EXPERT OPINION ON THERAPEUTIC PATENTS (ISSN 1354-3776 [PRINT], 1744-7674 [ELECTRONIC]) 是 MEDLINE 索引、同行评审的国际期刊，发表关于近期药物专利权利要求的评论文章，为未来发展提供专家意见，在科学文献的背景下。编辑欢迎：评论涵盖最近关于具有治疗潜力的化合物或应用的专利权利要求，包括具有特定分子靶标的生物治疗药物和小分子药物；和特定治疗领域的专利申请趋势专利评估审查个别专利的目的和化学和生物权利要求与知识产权相关问题的观点观众包括制药行业的科学家、管理人员和决策者以及与研发密切相关的其他人，例如我们的生物科学期刊，在此处登录以开始访问，最新的两卷完整卷免费提供给您 14 天。

Expert Opinion on Therapeutic Patents (ISSN 1354-3776 [PRINT], 1744-7674 [ELECTRONIC]) is an international peer-reviewed journal indexed in MEDLINE, focusing on commentaries regarding recent drug patent claims to provide expert insights for future developments. The editorial team welcomes reviews covering patent claims related to compounds or applications with therapeutic potential, including biotherapeutics and small molecules targeting specific molecular pathways, as well as trends in patent applications within specific therapeutic areas. The journal also evaluates the purposes of individual patents and discusses issues related to chemical and biological claims and intellectual property. The audience includes scientists, managers, and decision-makers in the pharmaceutical industry, as well as other professionals closely related to research and development. We offer free access to the latest two complete volumes for 14 days.

《Expert Opinion on Therapeutic Patents》（ISSN 1354-3776 [印刷版]，1744-7674 [电子版]）是一本国际同行评审的期刊，收录于MEDLINE，专注于近期药物专利的评论文章，旨在为未来的发展提供专家见解。编辑欢迎关于具有治疗潜力的化合物或应用的专利权利要求的评论，包括针对特定分子靶标的生物治疗药物和小分子药物，以及特定治疗领域的专利申请趋势。期刊还评估个别专利的目的，探讨与化学和生物权利要求及知识产权相关的问题。读者包括制药行业的科学家、管理人员和决策者，以及与研发密切相关的其他专业人士。我们提供最新的两卷完整卷，供您免费访问14天。

Expert Opinion on Therapeutic Patents

Introduction: The current SARS-CoV-2 pandemic urgently demands for both prevention and treatment strategies. RNA-dependent RNA-polymerase (RdRp), which has no counterpart in human cells, is an excellent target for drug development. Given the time-consuming process of drug development, repurposing drugs approved for other indications or at least successfully tested in terms of safety and tolerability, is an attractive strategy to rapidly provide an effective medication for severe COVID-19 cases.Areas covered: The currently available data and upcominSg studies on RdRp which can be repurposed to halt SARS-CoV-2 replication, are reviewed.Expert opinion: Drug repurposing and design of novel compounds are proceeding in parallel to provide a quick response and new specific drugs, respectively. Notably, the proofreading SARS-CoV-2 exonuclease activity could limit the potential for drugs designed as immediate chain terminators and favor the development of compounds acting through delayed termination. While vaccination is awaited to curb the SARS-CoV-2 epidemic, even partially effective drugs from repurposing strategies can be of help to treat severe cases of disease. Considering the high conservation of RdRp among coronaviruses, an improved knowledge of its activity invitro can provide useful information for drug development or drug repurposing to combat SARS-CoV-2 as well as future pandemics.

Ilaria Vicenti

Maurizio Zazzi

Francesco Saladini

SARS-CoV-2 RNA-dependent RNA polymerase as a therapeutic target for COVID-19

SARS-CoV-2 RNA依赖性RNA聚合酶作为COVID-19的治疗靶点

Introduction: Protease activated receptor 2 (PAR2) is a self-activated G protein-coupled receptor that has been implicated in several diseases, including inflammatory, gastrointestinal, respiratory, metabolic diseases, cancers and others, making it an important prospective drug target. No known endogenous ligands are available for PAR2, so having potent exogenous agonists and antagonists can be helpful for studying physiological functions of PAR2.Areas covered: This review covers agonist-, antagonist-, antibody- and pepducin-based modulators of PAR2 reported in patent applications between 2010–2015, along with their available structure-activity relationships, biological activities and potential uses for studying PAR2.Expert opinion: In the last six years, substantial efforts were made towards developing PAR2 modulators, but most lack potency or selectivity or have poor pharmacokinetic profiles. Many PAR2 modulators were assessed by measuring Gαq protein-mediated calcium release in cells. This may be insufficient to fully characterize ligand function, since different ligands signal through PAR2 via multiple signaling pathways. It may be feasible to develop biased ligands as drugs that can selectively modulate one or more specific signaling pathways linking PAR2 to a specific diseased state. Accordingly, potent, orally bioavailable, pathway- and receptor-selective PAR2 modulators may be an achievable goal to realizing effective drugs that can treat PAR2-mediated diseases.

Mei-Kwan Yau

Junxian Lim

Ligong Liu

David P. Fairlie

Protease activated receptor 2 (PAR2) modulators: a patent review (2010–2015)

蛋白酶激活受体2（PAR2）调节剂：专利综述（2010-2015）

Introduction: Human urate transporter 1 (URAT1), which is an influx transporter protein, is located at the apical surface of renal tubular cells and presumed to be the major transporter responsible for the reabsorption of urate from blood. About 90% of patients develop hyperuricemia due to insufficient urate excretion; thus, it is important to develop URAT1 inhibitors that could enhance renal urate excretion by blocking the reabsorption of urate anion.Areas covered: In this review, the authors addressed the patent applications (2016–2019) about URAT1 inhibitors and some medicinal chemistry strategies employed in these patents.Expert opinion: Substituent decorating, bioisosterism, and scaffold hopping are three common medicinal chemistry strategies used in the discovery of URAT1 inhibitors. Meanwhile, the introduction of sulfonyl group into small molecules has become one of the important strategies for structural optimization of URAT1 inhibitors. Furthermore, developing drug candidates targeting both URAT1 and xanthine oxidase (XOD) has attracted lots of interest and attention.

