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Bispecific anti-OX40/5T4 antibodies for cancer treatment. 用于癌症治疗的双特异性抗ox40 / 5t4抗体。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2021-03-01 Epub Date: 2021-03-12 DOI: 10.4155/ppa-2020-0030
Martin Perez-Santos

OX40 and 5T4 are molecules that play a role in T-cell expansion and cytoskeleton's disruption in cancer, respectively. US2019161555 patent describes a bispecific antibody that targets OX40/5T4 with the potential application of cancer treatment. The method of analysis of the US201916155 patent consisted of claim's analysis, as well as the chemical/biological information's analysis of the bispecific antibody. The patent includes independent claims related to bispecific antibodies that bind to OX40/5T4, DNA encoding the antibodies, a vector that harbors the DNA, a host cell that contains the vector, a pharmaceutical composition containing a pharmaceutically effective amount of the antibodies, medical use of the antibodies, use of the antibodies in the treatment or prevention of neoplastic disorders and a method of treating neoplastic disorders. Bispecific antibodies that target OX40/5T4 can activate IL-2 secretion in CD4+ T cells.

OX40和5T4分别在癌症中t细胞扩增和细胞骨架破坏中发挥作用。US2019161555专利描述了一种针对OX40/5T4的双特异性抗体,具有癌症治疗的潜在应用。US201916155专利的分析方法包括权利要求分析,以及双特异性抗体的化学/生物信息分析。本专利包括与与OX40/5T4结合的双特异性抗体、编码所述抗体的DNA、含有所述DNA的载体、含有所述载体的宿主细胞、含有所述抗体的药学有效量的药物组合物、所述抗体的医学用途、所述抗体在治疗或预防肿瘤疾病中的使用以及治疗肿瘤疾病的方法相关的独立权利要求。靶向OX40/5T4的双特异性抗体可激活CD4+ T细胞分泌IL-2。
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引用次数: 1
Treatment of solid tumors using bispecific anti-PDL-1/ICOS antibody. 双特异性抗pdl -1/ICOS抗体治疗实体瘤。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2021-03-01 Epub Date: 2021-04-08 DOI: 10.4155/ppa-2020-0035
Martin Perez-Santos, Maricruz Anaya-Ruiz, Gabriela Sanchez-Esgua, Luis Villafaña-Diaz, Diana Barron-Villaverde

PD-L1 and ICOS are immune control points in cancer and their presence in cancer tends to have a poor prognosis. WO2019122882 patent describes a bispecific antibody that targets PDL-1/ICOS with the potential application of cancer treatment. WO2019122882 patent describes a bispecific antibody with antitumor efficacy in CT26 model through of the depletion of TReg cells and improved ratio of CD8+ T cells: TReg in tumor microenvironment. The anti-PDL-1/ICOS antibody is new; however, only preclinical assays are shown using colon carcinoma model. So far, there are no reports of clinical trials to evaluate the safety, toxicity and efficacy, but it will be of great interest to analyze in the future if this antibody surpasses the action of the combinatorial therapy in cancer.

PD-L1和ICOS是肿瘤的免疫控制点,它们在肿瘤中的存在往往预后较差。WO2019122882专利描述了一种针对PDL-1/ICOS的双特异性抗体,具有潜在的癌症治疗应用前景。WO2019122882专利描述了一种通过在肿瘤微环境中耗竭TReg细胞,提高CD8+ T细胞:TReg比例,在CT26模型中具有抗肿瘤功效的双特异性抗体。抗pdl -1/ICOS抗体为新抗体;然而,只有结肠癌模型显示了临床前分析。到目前为止,还没有临床试验的报道来评估其安全性、毒性和有效性,但如果这种抗体在癌症中超过联合治疗的作用,将是未来研究的热点。
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引用次数: 0
Vaccines against antimicrobial resistance: a promising escape route for multidrug resistance. 抗微生物药物耐药性疫苗:一种有希望的多药耐药性逃避途径。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2021-03-01 Epub Date: 2021-04-08 DOI: 10.4155/ppa-2020-0022
Absar Talat, Asad U Khan

Antibiotic resistance has become a global health problem requiring urgent intervention. The pace of development and frequency of transmission of antimicrobial resistance have tremendously surpassed the number of antibiotics developed in the past few decades. Emergence and transmission of multidrug-resistant genes, for example, mcr-1 and mcr-5.3, against the last resort of antibiotics has challenged the treatment options. Vaccination is a promising approach with no instance of antimicrobial resistance generation or transmission reported so far. The time required for developing a vaccine, extensive pre- and post-licensure studies and the financial constraints for the R&D has hampered vaccine development over the past few decades. Vaccine can prove to be an effective future strategy for combating antimicrobial resistance.

抗生素耐药性已成为一个需要紧急干预的全球卫生问题。抗生素耐药性的发展速度和传播频率大大超过了过去几十年开发的抗生素数量。耐多药基因的出现和传播,例如mcr-1和mcr-5.3,对抗生素的最后手段提出了挑战。疫苗接种是一种很有希望的方法,迄今没有报告产生或传播抗微生物药物耐药性的实例。在过去几十年中,开发疫苗所需的时间、广泛的许可前和许可后研究以及研发的资金限制阻碍了疫苗的开发。疫苗可被证明是未来对抗抗菌素耐药性的有效战略。
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引用次数: 1
Protein-based nanoplatform for detection of tumorigenic polyps in the colon via noninvasive mucosal routes. 基于蛋白质的纳米平台,可通过非侵入性粘膜途径检测结肠中的肿瘤性息肉。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2021-01-20 DOI: 10.4155/ppa-2020-0034
Chun-Chieh Chen, Mo A Baikoghli, R Holland Cheng

The use of nanoparticulate systems to diagnose and treat tumors has gained momentum with the rapid development of nanomedicine. Many nanotheranostics fail due to insufficient bioavailability and low accumulation at the tumor site, resulting in undesirable side effects. We describe the use of an engineered hepatitis E viral nanoparticle (HEVNP) with enhanced bioavailability, tissue retention and mucosal penetration capacities. HEVNP is a modular nanocapsule that can encapsulate heterologous nucleotides, proteins and inorganic metals, such as ferrite oxide nanoparticles. Additionally, the exterior protruding arms of HEVNP is composed of loops that are used for chemical coupling of targeting and therapeutic peptides. We propose the use of HEVNP to target colorectal cancer (i.e., polyps) with imaging-guided delivery using colonoscopy.

随着纳米医学的快速发展,使用纳米颗粒系统诊断和治疗肿瘤的势头越来越猛。许多纳米otheranostics由于生物利用度不足和在肿瘤部位的蓄积量低而失败,从而导致不良副作用。我们介绍了一种工程化戊型肝炎病毒纳米粒子(HEVNP)的使用情况,它具有更强的生物利用度、组织保留和粘膜穿透能力。HEVNP 是一种模块化纳米胶囊,可封装异源核苷酸、蛋白质和无机金属,如氧化亚铁纳米粒子。此外,HEVNP 的外部突出臂由环形结构组成,可用于靶向肽和治疗肽的化学耦合。我们建议使用 HEVNP 靶向结肠直肠癌(即息肉),并利用结肠镜在成像引导下输送。
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引用次数: 0
Patent highlights August-September 2020. 专利要点 2020 年 8 月至 9 月。
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2021-01-01 Epub Date: 2021-01-14 DOI: 10.4155/ppa-2020-0032
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
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 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 & PHARMACY 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 & PHARMACY 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
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 & PHARMACY 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 & PHARMACY 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
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Pharmaceutical patent analyst
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