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Contact lens disinfectants against Acanthamoeba keratitis: an overview of recent patents and future needs. 抗棘阿米巴角膜炎的隐形眼镜消毒剂:近期专利和未来需求综述。
IF 1.3 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-05-01 Epub Date: 2023-08-31 DOI: 10.4155/ppa-2023-0012
Ruqaiyyah Siddiqui, Naveed A Khan
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引用次数: 0
Patent highlights August-September 2022. 专利亮点2022年8月至9月。
IF 1.3 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-03-01 DOI: 10.4155/ppa-2022-0049
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
Riluzole and its prodrugs for the treatment of Alzheimer's disease. 用于治疗阿尔茨海默病的利鲁唑及其原药。
IF 1.3 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-03-01 Epub Date: 2023-05-04 DOI: 10.4155/ppa-2023-0001
Rami A Al-Horani

Current medications for Alzheimer's disease help manage symptoms and behavioral problems. Nevertheless, they do not slow the progression of cognitive decline or dementia. A potential approach for treating Alzheimer's disease is to target neurons that are sensitive to disease pathobiology such as glutamatergic neurons. Several patents disclosed methods for treating Alzheimer's disease by administering riluzole or its prodrugs. Clinical trials revealed that 6 months treatment using riluzole or troriluzole is associated with a slower decline in the tomographic measures of the positron emissions of cerebral glucose metabolism in Alzheimer's patients. The proposed strategy claims to prevent and/or slow the cognitive decline of Alzheimer's patients and to enhance global functioning. These claims may also pave the way for other glutamate modulators to be used for Alzheimer's disease.

目前治疗阿尔茨海默病的药物有助于控制症状和行为问题。然而,这些药物并不能减缓认知能力下降或痴呆症的进展。治疗阿尔茨海默病的一种潜在方法是靶向对疾病病理生物学敏感的神经元,如谷氨酸能神经元。有几项专利披露了通过服用利鲁唑或其原药治疗阿尔茨海默病的方法。临床试验显示,使用利鲁唑或曲利鲁唑治疗 6 个月后,阿尔茨海默病患者脑葡萄糖代谢正电子发射断层扫描测量值的下降速度会减慢。拟议的策略声称可以预防和/或减缓阿尔茨海默氏症患者认知能力的衰退,并增强整体功能。这些主张还可能为其他谷氨酸调节剂用于治疗阿尔茨海默氏症铺平道路。
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引用次数: 0
Patents, pharmaceutical industry and healthcare. 专利,制药工业和医疗保健。
IF 1.3 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-03-01 DOI: 10.4155/ppa-2023-0009
Ruqaiyyah Siddiqui, Naveed A Khan
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引用次数: 0
Patent landscape highlighting double-edged scaffold of a WNT5A-agonizing peptide, Foxy5. 专利景观突出wnt5a痛苦肽Foxy5的双刃支架。
IF 1.3 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-03-01 DOI: 10.4155/ppa-2022-0037
Vikas Yadav, Rubina Islam, Hardeep Singh Tuli

Aberrant expression of the WNT signaling pathway has been associated with cancer progression and recurrence. Research over the decades has led to development of WNT-targetable small molecules, but has faced challenges in translating to clinics. Unlike WNT/β-catenin inhibitors, WNT5A-mimicking peptide, Foxy5 has shown encouraging efficacy in impairing metastasis of cancers with low or absent WNT5A expression. Recent patent application US20210008149 advocates the implication of Foxy5 for treatment and prevention of cancer relapse. The inventors have demonstrated the anti-stemness activity of Foxy5 in mice xenograft model via suppressing the expression of colonic cancer stem cell markers. Foxy5 also exhibits non-toxic nature when administered alone or in synergy with standard chemotherapy thus strengthening its candidature in the field of cancer therapeutics.

