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Patenting perspective of modulators of ClpP endopeptidase: 2019-present ClpP内肽酶调节剂的专利前景:2019年至今
IF 6.6 2区 医学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2024-09-16 DOI: 10.1080/13543776.2024.2404233
Zhenyu Wang, Liqing He, Ziheng Fan, Youfu Luo
ClpP is a highly conserved serine protease that plays a crucial role in maintaining protein homeostasis in both bacterial cells and human mitochondria. Several studies have demonstrated the potenti...
ClpP 是一种高度保守的丝氨酸蛋白酶,在维持细菌细胞和人类线粒体中的蛋白质平衡方面起着至关重要的作用。有几项研究已经证明了 ClpP 在细菌细胞和人类线粒体中的潜在作用。
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引用次数: 0
MEK inhibitors in oncology: a patent review and update (2016 - present) 肿瘤学中的 MEK 抑制剂:专利回顾与更新(2016 年至今)
IF 6.6 2区 医学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2024-09-14 DOI: 10.1080/13543776.2024.2403634
Anjali Suryavanshi, Vandana, Yugal Kishor Shukla, Vipul Kumar, Pragya Gupta, Vivek Asati, Debarshi Kar Mahapatra, Raj K. Keservani, Sanmati Kumar Jain, Sanjay Kumar Bharti
Mitogen-activated protein kinase (MEK) is one of the important components of Ras/Raf/MEK/ERK signaling pathway, transduces signal for cell growth, differentiation, and development. Deregulation of ...
丝裂原活化蛋白激酶(MEK)是Ras/Raf/MEK/ERK信号通路的重要组成部分之一,传递细胞生长、分化和发育的信号。对...
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引用次数: 0
Ephrin receptor type-A2 (EphA2) targeting in cancer: a patent review (2018-present). 癌症中的Ephrin受体A2型(EphA2)靶向治疗:专利回顾(2018年至今)。
IF 6.6 2区 医学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2024-09-11 DOI: 10.1080/13543776.2024.2402382
Massimiliano Tognolini,Francesca Romana Ferrari,Alfonso Zappia,Carmine Giorgio
INTRODUCTIONEphA2 is a tyrosine kinase receptor and is considered a promising target in cancer. Different approaches are used to target EphA2 receptor, and a lot of preclinical data demonstrate the potential exploitation of this receptor in clinical oncology for diagnosis and cancer therapy, including immunotherapy.AREAS COVEREDIn this review, we have summarized the recent patents involving the EphA2 targeting in cancer. For this aim, we used the patent database Patentscope covering the time period of 2018-present. Preclinical and clinical data of the inventions were considered when published on peer reviewed journals. Moreover, the clinicalTrial.gov identifiers (NCT numbers) were included when available. For an easier and more immediate reading, we classify the patents in different categories, considering the nature (aptamers, small molecules, antibodies, peptides, antigens and chimeric antigen receptors) of the inventions exploiting EphA2 in clinical oncology.EXPERT OPINIONDespite the availability of a plethora of chemically diverse agents, there are no approved anticancer drugs targeting EphA2 yet. However, these intellectual properties, some of which supported by strong preclinical evidence, keep the hope that, after more than 30 years from its discovery, we will finally see the first EphA2 targeting agent approved in clinical oncology.
导言EphA2是一种酪氨酸激酶受体,被认为是一种很有前景的癌症靶点。针对 EphA2 受体采用了不同的方法,大量临床前数据证明了该受体在临床肿瘤学诊断和癌症治疗(包括免疫疗法)中的潜在利用价值。 涵盖领域在本综述中,我们总结了近期涉及癌症中 EphA2 靶向的专利。为此,我们使用了专利数据库 Patentscope,时间跨度为 2018 年至今。在同行评审期刊上发表的发明的临床前和临床数据也在考虑之列。此外,如果有临床试验(clinicalTrial.gov)标识符(NCT 编号),我们也将其纳入其中。为了更方便、更直接地阅读,我们根据在临床肿瘤学中利用 EphA2 的发明的性质(aptamers、小分子、抗体、肽、抗原和嵌合抗原受体),将专利分为不同类别。不过,这些知识产权(其中一些有强有力的临床前证据支持)让我们看到了希望:在发现 EphA2 30 多年后,我们终于能看到首个 EphA2 靶向药物获批用于临床肿瘤学。
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引用次数: 0
Helicase-primase inhibitors for the treatment of herpes simplex virus infections - patent evaluation of WO2023/225162 from gilead sciences inc. 用于治疗单纯疱疹病毒感染的螺旋酶-primase 抑制剂--对吉利德科学公司的 WO2023/225162 的专利评估。
IF 6.6 2区 医学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2024-09-11 DOI: 10.1080/13543776.2024.2403618
Christian Gege,Gerald Kleymann
Helicase-primase is an interesting target for small molecule therapy of herpes simplex virus (HSV) infections. With amenamevir already approved for varicella-zoster virus and herpes simplex in Japan and with pritelivir's granted breakthrough therapy designation for the treatment of acyclovir-resistant HSV infections in immunocompromised patients, the target has sparked interest in helicase-primase inhibitors (HPIs). Here we analyze the first patent application from Gilead in this field, which pursued a me-too approach combining elements from an old Bayer together with a recent Medshine HPI application (which covers the Phaeno Therapeutics drug candidate HN0037). The asset was contributed to Assembly Biosciences, where it is under development as ABI-1179 at the investigational new drug (IND) enabling stage for high-recurrence genital herpes. A structure proposal for indolinoyl derivative ABI-1179 is presented, showing its potential opportunities and limitations compared to other HPIs.
螺旋酶-primase 是小分子疗法治疗单纯疱疹病毒(HSV)感染的一个有趣靶点。日本已批准阿米那韦用于治疗水痘-带状疱疹病毒和单纯疱疹,而普利特韦也被授予突破性疗法称号,用于治疗免疫力低下患者的阿昔洛韦耐药 HSV 感染,因此该靶点引发了人们对螺旋酶-primase 抑制剂(HPIs)的兴趣。在此,我们分析了吉利德公司在这一领域的首个专利申请,该专利申请采用了一种 "me-too "方法,将旧的拜耳专利申请元素与最近的 Medshine HPI 申请(涉及 Phaeno Therapeutics 候选药物 HN0037)结合在一起。该资产已转让给 Assembly Biosciences 公司,该公司正在开发 ABI-1179 药物,目前正处于新药临床试验 (IND) 阶段,用于治疗高复发性生殖器疱疹。本文介绍了吲哚啉酰衍生物 ABI-1179 的结构方案,展示了它与其他 HPI 相比的潜在机会和局限性。
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引用次数: 0
Selective COX-2 inhibitors as anticancer agents: a patent review (2018-2023). 作为抗癌剂的选择性 COX-2 抑制剂:专利综述(2018-2023 年)。
IF 5.4 2区 医学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2024-09-01 Epub Date: 2024-07-03 DOI: 10.1080/13543776.2024.2373771
Mohammad Mahboubi-Rabbani, Amir Hossein Abdolghaffari, Mahsa Ghesmati, Ali Amini, Afshin Zarghi

