Jorge Lima de Magalhães

Novel 1H-1,2,3-, 2H-1,2,3-, 1H-1,2,4- and 4H-1,2,4-triazole derivatives: a patent review (2008 – 2011)

Introduction: The triazoles represent a class of five-membered heterocyclic compounds of great importance for the preparation of new drugs with diverse biological activities because they may present several structural variations with the same numbers of carbon and nitrogen atoms. Due to the success of various triazoles that entered the pharmaceutical market and are still being used in medicines, many companies and research groups have shown interest in developing new methods of synthesis and biological evaluation of potential uses for these compounds. In this review, the authors explored aspects of patents for the 1H-1,2,3-, 2H-1,2,3-, 1H-1,2,4- and 4H-1,2,4-triazole families, including prototypes being considered in clinical studies between 2008 and 2011. Areas covered: The triazoles have been studied for over a century as an important class of heterocyclic compounds and still attract considerable attention due to their broad range of biological activities. More recently, there has been considerable interest in the development of novel triazoles with anti-inflammatory, antiplatelet, antimicrobial, antimycobacterial, antitumoral and antiviral properties and activity against several neglected diseases. This review emphasizes recent perspective and advances in the therapeutically active 1H-1,2,3-, 2H-1,2,3-, 1H-1,2,4- and 4H-1,2,4-triazole derivative patents between 2008 and 2011, covering the development of new chemical entities and new pharmaceuticals. Many studies have focused on these compounds as target structures and evaluated them in several biological targets. Expert opinion: The preparation of 1H-1,2,3-, 2H-1,2,3-, 1H-1,2,4- and 4H-1,2,4-triazole derivatives brings to light several issues. There is a need to find new, more efficient preparations for these triazoles that take into consideration current issues in green chemistry, energy saving and sustainability. New diseases are discovered and new viruses and bacteria continue to challenge mankind, so it is imperative to find new prototypes for these new diseases. Of great urgency is finding prototypes against bacteria that continue to increase resistance and for neglected diseases that affect a large part of humanity, especially the poor and vulnerable.

Identification of Brazilian expertise in the fight against some neglected tropical diseases

Introduction: Neglected diseases represent a threat for over one billion people around the world, of whom about 230 million are in Latin America. Around 10-20% of the Brazilian population is estimated to have suffered from one of the 17 neglected tropical diseases listed by the World Health Organization (WHO). Knowledge management, highlighted in the twentieth century, and industrial policymaking in Brazil have yielded technical and scientific progress in research and development, but there are difficulties in identifying the business and scientific expertise available, because it permeates several factors, including cooperative management. This work therefore aims to map out the senior experts in neglected tropical diseases in Brazil and identify potential partnerships. Methods : Consultation and analysis of information from Portal Inovacao (government innovation portal), Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq) (government science and technology research agency), and the bibliographical references indexed in Biblioteca Virtuais Saude, Scielo and Lilacs. Results : 40,770 experts working in NTDs were identified from Portal Inovacao, and 2,633 senior researchers from the CNPq database. Conclusions: The databases do not provide effective or practical data on Brazilian businesses and scientists with the competencies to contribute towards treatments for NTDs. The data extraction process lacks effective knowledge management. In the last 30 years, Chagas disease, dengue, Hansen disease, leishmaniasis, malaria and tuberculosis have been high on the government agenda. It is recommended that the 6.5% of the top level CNPq scientists who work in NTDs should constitute a source of consultation for the public and private sectors.

INTERNALIZAÇÃO DE FARMOQUÍMICOS & MEDICAMENTOS PARA DOENÇAS TROPICAIS NEGLIGENCIADAS: PROPOSTA DE INTERAÇÃO ENTRE GOVERNO - UNIVERSIDADE - EMPRESA

History shows that public health actions to combat epidemics are most effective when there is constant synergy of both government and society, exemplified by prevention actions in the fight against dengue fever, H1N1 influenza etc. Private-public-partnerships (PPP) can also provide more dynamic and consistent results in production through interaction among Government, University and Enterprise actors. This article puts forward proposals to tackle the problem of neglected tropical diseases via the formation of a Management Council using Etzkowitzs Triple Helix concept to attenuate this public health issue in Brazil.

