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4-(Imidazo[1,2-a]pyridin-3-yl): pyrimidine derivatives as anticancer agents. 4-(咪唑并[1,2-a]吡啶-3-基):作为抗癌剂的嘧啶衍生物。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 Epub Date: 2022-11-10 DOI: 10.4155/ppa-2022-0033
Rami A Al-Horani

A series of 4-(imidazo[1,2-a]pyridin-3-yl)-pyrimidine derivatives are claimed as inhibitors of c-KIT and as potential treatments for cancer. Their chemical preparation and biological evaluation against imatinib-resistant tumor cells have been described. Several claimed molecules have excellent IC50 values in the nanomolar range. Several molecules were also selective against a wide panel of kinases. Few specific inhibitors have been found to have promising oral bioavailability and acceptable to excellent values regarding the inhibition of hERG channel. This class represents a new platform for developing new anticancer treatment against a wide range of c-KIT mutations and secondary mutations that may arise in gastrointestinal stromal tumor patients.

一系列 4-(咪唑并[1,2-a]吡啶-3-基)嘧啶衍生物被认为是 c-KIT 的抑制剂和潜在的癌症治疗药物。这些衍生物的化学制备方法和针对伊马替尼耐药肿瘤细胞的生物学评价已经得到描述。一些声称的分子具有极佳的 IC50 值,在纳摩尔范围内。一些分子还对多种激酶具有选择性。研究发现,少数特异性抑制剂具有良好的口服生物利用度,对 hERG 通道的抑制作用也达到了可接受甚至优异的水平。这类药物代表了一种新的平台,可用于开发针对胃肠道间质瘤患者可能出现的各种 c-KIT 突变和继发性突变的新型抗癌疗法。
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引用次数: 0
Photoresponsive liposomes: an alternative of ELISA for the detection of low quantities of target substances. 光反应性脂质体:用于检测少量目标物质的ELISA替代方法。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.4155/ppa-2022-0046
Ramesh Joga, Hitesh Kumar Behera, Chetan Dushant Sabanis, Simran, Sandeep Kumar, Neeraj Kumar

Photoresponsive liposome development is needed to serve as a facile alternative to ELISA which is ineffective for detecting small levels of biomarkers due to low detection sensitivity. The US20210396744 patent application outlines novel photoresponsive liposomes for the detection of target substances with the aid of light. Although versatile, there may be possible stability issues that can be avoided with the appropriate selection of liposome components. Furthermore, the clinical success of this technology depends on many parameters like plasma stability, efficient loading of photosensitive components in the membrane and immobilization of molecular recognition elements to the membrane. Despite several challenges, they possess enormous potential to become a non-invasive tool for the detection of target substances.

光反应性脂质体的开发需要作为一种简便的替代ELISA,由于检测灵敏度低,对于检测小水平的生物标志物无效。US20210396744专利申请概述了用光检测目标物质的新型光反应脂质体。虽然用途广泛,但可能存在稳定性问题,可以通过适当选择脂质体成分来避免。此外,该技术的临床成功取决于许多参数,如等离子体稳定性,膜中光敏成分的有效负载以及分子识别元件在膜上的固定。尽管存在一些挑战,但它们具有成为检测目标物质的非侵入性工具的巨大潜力。
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引用次数: 1
Patent developments via Schiff bases in medicinal chemistry. 药物化学中希夫碱基的专利开发。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.4155/ppa-2022-0045
Maham Haider, Khalid Mohammed Khan
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引用次数: 0
Patent Highlights June-July 2022. 专利亮点2022年6月至7月。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.4155/ppa-2022-0043
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
Co-processed tablet excipient composition, its preparation and use: US10071059 B2: patent spotlight. 共加工片剂辅料组成,其制备及用途:US10071059 B2:专利聚光灯。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.4155/ppa-2022-0036
Sajal Jain, Ritu Rathi, Upendra Nagaich, Inderbir Singh

Co-processing involves the incorporation of one excipients into the particle structure of other excipients to overcome the deficiencies of each excipients. The current patent describes the co-processing of microcrystalline cellulose and mannitol via fluid bed agglomeration with an aim to limit the use of lubricant in tablet composition. The co-processed excipients blend was compared with the physical blend of excipients and characterized for scanning electron microscopy, disintegration and hardness. The average particle size of co-processed excipients was less than 0.55 mm, characterized by large individual lactose-coated particles whereas, the physical blend particles are uncoated and irregular in shape. Tablets made from both physical blend and co-processed excipients were compared. As per the hardness and disintegration studies, with increase in mixing time of excipients both hardness and disintegration time decreases.

