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Steroid sulfatase inhibitors and sulfated C19 steroids for proteotoxicity-related diseases: a patent spotlight. 类固醇磺化酶抑制剂和硫酸C19类固醇治疗蛋白质毒性相关疾病:专利焦点
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-01 Epub Date: 2023-11-20 DOI: 10.4155/ppa-2023-0010
Rami A Al-Horani

Aging and proteotoxicity go hand in hand. Inhibiting proteotoxicity has been proposed to extend lifespan. This invention describes a new strategy to limit proteotoxicity and to extend the lifespan. Loss of function of sul-2, the Caenorhabditis elegans steroid sulfatase, elevates the pool of sulfated steroid hormones, increases longevity and ameliorates protein aggregation diseases. The present invention provides a group of molecules for use in the prevention of aging-associated proteotoxicity caused by protein aggregation diseases and/or to increase the lifespan of a eukaryotic organism. These molecules are either steroid sulfatase inhibitors or sulfated C19 steroids, both of which reproduce the phenotype of sul-2 mutants. One particular representative example is STX-64. Potential applications of the claims have been demonstrated in animal models of Parkinson's disease, Huntington's disease and Alzheimer's disease.

衰老和蛋白质毒性是密切相关的。抑制蛋白质毒性被认为可以延长寿命。本发明描述了一种限制蛋白质毒性和延长寿命的新策略。秀丽隐杆线虫类固醇硫酸酯酶sul2功能的丧失,增加了硫酸类固醇激素的数量,延长了寿命,改善了蛋白质聚集性疾病。本发明提供了一组分子,用于预防由蛋白质聚集疾病引起的与衰老相关的蛋白质毒性和/或增加真核生物的寿命。这些分子要么是类固醇硫酸酯酶抑制剂,要么是硫酸C19类固醇,两者都能产生硫-2突变体的表型。一个典型的例子是STX-64。这些说法的潜在应用已经在帕金森病、亨廷顿病和阿尔茨海默病的动物模型中得到证实。
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引用次数: 0
Patent highlights February-March 2023. 专利亮点2023年2月至3月。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-01 Epub Date: 2023-11-20 DOI: 10.4155/ppa-2023-0023
Hermann Am Mucke

A snapshot of noteworthy recent developments in the patent literature of relevance to pharmaceutical and medical research and development.

与制药和医学研究与开发相关的专利文献中值得注意的最新发展概况。
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引用次数: 0
Recent patents in the treatment and prevention of leishmaniasis. 治疗和预防利什曼病的最新专利。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-01 Epub Date: 2023-12-08 DOI: 10.4155/ppa-2023-0022
Sukhbir K Shahid

Leishmaniasis, a neglected tropical disease, is caused by protozoal parasites of the genus Leishmania. Clinical manifestations vary from asymptomatic to lethal grade depending on the type of the disease. The currently available antileishmanial drugs suffer from considerable limitations. There is a dire need for better and safer drugs and/or vaccines to eradicate this disease. There are enormous developments ongoing in this field. Newer combinations of existing drugs and newer drugs targeting these intracellular parasites as well as their vectors are being tried to control the disease. Attempts to develop vaccines to enhance the immunity of the patient have shown some promise. This article is a peep into the recent patent developments in this field.

利什曼病是一种被忽视的热带疾病,由利什曼属原生动物寄生虫引起。临床表现因疾病类型而异,从无症状到致命程度不等。目前可用的抗利什曼病药物存在相当大的局限性。我们迫切需要更好、更安全的药物和/或疫苗来根除这种疾病。这一领域正在取得巨大进展。人们正在尝试将现有药物和针对这些细胞内寄生虫及其载体的新药组合起来,以控制这种疾病。开发疫苗以增强患者免疫力的尝试也已初见成效。本文将对这一领域的最新专利进展进行介绍。
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引用次数: 0
Drug repurposing of rimantadine for treatment of cancer. 金刚乙胺治疗癌症的药物再利用。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-01 Epub Date: 2023-11-20 DOI: 10.4155/ppa-2023-0019
Nemesio Villa-Ruano, Vianey Marin-Cevada, Gabriela Sanchez-Esgua, Luis Villafaña-Diaz, Martin Perez-Santos

Repurposing of approved drugs allows strong savings in time and investment. Rimantadine is an FDA-approved drug for prevention and treatment of influenza A infection. Patent US2021330605 describes the use of rimantadine, an adamantane derivative, for the treatment of melanoma, breast cancer and head and neck squamous cell carcinoma. Rimantadine inhibited proliferation of cell lines of melanoma, breast cancer, and head and neck squamous cell carcinoma, increased the survival of mice injected with cancer cell lines and restores the expression of MHC class I. Rimantadine has the potential to be used successfully in the treatment of head and neck squamous cell carcinoma.

