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1.
Health Res Policy Syst ; 22(1): 97, 2024 Aug 06.
Artigo em Inglês | MEDLINE | ID: mdl-39107767

RESUMO

Patent and proprietary medicine vendors in Nigeria play a very integral role in providing primary health care services and are an important source of care for the poor. They are located close to communities and are often the first source of care for hygiene and family planning (FP) products and treatment of child illnesses. Since 2017, Pharmacy Council of Nigeria (PCN) has partnered with Society for Family Health through the IntegratE project to address the poor quality of services by patent and proprietary medicine vendors (PPMVs) and reposition them for better service delivery through piloting the three-tier accreditation system. The partnership has engendered innovation for human resource for health, and considering the peculiarity of their situation, new emerging methods and arrangements to deliver the training to PPMVs in diverse geographical locations within their catchment areas are developed. In this study, we aimed to discuss the role of patent and proprietary medicine vendors in the provision of quality health delivery and provide key lessons and recommendations which have been learned from the pilot scaling of training facilities for PPMVs in Nigeria through the IntegratE project. From the lessons learnt, we propose that, for a successful scale-up of implementation of the three-tier accreditation of PPMVs, PCN will have to establish a budget line for accreditation. In addition, the government should also consider supporting this training through the Basic Healthcare Provision Fund as a way of strengthening human resources at the primary healthcare level. Other alternative sources of funding include licensing and registration fees and other dues generated internally by PCN.


Assuntos
Acreditação , Comércio , Atenção à Saúde , Nigéria , Humanos , Atenção Primária à Saúde , Patentes como Assunto , Política de Saúde , Qualidade da Assistência à Saúde
2.
Nat Commun ; 15(1): 6379, 2024 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-39090097

RESUMO

Unsustainable wildlife trade imperils thousands of species, but efforts to identify and reduce these threats are hampered by rapidly evolving commercial markets. Businesses trading wildlife-derived products innovate to remain competitive, and the patents they file to protect their innovations also provide an early-warning of market shifts. Here, we develop a novel machine-learning approach to analyse patent-filing trends and apply it to patents filed from 1970-2020 related to six traded taxa that vary in trade legality, threat level, and use type: rhinoceroses, pangolins, bears, sturgeon, horseshoe crabs, and caterpillar fungus. We found 27,308 patents, showing 130% per-year increases, compared to a background rate of 104%. Innovation led to diversification, including new fertilizer products using illegal-to-trade rhinoceros horn, and novel farming methods for pangolins. Stricter regulation did not generally correlate with reduced patenting. Patents reveal how wildlife-related businesses predict, adapt to, and create market shifts, providing data to underpin proactive wildlife-trade management approaches.


Assuntos
Animais Selvagens , Comércio , Aprendizado de Máquina , Patentes como Assunto , Comércio de Vida Silvestre , Animais , Conservação dos Recursos Naturais , Perissodáctilos , Ursidae , Comércio de Vida Silvestre/legislação & jurisprudência , Comércio de Vida Silvestre/tendências
3.
PLoS One ; 19(8): e0305238, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39116107

RESUMO

Majority customers of cosmetics are female. Would this imply a high proportion of inventors of cosmetics technology is female? Would the inventor's gender be related to the characteristics and quality of corresponding patent? This study tries to identify manifestation of gender equity in cosmetics technology in terms of patent application and grant, technical characteristics, and its performance. We apply topic modeling, zero-inflated Poisson regression, and survival analysis to patents related to cosmetics that were applied to the United States Patent and Trademark Office from 1970 to 2016. The results show that women's participation in cosmetic inventions is becoming active and has experienced many changes in technical characteristics, but in terms of performance, it is still sluggish. This study is expected to contribute to deepening our understanding about gender issues in technology development.


