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Remdesivir: an overview of patenting trends, clinical evidence on COVID-19 treatment, pharmacology and chemistry. 瑞德西韦:新冠肺炎治疗的专利趋势、临床证据、药理学和化学综述。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-05-31 DOI: 10.4155/ppa-2021-0023
Sandro G Viveiros Rosa, W. C. Santos
By December 2021, the COVID-19 caused approximately 6.1 million deaths around the world. Several vaccines have been approved, but there is still a need for non-prophylactic treatments for COVID-19. Remdesivir is an antiviral drug approved for emergency use against COVID-19 in several countries, but one of the first clinical trials was inconclusive about the mortality reduction, although the drug showed a reduction in the recovery time of hospitalized patients. Thus, the present investigation revisits the clinical evidence of using remdesivir for COVID-19 treatment, patent status, pharmacology and chemistry. We found 184 families of patents in the Cortellis database, and concerning the clinical evidence, we retrieved 14 systematic reviews with meta-analysis involving remdesivir as a treatment for COVID-19, discussing the reduction of adverse events, hospitalization days, mortality rate and the mechanical ventilation period.
截至2021年12月,新冠肺炎在全球造成约610万人死亡。一些疫苗已经获得批准,但仍需要对新冠肺炎进行非预防性治疗。Remdesivir是一种抗病毒药物,在几个国家被批准紧急用于治疗新冠肺炎,但首批临床试验之一对降低死亡率没有结论,尽管该药物显示住院患者的恢复时间缩短。因此,本研究重新审视了使用瑞德西韦治疗新冠肺炎的临床证据、专利状况、药理学和化学。我们在Cortellis数据库中发现了184个专利家族,关于临床证据,我们检索了14篇涉及瑞德西韦治疗新冠肺炎的系统综述和荟萃分析,讨论了不良事件的减少、住院天数、死亡率和机械通气期。
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引用次数: 2
Patent highlights October-November 2021. 专利亮点2021年10月至11月。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-05-31 DOI: 10.4155/ppa-2022-0003
H. Mucke
A snapshot of noteworthy recent developments in the patent literature of relevance to pharmaceutical and medical research and development.
与药物和医学研发相关的专利文献中值得注意的最新进展的快照。
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引用次数: 0
Patent highlights December 2021-January 2022. 专利亮点2021年12月至2022年1月。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-05-01 Epub Date: 2022-07-21 DOI: 10.4155/ppa-2022-0006
Hermann Am Mucke

A snapshot of noteworthy recent developments in the patent literature of relevance to pharmaceutical and medical research and development.

与制药和医学研究与开发相关的专利文献中值得注意的最新发展概况。
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引用次数: 0
Pharmaceutical agents for the treatment of Chagas disease: patenting trends in the 2016-2021 period. 治疗南美锥虫病的药剂:2016-2021年期间的专利申请趋势
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-05-01 Epub Date: 2022-07-21 DOI: 10.4155/ppa-2022-0005
Viridiana I Flores-Quiroz, Lino Zumaquero-Ríos, Martin Perez-Santos

American trypanosomiasis is a neglected tropical disease and an endemic problem in 21 Latin American countries, whose treatment relies on only two US FDA-approved drugs: benznidazole and nifurtimox. Patent literature reveals vital information on new trends in therapies for various diseases, including Chagas disease. The authors used the patent databases of the world's major patent offices to generate an overview of patent trends related to the treatment of Chagas disease. A total of 50 patent families were collected and grouped as 'small molecules', 'pharmaceutical compositions of known compounds' and vaccines. From the results and interpretation, it can be concluded that the treatment of Chagas disease receives little attention in the field of patents and that the upward trend is minimal.

美洲锥虫病是一种被忽视的热带病,在21个拉丁美洲国家是一个地方性问题,其治疗仅依赖于两种美国fda批准的药物:苯并硝唑和硝呋替莫。专利文献揭示了包括恰加斯病在内的各种疾病治疗新趋势的重要信息。作者利用世界主要专利局的专利数据库,概述了与恰加斯病治疗有关的专利趋势。总共收集了50个专利族,并将其归类为“小分子”、“已知化合物的药物组合物”和疫苗。从结果和解释中可以得出结论,恰加斯病的治疗在专利领域受到的关注很少,而且上升趋势很小。
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引用次数: 1
Potential of novel self-assembled functionalized carbon nanotubes for selective tumor targeting. 新型自组装功能化碳纳米管选择性靶向肿瘤的潜力。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-05-01 Epub Date: 2022-07-21 DOI: 10.4155/ppa-2022-0001
Chetan D Sabanis, Bharathi R Kannan, Ramesh Joga, Simran, Sandeep Kumar, Neeraj Kumar