协同加工包括将一种赋形剂结合到其他赋形剂的颗粒结构中,以克服每种赋形剂的缺陷。目前的专利描述了通过流化床团聚的微晶纤维素和甘露醇的协同加工,目的是限制润滑剂在片剂组合物中的使用。将共制辅料与物理共制辅料进行了比较,并对共制辅料进行了扫描电镜、崩解和硬度表征。共加工辅料的平均粒径小于0.55 mm,具有较大的单个乳糖包被颗粒,而物理共加工辅料颗粒无包被,形状不规则。比较了物理混合和共加工辅料制成的片剂。硬度和崩解研究表明,随着辅料混合时间的增加,硬度和崩解时间均减小。
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引用次数: 0
Patenting trends in the pharmaceutical field of Mexican universities. 墨西哥大学制药领域的专利趋势。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.4155/ppa-2022-0048
Gabriela Sanchez-Esgua, Juan Reyes-Alvarez, Martin Perez-Santos

Aim: pharmaceutical patenting activity in developing countries, including Mexico, is unknown. Objective: determine the activity of pharmaceutical patents by Mexican universities. Method: using 'university' as keyword and A61K, A61P and C07 as International Patent Classification codes, was searched to generate a perspective of pharmaceutical patent applications by Mexican universities. Results: 227 patents (186 granted patents + 41 not-granted patents) were claimed in the period 2000-2018. The leading university was the National Autonomous University of Mexico, followed by the Instituto Politecnico Nacional, Universidad Autonoma de Nuevo León and Universidad Autonoma de Puebla. The pharmaceutical concerns addressed were led by the fields of infectious, cancer and diabetes. Conclusion: in Mexican universities, the licensing of pharmaceutical patents is still in its early stages.

目的:包括墨西哥在内的发展中国家的药品专利活动尚不清楚。目的:测定墨西哥高校药品专利的活性。方法:以“university”为关键词,以A61K、A61P和C07为国际专利分类代码,检索墨西哥高校药品专利申请情况。结果:2000-2018年共申请专利227件(授权专利186件+未授权专利41件)。排名第一的大学是墨西哥国立自治大学,其次是国立理工学院、新自治大学León和普埃布拉自治大学。讨论的药物问题以传染病、癌症和糖尿病领域为主。结论:在墨西哥的大学中,药物专利的许可仍处于早期阶段。
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引用次数: 0
Oral insulin delivery: a patent review. 口服胰岛素:专利审查。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-11-01 DOI: 10.4155/ppa-2022-0017
Shivani Sharma, Amit Mittal, Anuradha Mehra

Insulin, on oral administration, is very troublesome because of its limited bioavailability. The evolution of oral insulin delivery formulations is greatly desired for non-invasive therapy by overcoming its low bioavailability, GIT enzymatic deactivation, poor lipophilicity and low stability. Different approaches have been proposed to boost oral insulin bioavailability in insulin-delivery systems and emerging effective therapies by using nanoparticle formulation, nanocapsid, modified chitosan particles, polydopamine microcapsules and nanoliposomes. The present review includes patents and patent applications that were published between 2017 and January 2022.

口服胰岛素由于其有限的生物利用度而非常麻烦。口服胰岛素给药配方的发展是非侵入性治疗的迫切需要,克服其低生物利用度,GIT酶失活,亲脂性差和低稳定性。为了提高口服胰岛素在胰岛素输送系统中的生物利用度,人们提出了不同的方法,如纳米颗粒制剂、纳米衣壳、改性壳聚糖颗粒、聚多巴胺微胶囊和纳米脂质体。本次审查包括2017年至2022年1月之间公布的专利和专利申请。
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引用次数: 1
Compulsory licensing of patents. 专利的强制许可。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-11-01 DOI: 10.4155/ppa-2022-0039
Narayanasamy Kumutha, Narayanasamy Amutha, Govindasamy S Venkatesh

Compulsory licensing (CL) is a mechanism made by the government to provide balance between the monopoly right holders and the third person with public interest by ensuring the ease availability of the patented products at reasonable rate. This paper discusses the background criteria for getting CL in India as per the Indian Patent Act, 1970 starting from the concepts outlined in the Trade-Related Aspects of Intellectual Property Rights agreement. We reviewed the case studies for the accepted and rejected CL in India. We also discuss important CL cases that were permitted internationally, including the present COVID pandemic CL. Finally, we provide our analytical perspectives regarding the pros and cons of CL.

