Therapeutic Patents Research Articles

Baicalein: Promising Therapeutic Applications With Special Reference to Published Patents

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 vesselsand protects the nervous systemand also reduces diabetes and diabetic complications. In addition, baicalein is known to decrease inflammatory markers such as IL-1β, IL-6and TNF-α. In this review, we have attempted to compile the list of recent therapeutic patents of baicalein used for treating different disorders.

COVID-19 Vaccines: Systematic review

World facing pandemic challenges of SARS-Co-2 (Severe Acute Respiratory Syndrome Corona Virus 2). Tyrrell and Bynoe identified first strain of human corona virus in 1965. Infection was originated from Wuhan city of China on November 2019. Virus officially named as COVID-19 which causes respiratory tract infections in humans. Preliminary symptoms like chest pain with difficulty in breathing, reduced in systemic oxygen level, cough and fever. At present, the majority of the pharmaceutical companies were in race to developing antiviral drug and vaccines against COVID-19. Industries conducting the experiment and clinical trial of various vaccines to ensure effectiveness and safety on human. Several of them were documentation for patent, authorization of clinical trial and marketing. We provide an overview of Covid-19 history, types of vaccine and mechanism of actions, current future therapeutic drugs and patents. Relative with the mechanism of actions such as inactivated vaccine, vector vaccines, DNA and RNA based vaccine and antiviral drugs already entered in (Phase II and III) clinical trials. The systemic study specified brief summary of various vaccines. Current status of clinical trial, safety and effectiveness according to ICH guidelines. A major adverse interaction with their toxicity study. The information of approved which give opportunity for upcoming scientist to improve the quality, and minimize the adverse effects. Scientist may face challenges during the post marketing clinical trial. This pandemic has provided various scopes for researchers to develop vaccine and antiviral drugs.

A therapeutic patent overview of MDM2/X-targeted therapies (2014–2018)

ABSTRACTIntroduction: MDM2 and MDMX proteins provide the inhibition of p53 tumor suppressor, thus allowing for accelerated mutation-driven cancer microevolution. A pharmacological blockade of MDM2/X-p53 interaction results in p53 reactivation in p53wt cells, leading to cancer growth inhibition. Throughout the past 20 years, multiple chemical entities have been proposed to reactivate p53 by antagonizing MDM2/X proteins.Areas covered: This manuscript reviews 2014–2018 therapeutic patents in the field of MDM2/X antagonists and is a continuation of previous reviews on similar matter. The patents covering the use of MDM2/X antagonists in drug combinations are also presented in this review, as they constitute an important trend in the field of cancer treatment with MDM2/X antagonists.Expert opinion: In the years 2014–2018, several previously-known chemical scaffolds have been further developed and disclosed. Importantly, in the same time period, many lead compounds have entered clinical trials for the treatment of cancer patients. Meanwhile, several important reports have pointed to serious limitations of anticancer properties of MDM2 antagonists. As a result, many efforts have been made to seek for positive, synergistic therapeutic effects of combined anti-cancer treatment strategies. One recent example is a dual targeting of MDM2 and additional protein targets by utilizing the PROTAC technology.Trial registration: ClinicalTrials.gov identifier: NCT02264613.Trial registration: ClinicalTrials.gov identifier: NCT02624986.Trial registration: ClinicalTrials.gov identifier: NCT02670044.Trial registration: ClinicalTrials.gov identifier: NCT02545283.

The introduction of patent agent privilege in Canada.

The introduction of patent agent privilege in Canada.

Selective and nonselective HDAC8 inhibitors: a therapeutic patent review.

Histone deacetylase 8 (HDAC8) is one of the attractive therapeutic anticancer targets. HDAC8 has been overexpressed in a variety of human cancers. Therefore, HDAC8 inhibitors offer beneficial effects in the treatment of solid and hematological tumors. Different HDAC inhibitors entered into different phases of clinical studies. However, selectivity towards specific HDAC8 enzyme is still demanding. In this patent review, a number of patented selective and nonselective HDAC8 inhibitors along with their implication as anticancer agents have been discussed in details. Molecules should possess modified fish-like structural arrangement to impart potency and selectivity towards HDAC8. This comprehensive patent analysis will surely provide newer aspects of designing selective HDAC8 inhibitors targeted to anticancer therapy in future.

New therapeutic patents used for the treatment of leprosy: a review.