Assuntos
Cosméticos , Patentes como Assunto , Feminino , Humanos , Invenções , Estados Unidos , Inventores , Masculino
4.
JAMA Health Forum ; 5(8): e242530, 2024 Aug 02.
Artigo em Inglês | MEDLINE | ID: mdl-39150730

RESUMO

Importance: Understanding how patent expirations affect drug prices is crucial because price changes directly inform accurate cost-effectiveness assessments. This study investigates the association between patent expirations and drug prices in 8 high-income countries and evaluates how the changes affect cost-effectiveness assessments. Objective: To analyze how the expiration of drug patents is associated with drug price changes and to assess the implications of these price changes for cost-effectiveness evaluations. Design, Setting, and Participants: This cohort study performed an event study design using data from 8 high-income countries to assess the association between patent expiration and drug prices, and created a simulation model to understand the implications for cost-effectiveness analyses. The simulation cost-effectiveness model analyzed the implications of including or ignoring postpatent price dynamics. Exposure: Drug patent expiration. Main Outcomes and Measures: Change in drug prices and differences in incremental cost-effectiveness ratios when considering vs ignoring postpatent price dynamics. Results: The sample comprised 505 drugs undergoing patent expiration in Australia, Canada, France, Germany, Japan, Switzerland, UK, and US. Price decreases were statistically significant over the 8 years after patent expiration, with the fastest price declines observed in the US: 32% (95% CI, 24%-39%) in year 1 after patent expiration and 82% (95% CI, 71%-89%) in the 8 years after patent expiration. Estimates for other nations ranged from a decrease of 64% in Australia to 18% in Switzerland in the 8 years after expiration. The cost-effectiveness simulation model indicated that not accounting for generic entry into the market may produce biased incremental cost-effectiveness ratios of 40% to -40%, depending on the scenario. Conclusions and Relevance: The findings of this cohort study demonstrate that drug prices were reduced substantially after patent expirations in high-income countries. Therefore, incorporating information on patent status and pricing dynamics in cost-effectiveness assessment analyses is necessary for producing accurate economic evaluations of new drugs.


Assuntos
Análise Custo-Benefício , Países Desenvolvidos , Custos de Medicamentos , Patentes como Assunto , Países Desenvolvidos/economia , Humanos , Custos de Medicamentos/estatística & dados numéricos , Estudos de Coortes , Medicamentos Genéricos/economia , Austrália , Comércio/economia , Comércio/estatística & dados numéricos , Comércio/legislação & jurisprudência , Estados Unidos
6.
Int J Pharm ; 661: 124462, 2024 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-39002819

RESUMO

Three-dimensional printing (3D printing) or "additive manufacturing" first came to prominence in the field of engineering, in particular in the transport sector where the value of its fast and accurate prototyping and manufacture of spare parts was quickly recognised. However, over the last ten years, this revolutionary technology has disrupted established manufacture in an increasingly diverse range of technical areas. Perhaps the most unexpected of these is pharmaceuticals - not merely the manufacture of products such as surgically inserted implants, but also of dosage formulations themselves - now available in all manner of printed delivery forms and vehicles and showing promising control of release properties though 3D printing process choices. This review will provide an overview of how 3D printing technology has developed and expanded across technological boundaries during the past decade, with a closer look at the current opportunities and barriers to its widespread adoption, particularly in the medical and pharmaceutical sectors. Special attention has been paid to patents as a boost and barrier to the expansion of 3D printing in the medical and pharmaceutical sector, with a focus on the patent literature.