Conventional cancer therapies are associated with toxicity toward healthy cells, which need to be addressed by novel therapeutic approaches. US2021/0230592 patent application discloses a carbon nanotube-based approach for tumor targeting, wherein a self-assembling single-wall nanotube complex has been developed and functionalized to deliver a molecule to a cancerous cell. The radiolabeled nanotubes exhibited markedly reduced toxicity as they did not depict any 'over toxicity' up to radioactivity value of 1350 nCi. The single-wall carbon nanotube conjugates were covalently connected to several chelators, therapeutic or diagnostic radionuclides, and showed promising results in the effective cancer management. Besides, this invention with further modifications paves an ideal pathway to researchers in effective diagnosis and treatment of cancer.

传统的癌症治疗与对健康细胞的毒性有关,这需要通过新的治疗方法来解决。US2021/0230592专利申请公开了一种基于碳纳米管的肿瘤靶向方法,其中开发了一种自组装的单壁纳米管复合物,并将其功能化以向癌细胞传递分子。放射性标记的纳米管表现出明显降低的毒性,因为它们没有描述任何“过度毒性”,直到放射性值为1350 nCi。单壁碳纳米管缀合物与几种螯合剂、治疗性或诊断性放射性核素共价连接,在有效的癌症治疗中显示出有希望的结果。此外,本发明经进一步修改,为研究人员有效诊断和治疗癌症铺平了理想的途径。
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引用次数: 1
Baicalein: promising therapeutic applications with special reference to published patents. 黄芩苷:有前景的治疗应用,特别参考已发表的专利。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-03-29 DOI: 10.4155/ppa-2021-0027
Shubhangi Gupta, H. Buttar, Ginpreet Kaur, H. Tuli
Baicalein is a medicinally important flavonoid present in Scutellaria baicalensis, which has numerous biological benefits like anti-oxidant, anti-inflammatory, antihepatotoxicity, anticancer properties, etc. Recent studies have revealed that baicalein is an efficient antihepatoma agent and has the strongest antiproliferative effect toward cancerous bladder cell lines, and suppression of cell cycle progression in prostate cancer cells. This natural substance has a high commercial value because it strengthens the heart and cerebral vessels and protects the nervous system and also reduces diabetes and diabetic complications. In addition, baicalein is known to decrease inflammatory markers such as IL-1β, IL-6 and TNF-α. In this review, we have attempted to compile the list of recent therapeutic patents of baicalein used for treating different disorders.
黄芩素是黄芩中一种重要的药用类黄酮,具有抗氧化、抗炎、抗肝毒性、抗癌等多种生物学功效。近年来的研究表明黄芩素是一种有效的抗肝癌药物,对膀胱癌细胞系的抗增殖作用最强,对前列腺癌细胞的细胞周期进展有抑制作用。这种天然物质具有很高的商业价值,因为它能增强心脏和脑血管,保护神经系统,还能减少糖尿病和糖尿病并发症。此外,已知黄芩素可以降低炎症标志物,如IL-1β, IL-6和TNF-α。在这篇综述中,我们试图汇编黄芩苷最近用于治疗不同疾病的治疗专利清单。
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引用次数: 11
Small-molecule inhibitors of Slack potassium channels as potential therapeutics for childhood epilepsies. 松弛钾通道小分子抑制剂作为儿童癫痫的潜在治疗药物。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-03-01 DOI: 10.4155/ppa-2022-0002
Alshaima'a M Qunies, Kyle A Emmitte
Slack channels are sodium-activated potassium channels that are encoded by the KCNT1 gene. Several KCNT1 gain of function mutations have been linked to malignant migrating partial seizures of infancy. Quinidine is an anti-arrhythmic drug that functions as a moderately potent inhibitor of Slack channels; however, quinidine use is limited by its poor selectivity, safety and pharmacokinetic profile. Slack channels represent an interesting target for developing novel therapeutics for the treatment of malignant migrating partial seizures of infancy and other childhood epilepsies; thus, ongoing efforts are directed toward the discovery of small-molecules that inhibit Slack currents. This review summarizes patent applications published in 2020-2021 that describe the discovery of novel small-molecule Slack inhibitors.
松弛通道是由KCNT1基因编码的钠活化钾通道。几个KCNT1功能突变的增加与婴儿期恶性迁移性部分癫痫发作有关。奎尼丁是一种抗心律失常药物,作为松弛通道的中等有效抑制剂;然而,奎尼丁的使用受到其选择性差、安全性和药代动力学特征的限制。松弛通道代表了一个有趣的目标,开发新的治疗方法,恶性迁移部分癫痫发作的婴儿和其他儿童癫痫;因此,正在进行的努力是为了发现抑制松弛电流的小分子。本文综述了2020-2021年发表的描述新型小分子Slack抑制剂发现的专利申请。
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引用次数: 3
Patent highlights August-September 2021. 专利亮点2021年8月至9月。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-01-01 Epub Date: 2022-02-03 DOI: 10.4155/ppa-2021-0025
Hermann Am Mucke

