更新于：2024-06-24
Topiroxostat
托匹司他
更新于：2024-06-24
概要
基本信息
非在研机构- |
最高研发阶段批准上市 |
最高研发阶段(中国)临床3期 |
特殊审评- |
登录后查看首次获批时间轴
结构
分子式C13H8N6 |
InChIKeyUBVZQGOVTLIHLH-UHFFFAOYSA-N |
CAS号577778-58-6 |
关联
51
项与 托匹司他 相关的临床试验托匹司他片人体生物等效性研究（空腹）
浙江兄弟药业有限公司研制的托吡司特片（规格：60 mg）与株式会社富士薬品托吡司特片（规格：60 mg；商品名：TOPILORIC®）在中国健康受试者中进行的单中心、随机、开放、两制剂、空腹/餐后、单次给药、2序列、4周期、交叉设计的生物等效性研究
托吡司特片随机、开放、单剂量、两制剂、重复交叉设计在中国健康受试者中的生物等效性试验
100 项与 托匹司他 相关的临床结果
登录后查看更多信息
100 项与 托匹司他 相关的转化医学
登录后查看更多信息
100 项与 托匹司他 相关的专利（医药）
登录后查看更多信息
405
项与 托匹司他 相关的文献（医药）2024-03-01Journal of clinical pharmacology
Urate‐Lowering Drugs and Muscle Injury: A Systematic Review and Network Meta‐Analysis
Review
作者: Morizumi, Makoto ; Narita, Ichiei ; Mitsuboshi, Satoru ; Kotake, Kazumasa ; Kaseda, Ryohei
Abstract:
Several urate‐lowering drugs have been linked to muscle injury. This study investigated the association of oral urate‐lowering drugs with the risk of muscle injury by performing a network meta‐analysis of randomized and non‐randomized controlled trials. A systematic search of MEDLINE, via PubMed, the ClinicalTrials.gov website, and the Cochrane Central Register of Controlled Trials was conducted to identify relevant studies with a primary outcome of “all muscle injuries.” A random‐effects model was used to perform a frequentist network meta‐analysis to estimate whether there was significant heterogeneity among the studies. In total, 32 studies including 28,327 participants with 2694 (9.5%) “all muscle injuries” were assessed, and the overall risk of bias was judged to be low to moderate. No statistically significant differences were found between placebo and 6 urate‐lowering therapies: allopurinol (risk ratio, RR, 1.05; 95% confidence interval, 95%CI, 0.63‐1.73), febuxostat (RR 1.10, 95%CI 0.71‐1.70), lesinurad (RR 7.00, 95%CI 0.31‐160.36), lesinurad concomitant with allopurinol (RR 0.85, 95%CI 0.34‐2.11), lesinurad concomitant with febuxostat (RR 1.97, 95%CI 0.55‐7.03), and topiroxostat (RR 0.99, 95%CI 0.37‐2.65). The findings suggest that there is little need to consider the risk of muscle injury when using urate‐lowering drugs in the clinical setting.
Scientific reports
Exploration of nonlinear optical properties of 4-methyl-4H-1,2,4-triazol-3-yl)thio)-N-phenylpropanamide based derivatives: experimental and DFT approach
Article
作者: Wu, Gang ; Bibi, Shamsa ; Chen, Ke ; Alhokbany, Norah ; Khan, Hammad Ali ; Ali, Akbar ; Khan, Samreen Gul ; Irfan, Muhammad ; Rasool, Faiz
Abstract:
Triazoles, nitrogen-containing heterocycles, have gained attention for their applications in medicinal chemistry, drug discovery, agrochemicals, and material sciences. In the current study, we synthesized novel derivatives of N-substituted 2-((5-(3-bromophenyl)-4-methyl-4H-1,2,4-triazol-3-yl)thio)-N-phenylpropanamide and conducted a comprehensive investigation using density functional theory (DFT). These novel structural hybrids of 1,2,4-triazole were synthesized through the multi-step chemical modifications of 3-bromobenzoic acid (1). Initially, compound 1 was converted into its methyl-3-bromobenzoate (2) which was then transformed into 3-bromobenzohydrazide (3). The final step involved the cyclization of compound 3, producing its 1,2,4-triazole derivative (4). This intermediate was then coupled with different electrophiles, resulting in the formation of the final derivatives (7a–7c). Additionally, the characterization of these triazole-based compounds (7a, 7b, and 7c) were carried out using techniques such as IR, HNMR, and UV–visible spectroscopy to understand their structural and spectroscopic properties. The DFT study utilized M06/6-311G(d,p) functional to investigate geometrical parameters, HOMO–LUMO energies, natural bond orbital analyses, transition density matrix (TDM), density of states, and nonlinear optical (NLO) properties. The FMO analysis revealed that compound 7c exhibited the lowest band gap value (4.618 eV). Notably, compound 7c exhibited significant linear polarizability (4.195 > × 10–23) and first and second hyperpolarizabilities (6.317 > × 10–30, 4.314 × 10–35), signifying its potential for nonlinear optical applications. These NLO characteristics imply that each of our compounds, especially 7c, plays a crucial part in fabricating materials showing promising NLO properties for optoelectronic applications.
