Tuberculosis still is the world’s leading cause of death from a single infectious agent and has affected approximately 10 million people in 2018. The development of new technologies for treating tuberculosis is among the priority goals for the global fight against the disease. The present work makes a technological prospecting from patent documents, aiming to identify new technologies developed for the treatment of the disease, analyzing the most promising trends. The identification of new technologies was carried out through the Orbit Intelligence portal using the sentence: “(+ tuberculosis +) / TI / AB AND (A 61K OR A 61P) / IPC AND PRD> =2015” as a search strategy. We identified 41 patent families with experimental evidence (in vitro / in vivo) of efficacy against Mycobacterium tuberculosis, including resistant strains. The new technologies mainly consist of chemical synthesis products. The patent protection was demanded in countries with promising markets, with potential licensors and strong intellectual property regulations. The use of patents as a source of information can contribute to orientate the development of new drugs for tuberculosis.
Serviço de Farmácia, Instituto Nacional de Infectologia Evandro Chagas, 21040-360 Rio de Janeiro - RJ, BrasilInstituto Nacional de Infectologia Evandro ChagasBrazilRio de Janeiro, RJ, BrazilServiço de Farmácia, Instituto Nacional de Infectologia Evandro Chagas, 21040-360 Rio de Janeiro - RJ, Brasil
Vanessa da Gama Oliveira
Serviço de Farmácia, Instituto Nacional de Infectologia Evandro Chagas, 21040-360 Rio de Janeiro - RJ, BrasilInstituto Nacional de Infectologia Evandro ChagasBrazilRio de Janeiro, RJ, BrazilServiço de Farmácia, Instituto Nacional de Infectologia Evandro Chagas, 21040-360 Rio de Janeiro - RJ, Brasil
Núcleo de Inovação Tecnológica, Instituto Carlos Chagas, 81350-010 Curitiba - PR, BrasilInstituto Carlos ChagasBrazilCuritiba, PR, BrazilNúcleo de Inovação Tecnológica, Instituto Carlos Chagas, 81350-010 Curitiba - PR, Brasil
Serviço de Farmácia, Instituto Nacional de Infectologia Evandro Chagas, 21040-360 Rio de Janeiro - RJ, BrasilInstituto Nacional de Infectologia Evandro ChagasBrazilRio de Janeiro, RJ, BrazilServiço de Farmácia, Instituto Nacional de Infectologia Evandro Chagas, 21040-360 Rio de Janeiro - RJ, Brasil
Núcleo de Inovação Tecnológica, Instituto Carlos Chagas, 81350-010 Curitiba - PR, BrasilInstituto Carlos ChagasBrazilCuritiba, PR, BrazilNúcleo de Inovação Tecnológica, Instituto Carlos Chagas, 81350-010 Curitiba - PR, Brasil
Tabela 1
Instituições detentoras das patentes de novas tecnologias para TB por país/ escritórioaa
AU= Austrália; BR = Brasil; CA = Canadá; CH = Suíça; CN = China; EP = EPO; GB = Reino Unido; IN = Índia ; KR = República da Coréia; RU = Rússia; UA = Ucrânia; US = EUA; WO = Organização Mundial de Propriedade Intelectual.
de proteção
Tabela 2
Estruturas e grupos químicos das 37 novas tecnologias obtidas por síntese química identificadas nos documentos de patente
Figura 1
Fluxo metodológico para identificação de novas tecnologias desenvolvidas para o tratamento da TB
Figura 2
Principais países de depósito das patentes de novas tecnologias desenvolvidas para o tratamento da TB
Tabela 1
Instituições detentoras das patentes de novas tecnologias para TB por país/ escritórioaa
AU= Austrália; BR = Brasil; CA = Canadá; CH = Suíça; CN = China; EP = EPO; GB = Reino Unido; IN = Índia ; KR = República da Coréia; RU = Rússia; UA = Ucrânia; US = EUA; WO = Organização Mundial de Propriedade Intelectual.
