Pub Date : 2022-05-01Epub Date: 2022-07-21DOI: 10.4155/ppa-2022-0005
Viridiana I Flores-Quiroz, Lino Zumaquero-Ríos, Martin Perez-Santos
American trypanosomiasis is a neglected tropical disease and an endemic problem in 21 Latin American countries, whose treatment relies on only two US FDA-approved drugs: benznidazole and nifurtimox. Patent literature reveals vital information on new trends in therapies for various diseases, including Chagas disease. The authors used the patent databases of the world's major patent offices to generate an overview of patent trends related to the treatment of Chagas disease. A total of 50 patent families were collected and grouped as 'small molecules', 'pharmaceutical compositions of known compounds' and vaccines. From the results and interpretation, it can be concluded that the treatment of Chagas disease receives little attention in the field of patents and that the upward trend is minimal.
{"title":"Pharmaceutical agents for the treatment of Chagas disease: patenting trends in the 2016-2021 period.","authors":"Viridiana I Flores-Quiroz, Lino Zumaquero-Ríos, Martin Perez-Santos","doi":"10.4155/ppa-2022-0005","DOIUrl":"https://doi.org/10.4155/ppa-2022-0005","url":null,"abstract":"<p><p>American trypanosomiasis is a neglected tropical disease and an endemic problem in 21 Latin American countries, whose treatment relies on only two US FDA-approved drugs: benznidazole and nifurtimox. Patent literature reveals vital information on new trends in therapies for various diseases, including Chagas disease. The authors used the patent databases of the world's major patent offices to generate an overview of patent trends related to the treatment of Chagas disease. A total of 50 patent families were collected and grouped as 'small molecules', 'pharmaceutical compositions of known compounds' and vaccines. From the results and interpretation, it can be concluded that the treatment of Chagas disease receives little attention in the field of patents and that the upward trend is minimal.</p>","PeriodicalId":20011,"journal":{"name":"Pharmaceutical patent analyst","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2022-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40610019","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-05-01Epub Date: 2022-07-21DOI: 10.4155/ppa-2022-0001
Chetan D Sabanis, Bharathi R Kannan, Ramesh Joga, Simran, Sandeep Kumar, Neeraj Kumar
Conventional cancer therapies are associated with toxicity toward healthy cells, which need to be addressed by novel therapeutic approaches. US2021/0230592 patent application discloses a carbon nanotube-based approach for tumor targeting, wherein a self-assembling single-wall nanotube complex has been developed and functionalized to deliver a molecule to a cancerous cell. The radiolabeled nanotubes exhibited markedly reduced toxicity as they did not depict any 'over toxicity' up to radioactivity value of 1350 nCi. The single-wall carbon nanotube conjugates were covalently connected to several chelators, therapeutic or diagnostic radionuclides, and showed promising results in the effective cancer management. Besides, this invention with further modifications paves an ideal pathway to researchers in effective diagnosis and treatment of cancer.
{"title":"Potential of novel self-assembled functionalized carbon nanotubes for selective tumor targeting.","authors":"Chetan D Sabanis, Bharathi R Kannan, Ramesh Joga, Simran, Sandeep Kumar, Neeraj Kumar","doi":"10.4155/ppa-2022-0001","DOIUrl":"https://doi.org/10.4155/ppa-2022-0001","url":null,"abstract":"<p><p>Conventional cancer therapies are associated with toxicity toward healthy cells, which need to be addressed by novel therapeutic approaches. US2021/0230592 patent application discloses a carbon nanotube-based approach for tumor targeting, wherein a self-assembling single-wall nanotube complex has been developed and functionalized to deliver a molecule to a cancerous cell. The radiolabeled nanotubes exhibited markedly reduced toxicity as they did not depict any 'over toxicity' up to radioactivity value of 1350 nCi. The single-wall carbon nanotube conjugates were covalently connected to several chelators, therapeutic or diagnostic radionuclides, and showed promising results in the effective cancer management. Besides, this invention with further modifications paves an ideal pathway to researchers in effective diagnosis and treatment of cancer.</p>","PeriodicalId":20011,"journal":{"name":"Pharmaceutical patent analyst","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2022-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40541575","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Shubhangi Gupta, H. Buttar, Ginpreet Kaur, H. Tuli
Baicalein is a medicinally important flavonoid present in Scutellaria baicalensis, which has numerous biological benefits like anti-oxidant, anti-inflammatory, antihepatotoxicity, anticancer properties, etc. Recent studies have revealed that baicalein is an efficient antihepatoma agent and has the strongest antiproliferative effect toward cancerous bladder cell lines, and suppression of cell cycle progression in prostate cancer cells. This natural substance has a high commercial value because it strengthens the heart and cerebral vessels and protects the nervous system and also reduces diabetes and diabetic complications. In addition, baicalein is known to decrease inflammatory markers such as IL-1β, IL-6 and TNF-α. In this review, we have attempted to compile the list of recent therapeutic patents of baicalein used for treating different disorders.
