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Expert Opinion on Therapeutic Patents

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https://www.readbyqxmd.com/read/27897041/novel-antifungal-agents-a-patent-review-2013-present
#1
María Victoria Castelli, Marcos Gabriel Derita, Silvia Noelí López
Superficial infections involving the skin and mucosa are the most common fungal disease in humans. Fungi can also produce invasive infections (IFI), which are increasing in incidence among the growing population of immunocompromised patients, and are characterized by a high mortality rate. Amphotericin B, new triazoles and echinocandins have improved treatment options in IFI. However, the frequency of less common and more resistant fungi, the limited activity of available antifungal drugs and their undesirable side effects reflect the urgent need for the development of new therapeutic strategies...
November 29, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27841036/parp-inhibitors-as-antitumor-agents-a-patent-update-2013-2015
#2
Zigao Yuan, Jiwei Chen, Wenlu Li, Dan Li, Changjun Chen, Chunmei Gao, Yuyang Jiang
PARP inhibitors have been extensively explored as antitumor agents and have shown potent efficacy both in vitro and in vivo. They can be used in monotherapy under the synthetic lethality concept or in combination with radiotherapy or chemotherapy, inducing a synergistic effect. Areas covered: This review covers relevant efforts in the development of PARP inhibitors with a particular focus on recently patented PARP inhibitors, combination therapy involving PARP inhibitors, tumor responsiveness to PARP inhibitors as detailed in reports made from 2013 - 2015, and PARP drugs in clinical trials and other novel inhibitors that emerged in 2013 - 2015...
November 21, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27828716/glycogen-synthase-kinase-3-gsk-3-inhibitors-a-patent-update-2014-2015
#3
Valle Palomo, Ana Martinez
Glycogen synthase kinase (GSK-3) is a serine/threonine kinase that phosphorylates more than one hundred different sequences within proteins in a variety of different pathways. It is a key component of a remarkably large number of cellular processes and diseases. Imbalance of GSK-3 activity is involved in various prevalent pathological diseases, such as diabetes, neurodegenerative diseases and cancer. Understanding its role in different disorders has been central in the last several decades and there has been a significantly large development of GSK-3 inhibitors, some of which, show promising results for the treatment of these devastating diseases...
November 21, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27855563/novel-diaryltriazines-with-a-picolinonitrile-moiety-as-potent-hiv-1-rt-inhibitors-a-patent-evaluation-of-wo2016059647-a2
#4
Boshi Huang, Zhongxia Zhou, Dongwei Kang, Wanzhuo Li, Zihui Chen, Peng Zhan, Xinyong Liu
Diaryltriazine derivatives, which are structurally related to diarylpyrimidines, are a representative class of HIV-1 reverse transcriptase inhibitors with remarkable antiviral activities against wild-type and several mutant strains of HIV-1. A series of novel diaryltriazines with a picolinonitrile moiety was reported as potent HIV-1 RT inhibitors in the patent WO2016059647(A2). Two representative compounds 5e (hydrochloride) and 6e (hydrochloride) exhibited outstanding activities against various HIV-1 strains in cell-based assays, which were superior to those of AZT...
November 18, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27855527/recent-advances-in-therapeutics-and-drug-delivery-for-the-treatment-of-inner-ear-diseases-a-patent-review-2011-2015
#5
Kim Nguyen, Judith S Kempfle, David H Jung, Charles E McKenna
Inner ear disorders such as hearing loss, tinnitus, and Ménière's disease significantly impact the quality of life of affected individuals. Treatment of such disorders is an ongoing challenge. Current clinical approaches relieve symptoms but do not fully restore hearing, and the search for more effective therapeutic methods represents an area of urgent current interest. Areas covered: Thirty four patents and patent applications published from 2011 to 2015 were selected from the database of the U.S. Patent and Trademark Office (USPTO) and World Intellectual Property Organization (WIPO), covering new approaches for the treatment of inner ear disorders described in the patent literature: 1) identification of new therapeutic agents, 2) development of sustained release formulations, and 3) medical devices that facilitate delivery of such agents to the inner ear...
