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更新于：2025-04-08
Mirodenafil dihydrochloride
更新于：2025-04-08
概要
基本信息
原研机构 |
非在研机构- |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)临床3期 |
特殊审评- |
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结构/序列
分子式C8H11N |
InChIKeyRIWRFSMVIUAEBX-UHFFFAOYSA-N |
CAS号103-67-3 |
关联
3
项与 Mirodenafil dihydrochloride 相关的临床试验NCT05531526
A Phase 3 Double-blind, Randomized, Placebo-controlled, Multi-center Trial to Evaluate the Efficacy and Safety of AR1001 Over 52 Weeks in Participants with Early Alzheimer's Disease (Polaris-AD)
NCT03625622
A Double-Blind, Randomized, Placebo-Controlled Study to Evaluate Efficacy and Safety of 26-Week Treatment of AR1001 in Patients With Mild to Moderate Alzheimer's Disease
CTR20244348
一项评价AR1001治疗早期阿尔茨海默病受试者持续52周的有效性和安全性的III期、双盲、随机、安慰剂对照、多中心试验
100 项与 Mirodenafil dihydrochloride 相关的临床结果
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100 项与 Mirodenafil dihydrochloride 相关的转化医学
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100 项与 Mirodenafil dihydrochloride 相关的专利（医药）
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4,629
项与 Mirodenafil dihydrochloride 相关的文献（医药）2025-06-01SEPARATION AND PURIFICATION TECHNOLOGY
Energy-efficient CO2 capture using novel low-viscosity water-lean aromatic amine solvent MBA/BDMA/EG/H2O: Performance, mechanism and thermodynamics
作者: Chi, Shudan ; Yang, Linjun ; Li, Wenrui ; Yu, Hang ; Hou, Dawei ; Wang, Xin ; Jin, Lijian ; Kong, Sining ; Yang, Hangqi ; Hou, Xueyan
To address the challenges of high regeneration energy and corrosion in traditional mixed amine absorbents, as well as the increased viscosity issues in water-lean absorbents post-saturation, this study introduces the co-solvent ethylene glycol (EG) to replace part of the water in the high stability N-methylbenzylamine (MBA) and N, N-dimethylbenzylamine (BDMA) systems, resulting in a novel water-lean aromatic amine solvent, MBA/BDMA/EG/H2O, is proposed as an alternative solutionThe addition of the tertiary amine BDMA significantly enhanced the regeneration efficiency of the absorbent.When the mass ratio of MBA/BDMA/EG/H2O is set at 1.5:1.5:3.5:3.5, the CO2 loading reaches 0.36 mol/mol, while the viscosity is only 10.82 mPa·s at room temperatureThe CO2 capture mechanism of this absorbent was elucidated using 13C NMR and quantum chem. calculationsInitially, CO2 reacts with MBA to form MBACOO-/MBAH+.Subsequently, MBA+COO- undergoes deprotonation to produce MBAH+ and BDMAH+.As the concentration of free MBA decreases to a certain level, BDMA undergoes hydrolysis, resulting in the formation of HCO-3.In the later stages of absorption, some of the carbamate products convert to unstable alkyl carbonates by reaction with EG.Notably, the regeneration energy of MBEH is reduced by 21.1% (estimate), compared to 30% MEA aqueous solutionThe corrosion rate of 30% MEA (after absorption) on carbon steel is 3.6 times higher than that of MBEH (after absorption).Therefore, the proposed MBEH solution presents a promising absorbent with excellent desorption performance, low viscosity, reduced regeneration energy, and low corrosion rate.
2025-04-01JOURNAL OF MOLECULAR STRUCTURE
Synthesis, biological activity, X-ray crystallographic, molecular docking and molecular dynamics simulation studies of pyrazole-1,3,5-triazine derivatives as potential butyrylcholinesterase inhibitors
作者: Hu, Peng-hong ; Bo Ding ; Yue Yang ; Zhao, Zhi-hai ; Chen, Si-zhu ; Shi, Da-Hua ; Xu, Lin-yu ; Ran He ; Cao, Yao-yao ; Rui-Zhu ; Xue, Xuan-Yi ; Cao, Yang ; Wei, Ming-yu
Thirteen novel pyrazole-1,3,5-triazine derivatives were synthesized and assessed for their potential as cholinesterase inhibitors.The structure of the compounds was characterized through 1H NMR, 13C NMR, IR, and HRMS.The purity of all compounds was determined by HPLC.The structure of compound 4j was further investigated by single-crystal X-ray diffraction, and compound 4j possesses a monoclinic crystal system with space group P21/c.The mol. conformation, crystal packing mode, and mol. interactions were discussed in depth through Hirshfeld surfaces and two-dimensional fingerprint diagrams.The in vitro enzyme inhibitory activity assays determined that all compounds showed weak inhibitory activity of acetylcholinesterase (AChE), and some compounds had selective inhibitory effect on butyrylcholinesterase (BuChE).Among them, compound 4h (Et 1-(4-chloro-6-(4-methylpiperidin-1-yl)-1,3,5-triazin-2-yl)-1H-pyrazole-3-carboxylate) exhibited the strongest inhibitory effect on BuChE, with an IC50 value of 1.03 ± 0.29 μM, closely approaching that of the pos. control donepezil (IC50 = 0.52 ± 0.04 μM).Mol. docking experiments demonstrated stable interaction between compound 4h and key amino acids in both the catalytic active site (CAS) and peripheral anionic site (PAS) of BuChE.Mol. dynamics simulations show that compound 4h can stably bind to BuChE.Simultaneously, the experiment further substantiated that compound 4h exhibited an excellent metal chelating effect with Cu(II).Furthermore, the prediction of absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties indicated characteristics suggestive of potential drug candidacy for these compoundsHence, compound 4h may be a selective BuChE inhibitor for the treatment of Alzheimer′s disease.