Leprosy is a granulomatous disease, infectious and transmissible, which affects the skin and peripheral nerves, having Mycobacterium leprae as causative agent. The manifestation of this disease causes cutaneous lesions, peripheral neuropathies and, in more extreme cases, may generate deformities and disabilities in affected individuals. Patents were identified using the descriptor 'leprosy' and code A61K of the international patent classification, which indicates only products that meet human needs. The analysis was made using the WIPO, ESPACENET and USPTO databases, until the month of September 2016. Through this review, we found a variety of in vitro, pre-clinical and clinical studies relating to the treatment of leprosy with different types of compounds and forms of administration. New treatment proposals should include pain reduction capabilities, prevention or limitation of the appearance of cutaneous lesions, as well as prevention of the progression of the disease to more severe stages that may lead to loss of function or potentiate the individual's immune response to the M. leprae bacillus in order to prevent bacterial spread. We concluded that any patents developed with natural products were not found in the treatment of leprosy. All the deposited products were synthetic origin, mostly tested in humans and of varied forms of administration.

Mapping the Patent Landscape in the Field of Personalized Medicine

This study aims to describe innovation profile in the field of personalized medicine. While the major market players have recognized the importance of personalizing health care as the next milestone towards improved clinical outcomes, a common framework has yet to emerge. In the absence of such governance framework, the practices of research and development can shape the progress of the field. The cognitive structure of the research and development in the personalized medicine is mapped by characterizing the attributes of underlying technological space. By exploring the technological trajectory and emerging patterns of personalized medicine discerned in patenting activity and citation relations, a detailed picture of innovation in the field is obtained. Moreover, a topic modeling technique was applied to understand the emergence and institutionalization of new technological fields. The results show that the patent landscape is dominated by therapeutic patents used in the oncology and therapeutic areas of neurodegenerative and infectious diseases. Increase in funding for the proper cycling between research, clinical care, and cost management program would accelerate the adoption of precision medicine and promote the convergence of IT-driven data science and the traditional natural sciences. This work offers a complementary perspective to the field of personalized medicine, focusing on the exploitation of patent information. We expect that systematic understanding of the technology landscape and evolving R&D process in the personalized medicine may help to provide insights for making future technology planning more rationally.

An update on obtaining and enforcing therapeutic antibody patent claims.

Therapeutic antibody patent owners face continuing challenges trying to obtain broad patents and enforce them in the United States and Europe.

Survivin Modulators: An Updated Patent Review (2011-2015).

Survivin is widely overexpressed in many forms of cancer and studies have related high survivin expression with poor survival rates. Although, there have been several attempts to target survivin, most therapeutics haven't shown substantial success in clinical trials therefore, authors wish to attract the focus towards many recent therapeutic innovations to target survivin. Survivin plays an essential role in the cell cycle progression, apoptosis, cell stress response, drug resistance and angiogenesis therefore the prognostic and targeting benefits of survivin have been underestimated. An update on the current and existing therapeutic strategies implemented to target survivin is provided. Therefore, the reader will gain an insight into the recent patents targeting survivin. The review has emphasised on patents for quantification of survivin, survivin peptides as immunotherapeutics, application of survivin promoters, RNA interference of survivin, small molecules inhibitors of survivin and nanoparticles targeting survivin. The review also encompasses the survivin targeted therapeutics being implemented at clinical stages which include survivin targeted immunotherapeutics, peptide-based vaccines, antisense oligonucleotides and chemical inhibitors. We reviewed recent patents based on preclinical anti-survivin therapies reported to date and it was concluded that gataparsen has been most widely used for anti-survivin therapy in clinical trials. It was also concluded that most therapeutic patents were focussed on development of natural anti-survivin therapeutics such as anti-survivin peptides or survivin anti-sense oligonucleotides in the recent years therefore, proving that natural proteins and nucleic acids has an upper hand over chemicals and synthetic drugs.

Natural product-based therapeutics for the treatment of cancer stem cells: a patent review (2010 - 2013).

Cancer stem cells (CSCs) are a subpopulation of tumor cells that possess self-renewal and tumor initiation capacity and the ability to give rise to the heterogenous lineages of cancer cells that comprise the tumor. CSCs possess numerous intrinsic mechanisms of resistance to chemotherapeutic drugs, novel tumor-targeted drugs and radiation therapy, allowing them to survive current cancer therapies and to initiate tumor recurrence and metastasis. This review presents the up-to-date natural product-based therapeutics for the treatment of CSCs. This review gives an account of the recent therapeutic patent literature (2010 - 2013) describing the applications of natural products on CSCs. In this review, many of the therapeutic applications of natural products reported in international patents have been discussed. In addition to selected biological data, some of pharmaceutical applications are also summarized. Because of the large number of patents registered in this period relative to natural products the attention was focused, in this first part of the review, on inhibitors of six cancers. This patent review aims to highlight the use of natural products to treat cancer by targeting CSCs. Most of the described products are shown to have beneficial therapeutic effects and their uses for developing new formulations.