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.

简介COX-2 是制造前列腺素的关键酶。该酶的代谢产物可能具有调节炎症反应和癌症等其他疾病的重要功能。据信,选择性 COX-2 抑制剂可增强或逆转癌症化疗药物的反应:本研究探讨了近五年来产生的新型 COX-2 抑制剂的化学结构和抗肿瘤活性,旨在深入了解 COX-2 诱导 PGE2 强信号在癌症发展中的作用机制:选择性 COX-2 抑制剂作为具有抗炎、抗老年痴呆症、抗帕金森病和抗癌特性的高效化合物超家族,其重要意义激发了学术界在药物开发领域的热情。临床试验证明,长期使用选择性 COX-2 抑制剂(如塞来昔布)可降低多种人类恶性肿瘤的发病率。此外,塞来昔布还有可能大大提高化疗的效果。我们对选择性 COX-2 抑制剂 SAR 的广泛了解有助于开发更安全、更有效的选择性 COX-2 抑制剂作为癌症化学预防药物。本综述将重点介绍不同结构类别的选择性 COX-2 抑制剂,并特别强调其 SAR。
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引用次数: 0
SGLT2 inhibitors for the treatment of diabetes: a patent review (2019-23). 用于治疗糖尿病的 SGLT2 抑制剂:专利回顾(2019-23)。
IF 5.4 2区 医学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2024-09-01 Epub Date: 2024-08-02 DOI: 10.1080/13543776.2024.2379929
Rahul Baghel, Nikita Chhikara, Pawan Kumar, Akhilesh Kumar Tamrakar

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.