Yue Dong

Tong Zhao

Wei Ai

Waleed A. Zalloum

Dongwei Kang

Ting Wu

Xinyong Liu

Peng Zhan

Novel urate transporter 1 (URAT1) inhibitors: a review of recent patent literature (2016–2019)

新型尿酸转运蛋白1（URAT1）抑制剂：近期专利文献综述（2016-2019）

The E3 ubiquitin ligase Cbl-b is a novel target in immune-oncology, with critical roles in regulating T-cell activation and signaling pathways. By facilitating the ubiquitination and degradation of key signaling proteins, Cbl-b modulates immune responses, maintaining immune homeostasis and preventing unwarranted T-cell proliferation. The therapeutic potential of Cbl-b as a cancer immunotherapy target is underscored by its contribution to an immunosuppressive tumor microenvironment, with efforts currently underway to develop small-molecule inhibitors.

Riccardo Fusco

Zeinab Saedi

Imma Capriello

Andriy Lubskyy

Alexander Dömling

Expert opinion on therapeutic patents - manuscript ID EOTP-2024-ST-0024 has been submitted online

治疗专利专家意见 - 稿件编号 EOTP-2024-ST-0024 已在线提交

is a gram-negative bacterium that infects almost half of the World population. Although many infected people are symptom free, the microorganism can still cause a variety of gastrointestinal disorders and even gastric adenocarcinoma. It is considered a priority pathogen for the development of new antibiotics by the World Health Organisation (WHO). Many virulence factors of

Özlen Güzel-Akdemir

Atilla Akdemir

Urease inhibitors for the treatment of <i>H. pylori</i>

尿素酶抑制剂用于治疗<i>幽门螺杆菌</i>

Introduction UNC-51-like kinase 1/2 (ULK1/2) are serine/threonine kinases that play a crucial role in autophagy activation and maintaining cellular homeostasis. Given their broad physiological relevance, ULK1/2 are candidate targets for treating various diseases. In recent years, ULK1/2 inhibitors have made significant progress, and the highly potent ULK1/2 inhibitors have entered clinical trials.

Zhiqi Zhang

Dejuan Sun

Yueying Yang

Samir Y. Abbas

Hua Li

Lixia Chen

A patent review of UNC-51-like kinase 1/2 inhibitors (2019-present)

UNC-51样激酶1/2抑制剂的专利综述（2019年至今）

The main enzymes that hydrolyses nucleotides at the cell surface are nucleoside triphosphate diphosphohydrolases (NTPDases), ecto-nucleotide pyrophosphatases/phosphodiesterases (ENPPs), alkaline phosphatases (APs) and ecto-5'-nucleotidase (e5'NT, CD73) and by regulating the concentration of nucleotides at the cell surface, these enzymes have the potential to affect various conditions such as fibrosis, cancer metastasis, pruritus, inflammation, and autoimmune diseases. Thus, they represent a prospective therapeutic target.

Jamshed Iqbal

Sehrish Bano

Imtiaz Ali Khan

Jean Sévigny

Qing Huang

Ectonucleotidase inhibitors: an updated patent review (2017- 2023)

外核苷酸酶抑制剂：最新专利综述（2017-2023）

CD38 and BCMA are proteins expressed at high levels in multiple myeloma cells, so they are targets for the development of mono- or multispecific antibodies.

Cindy Bandala

Donaciano Flores-Robles

Pavel Sierra-Martínez

Alejandro Millán-Vega

Eunice Ruíz González

Martin Perez-Santos

Trispecific anti-CD3/BCMA/CD38 antibodies for multiple myeloma: a patent evaluation of US20240132615

三特异性抗CD3/BCMA/CD38抗体用于多发性骨髓瘤：US20240132615专利评估

Abbreviation	Expert Opin. Ther. Pat.
Journal Impact	5.46
Quartiles(Global)	PHARMACOLOGY & PHARMACY(Q1)

ISSN	1354-3776, 1744-7674
h-index	88

Publication Information	Publisher: Taylor and Francis Ltd.，Publishing cycle: Monthly，Journal Type: journal，Open Access Journals: No
Basic data	Year of publication: 1991，Proportion of original research papers: 16.33%，Self Citation Rate:1.90%， Gold OA Rate: 4.14%
Average review cycle	网友分享经验：较慢,6-12周
Average recruitment ratio	网友分享经验：一般

Expert Opinion on Therapeutic Patents

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SARS-CoV-2 RNA-dependent RNA polymerase as a therapeutic target for COVID-19

Protease activated receptor 2 (PAR2) modulators: a patent review (2010–2015)

Novel urate transporter 1 (URAT1) inhibitors: a review of recent patent literature (2016–2019)

Expert opinion on therapeutic patents - manuscript ID EOTP-2024-ST-0024 has been submitted online

Urease inhibitors for the treatment of H. pylori

Expert opinion on therapeutic patents - manuscript ID EOTP-2024-ST-0024 has been submitted online

Urease inhibitors for the treatment of H. pylori

A patent review of UNC-51-like kinase 1/2 inhibitors (2019-present)

Ectonucleotidase inhibitors: an updated patent review (2017- 2023)

Trispecific anti-CD3/BCMA/CD38 antibodies for multiple myeloma: a patent evaluation of US20240132615