A Key Opinion Leader interview: insight into the research and career of Dr KA Jacobson

Welcome to the first Key Opinion Leader interview for Expert Opinion on Therapeutic Patents. Today, I am talking with Professor Kenneth A. Jacobson, who is an esteemed member of our editorial board.

The vexed issue of therapeutic combinations and contributory patent infringement in Australia

The Australian Patents Act includes a provision which deems the supplier of a product to a person who will use that product in a manner which infringes a patent to infringe that patent as a contributory infringer. The concept of contributory patent infringement is one known to the patent laws of many countries, but in many respects the way in which Australian Courts have approached contributory patent infringement gives far greater scope to a patentee than in many of those jurisdictions. The consequence for the generic pharmaceutical industry in Australia is potentially far-reaching. This article looks at the practical consequences of some recent Australian Federal Court decisions which have been decided in the area and which create practical hurdles that any generic entrant into the Australian marketplace will need to navigate.

Diagnostic and Therapeutic Patents and Patent Applications on Biomarkers for Acute Kidney Injury

Acute kidney injury (AKI), a syndrome that is defined by a sudden and substantial decrease in kidney function, can be caused by a variety of mechanisms including circulatory collapse, ischemia-reperfusion injury, systemic inflammatory response, endogenous or exogenous toxicants or urinary obstruction. The causal and temporal sequence of kidney injury leading to reduced function and in turn causing an increment in serum creatinine, however, hinders a timely detection of this syndrome and may therefore also delay its early and effective treatment. In recent years, an increasing number of promising biomarker candidates were described and patented to help in the detection, prognostic stratification and treatment of AKI. The discovery and evaluation of novel biomarkers for AKI holds the promise to improve early detection and allow for the development of effective treatments for this condition. This narrative review summarizes recent developments in AKI biomarker patenting with a focus on both diagnosis and treatment-oriented patents and patent applications. In addition, alternative methods for early detection of AKI, particularly patents and patent applications on continuous urine output- and glomerular filtration rate monitoring, are presented and discussed in comparison. Finally, important potential limitations for the application of biomarkers for AKI as well as alternative techniques for the measurement of kidney function are discussed. Keywords: Acute kidney injury, acute renal failure, biological markers, biomarkers, clinical research, diagnostics, patents, Urinary Biomarkers, Functional Kidney Markers, NGAL, GFR monitors.

The Hypothalamic-Neurohypophyseal System: Current and Future Treatment of Vasopressin and Oxytocyn Related Disorders

The hypothalamus and posterior pituitary form a complex neurohumoral system playing a key role in maintaining body fluid homeostasis and reproductive function. We review the pathophysiology mechanisms of posterior pituitary hormones and their implications, beyond water balance and delivery, in social functioning, pair bonding and affiliative behavior. Actual and future treatments for neurohypophysis related disorders are also discussed, particularly focusing on the development of new therapeutic compounds and patents.

The landscape of drug discovery in atherosclerosis and dyslipidaemia revisited: an update of patenting activity

Introduction: This paper is an update of a previous paper I published in Expert Opinion of Therapeutic Patents in 2008. The paper was a survey of patenting activity in the fields of atherosclerosis and dyslipidaemia, which identified trends in patenting by reviewing two major mechanistic categories, metabolic/dyslipidaemia and vascular/inflammation, as well as examining the interest in certain specific targets over a period of 10 years.Methods: In this update, the same methodology was followed using the Espacenet of the European Patent Office (EPO) to identify patents claiming therapeutics for atherosclerosis or dyslipidaemia (excluding the wider metabolic syndrome).Expert opinion: A major change in the field over the past 5 years has been the departure of larger companies from the field. This is reflected in the patenting activity. Patenting has been at a stable rate over the recent years with few new targets being highlighted. It is suggested that, for this field to return to the higher rates of patenting seen over 10 years ago, breakthroughs in translational medicine and in the ability to conduct clinical trials, particularly in biomarkers and imaging, will need to take place.

Current diagnosis and management of infectious mononucleosis

Infectious mononucleosis is a common, usually self-limited disease. However, infectious mononucleosis may present with severe manifestations. Complications may also occur. Consequently, diagnostic and treatment issues regarding infectious mononucleosis are of major importance. In this review, we focus on the evaluation of articles providing diagnosis and treatment data for infectious mononucleosis, published during the past 2 years. Twelve studies, deriving from extended search in PubMed, were included. Nine studies provided diagnosis data. The evaluated diagnostic methods were real-time PCR (RT-PCR), IgM/IgG antibodies measured with different assays [measurement of Epstein-Barr virus viral load (EBV-VL) in peripheral blood, neutrophil/lymphocyte/monocyte counts, C-reactive protein values, and monospot test]. The sensitivities reported for RT-PCR were high. The available treatment data were scarce (three studies). Two of them suggested that antivirals (mainly acyclovir and valacyclovir) may have a role in the treatment of infectious mononucleosis with complications, whereas the remaining study presented novel potential therapeutic patents including 5-substituted uracyle, azacytosine derivatives, and peptides inhibiting EBV-mediated membrane fusion. RT-PCR and measurement of EBV-VL may provide useful tools for the early diagnosis of infectious mononucleosis in cases with inconclusive serological results. Antiviral agents may provide a useful treatment option in patients with severe infectious mononucleosis.