An Evaluation of Partnership for Productive Development in Brazil's Healthcare: Measuring the Knowledge Translation from Implementation to the Impact

21st Century brings great challenges in the information and knowledge areas. The public health is intensified in Developing and Less Developed Countries on account of parasitic diseases as well as developed countries because emerging and reemerging diseases. This diseases associated with chronic or acute diseases can intensify causing a serious health problem as drugs resistance, neglected disease and to afford perpetuate poverty. Thus, it is urgent new ways for information management. The management of the Partnership for Productive Development (PDP) have been shown a promising tool to help internalize new technologies and foster R,D&I. This chapter gives an evaluation for Healthcare using the example of the Brazilian PDP whose last way may be considered as a Knowledge Translation. In five years were conducted 103 PDP involving public and private pharmaceutical companies and international producer, promoting the development of local economy and reducing government spending from medicines derived from PDP. An Evaluation of Partnership for Productive Development in Brazil’s Healthcare: Measuring the Knowledge Translation from Implementation to the Impact

Big Data e a saúde negligenciada em dengue, zika e chicungunha: uma análise translacional da tríplice ameaça no século 21

Nos ultimos anos, a literatura associada ao Big Data em saude tem crescido rapidamente, necessitando de estudos bibliometricos e cientometricos para uma abordagem com visualizacao que conduza a mineracao profunda e revele um panorama de informacoes essenciais para subsidiar os tomadores de decisao. O uso da informatica na saude e crucial e e definida como a aplicacao sistematica de informacao, informatica e tecnologia em areas de saude publica, incluindo vigilância, prevencao, preparacao e promocao da saude. As principais aplicacoes sao promover a saude de toda a populacao e prevencao de doencas. A enfase na prevencao de doencas usando grande variedade de intervencoes e aspecto que torna a saude publica, via informatica, diferente dos demais campos da area da ciencia da informacao. Este trabalho explora 100 milhoes de patentes na base European Patent Office usando o software livre Patent2Net. As tendencias tecnologicas e oportunidades a saude publica global de dengue, zika e chicungunha permitem analisar os dados cientificos e tecnologicos desta triplice ameaca, bem como suas correlacoes. Sao identificados oportunidades de inovacao e geracao de informacoes essenciais para os gestores. Foram extraidas 1.975 patentes e 3.177 familias de patentes, com maior indice de classificacao CIP A61K, o que configura varias oportunidades para preparacoes medicas em suas variadas formas. O pico de publicacao ocorreu no ano de 2016, sendo os ultimos 10 anos os mais intensos em depositos concedidos. Os maiores detentores de patentes sao cientistas e empresas localizadas nos EUA. A localizacao dos pesquisadores e respectivos detentores e identificada.

Research on Pharmaceuticals Patents in Times of Big Data: A Contribution of the Web 2.0 for Medicinal Chemistry

This work aims to demonstrate the use of tools of Information Science applied to pharmaceutical patents. Given that existence of big data in the new century providing a massive and growing wave of information, it becomes necessary for new ways to rescue data and analyze them consistently. In the public health area is no different, especially with regard to intellectual property for new potential molecules to treat diseases of the global population. The triazoles were used as a study case due the great interest these compounds arouse in the pharmaceutical industry due their biological activities. In this regards, the approach are by consulting databases indexed (PubMed, Web of Science, Medline, Scopus, SciFinder Scholar), beyond to use search engines for data mining and software’s from collaborative intelligence to generate graphical analysis. The results demonstrate the potential of four series of triazoles derivatives and illustrate several correlations between patent and pharmaceutical industry extracted from the deep web.