2024-01-01Chemical biology & drug design
Design, synthesis, and molecular docking studies of benzimidazole‐1,3,4‐triazole hybrids as carbonic anhydrase I and II inhibitors
Article
作者: Bostancı, Hayrani Eren ; Özkay, Yusuf ; Acar Çevik, Ulviye ; Çelik, İsmail ; Küçükoğlu, Kaan ; Işık, Ayşen ; Nadaroglu, Hayrunnisa ; Kaplancıklı, Zafer Asım
Abstract:
In this study, with an aim to develop novel heterocyclic hybrids as potent enzyme inhibitors, we synthesized a series of 10 novel 2‐(4‐(4‐ethyl‐5‐(2‐(substitutedphenyl)‐2‐oxo‐ethylthio)‐4H‐1,2,4‐triazol‐3‐yl)‐phenyl)‐5,6‐dimethyl‐1H‐benzimidazole (5a–5j) derivatives and characterized by 1H‐NMR, 13C‐NMR, and HRMS. These compounds were evaluated for their inhibitory activity against hCA I and hCA II. All the compounds exhibited good hCA I and hCA II inhibitory activities with IC50 values in range of 1.288 μM–3.122 μM. Among all these compounds, compound 5e, with an IC50 value of 1.288 μM is the most active against carbonic hCA I. Compound 5h with an IC50 value of 1.532 μM is the most active against carbonic hCA‐II. Compounds 5a–5j were also evaluated for their cytotoxic effects on the L929 mouse fibroblast (normal) cell line. The compounds were also analyzed for their antioxidant capacity by TAS, FRAP, and DPPH activity. Enzyme inhibition kinetics showed all compounds 5a–5j to inhibit the enzyme by non‐competitive. The most active compound 5e for hCA I and compound 5h for hCA‐II were subjected to molecular docking, which revealed their binding interactions with the enzyme's active site, confirming the experimental findings.
100 项与 托匹司他 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 痛风 | 日本 | 2013-06-28 | |
| 痛风 | 日本 | 2013-06-28 | |
| 痛风 | 日本 | 2013-06-28 | |
| 高尿酸血症 | 日本 | 2013-06-28 | |
| 高尿酸血症 | 日本 | 2013-06-28 | |
| 高尿酸血症 | 日本 | 2013-06-28 |
未上市
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 糖尿病肾病 | 临床2期 | 日本 | 2014-12-30 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | serum urate levels | urinary albumin excretion | - | 構襯製範壓鹽鹽襯鬱選(構選壓壓窪鏇製餘淵鑰) = 製網範製鑰顧糧繭繭夢 膚餘窪艱築蓋襯窪醖膚 (衊襯憲積淵蓋網範觸鑰 ) | 积极 | 2015-05-21 | ||
Placebo | 構襯製範壓鹽鹽襯鬱選(構選壓壓窪鏇製餘淵鑰) = 網壓淵獵膚壓襯築淵築 膚餘窪艱築蓋襯窪醖膚 (衊襯憲積淵蓋網範觸鑰 ) |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用