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Recent patents on therapeutic activities of xanthohumol: a prenylated chalconoid from hops (Humulus lupulus L.). 黄腐酚:一种从啤酒花(Humulus lupulus L.)中提取的烯基化chalconoid。
IF 1.3 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-01-01 Epub Date: 2021-01-15 DOI: 10.4155/ppa-2020-0026
Diwakar Aggarwal, Sushil K Upadhyay, Raj Singh, Hardeep S Tuli

There is expanding proof that specific natural compounds found in plants have additional conventional medicinal properties. One such compound is xanthohumol (XN), which is being explored as an antimicrobial, anticarcinogenic, antidiabetic and anti-inflammatory agent - aside from its utilization in dealing with conditions like autism, bone and skin improvement and microbial infections, lipid-related illnesses, and so on. XN is reported to suppress the uncontrolled production of inflammatory mediators responsible for diseases including cardiovascular disease, neurodegeneration and tumors. Further, it is accounted to limit adipogenesis and control obesity by focusing on principal adipocyte marker proteins. It is most generally utilized in the brewing industry as an additive and flavoring agent to add bitterness and aroma to beer. Present investigation sum up the patents filed in most recent 2 years on development of different pharmaceutical mixes and strategies dependent on various therapeutic potentials of XN.

越来越多的证据表明,在植物中发现的特定天然化合物具有额外的传统药用特性。其中一种化合物是黄腐酚(XN),除了用于治疗自闭症、骨骼和皮肤改善、微生物感染、脂质相关疾病等疾病外,它还被用作抗菌、抗癌、抗糖尿病和抗炎剂。据报道,XN可抑制导致心血管疾病、神经变性和肿瘤等疾病的炎症介质的不受控制的产生。此外,它被认为通过关注主要脂肪细胞标记蛋白来限制脂肪生成和控制肥胖。它在酿造工业中最常用作添加剂和调味剂,以增加啤酒的苦味和香气。本调查总结了近2年来根据XN的不同治疗潜力开发不同药物组合和策略的专利申请。
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引用次数: 5
Mnk inhibitors: a patent review. 锰酸盐抑制剂:专利审查。
IF 1.3 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-01-01 Epub Date: 2021-01-14 DOI: 10.4155/ppa-2020-0028
Ahmed M Abdelaziz, Mingfeng Yu, Shudong Wang

The alteration of mRNA translation has a crucial role in defining the changes in cellular proteome. The phosphorylation of eukaryotic initiation factor 4E by mitogen-activated protein kinase-interacting kinases (Mnks) leads to the release and translation of mRNAs of specific oncogenic proteins. In recent years, the efforts made by the pharmaceutical industry to develop novel chemical skeletons to create potent and selective Mnk inhibitors have been fruitful. The pyridone-aminal scaffold has been utilized to generate several series of Mnk inhibitors presented in multiple patent applications and research articles. Tomivosertib (eFT508) is one of the molecules with such scaffold. It is one of the first two Mnk inhibitors that entered clinical trials, and has displayed momentous activity against several solid and hematological cancers. The present compilation provides a succinct review of the current state of development of pyridone-aminal-derived Mnk inhibitors through the analysis of relevant patent applications filed in the last 5 years.

