87687-75-0Relevant academic research and scientific papers
COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR
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Paragraph 0781-0787, (2021/06/26)
This disclosure pertains to compounds, the preparation thereof, and the use of these compounds in the treatment of prostate cancer, including metastatic and/or castrate-resistant prostate cancer, in subjects in need thereof.
Adventitious isolation of a pseudorotaxane complex of a trans-bis(Hydroxymethylbenzo)-27-crown-9 pyridyl cryptand and a viologen
Pederson, Adam M.-P.,Gibson, Harry W.,Slebodnick, Carla
, p. 452 - 455 (2020/07/07)
The adventitious isolation and crystal structure of a pseudorotaxane complex of a trans-substituted dibenzo-27-crown-9-based pyridyl cryptand (6) and N,N’-dimethyl-4,4?-bipyridinium bis(hexafluorophosphate) (5) are reported.
NOVEL ISOINDOLINE DERIVATIVE, AND PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF
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Paragraph 0126; 0128; 0130, (2020/01/22)
Disclosed are a novel isoindoline derivative, a pharmaceutical composition and use thereof. The compound of formula I, or the pharmaceutically acceptable salt, solvate, polymorph, co-crystal, stereoisomer, isotopic compound, metabolite or prodrug thereof disclosed in the invention can regulate the generation and/or activity of PDE4 and/or TNF-α so as to effectively treat cancer and inflammatory diseases.
Compound for treating or preventing hepatopathy (by machine translation)
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Paragraph 0135-0136; 0140, (2019/10/01)
The invention discloses a compound, an optical isomer or a pharmaceutically acceptable salt, an optical isomer or a pharmaceutically acceptable salt thereof for treating or preventing hepatopathy, and the compound, optical isomer or pharmaceutically acceptable salt thereof can be applied to the preparation of a medicine for treating or preventing liver diseases. (by machine translation)
Type III-C rotaxane dendrimers: Synthesis, dual size modulation and: In vivo evaluation
Kwan, Chak-Shing,Wang, Tao,Li, Min,Chan, Albert S. C.,Cai, Zongwei,Leung, Ken Cham-Fai
supporting information, p. 13426 - 13429 (2019/11/16)
Type III-C rotaxane dendrimers were synthesized by a divergent approach. Dual shuttling behavior and size modulation were observed from non-methylated/methylated rotaxane dendrimers under the same external stimuli. The biological distribution of dendrimers in C57BL/6J mice determined by MALDI-TOF-MS shows predominant accumulation in the spleen and liver. Drug encapsulations with chlorambucil and lithocholic acid were demonstrated.
Discovery of N-hydroxy-3-alkoxybenzamides as direct acid sphingomyelinase inhibitors using a ligand-based pharmacophore model
Yang, Kan,Nong, Keyi,Gu, Qinlan,Dong, Jibin,Wang, Jinxin
, p. 389 - 400 (2018/04/12)
Acid sphingomyelinase (ASM) has been shown to be involved in many physiological processes, emerging to be a promising drug target. In this study, we constructed a ligand-based pharmacophore model of ASM inhibitors and applied this model to optimize the lead compound α-mangostin, a known inhibitor of ASM. 23 compounds were designed and evaluated in vitro for ASM inhibition, of these, 10 compounds were found to be more potent than α-mangostin. This high hit ratio confirmed that the presented model is very effective and practical. The most potent hit, 1c, was found to selectively and competitively inhibit the enzyme and inhibit the generation of ceramide in a dose-dependent manner. Furthermore, 1c showed favorable anti-apoptosis and anti-inflammatory activity. Interactions with key residues and the Zn2+ cofactor of 1c were found by docking simulation. These results provide promising leads and important guidance for further development of efficient ASM inhibitors and drug candidates.
AMIDO THIADIAZOLE DERIVATIVES AS NADPH OXIDASE INHIBITORS
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Page/Page column 63, (2016/07/05)
The present invention is related to amino thiazole derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
A novel benzoyl amide compounds
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Paragraph 0477-0479, (2016/11/21)
The invention relates to the field of medicinal chemistry, in particular to a novel benzamides compound or a salt acceptable in parmacy of the novel benzamides compound, a preparation method of the novel benzamides compound, a pharmaceutical composition containing the novel benzamides compound and an application of the pharmaceutical composition in preparation of antineoplastic drugs.
One-step radiosynthesis of18F-IRS: A novel radiotracer targeting mutant EGFR in NSCLC for PET/CT imaging
Xiao, Zunyu,Song, Yan,Wang, Kai,Sun, Xilin,Shen, Baozhong
supporting information, p. 5985 - 5988 (2016/12/09)
EGFR (epidermal growth factor receptor) targeted therapy has shown great success in clinical comparing with chemotherapy in EGFR mutation NSCLCs. Such as, gefitinib, first generation EGFR TKI, has obviously prolonged the FPS (progression free survival) of the subgroup of patients, but to those who did not get a certain mutation in EGFR kinase domain, the outcome is poor. In view of this situation, scientists have synthesized many radiotracers for selecting the right people by PET/CT imaging to NSCLC TKI therapy. In this study, we developed a novel PET radiotracer18F-IRS in one-step with a radio yield 20% (non-corrected), radiochemistry > 98.5%, specific activity > 105G Bq/μmol, the pharmacokinetics and capacity of the tracer binding to mutant EGFR were evaluated both in vitro and in vivo.
ANTIVIRAL COMPOUNDS
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Paragraph 0251; 0254, (2016/09/26)
Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus v