Latest Therapeutic Novelties and Patents in Pulmonary Hypertension

Recent advances in technology and novel pharmaceutical research findings have added new grounds in the fields of medical treatment and quality of life of patients diagnosed with pulmonary arterial hypertension (PAH). Collective assessment of new data is mandatory and useful for specialist medical doctors. This review aims to present the latest therapeutic developments of the last two years (2009-2010) in PAH. Moreover, recent patents (of the year 2010) regarding therapeutic novelties in PAH that expand treatment modalities, are hereby presented.

Patents of drugs extracted from Brazilian medicinal plants

Background: Plants synthesise a vast repertoire of chemicals with various biological activities. Brazilian enormous botanical diversity facilitates the development of novel ethical drugs for the treatment of diseases in humans. Objective: To present therapeutic patent applications comprising Brazilian native plants published in the 2003 – 2008 period in light of legal aspects of patentability of biodiversity and public health concerns. Methods: Therapeutic patent applications related to Brazilian medicinal plants available at both the European Patent Office and the Brazilian National Institute of Industrial Property databases were reviewed. Results/conclusion: Twenty-five patents are presented, most of which concern inflammatory, allergic, parasitic, infectious or digestive diseases, including extracts from Carapa guianensis, Copaifera genus, Cordia verbenacea, Erythrina mulungu, Physalis angulata and other pharmaceutical compositions with antileishmanial, antimalarial or trypanocidal activity. Brazilian research centres and universities are responsible for most of these inventions.

Serotonin 5-HT 2B Receptor in Cardiac Fibroblast Contributes to Cardiac Hypertrophy

See related article, pages 113–123 Cardiac hypertrophy is often accompanied by cardiac remodeling characterized by loss of cardiac myocytes, interstitial fibroblasts, and collagen deposition, leading to decreased ventricular compliance and an increased risk for heart failure. The mortality for patients with heart failure is still high, although some improvements have been demonstrated in patients with systolic heart failure.1–3 To improve the therapeutic strategy for patients with heart failure, especially diastolic heart failure, further research and investigations to better understand the molecular and biochemical mechanism are needed. Serotonin (5-hydroxytryptamine [5-HT]) affects many physiological functions through the interaction with specific G-coupled membrane receptors, 5-HT receptors. There are 4 classes of 5-HT receptors (5-HT1/5, 5-HT2, 5-HT3, and 5-HT4/6/7).4 Serotonin, via the 5-HT2B receptor, regulates cardiac development and function.5 Transgenic mice with a 5-HT2B receptor gene ablation show embryonic and neonatal death caused by lack of trabeculae in the heart.6 5-HT2B receptors are essential for isoproterenol-induced cardiac hypertrophy, which involves the regulation of interleukin-6, interleukin-1β, and tumor necrosis factor-α cytokine production by cardiac fibroblasts.7 The 5-HT2B receptor has been shown functionally coupled to reactive oxygen species synthesis through NAD(P)H oxidase stimulation in neuronal cells8 and in angiotensin II and isoproterenol-induced cardiac hypertrophy.9 Recently, 5-HT2B receptor blockade has been shown to prevent the cardiac hypertrophy induced by angiotensin II or isoproterenol infusion.9 …

Cancer stem cell patents

Background: Cancer stem cells (CSCs) are a small subpopulation of the tumour mass that are capable of sustaining its growth, are resistant to many cancer specific therapies, and can reinitiate disease relapse. CSCs are resistant to current cancer treatments due to specialised transporters, cell cycle changes, DNA repair and antiapoptotic mechanisms. Objective: This paper reviews CSC biology and diagnostic and therapeutic patents as well as those associated with the isolation of CSCs. Methods: Literature and patent searches using the NCBI PubMed, European Patent Office, Scopus, and PATENTSCOPE® websites were conducted to examine and link CSC biology and therapy development with current patent literature. Conclusion: Development in basic CSC biology research is increasing the patents filed in this area; however, therapeutic patents directly targeting CSCs are more limited, as research in this area remains in its infancy.