2025-04-01ADVANCED FUNCTIONAL MATERIALS
From Original Ferrocene‐Based Small‐Molecule Design to Multifunctional Supramolecular Bactericides: Their Efficient Applications in Controlling Biofilm‐Associated Bacterial Infections
作者: He, Xinyu ; Zhao, Haicong ; Wang, Peiyi ; Chen, Xue ; Yang, Jinghan ; Liu, Min
Abstract:
Conventional bactericides struggle with biofilm barriers and inefficient deposition on hydrophobic leaves, resulting in undesirable control of plant bacterial diseases. To overcome these challenges, an innovative ferrocene‐based small‐molecule (FccA8R) is conceived, featuring biofilm disruption capabilities. Further optimizing FccA8R with seven‐membered oligosaccharide‐involved host–guest supramolecular strategy creates two kinds of biocompatible multifunctional supramolecular nanospheres (FccA8R@β‐CD and FccA8R@HP‐β‐CD). This manipulation efficiently eradicates mature biofilm barriers while enhancing droplet retention on hydrophobic leaves. At a concentration of 56.64 µg mL−1, the two materials remove Xanthomonas‐biofilms by 76.32–76.83%, notably surpassing that of single FccA8R (57.96%). Their versatility extends to the enhanced inhibition of bacterial motility, extracellular enzymes secretion, and exopolysaccharides production, all reducing the bacterial virulence. In vivo pot experiments, FccA8R@β‐CD and FccA8R@HP‐β‐CD demonstrate workable control efficacies of 48.91–52.03% against rice bacterial blight at 200 µg mL−1, superior to the commercial thiodiazole‐copper‐20%SC (36.42%) and FccA8R‐0.1%Tween (39.54%). Furthermore, these supramolecular assemblies disclose broad‐spectrum bactericidal efficacy (71.45–73.19%) against kiwifruit canker, significantly higher than thiodiazole‐copper‐20%SC (43.05%) and FccA8R‐0.1%Tween (57.24%). Besides, supramolecular bactericides are safe for plants and non‐target organisms like zebrafish and earthworms. Briefly, this research builds a key foundation for creating green bactericides from small‐molecule conception to eco‐friendly supramolecular assemblies, realizing the prevention of bacterial diseases and environmental safety.
25
项与 Mirodenafil dihydrochloride 相关的新闻（医药）2024-12-31
2024-12-27
临床2期临床3期申请上市临床成功
100 项与 Mirodenafil dihydrochloride 相关的药物交易
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研发状态
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 阿尔茨海默症 | 临床3期 | 美国 | 2022-12-23 | |
| 阿尔茨海默症 | 临床3期 | 中国 | 2022-12-23 | |
| 阿尔茨海默症 | 临床3期 | 捷克 | 2022-12-23 | |
| 阿尔茨海默症 | 临床3期 | 丹麦 | 2022-12-23 | |
| 阿尔茨海默症 | 临床3期 | 法国 | 2022-12-23 | |
| 阿尔茨海默症 | 临床3期 | 德国 | 2022-12-23 | |
| 阿尔茨海默症 | 临床3期 | 意大利 | 2022-12-23 | |
| 阿尔茨海默症 | 临床3期 | 荷兰 | 2022-12-23 | |
| 阿尔茨海默症 | 临床3期 | 波兰 | 2022-12-23 | |
| 阿尔茨海默症 | 临床3期 | 西班牙 | 2022-12-23 |
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适应症
分期
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临床2期 | 210 | 齋鹽鹹顧鏇積齋蓋醖齋(積蓋艱膚構淵選廠繭遞) = 獵夢願膚鹹願膚蓋餘製 鬱鹽網簾餘鬱憲壓願鏇 (糧夢顧廠壓鹹夢構壓簾 ) | 积极 | 2021-11-04 | |||
獵繭範顧遞憲糧憲網遞(遞壓蓋壓選範繭網糧鑰) = 鏇餘繭齋醖淵網簾齋範 鬱艱製壓築鑰鹹壓積蓋 (醖製築衊齋網窪網築繭 ) 更多 |
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