重新利用已批准的药物可以大大节省时间和投资。金刚乙胺是fda批准的预防和治疗甲型流感感染的药物。专利US2021330605描述了金刚烷衍生物金刚乙胺用于治疗黑色素瘤、乳腺癌和头颈部鳞状细胞癌的用途。金刚乙胺抑制黑色素瘤、乳腺癌和头颈部鳞状细胞癌细胞系的增殖,增加注射癌细胞的小鼠的存活率,恢复MHC i类的表达。金刚乙胺有可能成功用于头颈部鳞状细胞癌的治疗。
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引用次数: 0
Patent highlights December 2022-January 2023. 专利亮点2022年12月至2023年1月。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-07-01 Epub Date: 2023-10-06 DOI: 10.4155/ppa-2023-0016
Hermann Am Mucke
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引用次数: 0
Recent patent-based review on the role of three-dimensional printing technology in pharmaceutical and biomedical applications. 关于三维打印技术在制药和生物医学应用中的作用的最新专利综述。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-07-01 Epub Date: 2023-10-26 DOI: 10.4155/ppa-2023-0018
Palak Rani, Vikas Yadav, Parijat Pandey, Kiran Yadav

Three-dimensional printing (3DP) is emerging as an innovative manufacturing technology for biomedical and pharmaceutical applications, since the US FDA approval of Spritam as a 3D-printed drug. In the present review, we have highlighted the potential benefits of 3DP technology in healthcare, such as the ability to create patient-specific medical devices and implants, as well as the possibility of on-demand production of drugs and personalized dosage forms. We have further discussed future research to optimize 3DP processes and materials for pharmaceutical and biomedical applications. Cohesively, we have put forward the current state of active patents and applications related to 3DP technology in the healthcare and pharmaceutical industries including hearing aids, prostheses, medical devices and drug-delivery systems.

自从美国食品药品监督管理局批准Spritam作为3D打印药物以来,三维打印(3DP)正成为生物医学和制药应用的一种创新制造技术。在本综述中,我们强调了3DP技术在医疗保健中的潜在优势,例如创建患者专用医疗设备和植入物的能力,以及按需生产药物和个性化剂型的可能性。我们进一步讨论了未来优化3DP工艺和材料用于制药和生物医学应用的研究。我们共同提出了3DP技术在医疗保健和制药行业的活跃专利和应用现状,包括助听器、假肢、医疗器械和药物输送系统。
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引用次数: 0
Therapeutic charisma of imidazo [2,1-b] [1,3,4]-thiadiazole analogues: a patent review. 咪唑 [2,1-b] [1,3,4]- 噻二唑类似物的治疗魅力:专利回顾。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-07-01 Epub Date: 2023-09-06 DOI: 10.4155/ppa-2023-0006
Anuradha Mehra, Rekha Sangwan, Aryan Mehra, Shivani Sharma, Pankaj Wadhwa, Amit Mittal

Imidazothiadiazole was discovered around the 1950s era, containing an imidazole ring fused to a thiadiazole ring. Imidazothiadiazole exhibit versatile pharmacological properties including anticonvulsant, cardiotonic, anti-inflammatory, diuretic, antifungal, antibacterial and anticancer. Despite of the being discovered in 1950s, the imidazothiadiazole derivatives are unable to being processed to clinical trials because of lack of bioavailability, efficacy and cytotoxicity. The recent patent literature focused on structural modification of imidazothiadiazole core to overcome these problems. This review limelight a disease-centric perspective on patented imidazothiadiazole from 2015-2023 and to understand their mechanism of action in related diseases. The relevant granted patent applications were located using patent databases, Google Patents, USPTO, EPO, WIPO, Espacenet and Lens.

咪唑噻二唑是在 20 世纪 50 年代左右发现的,含有一个咪唑环和一个噻二唑环。咪唑噻二唑具有抗惊厥、强心、消炎、利尿、抗真菌、抗菌和抗癌等多种药理特性。尽管咪唑噻二唑衍生物早在 20 世纪 50 年代就已被发现,但由于缺乏生物利用度、药效和细胞毒性,一直未能进入临床试验阶段。最近的专利文献主要集中在对咪唑噻二唑核心进行结构改造,以克服这些问题。本综述从疾病为中心的角度对2015-2023年的咪唑噻二唑专利进行分析,并了解其在相关疾病中的作用机制。相关已授权专利申请是通过专利数据库、谷歌专利、美国专利商标局、欧洲专利局、世界知识产权组织、Espacenet 和 Lens 查找的。
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引用次数: 0
Patent landscape of platelet growth factor receptor and c-KIT targets. 血小板生长因子受体和c-KIT靶点的专利前景。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-07-01 Epub Date: 2023-09-27 DOI: 10.4155/ppa-2023-0005
Hai-Long Zhang, Qian Kong