强制许可是政府制定的一种机制,旨在通过确保专利产品以合理的价格易于获得,从而在垄断权持有人和具有公共利益的第三人之间取得平衡。本文从《与贸易有关的知识产权协定》中概述的概念出发,讨论了根据1970年《印度专利法》在印度获得CL的背景标准。我们回顾了印度接受和拒绝CL的案例研究。我们还讨论了国际上允许的重要CL病例,包括目前的COVID大流行CL。最后,我们就CL的利弊提供了我们的分析观点。
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引用次数: 5
Papers from the First International Conference on Innovation and Intellectual Property Rights. 首届创新与知识产权国际会议论文。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-11-01 DOI: 10.4155/ppa-2023-0004
Michael Bell, Runjhun Tandon
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引用次数: 1
Therapeutic potential of Pogostemon cablin herb: a comprehensive review. 广藿香的治疗潜力综述。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-11-01 DOI: 10.4155/ppa-2022-0021
Archana Thakur

Pogostemon cablin (Pogostemon patchouli or Patchouli) is known for its essential oil and is a popular medicinal herb in Indian Ayurveda and traditional Chinese medicine. This review covers patent articles on the P. cablin plant's therapeutic effects. The patent literature was collected using a thorough, comprehensive search on databases like Thomson Innovation, Espacenet, Patentscope, The Lens and Patent digital libraries of different Jurisdictions, including IPO, USPTO, CNIPA, inPASS, KIPO, JPO, etc. Despite the vast number of review articles on non-patent literature, none of the articles reviewed the patent literature. This current P. cablin literature analysis study will facilitate bridging the gap between further exploring the potential of this plant through novel investigations.

广藿香(广藿香或广藿香)以其精油而闻名,是印度阿育吠陀和传统中医中很受欢迎的草药。本文综述了有关长叶草治疗作用的专利文章。专利文献是通过对Thomson Innovation、Espacenet、Patentscope、The Lens等数据库和不同司法管辖区的专利数字图书馆(包括IPO、USPTO、CNIPA、inPASS、KIPO、JPO等)进行彻底、全面的检索收集的。尽管有大量关于非专利文献的评论文章,但没有一篇文章对专利文献进行了评论。目前的文献分析研究将有助于通过新的研究进一步探索该植物的潜力。
{"title":"Therapeutic potential of <i>Pogostemon cablin</i> herb: a comprehensive review.","authors":"Archana Thakur","doi":"10.4155/ppa-2022-0021","DOIUrl":"https://doi.org/10.4155/ppa-2022-0021","url":null,"abstract":"<p><p><i>Pogostemon cablin</i> (<i>Pogostemon patchouli</i> or Patchouli) is known for its essential oil and is a popular medicinal herb in Indian Ayurveda and traditional Chinese medicine. This review covers patent articles on the <i>P. cablin</i> plant's therapeutic effects. The patent literature was collected using a thorough, comprehensive search on databases like Thomson Innovation, Espacenet, Patentscope, The Lens and Patent digital libraries of different Jurisdictions, including IPO, USPTO, CNIPA, inPASS, KIPO, JPO, etc. Despite the vast number of review articles on non-patent literature, none of the articles reviewed the patent literature. This current <i>P. cablin</i> literature analysis study will facilitate bridging the gap between further exploring the potential of this plant through novel investigations.</p>","PeriodicalId":20011,"journal":{"name":"Pharmaceutical patent analyst","volume":"11 6","pages":"213-224"},"PeriodicalIF":1.3,"publicationDate":"2022-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9158148","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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Pharmaceutical patent analyst
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