mRNA翻译的改变在确定细胞蛋白质组的变化中起着至关重要的作用。真核起始因子4E被丝裂原激活的蛋白激酶相互作用激酶(Mnks)磷酸化,导致特定致癌蛋白mrna的释放和翻译。近年来,制药行业开发新型化学骨架以制造有效和选择性的Mnk抑制剂的努力取得了丰硕成果。吡啶酮-动物支架已被用于生成多个系列的Mnk抑制剂,并在多个专利申请和研究文章中提出。Tomivosertib (eFT508)就是具有这种支架的分子之一。它是首批进入临床试验的两种Mnk抑制剂之一,并已显示出对几种实体和血液系统癌症的重大活性。本文通过对近5年来相关专利申请的分析,简要回顾了吡酮-氨基衍生的Mnk抑制剂的发展现状。
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引用次数: 8
Repurposing drugs during the COVID-19 pandemic and beyond. 在 COVID-19 大流行期间及其后重新设计药物用途。
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2021-01-01 Epub Date: 2021-01-15 DOI: 10.4155/ppa-2020-0031
Srividya Ravi, Sammita Jadhav, Anuradha Vaidya, Ravindra Ghooi
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引用次数: 0
Recent patents in dengue disease management. 登革热疾病管理方面的最新专利。
IF 1.3 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2020-12-01 Epub Date: 2020-12-22 DOI: 10.4155/ppa-2020-0012
Sukhbir K Shahid

Dengue, an illness caused by four serotypes of the dengue virus is most prevalent in Asia and Latin America. Its manifestation varies from asymptomatic cases to severe forms and even deaths and is a growing health concern. Despite attempts to curtail it, the infection continues to intensify in endemic areas and spread to new areas of the world. Development of a safe and effective vaccine and a potent antiviral drug is ongoing but so far there has been no breakthrough. Nonetheless, researchers are carrying out studies with newer vaccine candidates and antiviral moieties, and some of these hold promise for the future. The current article describes the recent patents targeted at dengue control.

登革热是一种由四种血清型登革热病毒引起的疾病,在亚洲和拉丁美洲最为流行。其表现从无症状病例到严重形式甚至死亡不等,是一个日益严重的健康问题。尽管采取了遏制措施,但这种感染在流行地区继续加剧,并蔓延到世界上新的地区。目前正在研制安全有效的疫苗和强效抗病毒药物,但迄今尚未取得突破。尽管如此,研究人员正在对较新的候选疫苗和抗病毒部分进行研究,其中一些在未来有希望。本文描述了最近针对登革热控制的专利。
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引用次数: 0
Two drugs facing key patent expirations and potential generic entry from November 2020 to December 2020. 2020年11月至2020年12月,两种药物面临关键专利到期和可能进入仿制药市场。
IF 1.3 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2020-12-01 Epub Date: 2020-12-22 DOI: 10.4155/ppa-2020-0033
Yali Friedman
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引用次数: 0
Patent Prosecution Highway program in Brazil and second medical indication patents challenges. 巴西专利审查高速公路项目和第二医学指征专利挑战。
IF 1.3 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2020-12-01 Epub Date: 2020-12-04 DOI: 10.4155/ppa-2020-0024
Carlos A Suganuma, Erica Mano
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引用次数: 0
Patent highlights June-July 2020. 专利要点 2020 年 6 月至 7 月。
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2020-12-01 Epub Date: 2020-12-04 DOI: 10.4155/ppa-2020-0027
Hermann Am Mucke

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

与制药和医疗研发相关的专利文献中值得关注的最新进展快照。
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引用次数: 0
Selective inhibitors of human lactate dehydrogenase A to fight against metabolic cancer: a patent landscape. 人类乳酸脱氢酶A选择性抑制剂对抗代谢性癌症:专利景观。
IF 1.3 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2020-12-01 Epub Date: 2020-12-04 DOI: 10.4155/ppa-2020-0025
Vinit Kumar, Reshma Rani
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引用次数: 2
Patent highlights April-May 2020. 2020 年 4 月至 5 月的专利要点。
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2020-09-01 Epub Date: 2020-09-22 DOI: 10.4155/ppa-2020-0018
Hermann Am Mucke

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

与制药和医疗研发相关的专利文献中值得关注的最新进展快照。
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引用次数: 0
Three drugs facing key patent expirations and potential generic entry from September to October 2020. 2020年9月至10月,三种药物面临关键专利到期和可能进入仿制药市场。
IF 1.3 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2020-09-01 Epub Date: 2020-10-22 DOI: 10.4155/ppa-2020-0029
Yali Friedman
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引用次数: 0
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