Assuntos
Impressão Tridimensional , Humanos , Tecnologia Farmacêutica/métodos , Patentes como Assunto , Sistemas de Liberação de Medicamentos , Preparações Farmacêuticas/química
7.
Expert Opin Ther Pat ; 34(8): 593-610, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38946486

RESUMO

INTRODUCTION: Focal adhesion kinase (FAK) is a cytoplasmic non-receptor tyrosine kinase over-expressed in various malignancies which is related to various cellular functions such as adhesion, metastasis and proliferation. AREAS COVERED: There is growing evidence that FAK is a promising therapeutic target for designing inhibitors by regulating the downstream pathways of FAK. Some potential FAK inhibitors have entered clinical phase research. EXPERT OPINION: FAK could be an effective target in medicinal chemistry research and there were a variety of FAKIs have been patented recently. Here, we updated an overview of design, synthesis and structure-activity relationship of chemotherapeutic FAK inhibitors (FAKIs) from 2017 until now based on our previous work. We hope our efforts can broaden the understanding of FAKIs and provide new ideas and insights for future cancer treatment from medicinal chemistry point of view.


Assuntos
Antineoplásicos , Desenho de Fármacos , Proteína-Tirosina Quinases de Adesão Focal , Neoplasias , Patentes como Assunto , Inibidores de Proteínas Quinases , Animais , Humanos , Antineoplásicos/farmacologia , Antineoplásicos/química , Química Farmacêutica , Desenvolvimento de Medicamentos , Proteína-Tirosina Quinases de Adesão Focal/antagonistas & inibidores , Proteína-Tirosina Quinases de Adesão Focal/metabolismo , Terapia de Alvo Molecular , Neoplasias/tratamento farmacológico , Neoplasias/patologia , Neoplasias/enzimologia , Inibidores de Proteínas Quinases/farmacologia , Inibidores de Proteínas Quinases/química , Relação Estrutura-Atividade
8.
PLoS One ; 19(7): e0307165, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39012865

RESUMO

This study is the first to examine the gender gap in academic patenting among faculty members in Chinese universities, a critical issue for the sustainable development of scientific research and innovation. Using a unique dataset that includes the patenting activities and professional status of 1,836 faculty members in life science-related departments at 36 top Chinese universities, this research reveals an evolving landscape of patenting dynamics. The trend of male faculty members leading in the annual number of patent applications and patents granted has shifted among newly graduated faculty members. Female faculty submit and receive their first patent applications significantly earlier than male faculty. However, male faculty are more likely to be lead inventors, and this gender gap remains difficult to close, with female faculty more likely to be supporting inventors. This research is contextualized within the broader framework of China's university tenure reform and the growing presence of women in the life sciences. While progress is evident, the study uncovers persistent systemic barriers that prevent women from fully translating their research into patentable innovations. By identifying these social and institutional barriers, our study not only sheds light on the gender gap, but also suggests policy measures to promote gender equity in scientific innovation, making it a critical read for policymakers and academic leaders.


Assuntos
Disciplinas das Ciências Biológicas , Docentes , Patentes como Assunto , Universidades , Humanos , Feminino , China , Masculino , Patentes como Assunto/estatística & dados numéricos , Docentes/estatística & dados numéricos , Fatores Sexuais
9.
Environ Sci Pollut Res Int ; 31(33): 45970-46001, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38981964

RESUMO

Natural gas hydrate (NGH) is a significant alternative energy resource in achieving carbon neutrality. The developmental trend and competitive landscape of NGH exploitation and production are crucial for policymakers in government, managers of enterprises, and researchers. This study introduces a novel framework for conducting an in-depth analysis of NGH, integrating patentometrics, technology evolution, and correlation relationships to monitor developmental trends and competitive landscape through patent analysis. The results indicate that China, the USA, and Japan have distinct technology advantages. Current technological developments in the NGH field focus primarily on extraction technologies, equipment, and processing systems. The co-opetition analysis among countries reveals that the most extensive international cooperation network is primarily in Europe and the USA, with national partnerships in Asia concentrated in China and Japan. Institutional cooperation remains limited, primarily within universities in China, while both the USA and Japan foster collaboration between enterprises. The competitive landscapes of key NGH-related technologies among countries and institutions are also examined. This study contributes not only to monitoring the developmental trend and competitive landscape in NGH but also to providing policy recommendations for government and enterprises regarding strategic management and collaborative innovation.