de proteção
Instituição detentora (país) / País de proteção
CN
WO
US
EP
BR
RU
IN
KR
Institute of Medicinal Biotechnology Chinese Academy of Medical Sciences (CN)
10
Zhejiang Starry Pharmaceutical (CN)
7
Institute of Materia Medica Chinese Academy of Medical Sciences (CN)
2
2
Yuria Pharm (UA)
3
Beijing Tuberculosis and Thoracic Tumor Research Institute (CN)
2
Glaxosmithkline Intellectual Property Development Limited (GB)
1
2
1
1
1
1
1
Johns Hopkins University (US)
1
2
1
Cisen Pharmaceutical (CN)
1
1
1
1
1
1
Curtin University (AU)
1
1
East China Normal University (CN)
1
1
L'Ecole polytechnique fédérale de Lausanne (CH)
1
1
1
Federal State Budgetary Institution of Science Institute (RU)
Konkuk University Industrial Cooperation Corp (KR)
1
Leland Stanford Junior University (US)
1
The People's Liberation Army (PLA) No. 309 Hospital (CN)
1
Qifang Pharmaceutical Industry (CN)
1
Research Foundation of Suny (US)
1
1
1
1
1
1
Rutgers University (US)
1
Shangai Jia Tan Pharmatec (CN)
1
1
1
1
1
1
Shanghai Sun Sail Pharmaceutical Science & Technology (CN)
1
1
1
South Ural State University (RU)
1
Texas A&M University (US)
1
1
1
União Brasileira de Educação e Assistência Mantenedora da PUCRS (BR)
1
1
Universidade Estadual Paulista Júlio de Mesquita Filho (BR)
1
1
University of British Columbia (CA)
1
University of Illinois at Chicago (US)
1
1
University System of Georgia Valdosta State University (US)
1
1
1
Tabela 2
Estruturas e grupos químicos das 37 novas tecnologias obtidas por síntese química identificadas nos documentos de patente
Patente
Estrutura química
Grupo químico
(RU2604068) N-(2-aminopurin-6-yl)glycyl-(s)-glutamic acid, having anti-tuberculosis activity
Aminopurina
(EP3448869) Azasteroids for treatment of tuberculosis
Estrutura não indicada no documento de patente
Azasteroide
(EP3050565) Benzimidazole sulfide derivatives for the treatment or prevention of tuberculosis
Benzimidazol
(CN106543106) N-benzylbenzamide compounds and preparation method thereof
Benzilbenzamida
(EP3285873) Substituted benzofuran derivatives as novel antimycobacterial agents
Estrutura não indicada no documento de patente
Benzofurano
(CN105669664) Benzothiazine-4-ketone compounds containing basic nitrogen heterocyclic fragments and preparing methods of benzothiazine-4-ketone compounds
Estrutura não indicada no documento de patente
Benzotiazina
(CN105622596) Benzothiazine-4-ketone compound containing alkoxyimino azacyclo-fragments and preparation method of benzothiazine-4-ketone compound
Benzotiazina
(CN108440446) Benzothiazine-4-acetone compound containing oximido fragment and preparation method thereof
Benzotiazina
(CN108976227) Benzothiazine-4-one compound containing alkaline bridge ring fragment and preparation method thereof
Benzotiazina-4-ona
(RU2663848) 5-fluoro-2-(4-ethoxycarbonyldipiperazine-1-yl)-1,3-benzothiazine-4-one, which has anti-tuberculosis activity
Benzotiazina e piperazina
(RU2683573) Anti-tuberculosis agent based on n-[4-(4-aminobenzsulfanyl)-phenyl-2-benzoylaminobenzamide with low toxicity
Benzamida e sulfanil
(US20180111913) Substituted benzofuran derivatives as novel antimycobacterial agents
Benzofurano
(WO2019120210) Benzofuran, coumestans derivatives, preparation method and use thereof
Benzofurano
(KR101923514) Composition comprising Phloretin or as active ingredients for preventing or treating of Tuberculosis
Flavonoide
(CN108059627) Anti-mycobacterium tuberculosis compound as well as preparation method and application thereof
Furano e tioamida
(WO2015164482) Inhibitors of drug-resistant mycobacterium tuberculosis
Indol
(WO201946465) Therapeutic indoles
Indol
(WO2018206466) Sanfetrinem or a salt or ester thereof for use in treating mycobacterial infection
Isoindol
(CN107674014) 3,5-dinitrobenzene formamide compound containing isoindoline fragment and preparation method thereof
Isoindol
(CN106588916) N-(phenoxyethyl)imidazo [1,2-a] pyridine-3-amide compound and preparation method thereof
Imidazol
(CN108358917) Imidazo[1,2-a]pyridine-3-amide compound containing alkaline fused ring fragment and preparation method thereof
Imidazol
(CN109503631) Diazospiro fragment-containing imidazo[1,2-alpha]pyridine-3-amide compound and preparation method and application thereof
Estrutura não indicada no documento de patente
Imidazo [1,2-a] piridina -3- amida
(WO201691207) Nitroimidazole compound, preparation method therefor and use thereof in drug manufacturing
Nitroimidazol
(WO201662151) Pyrazolo[1,5-a]pyridine compounds and use thereof
Pirazol
(EP3170810) Pyridine derivatives and anti-mycobacterial use thereof
Piridina
(WO2018116260) Pharmaceutical composition with anti-tubercular effect
Piridina, hidrazona e pirrol
(EP3432887) Antituberculosis agent
Pirimidina e piperidina
(WO201942267) Pyrrole-2-formamide compound, and preparation method therefor and applications thereof
Pirrol
(US20160113919) Chloroquine stereoisomer for treating tuberculosis related diseases
Quinolina
(WO2016201541) Compound, method for producing the compound, pharmaceutical composition, use of the compound for preparing a medicinal drug for treating a disorder caused by bacteria of the genus mycobacterium and method for treating a disorder caused by bacteria of the genus mycobacterium
Sociedade Brasileira de Química
Instituto de Química, Universidade Estadual de Campinas (Unicamp), CP6154, 13083-0970 -
Campinas -
SP -
Brazil E-mail: quimicanova@sbq.org.br
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