简介钠-葡萄糖协同转运体 2(SGLT2)抑制剂是美国食品及药物管理局批准的一类糖尿病治疗药物。它们通过诱导葡萄糖尿改善血糖控制。尽管 SGLT2 抑制剂具有强大的降糖活性,但它正在成为具有多方面治疗潜力的药物,其心脏保护、肾脏保护、抗高血压和神经保护活性已得到证实。人们正不断尝试通过结构改造、开发新制剂或与其他药物联用来增强 SGLT2 抑制剂的生物活性,从而更好地控制糖尿病及相关并发症:本综述包括通过 Espacenet 专利检索数据库获取的 2019-2023 年有关 SGLT2 抑制剂的专利申请摘要,重点关注提高糖尿病和代谢并发症的治疗潜力:SGLT2抑制剂为糖尿病提供了一种令人振奋的治疗选择。SGLT2 抑制剂最初是作为抗高血糖药物开发的,现在已产生了多种代谢反应,并已成为具有心脏保护和肾脏保护活性的有前途的抗糖尿病药物。鉴于其独特的治疗特性,SGLT2 抑制剂彻底改变了糖尿病及相关并发症的治疗。有关其对癌症、男性生殖功能障碍和神经退行性疾病的治疗潜力的新证据表明,该领域的进一步研究可能会为其在其他慢性疾病的治疗中的合理应用带来新的前景。
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引用次数: 0
Progress with polo-like kinase (PLK) inhibitors: a patent review (2018-present). 多聚样激酶(PLK)抑制剂的进展:专利回顾(2018年至今)。
IF 5.4 2区 医学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2024-09-01 Epub Date: 2024-07-15 DOI: 10.1080/13543776.2024.2379924
Shirong Bian, Ru Zhang, Jianyu Nie, Mingxing Zhu, Zhouling Xie, Chenzhong Liao, Qin Wang

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.

导言:Polo-like激酶(PLKs)有五种同工酶,它们都在细胞周期和细胞增殖中发挥关键作用,为癌症和其他相关疾病的药物设计和治疗提供了机会。值得注意的是,PLK1 和 PLK4 已作为癌症药物靶点被广泛研究。PLK 的一个显著特点是存在一个独特的多聚酶盒结构域 (PBD),该结构域可调节激酶活性和亚细胞定位。这为特异性靶向 PLKs 提供了可能性:本文概述了 PLKs 在各种癌症和相关疾病中的作用,以及涉及 PLKs 的药物开发,尤其关注 PLK1 和 PLK4。文章总结了已在专利或文献中公开的 PLK1 和 PLK4 抑制剂(从 2018 年至今),这些专利或文献均来自 SciFinder 和 WIPO 数据库:经过二十年的PLKs药物研发,一些药物已进入临床试验阶段,用于治疗多种癌症,但目前还没有一种药物获得批准。进一步阐明PLKs的作用机制,鉴定和开发高选择性ATP竞争性抑制剂、强效类药物PBD抑制剂、降解剂等,可为癌症治疗和多种非肿瘤性疾病的治疗提供新的机遇。以 PLKs 抑制剂为基础的联合疗法可能是另一种有用的策略。
{"title":"Progress with polo-like kinase (PLK) inhibitors: a patent review (2018-present).","authors":"Shirong Bian, Ru Zhang, Jianyu Nie, Mingxing Zhu, Zhouling Xie, Chenzhong Liao, Qin Wang","doi":"10.1080/13543776.2024.2379924","DOIUrl":"10.1080/13543776.2024.2379924","url":null,"abstract":"<p><strong>Introduction: </strong>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.</p><p><strong>Area covered: </strong>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.</p><p><strong>Expert opinion: </strong>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.</p>","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":null,"pages":null},"PeriodicalIF":5.4,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141590093","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
A patent review of small molecule CDK4/6 inhibitors in the treatment of cancer: 2020-present. 治疗癌症的小分子 CDK4/6 抑制剂专利回顾:2020 年至今。
IF 5.4 2区 医学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2024-09-01 Epub Date: 2024-07-17 DOI: 10.1080/13543776.2024.2379926
Xiaoling Huang, Shidi Xu, Lei Duan, Shan Xu, Wufu Zhu

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.