Assuntos
Gás Natural , China , Japão , Estados Unidos , Patentes como Assunto
11.
Expert Opin Ther Pat ; 34(9): 789-806, 2024 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-38994687

RESUMO

INTRODUCTION: Polo-like kinases (PLKs) have five isoforms, all of which play crucial roles in cell cycle and cell proliferation, offering opportunities for drug design and treatment of cancers and other related diseases. Notably, PLK1 and PLK4 have been extensively investigated as cancer drug targets. One distinctive feature of PLKs is the presence of a unique polo-box domain (PBD), which regulates kinase activity and subcellular localization. This provides possibilities for specifically targeting PLKs. AREA COVERED: This article provides an overview of the roles of PLKs in various cancers and related diseases, as well as the drug development involving PLKs, with a particular focus on PLK1 and PLK4. It summarizes the PLK1 and PLK4 inhibitors that have been disclosed in patents or literature (from 2018 - present), which were sourced from SciFinder and WIPO database. EXPERT OPINION: After two decades of drug development on PLKs, several drugs progressed into clinical trials for the treatment of many cancers; however, none of them has been approved yet. Further elucidating the mechanisms of PLKs and identifying and developing highly selective ATP-competitive inhibitors, highly potent drug-like PBD inhibitors, degraders, etc. may provide new opportunities for cancer therapy and the treatment for several nononcologic diseases. PLKs inhibition-based combination therapies can be another helpful strategy.


Assuntos
Antineoplásicos , Proteínas de Ciclo Celular , Desenho de Fármacos , Desenvolvimento de Medicamentos , Neoplasias , Patentes como Assunto , Quinase 1 Polo-Like , Inibidores de Proteínas Quinases , Proteínas Serina-Treonina Quinases , Proteínas Proto-Oncogênicas , Humanos , Proteínas Serina-Treonina Quinases/antagonistas & inibidores , Proteínas Serina-Treonina Quinases/metabolismo , Neoplasias/tratamento farmacológico , Neoplasias/patologia , Neoplasias/enzimologia , Inibidores de Proteínas Quinases/farmacologia , Proteínas de Ciclo Celular/antagonistas & inibidores , Proteínas de Ciclo Celular/metabolismo , Animais , Antineoplásicos/farmacologia , Proteínas Proto-Oncogênicas/antagonistas & inibidores , Proteínas Proto-Oncogênicas/metabolismo , Proliferação de Células/efeitos dos fármacos , Terapia de Alvo Molecular
12.
Expert Opin Ther Pat ; 34(9): 825-842, 2024 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-39011556

RESUMO

INTRODUCTION: Cyclin-dependent protein kinase 4/6 (CDK4/6) is a class of serine/threonine protein kinases that plays a key role in the regulation of the cell cycle. CDK4/6 is highly expressed in cancers such as breast cancer, melanoma, and non-small cell lung cancer (NSCLC). Currently, a variety of CDK4/6 inhibitors have been developed, aiming to develop effective inhibitors to solve CDK4/6 resistance and toxicity. AREAS COVERED: This article searches patents through Espacenet and reviews the development of widely studied CDK inhibitors and FDA-approved CDK4/6 inhibitors, as well as the latest progress of patented inhibitors with good inhibitory activity against CDK4/6 from 2020 to now. EXPERT OPINION: CDK4/6 is highly expressed in many tumors and has become an important anti-tumor target. Among the patents from 2020 to the present, many inhibitors have good kinase inhibitory effects on CDK4/6 and also show great development potential in anti-tumor. However, there is still an urgent need to develop novel CDK4/6 inhibitors that address challenges such as drug resistance, toxicity, and selectivity.