Type III receptor tyrosine kinase, e.g., PDGFR, are associated with various autoimmune diseases. To show the status of PDGFR and c-KIT targets, we performed the US patent analysis. The present study showed that the R&D of c-KIT target was much earlier than the R&D of PDGFR targets. Currently, the PDGFR-based target demonstrates more applications in the development of biological therapy. Our findings indicated that some inhibitors of c-KIT target contained sulfur elements or 1,3-diazine rings. The c-KIT target has more competitive edges for chemical drug discovery than the PDGFR target. c-KIT and PDGFR targets are currently preferable for drug discovery in autoimmune diseases. This study was the first to show R&D differentiation between PDGFR and c-KIT targets in drug development.

III型受体酪氨酸激酶,例如PDGFR,与各种自身免疫性疾病有关。为了显示PDGFR和c-KIT靶点的状态,我们进行了美国专利分析。本研究表明,c-KIT靶点的研发远早于PDGFR靶点的开发。目前,基于PDGFR的靶点在生物治疗的发展中有更多的应用。我们的研究结果表明,一些c-KIT靶向抑制剂含有硫元素或1,3-二嗪环。c-KIT靶点在化学药物发现方面比PDGFR靶点更有竞争力。c-KIT和PDGFR靶点目前优选用于自身免疫性疾病中的药物发现。这项研究首次表明PDGFR和c-KIT靶点在药物开发中的研发差异。
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引用次数: 0
Drug repurposing of mito-atovaquone for cancer treatment. Mito-Atovaquone用于癌症治疗的药物再利用。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-07-01 Epub Date: 2023-10-06 DOI: 10.4155/ppa-2023-0015
Nemesio Villa-Ruano, Maricruz Anaya-Ruiz, Luis Villafaña-Diaz, Diana Barron-Villaverde, Martin Perez-Santos

Repurposing of approved drugs in a new strategy to combat cancer that leads to savings in time and investment. Atovaquone is a US FDA-approved drug for treatment of Pneumocystis carinii pneumonia and malaria. Patent US2023017373 describe the use of mito-atovaquone for the treatment of several types of cancer. Mito-atovaquone demonstrated antiproliferative activity in cell lines of pancreatic cancer, lung cancer and brain cancer and inhibited tumor growth in syngeneic mouse models and in animals genetically prone to breast cancer. Mito-atovaquone has the potential to be used successfully in the treatment of various types of tumors.

在抗击癌症的新战略中重新利用已批准的药物,从而节省时间和投资。阿托伐醌是美国食品药品监督管理局批准的治疗卡氏肺孢子虫肺炎和疟疾的药物。专利US2023017373描述了mito-atovaquone用于治疗几种类型的癌症的用途。Mito-Atovaquone在胰腺癌症、癌症和脑癌症的细胞系中表现出抗增殖活性,并在同基因小鼠模型和遗传上易患癌症的动物中抑制肿瘤生长。Mito-Atovaquone有潜力成功用于治疗各种类型的肿瘤。
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引用次数: 0
Patent profile for the approved and in clinical trials Mpox vaccines. 已批准和正在进行临床试验的猴痘疫苗的专利简介。
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-05-01 Epub Date: 2023-09-06 DOI: 10.4155/ppa-2023-0017
Irene von der Weid, Cristina d'Urso de Souza Mendes, Paula C Fonseca, Sandro G Viveiros Rosa

Mpox disease was reported in 110 countries since May 2022, with 88,026 cases and 148 deaths by 21 June 2023. Although some drugs were already approved for Mpox treatment, the available smallpox vaccines can provide 85% cross-prevention, but there are no scientific publications describing the patent portfolio for Mpox vaccines. This paper aims to contribute to the identification of the status of the smallpox vaccine patents now applied for Mpox. We retrieved ten vaccines, but only a few had a patent portfolio and one under patent litigation processes in three continents. Also, no specific Mpox vaccine was retrieved and, in this sense, technological monitoring studies should be performed to provide a future vision regarding Mpox prophylaxis.

自2022年5月以来,110个国家报告了猴痘病,截至2023年6月21日,已有88026例病例和148例死亡。尽管一些药物已经被批准用于猴痘治疗,但现有的天花疫苗可以提供85%的交叉预防,但没有科学出版物描述猴痘疫苗的专利组合。本文旨在为查明猴痘目前申请的天花疫苗专利状况做出贡献。我们检索到了十种疫苗,但只有少数疫苗拥有专利组合,其中一种正在三大洲的专利诉讼程序中。此外,没有检索到特定的猴痘疫苗,从这个意义上说,应该进行技术监测研究,以提供猴痘预防的未来愿景。
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引用次数: 0
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Pharmaceutical patent analyst
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