November 18, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27852111/ror%C3%AE-t-inhibitors-as-potential-back-ups-for-the-phase-ii-candidate-vtp-43742-from-vitae-pharmaceuticals-patent-evaluation-of-wo2016061160-and-us20160122345
#6
Christian Gege
Retinoic acid receptor-related orphan nuclear receptor gamma t (RORγt or RORc2) is a key transcription factor for the differentiation of naïve proinflammatory CD4(+) T cells and the production of T helper-17 (TH17) cells. Inhibiting RORγt activity is thought to be beneficial in targeting a variety of inflammatory and autoimmune disorders. Recently Vitae Pharmaceuticals (to be acquired by Allergan) reported positive top-line results from a Phase 2a clinical trial of RORγt inhibitor VTP-43742 in psoriatic patients...
November 17, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27744724/mcl-1-inhibitors-a-patent-review
#7
Lijia Chen, Steven Fletcher
The myeloid cell leukemia-1 (MCL-1) protein is one of the key anti-apoptotic members of the B-cell lymphoma-2 (BCL-2) protein family. Over-expression of MCL-1 has been closely related to tumor progression as well as to resistance, not only to traditional chemotherapies but also to targeted therapeutics including BCL-2 inhibitors such as ABT-263. Therefore, there has been extensive research and development in the last decade in both academic and industrial settings to address this unmet medical need. Areas covered: This review covers the research and patent literature of the past 10 years in the field of discovery and development of small-molecule inhibitors of the MCL-1 anti-apoptotic protein...
November 17, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27841042/treatments-and-compositions-targeting-%C3%AE-synuclein-a-patent-review-2010-2016
#8
Henryk Jęśko, Anna M Lenkiewicz, Agata Adamczyk
Abnormal deposition of α-synuclein (ASN) is a hallmark and possible central mechanism of Parkinson's disease and other synucleinopathies. Their therapy is currently hampered by the lack of early, screening-compatible diagnostic methods and efficient treatments. Areas covered: Patent applications related to synucleinopathies obtained from Patentscope and Espacenet databases are described against the background of current knowledge regarding the regulatory mechanisms of ASN behavior including alternative splicing, post-translational modifications, molecular interactions, aggregation, degradation, and changes in localization...
November 14, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27841045/an-updated-patent-review-xanthine-oxidase-inhibitors-for-the-treatment-of-hyperuricemia-and-gout-2011-2015
#9
Ritu Ojha, Jagjeet Singh, Anu Ojha, Harbinder Singh, Sahil Sharma, Kunal Nepali
Xanthine oxidase (XO) is a versatile molybdoflavoprotein, widely distributed, occurring in milk, kidney, lung, heart, and vascular endothelium. Catalysis by XO to produce uric acid and reactive oxygen species leads to many diseases. Anti hyperuricemic therapy by xanthine oxidase inhibitors has been mainly employed for the treatment of gout. Area covered: This review covers the patent literature (2011-2015) and also presents the interesting strategies/rational approaches employed for the design of xanthine oxidase inhibitors reported recently...
November 12, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27828733/trends-in-therapeutic-drug-conjugates-for-bacterial-diseases-a-patent-review
#10
Pedro M S D Cal, Maria J Matos, Gonçalo J L Bernardes
Introduction Drug conjugates are trend topics in Chemical Biology. These entities are an emerging class of highly potent biopharmaceutical drugs, best known in the field of oncology, that have been also designed as a targeted therapy/diagnosis for the treatment/prevention of several bacterial diseases. Antibiotic resistance is now a major threat to public health, and targeted strategies can reduce resistance. The following review aims at giving an overview of the patented therapeutic innovations covering these areas...