Assuntos
Antineoplásicos , Quinase 4 Dependente de Ciclina , Quinase 6 Dependente de Ciclina , Desenvolvimento de Medicamentos , Resistencia a Medicamentos Antineoplásicos , Neoplasias , Patentes como Assunto , Inibidores de Proteínas Quinases , Humanos , Quinase 4 Dependente de Ciclina/antagonistas & inibidores , Quinase 6 Dependente de Ciclina/antagonistas & inibidores , Inibidores de Proteínas Quinases/farmacologia , Neoplasias/tratamento farmacológico , Neoplasias/patologia , Antineoplásicos/farmacologia , Animais
13.
Expert Opin Ther Pat ; 34(9): 773-788, 2024 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-39023243

RESUMO

INTRODUCTION: Nearly two decades after leucine rich repeat kinase 2 (LRRK2) was discovered as a genetic determinant of Parkinson's disease (PD), LRRK2 has emerged a priority therapeutic target in PD and inhibition of its activity is hypothesized to be beneficial. AREAS COVERED: LRRK2 targeting agents, in particular kinase inhibitors and agents reducing LRRK2 expression show promise in model systems and have progressed to phase I and phase II clinical testing for PD. Several additional targeting strategies for LRRK2 are emerging, based on promoting specific 'healthy' LRRK2 quaternary structures, heteromeric complexes and conformations. EXPERT OPINION: It can be expected that LRRK2 targeting strategies may proceed to phase III clinical testing for PD in the next five years, allowing the field to discover the real clinical value of LRRK2 targeting strategies.


Assuntos
Antiparkinsonianos , Serina-Treonina Proteína Quinase-2 com Repetições Ricas em Leucina , Doença de Parkinson , Patentes como Assunto , Inibidores de Proteínas Quinases , Serina-Treonina Proteína Quinase-2 com Repetições Ricas em Leucina/antagonistas & inibidores , Serina-Treonina Proteína Quinase-2 com Repetições Ricas em Leucina/genética , Humanos , Doença de Parkinson/tratamento farmacológico , Doença de Parkinson/fisiopatologia , Animais , Inibidores de Proteínas Quinases/farmacologia , Antiparkinsonianos/farmacologia , Terapia de Alvo Molecular , Desenvolvimento de Medicamentos
14.
Expert Opin Ther Pat ; 34(9): 807-823, 2024 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-39078140

RESUMO

INTRODUCTION: The sodium-glucose co-transporter 2 (SGLT2) inhibitors are FDA-approved class of drugs for diabetes management. They improve glycemic control by inducing glucosuria. Notwithstanding with potent anti-hyperglycemic activity, SGLT2 inhibitors are emerging as drugs with multifaceted therapeutic potential, evidenced for cardioprotective, renoprotective, antihypertensive, and neuroprotective activities. Continuous attempts are being accomplished through structural modification, development of new formulation, or combination with other drugs, to enhance the bioactivity spectrum of SGLT2 inhibitors for better management of diabetes and related complications. AREAS COVERED: This review comprises a summary of patent applications, acquired using the Espacenet Patent Search database, concerning SGLT2 inhibitors from 2019 to 2023, with focus on improving therapeutic potentials in management of diabetes and metabolic complications. EXPERT OPINION: SGLT2 inhibitors have provided an exciting treatment option for diabetes. Originally developed as anti-hyperglycemic agents, SGLT2 inhibitors exert pleiotropic metabolic responses and have emerged as promising antidiabetic agents with cardio-protective and reno-protective activities. Given their distinct therapeutic profile, SGLT2 inhibitors have revolutionized the management of diabetes and associated complications. Emerging evidences on their therapeutic potential against cancer, male reproductive dysfunctions, and neurodegenerative diseases indicate that further research in this field may unfold novel prospective on their plausible use in the management of other chronic conditions.