{"title":"Baicalein: promising therapeutic applications with special reference to published patents.","authors":"Shubhangi Gupta, H. Buttar, Ginpreet Kaur, H. Tuli","doi":"10.4155/ppa-2021-0027","DOIUrl":"https://doi.org/10.4155/ppa-2021-0027","url":null,"abstract":"Baicalein is a medicinally important flavonoid present in Scutellaria baicalensis, which has numerous biological benefits like anti-oxidant, anti-inflammatory, antihepatotoxicity, anticancer properties, etc. Recent studies have revealed that baicalein is an efficient antihepatoma agent and has the strongest antiproliferative effect toward cancerous bladder cell lines, and suppression of cell cycle progression in prostate cancer cells. This natural substance has a high commercial value because it strengthens the heart and cerebral vessels and protects the nervous system and also reduces diabetes and diabetic complications. In addition, baicalein is known to decrease inflammatory markers such as IL-1β, IL-6 and TNF-α. In this review, we have attempted to compile the list of recent therapeutic patents of baicalein used for treating different disorders.","PeriodicalId":20011,"journal":{"name":"Pharmaceutical patent analyst","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2022-03-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42953257","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-03-01Epub Date: 2022-06-27DOI: 10.4155/ppa-2022-0004
Samson A Adeyemi, Yahya E Choonara
Water-soluble polysaccharides have unique properties and have found wide application in the design of advanced drug-delivery systems and the biofabrication of tissue engineered scaffolds in regenerative medicine. This patent review provides a concise incursion into the mechanisms that define the key properties of water-soluble polysaccharides that have found embodiment within active patents recently granted (2020-2021). In addition, the relationship between their solubility and structural features such as molecular weight, ionic profile, degree of branching/crosslinking, side-chain flexibility and the presence/modification of functional groups that have been discusses. An assimilation of patents in which water-soluble polysaccharides are central to the design of therapeutic interventions applied to specialized treatments in oncology, infectious diseases and neuronal disorders is provided.
{"title":"Recent patents on water-soluble polysaccharides for advanced drug delivery, tissue engineering and regenerative medicine.","authors":"Samson A Adeyemi, Yahya E Choonara","doi":"10.4155/ppa-2022-0004","DOIUrl":"https://doi.org/10.4155/ppa-2022-0004","url":null,"abstract":"<p><p>Water-soluble polysaccharides have unique properties and have found wide application in the design of advanced drug-delivery systems and the biofabrication of tissue engineered scaffolds in regenerative medicine. This patent review provides a concise incursion into the mechanisms that define the key properties of water-soluble polysaccharides that have found embodiment within active patents recently granted (2020-2021). In addition, the relationship between their solubility and structural features such as molecular weight, ionic profile, degree of branching/crosslinking, side-chain flexibility and the presence/modification of functional groups that have been discusses. An assimilation of patents in which water-soluble polysaccharides are central to the design of therapeutic interventions applied to specialized treatments in oncology, infectious diseases and neuronal disorders is provided.</p>","PeriodicalId":20011,"journal":{"name":"Pharmaceutical patent analyst","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2022-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40403035","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Slack channels are sodium-activated potassium channels that are encoded by the KCNT1 gene. Several KCNT1 gain of function mutations have been linked to malignant migrating partial seizures of infancy. Quinidine is an anti-arrhythmic drug that functions as a moderately potent inhibitor of Slack channels; however, quinidine use is limited by its poor selectivity, safety and pharmacokinetic profile. Slack channels represent an interesting target for developing novel therapeutics for the treatment of malignant migrating partial seizures of infancy and other childhood epilepsies; thus, ongoing efforts are directed toward the discovery of small-molecules that inhibit Slack currents. This review summarizes patent applications published in 2020-2021 that describe the discovery of novel small-molecule Slack inhibitors.