A snapshot of noteworthy recent developments in the patent literature of relevance to pharmaceutical and medical research and development.

与制药和医学研究与开发相关的专利文献中值得注意的最新发展概况。
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引用次数: 0
Drug repurposing of adapalene for melanoma treatment. 阿达帕林用于黑色素瘤治疗的药物再利用。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-01-01 Epub Date: 2022-02-16 DOI: 10.4155/ppa-2021-0021
Maricruz Anaya-Ruiz, Martin Perez-Santos

Cancer drug repurposing is an attractive approach that leads to savings in time and investment. Adapalene, the first medical application of which was for the treatment of acne, has been described as a repurposing drug for the treatment of various types of cancer. Patent application CN111329851 describes the use of adapalene for the treatment of melanoma, by assays carried out on melanoma cell lines. Adapalene demonstrated antiproliferative activity in melanoma cell lines via S-phase arrest-dependent apoptosis mediated by DNA damage through an increase in the expression of p-ATM and p-chk2 and a decrease in the expression of p-BRCA1 and Rad51. Even though no evidence on efficacy and efficiency is shown in preclinical and clinical studies, CN111329851 patent shows that adapalene may be a repurposing drug for the treatment of melanoma.

癌症药物再利用是一种有吸引力的方法,可以节省时间和投资。阿达帕林,它的第一个医学应用是治疗痤疮,被描述为一种用于治疗各种类型癌症的重新用途药物。专利申请CN111329851描述了通过对黑素瘤细胞系进行测定来治疗黑素瘤的阿达帕烯的使用。阿达帕林通过增加p-ATM和p-chk2的表达以及降低p-BRCA1和Rad51的表达,在DNA损伤介导的s期阻滞依赖性细胞凋亡中显示出抗增殖活性。尽管在临床前和临床研究中没有疗效和效率的证据,但CN111329851专利表明,阿达帕林可能是治疗黑色素瘤的一种再利用药物。
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引用次数: 2
Multicomponent crystal compromising dasatinib and selected co-crystals formers: a patent evaluation of EP2861589B1. 多组分晶体损害达沙替尼和选择的共晶体形成:EP2861589B1的专利评估。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-01-01 Epub Date: 2022-02-17 DOI: 10.4155/ppa-2021-0024
Ritu Rathi, Inderbir Singh

Cocrystallization has gained significant prominence in pharmaceutical product development because of the enhancement of physical, chemical and pharmacological properties of active pharmaceutical ingredients, such as stability, solubility, dissolution rate, taste, hygroscopicity, mechanical property, bioavailability, permeability and therapeutic activity. Traditionally, co-crystals can be prepared by a grinding, solvent evaporation and slurry method. However, sophisticated methods such as spa drying, hot-melt extrusion, supercritical fluid and laser irradiation are also reported to be used for producing co-crystals. The selected patent describes the development of multicomponent crystals of dasatinib, with an aim to enhance the aqueous solubility of a selected drug. However issues surrounding the toxicity, stability, large scale manufacture, in vivo performance in human beings and regulations require adequate addressal prior to exploring the commercial viability of pharmaceutical co-crystals.

由于共结晶技术可以提高药物活性成分的物理、化学和药理学性能,如稳定性、溶解度、溶出率、味道、吸湿性、机械性能、生物利用度、渗透性和治疗活性,因此在药品开发中取得了显著的进展。传统上,共晶可以通过研磨、溶剂蒸发和浆料法制备。然而,复杂的方法,如spa干燥,热熔挤压,超临界流体和激光辐照也被用于生产共晶。所选专利描述了达沙替尼多组分晶体的开发,目的是提高所选药物的水溶性。然而,在探索药用共晶的商业可行性之前,需要充分解决有关毒性、稳定性、大规模生产、人体体内性能和法规的问题。
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引用次数: 2
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Pharmaceutical patent analyst
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