was able to induce autophagy in in vitro assays and displayed significant hepatoprotective effects in the acetaminophen (APAP)-induced liver injury mouse model. Collectively, due to its potency and selectivity, compound 25 could be used as a chemical probe or agent in future mechanism-of-action or autophagy-related disease therapy studies.
COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF MEK
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Paragraph 0338, (2015/02/25)
The present invention relates to compounds of formula I: in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.
COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF MEK
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Paragraph 00202; 00203; 00204; 00205, (2015/02/25)
The present invention relates to compounds of formula I: in which n, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a pro
COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF MEK
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Paragraph 00216; 00217; 00218; 00219, (2015/02/25)
The present invention relates to compounds of formula I in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.