{"title":"Small-molecule inhibitors of Slack potassium channels as potential therapeutics for childhood epilepsies.","authors":"Alshaima'a M Qunies, Kyle A Emmitte","doi":"10.4155/ppa-2022-0002","DOIUrl":"https://doi.org/10.4155/ppa-2022-0002","url":null,"abstract":"Slack channels are sodium-activated potassium channels that are encoded by the KCNT1 gene. Several KCNT1 gain of function mutations have been linked to malignant migrating partial seizures of infancy. Quinidine is an anti-arrhythmic drug that functions as a moderately potent inhibitor of Slack channels; however, quinidine use is limited by its poor selectivity, safety and pharmacokinetic profile. Slack channels represent an interesting target for developing novel therapeutics for the treatment of malignant migrating partial seizures of infancy and other childhood epilepsies; thus, ongoing efforts are directed toward the discovery of small-molecules that inhibit Slack currents. This review summarizes patent applications published in 2020-2021 that describe the discovery of novel small-molecule Slack inhibitors.","PeriodicalId":20011,"journal":{"name":"Pharmaceutical patent analyst","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2022-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9260495/pdf/ppa-11-45.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10810199","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-01-01Epub Date: 2022-02-03DOI: 10.4155/ppa-2021-0025
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。
{"title":"Patent highlights August-September 2021.","authors":"Hermann Am Mucke","doi":"10.4155/ppa-2021-0025","DOIUrl":"https://doi.org/10.4155/ppa-2021-0025","url":null,"abstract":"<p><p>A snapshot of noteworthy recent developments in the patent literature of relevance to pharmaceutical and medical research and development.</p>","PeriodicalId":20011,"journal":{"name":"Pharmaceutical patent analyst","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39758418","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-01-01Epub Date: 2022-02-16DOI: 10.4155/ppa-2021-0021
Maricruz Anaya-Ruiz, Martin Perez-Santos
Cancer drug repurposing is an attractive approach that leads to savings in time and investment. Adapalene, the first medical application of which was for the treatment of acne, has been described as a repurposing drug for the treatment of various types of cancer. Patent application CN111329851 describes the use of adapalene for the treatment of melanoma, by assays carried out on melanoma cell lines. Adapalene demonstrated antiproliferative activity in melanoma cell lines via S-phase arrest-dependent apoptosis mediated by DNA damage through an increase in the expression of p-ATM and p-chk2 and a decrease in the expression of p-BRCA1 and Rad51. Even though no evidence on efficacy and efficiency is shown in preclinical and clinical studies, CN111329851 patent shows that adapalene may be a repurposing drug for the treatment of melanoma.
{"title":"Drug repurposing of adapalene for melanoma treatment.","authors":"Maricruz Anaya-Ruiz, Martin Perez-Santos","doi":"10.4155/ppa-2021-0021","DOIUrl":"https://doi.org/10.4155/ppa-2021-0021","url":null,"abstract":"<p><p>Cancer drug repurposing is an attractive approach that leads to savings in time and investment. Adapalene, the first medical application of which was for the treatment of acne, has been described as a repurposing drug for the treatment of various types of cancer. Patent application CN111329851 describes the use of adapalene for the treatment of melanoma, by assays carried out on melanoma cell lines. Adapalene demonstrated antiproliferative activity in melanoma cell lines via S-phase arrest-dependent apoptosis mediated by DNA damage through an increase in the expression of p-ATM and p-chk2 and a decrease in the expression of p-BRCA1 and Rad51. Even though no evidence on efficacy and efficiency is shown in preclinical and clinical studies, CN111329851 patent shows that adapalene may be a repurposing drug for the treatment of melanoma.</p>","PeriodicalId":20011,"journal":{"name":"Pharmaceutical patent analyst","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39633611","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-01-01Epub Date: 2022-02-17DOI: 10.4155/ppa-2021-0024
Ritu Rathi, Inderbir Singh
Cocrystallization has gained significant prominence in pharmaceutical product development because of the enhancement of physical, chemical and pharmacological properties of active pharmaceutical ingredients, such as stability, solubility, dissolution rate, taste, hygroscopicity, mechanical property, bioavailability, permeability and therapeutic activity. Traditionally, co-crystals can be prepared by a grinding, solvent evaporation and slurry method. However, sophisticated methods such as spa drying, hot-melt extrusion, supercritical fluid and laser irradiation are also reported to be used for producing co-crystals. The selected patent describes the development of multicomponent crystals of dasatinib, with an aim to enhance the aqueous solubility of a selected drug. However issues surrounding the toxicity, stability, large scale manufacture, in vivo performance in human beings and regulations require adequate addressal prior to exploring the commercial viability of pharmaceutical co-crystals.