November 9, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27788040/neuropeptide-s-receptor-ligands-a-patent-review-2005-2016
#11
Chiara Ruzza, Girolamo Calò, Salvatore Di Maro, Salvatore Pacifico, Claudio Trapella, Severo Salvadori, Delia Preti, Remo Guerrini
Neuropeptide S (NPS) is a 20-residue peptide and endogenous ligand of the NPS receptor (NPSR). This receptor was a formerly orphan GPCR whose activation increases calcium and cyclic adenosine monophosphate levels. The NPS/NPSR system is expressed in several brain regions where it controls important biological functions including locomotor activity, arousal and sleep, anxiety, food intake, memory, pain, and drug addiction. Areas covered: This review furnishes an updated overview of the patent literature covering NPSR ligands since 2005, when the first example of an NPSR antagonist was disclosed...
November 9, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27813440/amino-acid-deprivation-using-enzymes-as-a-targeted-therapy-for-cancer-and-viral-infections
#12
H S Fernandes, C S Silva Teixeira, P A Fernandes, M J Ramos, N M F S A Cerqueira
INTRODUCTION: Amino acid depletion in the blood serum is currently being exploited and explored for therapies in tumors or viral infections that are auxotrophic for a certain amino acid or have a metabolic defect and cannot produce it. The success of these treatments is because normal cells remain unaltered since they are less demanding and/or can synthesize these compounds in sufficient amounts for their needs by other mechanisms. AREAS COVERED: This review is focused on amino acid depriving enzymes and their formulations that have been successfully used in the treatment of several types of cancer and viral infections...
November 4, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27796146/new-antimycobacterial-agents-in-the-pre-clinical-phase-or-beyond-recent-advances-in-patent-literature-2001-2016
#13
Patricia Bento da Silva, Débora L Campos, Camila M Ribeiro, Isabel C Silva, Fernando Rogério Pavan
Tuberculosis, an infectious disease, has caused more deaths worldwide than any other single infectious disease, killing more than 1.5 million people each year; equating to 4,100 deaths a day. In the past 60 years, no new drugs have been added to the first line regimen, in spite of the fact that thousands of papers have been published on drugs against tuberculosis and hundreds of drugs have received patents as new potential products. Thus, there is undoubtedly an urgent need for the deployment of new effective drugs against tuberculosis...
October 31, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27788608/boron-s-journey-advances-in-the-study-and-application-of-pharmacokinetics
#14
Ana L Ocampo-Néstor, José G Trujillo-Ferrara, Antonio Abad-García, Cynthia Reyes-López, Simonetta Geninatti-Crich, Marvin A Soriano-Ursúa
Boron-containing compounds (BCCs) are attractive chemical entities in drug development. Some of these compounds have been used in the treatment of human disease, and studies on their pharmacodynamics suggest that they employ multiple forms of activity. However, less is known about the pharmacokinetic profile of these molecules. Areas covered: The herein compiled reported data is presented in accordance with the classical 'ADME' system for identifying the scope of BCCs in the respective fields. Our analysis suggests that these compounds have several distinct ways to move within the human body, and that the specific structural features of each molecule account for its distinct pharmacokinetic profile...
October 28, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27785931/role-of-glutathione-s-transferases-in-neurological-problems
#15
Anil Kumar, Dinesh K Dhull, Varun Gupta, Priyanka Channana, Arti Singh, Manveen Bhardwaj, Poonam Ruhal, Ruchika Mittal
Role of Glutathione-S-transferases (GSTs) has been well explored in the cellular detoxification process, regulation of redox homeostasis and S-glutothionylation of target proteins like JNK, ASK1 etc. However, altered levels or functions of this enzyme or their subtypes have emerged in the development of several pathologies diseases such as Alzheimer's disease, Parkinson's disease, cancer and related conditions. Oxidative stress is one of the possible pathological events that contributes significantly to activation of degenerating cascades inside neuronal cells...