WNT信号通路的异常表达与癌症的进展和复发有关。几十年来的研究已经导致了wnt靶向小分子的发展,但在转化为临床方面面临着挑战。与WNT/β-catenin抑制剂(模仿WNT5A的肽)不同,Foxy5在抑制WNT5A低表达或缺失的癌症转移方面显示出令人鼓舞的疗效。最近的专利申请US20210008149倡导fox5在治疗和预防癌症复发方面的意义。发明人通过抑制结肠癌干细胞标记物的表达,在小鼠异种移植模型中证明了Foxy5的抗干细胞活性。Foxy5在单独使用或与标准化疗协同使用时也表现出无毒性,从而加强了其在癌症治疗领域的候选性。
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引用次数: 0
Review of EPO Board of Appeal antibody decisions in 2022. 2022年对欧洲专利局上诉委员会抗体决定的复审。
IF 1.3 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-03-01 DOI: 10.4155/ppa-2023-0014
Daniel Hilton, Vicki Allen, Graham Lewis
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引用次数: 0
4-(Imidazo[1,2-a]pyridin-3-yl): pyrimidine derivatives as anticancer agents. 4-(咪唑并[1,2-a]吡啶-3-基):作为抗癌剂的嘧啶衍生物。
IF 1.3 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-01-01 Epub Date: 2022-11-10 DOI: 10.4155/ppa-2022-0033
Rami A Al-Horani

A series of 4-(imidazo[1,2-a]pyridin-3-yl)-pyrimidine derivatives are claimed as inhibitors of c-KIT and as potential treatments for cancer. Their chemical preparation and biological evaluation against imatinib-resistant tumor cells have been described. Several claimed molecules have excellent IC50 values in the nanomolar range. Several molecules were also selective against a wide panel of kinases. Few specific inhibitors have been found to have promising oral bioavailability and acceptable to excellent values regarding the inhibition of hERG channel. This class represents a new platform for developing new anticancer treatment against a wide range of c-KIT mutations and secondary mutations that may arise in gastrointestinal stromal tumor patients.

一系列 4-(咪唑并[1,2-a]吡啶-3-基)嘧啶衍生物被认为是 c-KIT 的抑制剂和潜在的癌症治疗药物。这些衍生物的化学制备方法和针对伊马替尼耐药肿瘤细胞的生物学评价已经得到描述。一些声称的分子具有极佳的 IC50 值,在纳摩尔范围内。一些分子还对多种激酶具有选择性。研究发现,少数特异性抑制剂具有良好的口服生物利用度,对 hERG 通道的抑制作用也达到了可接受甚至优异的水平。这类药物代表了一种新的平台,可用于开发针对胃肠道间质瘤患者可能出现的各种 c-KIT 突变和继发性突变的新型抗癌疗法。
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引用次数: 0
Patent developments via Schiff bases in medicinal chemistry. 药物化学中希夫碱基的专利开发。
IF 1.3 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-01-01 DOI: 10.4155/ppa-2022-0045
Maham Haider, Khalid Mohammed Khan
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引用次数: 0
Photoresponsive liposomes: an alternative of ELISA for the detection of low quantities of target substances. 光反应性脂质体:用于检测少量目标物质的ELISA替代方法。
IF 1.3 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-01-01 DOI: 10.4155/ppa-2022-0046
Ramesh Joga, Hitesh Kumar Behera, Chetan Dushant Sabanis, Simran, Sandeep Kumar, Neeraj Kumar

Photoresponsive liposome development is needed to serve as a facile alternative to ELISA which is ineffective for detecting small levels of biomarkers due to low detection sensitivity. The US20210396744 patent application outlines novel photoresponsive liposomes for the detection of target substances with the aid of light. Although versatile, there may be possible stability issues that can be avoided with the appropriate selection of liposome components. Furthermore, the clinical success of this technology depends on many parameters like plasma stability, efficient loading of photosensitive components in the membrane and immobilization of molecular recognition elements to the membrane. Despite several challenges, they possess enormous potential to become a non-invasive tool for the detection of target substances.

光反应性脂质体的开发需要作为一种简便的替代ELISA,由于检测灵敏度低,对于检测小水平的生物标志物无效。US20210396744专利申请概述了用光检测目标物质的新型光反应脂质体。虽然用途广泛,但可能存在稳定性问题,可以通过适当选择脂质体成分来避免。此外,该技术的临床成功取决于许多参数,如等离子体稳定性,膜中光敏成分的有效负载以及分子识别元件在膜上的固定。尽管存在一些挑战,但它们具有成为检测目标物质的非侵入性工具的巨大潜力。
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引用次数: 1
Patent Highlights June-July 2022. 专利亮点2022年6月至7月。
IF 1.3 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-01-01 DOI: 10.4155/ppa-2022-0043
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
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