{"title":"Multicomponent crystal compromising dasatinib and selected co-crystals formers: a patent evaluation of EP2861589B1.","authors":"Ritu Rathi, Inderbir Singh","doi":"10.4155/ppa-2021-0024","DOIUrl":"https://doi.org/10.4155/ppa-2021-0024","url":null,"abstract":"<p><p>Cocrystallization has gained significant prominence in pharmaceutical product development because of the enhancement of physical, chemical and pharmacological properties of active pharmaceutical ingredients, such as stability, solubility, dissolution rate, taste, hygroscopicity, mechanical property, bioavailability, permeability and therapeutic activity. Traditionally, co-crystals can be prepared by a grinding, solvent evaporation and slurry method. However, sophisticated methods such as spa drying, hot-melt extrusion, supercritical fluid and laser irradiation are also reported to be used for producing co-crystals. The selected patent describes the development of multicomponent crystals of dasatinib, with an aim to enhance the aqueous solubility of a selected drug. However issues surrounding the toxicity, stability, large scale manufacture, <i>in vivo</i> performance in human beings and regulations require adequate addressal prior to exploring the commercial viability of pharmaceutical co-crystals.</p>","PeriodicalId":20011,"journal":{"name":"Pharmaceutical patent analyst","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39790790","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Inhibition of the PD-1/PD-L1 pathway is a target for the development of new therapies. US10710986 patent describes a small molecule that targets PDL-1/PD-1 interactions and triggers antitumor activity against colorectal cancer. However, it does not describe biological assays that allow us to suppose that this small molecule may be active in other types of cancer. So far, there are no reports of clinical trials to evaluate the safety, toxicity and efficacy, but it will be of great interest to analyze in the future if this compound surpasses the action of therapy in cancer.
{"title":"Small-molecule inhibitor PD-1/PD-L1 interaction for colorectal cancer treatment.","authors":"Maricruz Anaya-Ruiz, Martin Perez-Santos","doi":"10.4155/ppa-2021-0016","DOIUrl":"10.4155/ppa-2021-0016","url":null,"abstract":"<p><p>Inhibition of the PD-1/PD-L1 pathway is a target for the development of new therapies. US10710986 patent describes a small molecule that targets PDL-1/PD-1 interactions and triggers antitumor activity against colorectal cancer. However, it does not describe biological assays that allow us to suppose that this small molecule may be active in other types of cancer. So far, there are no reports of clinical trials to evaluate the safety, toxicity and efficacy, but it will be of great interest to analyze in the future if this compound surpasses the action of therapy in cancer.</p>","PeriodicalId":20011,"journal":{"name":"Pharmaceutical patent analyst","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2021-12-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39700288","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-11-01Epub Date: 2021-11-10DOI: 10.4155/ppa-2021-0022
Hermann Am Mucke
A snapshot of noteworthy recent developments in the patent literature of relevance to pharmaceutical and medical research and development.
与制药和医疗研发相关的专利文献中值得关注的最新进展快照。
{"title":"Patent highlights June-July 2021.","authors":"Hermann Am Mucke","doi":"10.4155/ppa-2021-0022","DOIUrl":"10.4155/ppa-2021-0022","url":null,"abstract":"<p><p>A snapshot of noteworthy recent developments in the patent literature of relevance to pharmaceutical and medical research and development.</p>","PeriodicalId":20011,"journal":{"name":"Pharmaceutical patent analyst","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2021-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39692971","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}