October 27, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27782764/oleanane-derivatives-for-pharmaceutical-use-a-patent-review-2000-2016
#16
Milena Masullo, Cosimo Pizza, Sonia Piacente
Oleanolic acid has been considered a good start molecule for synthetic exploitation. Thus hundreds of oleanane triterpenoids have been synthesized and patented. Also many oleanane saponins have been patented for their biological activities and possible pharmaceutical use. Areas covered: Patents reporting the biological activities of oleanane derivatives and saponins with oleanane-type aglycones were examined. Among the synthesized oleanane derivatives, the most promising seem to be 2-cyano-3,12-dioxoolean-1,9(11)-dien-28-oic acid derivatives which interfere with many pathways involved in inflammation, oxidative stress and cell proliferation...
October 26, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27774824/inhibitors-of-jak-family-kinases-an-update-on-the-patent-literature-2013-2015-part-1
#17
Jason G Kettle, Annika Åstrand, Matthew Catley, Neil P Grimster, Magnus Nilsson, Qibin Su, Richard Woessner
Introduction Janus kinases (JAKs) are a family of four enzymes; JAK1, JAK2, JAK3 and tyrosine kinase 2 (TYK2) that are critical in cytokine signalling and are strongly linked to both cancer and inflammatory diseases. There are currently two launched JAK inhibitors for the treatment of human conditions: tofacitinib for Rheumatoid arthritis (RA) and ruxolitinib for myeloproliferative neoplasms including intermediate or high risk myelofibrosis and polycythemia vera. Areas covered This review covers patents claiming activity against one or more JAK family members in the period 2013-2015 inclusive, and covers 95 patents from 42 applicants, split over two parts...
October 24, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27774822/inhibitors-of-jak-family-kinases-an-update-on-the-patent-literature-2013-2015-part-2
#18
Jason G Kettle, Annika Åstrand, Matthew Catley, Neil P Grimster, Magnus Nilsson, Qibin Su, Richard Woessner
Introduction Janus kinases (JAKs) are a family of four enzymes; JAK1, JAK2, JAK3 and tyrosine kinase 2 (TYK2) that are critical in cytokine signalling and are strongly linked to both cancer and inflammatory diseases. There are currently two launched JAK inhibitors for the treatment of human conditions: tofacitinib for Rheumatoid arthritis (RA) and ruxolitinib for myeloproliferative neoplasms including intermediate or high risk myelofibrosis and polycythemia vera. Areas covered This review covers patents claiming activity against one or more JAK family members in the period 2013-2015 inclusive, and covers 95 patents from 42 applicants, split over two parts...
October 24, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27774821/schiff-bases-in-medicinal-chemistry-a-patent-review-2010-2015
#19
Abdul Hameed, Mariya Al-Rashida, Maliha Uroos, Syed Ali, Khalid M Khan
Schiff bases are synthetically accessible and structurally diverse compounds, typically obtained by facile condensation between an aldehyde, or a ketone with primary amines. Schiff bases contain an azomethine (-C=N-) linkage that stitches together two or more biologically active aromatic/heterocyclic scaffolds to form various molecular hybrids with interesting biological properties. Schiff bases are versatile metal complexing agents and have been known to coordinate all metals to form stable metal complexes with vast therapeutic applications...
October 24, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27724045/p2x7-receptor-antagonists-a-patent-review-2010-2015
#20
Jin-Hee Park, Yong-Chul Kim
The P2X7 receptor (P2X7R) is a unique subtype among the family of seven purinergic P2X receptors, which are ATP-gated non-selective cation channels. P2X7R has been reported to have pathological roles in various diseases, including autoimmune diseases such as arthritis and inflammatory bowel disease, neurodegenerative diseases, chronic pain, mood disorders and cancers. Therefore, many pharmaceutical companies have endeavored to develop a clinical candidate targeting P2X7R. Areas covered: This review provides a summary of various patents on chemicals and biologics and their clinical use published between 2010 and 2015...
October 10, 2016: Expert Opinion on Therapeutic Patents
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