简介细胞周期蛋白依赖性蛋白激酶4/6(CDK4/6)是一类丝氨酸/苏氨酸蛋白激酶,在细胞周期调控中发挥着关键作用。CDK4/6在乳腺癌、黑色素瘤和非小细胞肺癌(NSCLC)等癌症中高度表达。目前,已开发出多种 CDK4/6 抑制剂,旨在开发有效的抑制剂来解决 CDK4/6 的耐药性和毒性问题:本文通过Espacenet检索专利,回顾了被广泛研究的CDK抑制剂和FDA批准的CDK4/6抑制剂的发展情况,以及2020年至今对CDK4/6具有良好抑制活性的专利抑制剂的最新进展:CDK4/6在许多肿瘤中高表达,已成为重要的抗肿瘤靶点。在2020年至今的专利中,许多抑制剂对CDK4/6具有良好的激酶抑制作用,在抗肿瘤方面也显示出巨大的发展潜力。然而,目前仍迫切需要开发新型 CDK4/6 抑制剂,以解决耐药性、毒性和选择性等难题。
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引用次数: 0
Leucine-rich repeat kinase 2 (LRRK2) inhibitors for Parkinson's disease: a patent review of the literature to date. 治疗帕金森病的富亮氨酸重复激酶 2 (LRRK2) 抑制剂:迄今为止的专利文献综述。
IF 5.4 2区 医学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2024-09-01 Epub Date: 2024-07-19 DOI: 10.1080/13543776.2024.2378076
Margaux Morez, Antonio Jesús Lara Ordóñez, Patricia Melnyk, Maxime Liberelle, Nicolas Lebègue, Jean-Marc Taymans

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.

简介:在富亮氨酸重复激酶 2 (LRRK2) 被发现是帕金森病 (PD) 的遗传决定因素近二十年后,LRRK2 已成为帕金森病的优先治疗靶点,抑制其活性被认为是有益的:LRRK2靶向药物,特别是激酶抑制剂和减少LRRK2表达的药物在模型系统中显示出前景,并已进入治疗帕金森病的I期和II期临床试验阶段。基于促进特定的 "健康 "LRRK2四元结构、异构体复合物和构象,正在出现其他几种LRRK2靶向策略:可以预计,LRRK2靶向策略可能会在未来五年内进入治疗帕金森病的III期临床试验阶段,从而让该领域发现LRRK2靶向策略的真正临床价值。
{"title":"Leucine-rich repeat kinase 2 (LRRK2) inhibitors for Parkinson's disease: a patent review of the literature to date.","authors":"Margaux Morez, Antonio Jesús Lara Ordóñez, Patricia Melnyk, Maxime Liberelle, Nicolas Lebègue, Jean-Marc Taymans","doi":"10.1080/13543776.2024.2378076","DOIUrl":"10.1080/13543776.2024.2378076","url":null,"abstract":"<p><strong>Introduction: </strong>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.</p><p><strong>Areas covered: </strong>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.</p><p><strong>Expert opinion: </strong>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.</p>","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":null,"pages":null},"PeriodicalIF":5.4,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141633115","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
The therapeutic potential of phosphodiesterase 9 (PDE9) inhibitors: a patent review (2018-present). 磷酸二酯酶 9(PDE9)抑制剂的治疗潜力:专利综述(2018 年至今)。
IF 5.4 2区 医学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2024-09-01 Epub Date: 2024-07-09 DOI: 10.1080/13543776.2024.2376632
Chen Zhang, Zhao-Hang Xue, Wei-Hao Luo, Mei-Yan Jiang, Yinuo Wu

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.

简介磷酸二酯酶9(PDE9)已被证明是神经系统疾病和心血管疾病(如阿尔茨海默病和心力衰竭)的潜在靶点。过去几年中,研究人员和制药公司开发了一系列结构多样化的 PDE9 抑制剂并申请了专利,为 PDE9 候选药物的一流疗法提供了启示:本综述概述了2018年至今的专利中的PDE9抑制剂.专家观点:本综述概述了2018年至今的专利中的PDE9抑制剂:目前的PDE9抑制剂中只有少数对其他PDE具有高选择性,这限制了它们在药理学和临床研究中的应用。设计和开发高选择性的PDE9抑制剂仍是未来研究的重中之重。在治疗神经退行性疾病方面,靶向 PDE9 而非其他 PDEs 的优势需要得到深入解释。此外,基于 PDE9 抑制剂的联合疗法在治疗糖尿病和难治性心脏病方面的应用也会带来启示。最后,除了神经系统疾病和心血管疾病之外,PDE9 抑制剂在临床适应症方面的应用也有待进一步探索。
{"title":"The therapeutic potential of phosphodiesterase 9 (PDE9) inhibitors: a patent review (2018-present).","authors":"Chen Zhang, Zhao-Hang Xue, Wei-Hao Luo, Mei-Yan Jiang, Yinuo Wu","doi":"10.1080/13543776.2024.2376632","DOIUrl":"10.1080/13543776.2024.2376632","url":null,"abstract":"<p><strong>Introduction: </strong>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.</p><p><strong>Area covered: </strong>This review provides an overview of PDE9 inhibitors in patents from 2018 to the present.</p><p><strong>Expert opinion: </strong>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.</p>","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":null,"pages":null},"PeriodicalIF":5.4,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141558497","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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Expert Opinion on Therapeutic Patents
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