Assuntos
Desenvolvimento de Medicamentos , Hipoglicemiantes , Patentes como Assunto , Inibidores do Transportador 2 de Sódio-Glicose , Humanos , Inibidores do Transportador 2 de Sódio-Glicose/farmacologia , Animais , Hipoglicemiantes/farmacologia , Diabetes Mellitus Tipo 2/tratamento farmacológico , Diabetes Mellitus Tipo 2/fisiopatologia , Diabetes Mellitus/tratamento farmacológico , Diabetes Mellitus/fisiopatologia
15.
JAMA Health Forum ; 5(7): e241886, 2024 Jul 05.
Artigo em Inglês | MEDLINE | ID: mdl-39028656

RESUMO

This study examines the use of the Track One prioritized patent examination program by pharmaceutical manufacturers from 2011 to 2022.


Assuntos
Patentes como Assunto , Patentes como Assunto/legislação & jurisprudência , Humanos , Indústria Farmacêutica/legislação & jurisprudência , Estados Unidos , Preparações Farmacêuticas
16.
Expert Opin Ther Pat ; 34(8): 723-732, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38965930

RESUMO

INTRODUCTION: Boswellic acids (BAs) are a group of pentacyclic triterpenoids of the ursane and oleanane type. They have shown very interesting biological properties that have led to the development of a number of synthesis protocols. Both natural BAs and their synthetic derivatives may be useful in the treatment of a variety of cancers, viral infections and inflammatory diseases. AREAS COVERED: This review covers patents relating to the therapeutic activities of natural BAs and their synthetic derivatives. The latest patented studies of boswellic acids (are summarized by using the keywords 'boswellic acid,' in SciFinder, PubMed, and Google Patents and databases in the year from 2016 to 2023. EXPERT OPINION: Boswellic acids have shown potent antiviral, anticancer and anti-inflammatory potential. Few BAs analogues have been prepared by modification at the C24-CO2H functional groups. In particular, the C-24 amide and amino analogues have shown enhanced anticancer effects compared to the parent AKBA. In addition, BAs have the ability to form conjugates with other antiviral, anti-inflammatory and anticancer drugs that synergistically enhance their biological efficacy. In addition, this conjugation strategy will increase the solubility and bioavailability of BAs, which is one of the most important issues in the development of BAs.


Assuntos
Anti-Inflamatórios , Antivirais , Desenvolvimento de Medicamentos , Neoplasias , Patentes como Assunto , Triterpenos , Humanos , Triterpenos/farmacologia , Triterpenos/química , Animais , Antivirais/farmacologia , Anti-Inflamatórios/farmacologia , Neoplasias/tratamento farmacológico , Antineoplásicos/farmacologia , Inflamação/tratamento farmacológico , Viroses/tratamento farmacológico , Disponibilidade Biológica
17.
Drug Res (Stuttg) ; 74(6): 255-268, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38968949

RESUMO

This comprehensive review endeavors to illuminate the nuanced facets of linalool, a prominent monoterpene found abundantly in essential oils, constituting a massive portion of their composition. The biomedical relevance of linalool is a key focus, highlighting its therapeutic attributes observed through anti-nociceptive effects, anxiolytic properties, and behavioral modulation in individuals affected by dementia. These findings underscore the compound's potential application in biomedical applications. This review further explores contemporary formulations, delineating the adaptability of linalool in nano-emulsions, microemulsions, bio-capsules, and various topical formulations, including topical gels and lotions. This review covers published and granted patents between 2018-2024 and sheds light on the evolving landscape of linalool applications, revealing advancements in dermatological, anti-inflammatory, and antimicrobial domains.


Assuntos
Monoterpenos Acíclicos , Humanos , Monoterpenos Acíclicos/farmacologia , Monoterpenos Acíclicos/uso terapêutico , Monoterpenos Acíclicos/química , Anti-Inflamatórios/uso terapêutico , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/administração & dosagem , Animais , Anti-Infecciosos/uso terapêutico , Anti-Infecciosos/farmacologia , Ansiolíticos/uso terapêutico , Ansiolíticos/farmacologia , Analgésicos/uso terapêutico , Analgésicos/farmacologia , Patentes como Assunto , Emulsões , Óleos Voláteis/uso terapêutico , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Fármacos Dermatológicos/uso terapêutico , Fármacos Dermatológicos/farmacologia , Fármacos Dermatológicos/administração & dosagem
18.
Expert Opin Ther Pat ; 34(9): 733-757, 2024 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-38958471

