Recent Patents on Anti-Infective Drug Discovery (v.5, #3)

New Perspectives in HCV Therapy: Entry Inhibitors by Marco Donia, Bruno Cacopardo, Massimo Libra, Guido Scalia, James A. McCubrey, Ferdinando Nicoletti (181-194).
Despite the improvements in HCV-therapy achieved in the last 20 years, the occurrence of high frequency of non-responders and of therapy-related side effects has lead to an ongoing interest in optimizing duration and dosage of current antiviral regimens as well as to the research and development of new antiviral treatment. Recently, the discovery of a system for in vitro HCV replication provided a useful tool for a better understanding of the viral life cycle followed by the discovery of new compounds that unlike classical drugs specifically target fundamental steps of this process. The aim of this review is to provide an update on the preclinical and clinical development of novel anti-HCV treatments targeting the first steps of the viral life cycle. The recent patents in this review article discuss the new perspectives in HCV therapy.

Malaria Chemotherapy: Recent Advances in Drug Development by Sandra Gemma, Valter Travagli, Luisa Savini, Ettore Novellino, Giuseppe Campiani, Stefania Butini (195-225).
Malaria is a disease caused by parasitic protozoa of the genus Plasmodium. Despite significant advances in understanding the disease and the parasite biology, malaria still remains one of the leading causes of morbidity and mortality, particularly in malaria-endemic regions of the world. The main factor hampering malaria control is the high degree of resistance developed by Plasmodium species against several classes of drugs. Artemisinin-based Combination Therapy (ACT) is the most rapidly acting antimalarial treatment effective against multi-drug resistant strains, and is, at present, the only group of antimalarial drugs to which resistance by Plasmodium falciparum has not developed yet in the field, even though the isolation of artemisinin-resistant strains is raising concern. As a result, discovering and developing novel antimalarial agents is one of the greatest challenges facing malaria control today. This review covers patent literature from 2007 to date regarding small molecules or natural compounds targeting the asexual forms of the parasite. Recent patents filed and issued for ameliorating conventional antimalarial treatment methods by non-conventional dosage forms are also reviewed.

Short interfering RNAs, or siRNAs, belong to a class of RNA species which play a role in both cellular defence and gene regulation. siRNAs comprise a larger portion of the RNA interference pathway that includes the degradation of RNAs which possess complementarily to specific target sequences. This property has given siRNA technology the potential to become a powerful new tool for a wide variety of disciplines, ranging from the design of novel anti-cancer agents to applications in agriculture. The following review outlines patents that have been issued over the past 6 months concerning siRNA technology. Patents are discussed which encompass improved delivery systems for cellular uptake of siRNAs, new therapeutics to combat human diseases, and unique uses of siRNAs to advance plant science. The review also provides detailed lists of the most recent patents that have been issued which cover these areas of siRNA technology, and paves the way for future innovations based on RNA interference in the life sciences.

Patent Landscape of Countermeasures Against Smallpox and Estimation of Grant Attraction Capability Through Patent Landscape Data by Anatoly L. Mayburd, Govind Kedia, Haydn W. Evans, Pritesh C. Kaslival (240-254).
The study was concerned with countermeasures against a possible smallpox outbreak. In the process of assessment 18 landscaping sectors were defined and described, the advantages and drawbacks of the corresponding countermeasures being reviewed. The data of the previously published influenza landscape were revisited. The current economic climate of deficit cutting (austerity) also puts emphasis on the optimization of capital investment. We used the materials of the landscape to define and analyze metrics of capital placement optimization. Value score was obtained by fitting patent landscape internals to the sale price of individual patents. Success score was obtained as a product of and#945;-priori parameters that measure likelihood of emergence of a marketable product in a technological sector. Both scores were combined in a qualitative metric. Our methodology defined weight as a product of the sector size by the success score. We hypothesized - based on the material of two landscapes- that a life cycle of a technology begins in IP space with a high patent quality low volume and#x201C;budand#x201D; of low weight, reaches maximum weight and then weight falls again when the technology becomes outdated. The weight and the annual dynamic of weight can serve a measure of investment risk and return. In this report, we modeled investment by issue of government grants or purchase of patents by government. In the smallpox landscape the number of patents purchased by government agencies was the highest in the sectors with the highest weight and the trend was confirmed by the count of NIH grants issued in support of the technological sectors. In the influenza landscape only grant issue count was statistically meaningful and the trend was also confirmed. To better fit the grant support levels, the weight expression was optimized by using training coefficients. We propose to use value scores for evaluation of individual patent publications/company portfolios and to use weights for assessment of technological sectors. Such a combination of automated analytical tools may lead to optimized allocation of capital and is intended to support the decisions taken by human experts.

Recent Patents on Nucleic Acid-Based Antiviral Therapeutics by Sumita Mishra, Soyoun Kim, Dong-ki Lee (255-271).
The concept of using nucleic acids as a prospective antiviral therapeutics has been one of the major areas of study for researchers since the last three decades. Among the many proposed technologies for specifically perturbing gene expression, four potent nucleic acids based technologies such as Antisense (AS), Ribozyme, Aptamer and RNA Interference (RNAi) have emerged. Though being technically different from each other, these technologies share among themselves the features of conceptual simplicity, straightforward designing and quick drug identification methods, which enable them to be pre-clinically and clinically tested at a rapid pace. The scale of growth, in the level of scientific interest and in the number of patents claimed based on these technologies, is not surprising considering the aforementioned factors. As more and more drugs continue to appear with the promise of actually curing diseases, instead of merely offering temporary symptomatic relief, this study is becoming even more intriguing, both scientifically and commercially. This review article puts together and discusses the latest patents filed based on the above mentioned technologies with an objective to provide an insight into the latest developments in this field of study that projects these technologies as prospective antiviral therapeutics. The listed patents have been classified technology wise and further sub-classified on the basis of their target disease.

Patent Selections: by Bentham Science Publishers (272-273).
The patents annotated in this section have been selected from various patent databases. These recent patents are relevant to the articles published in this journal issue, categorized by therapeutic areas/targets and therapeutic agents related to antiinfective drug discovery.