141699-57-2Relevant academic research and scientific papers
ATF6 MODULATORS AND USES THEREOF
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Paragraph 258, (2021/04/17)
Compounds (1-2) as modulators of Activating Transcription Factor 6 (ATF6) are provided. The compounds may find use as therapeutic agents for the treatment of diseases or disorders mediated by ATF6 and may find particular use in the treatment of viral infections, neurodegenerative diseases, vascular diseases, or cancer. (Formula (1-2))
HTS-based discovery and optimization of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor
Holm, Patrik,éles, János,Balázs, Ottilia,Fodor, László,Greiner, István,Horváth, Anita,Kóti, János,Kiss, László,Kolok, Sándor,Kostyalik, Diána,Krámos, Balázs,Lévay, Gy?rgy,Ledneczki, István,Lendvai, Balázs,Mahó, Sándor,Molnár, Katalin Dudás,Némethy, Zsolt,Szigetvári, áron,Tapolcsányi, Pál,Thán, Márta,Vágó, István,Vastag, Mónika,Visegrády, András
, (2021/06/22)
HTS campaign of the corporate compound collection resulted in a novel, oxalic acid diamide scaffold of α7 nACh receptor positive allosteric modulators. During the hit expansion, several derivatives, such as 4, 11, 17 demonstrated not only high in vitro potency, but also in vivo efficacy in the mouse place recognition test. The advanced hit molecule 11 was further optimized by the elimination of the putatively mutagenic aromatic-amine building block that resulted in a novel, aminomethylindole compound family. The most balanced physico-chemical and pharmacological profile was found in case of compound 55. Docking study revealed an intersubunit binding site to be the most probable for our compounds. 55 demonstrated favorable cognitive enhancing profile not only in scopolamine-induced amnesia (place recognition test in mice) but also in natural forgetting (novel object recognition test in rats). Compound 55 was, furthermore, active in a cognitive paradigm of high translational value, namely in the rat touch screen visual discrimination test. Therefore, 55 was selected as a lead compound for further optimization. Based on the obtained favorable results, the invented aminomethylindole cluster may provide a viable approach for cognitive enhancement through positive allosteric modulation of α7 nAChRs.
Compound used as RET kinase inhibitor and application thereof
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Paragraph 0227-0230; 0247-0248, (2021/07/01)
The invention relates to a compound used as an RET kinase inhibitor and application thereof, wherein the compound has a structure as shown in a formula F, has good inhibition capability on RET kinase, and has good pharmacodynamic and pharmacokinetic performance and lower toxic and side effects.
Design, synthesis, and structure activity relationship (SAR) studies of novel imidazo[1,2-a] pyridine derivatives as Nek2 inhibitors
Chen, Yunzhong,Du, Yijie,Duan, Yanhong,Gu, Xiaofan,Li, Hongyu,Ma, Mingliang,Ren, Ziwei,Wang, Haili,Wang, Shuting,Xi, Jianbei,Zhang, Xiongwen,Zhu, Tong
, (2020/10/02)
Never in mitosis (NIMA) related kinase 2 (Nek2) is involved in multiple cellular processes such as cell cycle checkpoint regulation, cell division, DNA damage response and cell apoptosis. Nek2 has been reported to be overexpressed in various tumors and correlated with poor prognosis. Herein, a series of imidazo[1,2-a] pyridines Nek2 inhibitors were designed, synthesized, and their biological activities were investigated. Besides, structure activity relationship analysis of these compounds were performed in the MGC-803 cell. The screening results are promising, and compound 28e shows good proliferation inhibitory activity with an IC50 of 38 nM. The results would be helpful to design and develop more effective Nek2 inhibitors for the treatment of gastric cancer.
NOVEL COMPOUNDS FOR INHIBITION OF JANUS KINASE 1
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Page/Page column 89-90, (2020/12/11)
An object of the invention is to provide compounds as selective JAK1 inhibitor, a process for preparation of the inhibitors, a composition containing the compounds and utility of the compounds.
NEW COMPOUND HAVING FGFR INHIBITORY ACTIVITY AND PREPARATION AND APPLICATION THEREOF
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Paragraph 0141; 0142, (2019/05/30)
The present invention relates to a new compound having an FGFR inhibitory activity and preparation and application thereof. In particular, the compound according to the present invention has a structure as shown in formula I, wherein each group and substituent are as defined in the description. Also disclosed in the present invention are a preparation method for the compound and a use thereof in preparation of a drug for treating and/or preventing a tumor-related disease and/or an FGFR-related disease.
Alkenyl compound and its method and use thereof
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Paragraph 0763; 0769; 0770, (2018/03/01)
The invention provides a new substituted alkenyl compound, pharmaceutically acceptable salts of the new substituted alkenyl compound, a medicinal preparation of the new substituted alkenyl compound, and application of the new substituted alkenyl compound, the pharmaceutically acceptable salts and the medicinal preparation of the new substituted alkenyl compound in aspects of regulating the activity of protein kinase and regulating the intercellular or intracellular signal response. The invention also relates to a medicament composition containing the compound at the same time, and relates to a method for treating high-proliferative diseases of mammals especially the human by using the medicament composition.
Saturated Heterocyclic Aminosulfonyl Fluorides: New Scaffolds for Protecting-Group-Free Synthesis of Sulfonamides
Zhersh, Sergey A.,Blahun, Oleksandr P.,Sadkova, Iryna V.,Tolmachev, Andrey A.,Moroz, Yurii S.,Mykhailiuk, Pavel K.
supporting information, p. 8343 - 8349 (2018/06/04)
Cyclic saturated aminosulfonyl fluorides were synthesized as their HCl salts. The compounds were found to be stable upon storage and could be used for the protecting-group-free synthesis of sulfonamides. In the presence of the ?SO2F group, the nitrogen atom could be modified by means of acylation, arylation, or reductive amination to give products that have high potential for the synthesis of bioactive compounds.
Glutaminase inhibitors as well as compositions and applications thereof
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Paragraph 0385; 0389; 0390; 0391, (2018/01/09)
The invention provides a series of heterocyclic compounds expressed in a formula I. The compound comprises glutaminase inhibition activity, and can be used for treating diseases and symptoms related to dysfunction of glutaminase or raising activity of glutaminase.
AMIDE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN
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Page/Page column 132; 133, (2017/02/24)
The present invention relates to amide derivatives having dual pharmacological activity towards both the sigma (σ) receptor, and the μ-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to t