RESUMO

INTRODUCTION: COX-2 is a crucial enzyme in the manufacture of prostaglandins. The enzyme's metabolites might have an important function as regulators of the inflammatory response and other medical conditions such as cancer. Selective COX-2 inhibitors are believed to enhance or reverse the response of cancer chemotherapeutics. AREAS COVERED: This study addresses the chemical structures as well as the antitumor activity of new COX-2 inhibitors produced in the recent five years, aiming to provide an insight into the mechanism of COX-2 induced PGE2 powerful signal in cancer development. EXPERT OPINION: The significance of selective COX-2 inhibitors as an efficient superfamily of compounds with anti-inflammatory, anti-Alzheimer's, anti-Parkinson's disease, and anticancer properties has piqued the passion of academics in the field of drug development. Long-term usage of selective COX-2 inhibitors, such as celecoxib has been proven in clinical trials to lower the incidence of several human malignancies. Furthermore, celecoxib has the potential to greatly increase the effectiveness of chemotherapy. Our extensive understanding of selective COX-2 inhibitor SAR may aid in the development of safer and more effective selective COX-2 inhibitors as cancer chemopreventive agents. This review focuses on the different structural classes of selective COX-2 inhibitors, with a particular emphasis on their SAR.


Assuntos
Antineoplásicos , Inibidores de Ciclo-Oxigenase 2 , Ciclo-Oxigenase 2 , Desenvolvimento de Medicamentos , Neoplasias , Patentes como Assunto , Humanos , Inibidores de Ciclo-Oxigenase 2/farmacologia , Antineoplásicos/farmacologia , Neoplasias/tratamento farmacológico , Neoplasias/enzimologia , Animais , Ciclo-Oxigenase 2/metabolismo , Ciclo-Oxigenase 2/efeitos dos fármacos , Relação Estrutura-Atividade , Dinoprostona/metabolismo , Desenho de Fármacos
19.
Expert Opin Ther Pat ; 34(9): 759-772, 2024 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-38979973

RESUMO

INTRODUCTION: Phosphodiesterase 9 (PDE9) has been demonstrated as a potential target for neurological disorders and cardiovascular diseases, such as Alzheimer's disease and heart failure. For the last few years, a series of PDE9 inhibitors with structural diversities have been developed and patented by researchers and pharmaceutical companies, providing insights into first-in-class therapies of PDE9 drug candidates. AREA COVERED: This review provides an overview of PDE9 inhibitors in patents from 2018 to the present. EXPERT OPINION: Only a few of the current PDE9 inhibitors are highly selective over other PDEs, which limits their application in pharmacological and clinical research. The design and development of highly selective PDE9 inhibitors remain the top priority in future research. The advantages of targeting PDE9 rather than other PDEs in treating neurodegenerative diseases need to be explained thoroughly. Besides, application of PDE9 inhibitor-based combination therapies sheds light on treating diabetes and refractory heart diseases. Finally, PDE9 inhibitors should be further explored in clinical indications beyond neurological disorders and cardiovascular diseases.


Assuntos
Doenças Cardiovasculares , Desenvolvimento de Medicamentos , Patentes como Assunto , Inibidores de Fosfodiesterase , Humanos , Animais , Inibidores de Fosfodiesterase/farmacologia , Doenças Cardiovasculares/tratamento farmacológico , Desenho de Fármacos , Doenças do Sistema Nervoso/tratamento farmacológico , 3',5'-AMP Cíclico Fosfodiesterases/antagonistas & inibidores , 3',5'-AMP Cíclico Fosfodiesterases/metabolismo , Doenças Neurodegenerativas/tratamento farmacológico , Doenças Neurodegenerativas/fisiopatologia
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