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Expert Opinion on Therapeutic Patents

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https://www.readbyqxmd.com/read/28447479/autotaxin-inhibitors-a-patent-review-2012-2016
#1
Aikaterini Nikolaou, Maroula G Kokotou, Dimitris Limnios, Anastasia Psarra, George Kokotos
Autotaxin (ATX) is a secreted enzyme that hydrolyzes lysophosphatidylcholine to lysophosphatidic acid (LPA) and choline. The ATX/LPA axis has received increasing interest in recent years because both the enzyme ATX and the bioactive lipid LPA are involved in various pathological conditions such as tumor progression and metastasis, fibrotic diseases, autoimmune diseases, arthritis, chronic hepatitis, obesity and impaired glucose homeostasis. Thus, a great effort has been devoted in developing synthetic ATX inhibitors as new agents to treat various diseases including cancer and fibrotic diseases...
April 27, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28425830/tryptase-inhibitors-a-patent-review
#2
Wei-Wei Ni, Meng-Da Cao, Wen Huang, Ling Meng, Ji-Fu Wei
Tryptase is one of the main serine-proteinases located in the secretory granules of mast cells, and is released through degranulation, which is involved in the pathogenesis of allergic inflammatory disease, cardiovascular diseases, lung fibrosis and tumor. Therefore, inhibitors targeting tryptase may represent a new direction for the treatment of allergic inflammatory disease and other diseases. Areas covered: In this article, we discussed the history and development of tryptase inhibitors and described a variety of tryptase inhibitors via their structures and biological importance in clinical studies and drug development for tryptase-related diseases...
April 20, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28394193/ezh2-inhibitors-a-patent-review-2014-2016
#3
Giulia Stazi, Clemens Zwergel, Antonello Mai, Sergio Valente
The histone methyltransferase EZH2 is the catalytic subunit of the PRC2 complex involved in H3K27 trimethylation. Aberrant PRC2 activity has been reported in several cancers and EZH2 overexpression has been associated with poor outcome in different tumors. EZH2 somatic mutations and deletions was found in lymphomas, myelodysplastic and myeloproliferative disorders and associated with higher H3K27me3 levels. Numerous chemical entities have been studied as EZH2 inhibitors in the recent years and some of them entered the cancer clinical arena...
April 20, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28355094/advances-in-treatment-of-pulmonary-arterial-hypertension-patent-review
#4
Bhuvaneshwar Vaidya, Matthew Pangallo, Gregoire Ruffenach, Christine Marie Cunningham, Jeanette C Perron, Srikanth Kolluru, Mansoureh Eghbali, Vivek Gupta
Current therapeutic approaches for pulmonary arterial hypertension (PAH) commonly include use of prostacyclins, endothelin pathway antagonists or NO (nitric oxide) pathway modulators. These agents are non-specific and suffer from several important shortcomings including short half-lives, invasive routes of administration, higher dose and frequency requirements, and several dose-related systemic side effects. Hence, discovery of novel agents with improved therapeutic efficacy with respect to survival benefits and the development of non-invasive routes of administration are in critical need...
March 29, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28350212/gamma-secretase-inhibitors-a-patent-review-2013-2015
#5
Kai Gu, Qi Li, Hongzhi Lin, Jie Zhu, Jun Mo, Siyu He, Xin Lu, Xueyang Jiang, Haopeng Sun
Gamma secretase (GS) is an intricate and multi-subunits complex, and it can cut various transmembrane proteins. Now it is a therapeutic target for a number of diseases. However, due to some side effects, the clinical development of GSI is not successful. Therefore, searching for effective GSIs has become a key point in drug discovery. Areas covered: This review discusses the structure and function of GS and various types of GSIs. And this article seeks to give an overview of the patents or applications published from 2013 to 2015 in which novel chemical classes are claimed to inhibit the GS...
March 28, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28276280/patent-disclosure-requirements-for-therapeutic-antibody-patents
#6
Carmela De Luca, Anastassia Trifonova
Therapeutic antibodies have grown to become an important product class within the biopharmaceutical market. A prerequisite to their commercialization is adequate patent protection. Disclosure requirements and the types of claims available in different jurisdictions can impact the scope of protection available for antibodies. Areas covered: A comparative review of statutory bases, patent office practices and selected decisions in Canada, the United States and the United Kingdom related to disclosure requirements is provided...
March 9, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28270021/tropomyosin-receptor-kinase-inhibitors-an-updated-patent-review-for-2010-2016-part-ii
#7
Justin J Bailey, Ralf Schirrmacher, Kristen Farrell, Vadim Bernard-Gauthier
TrkA/B/C receptor activation supports growth, survival, and differentiation of discrete neuronal populations during development, adult life, and ageing but also plays numerous roles in human disease onset and progression. Trk-specific inhibitors have therapeutic applications in cancer and pain and thus constitute a growing area of interest in oncology and neurology. There has been substantial growth in the number of structural classes of Trk inhibitors and the number of industrial entrants to the Trk inhibitor field over the past six years...
March 8, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28270010/tropomyosin-receptor-kinase-inhibitors-an-updated-patent-review-for-2010-2016-part-i
#8
Justin J Bailey, Ralf Schirrmacher, Kristen Farrell, Vadim Bernard-Gauthier
Tropomyosin receptor kinases (TrkA/B/C) play crucial roles in the development and maintenance of the nervous system, and aberrant expression of Trk has been implicated in neurological disorders as well as neural and non-neural neoplasms. Patent activity encompassing Trk inhibitors has grown substantially over the last 6 years, recognized by a rise in the number of pharmaceutical entrants to the field and the escalation of novel inhibitor chemotypes. Area covered: In Part I of this two part review, a biological and structural overview of Trk is provided in the context of Trk as a therapeutic target for cancer and pain, followed by the report of recent patent literature claiming small molecule inhibitors of Trk family kinases or which describe inhibitors developed for other kinase targets but include noteworthy Trk inhibition/application...
March 8, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28117607/leucine-rich-repeat-kinase-2-inhibitors-a-patent-review-2014-2016
#9
Paul Galatsis
Leucine-rich repeat kinase 2 (LRRK2) is a member of the Tyrosine Kinase-Like (TKL) branch of the kinome tree and is a multi-domain protein that includes GTPase and kinase activity. While genome-wide association studies (GWAS) has linked LRRK2 with Crohn's disease and leprosy, it has received the greatest attention due to it being implicated as one of the genetic loci associated with autosomal dominant inheritance in Parkinson's disease (PD). Areas covered: In this review, the small molecule patent literature from 2014-2016 with a focus on composition of matter and use patents was surveyed...
January 31, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28366103/methods-of-selecting-combination-therapy-for-colorectal-cancer-patients-a-patent-evaluation-of-us20160025730a1
#10
Daniel Plano, Verónica Alcolea, Carmen Sanmartín, Arun K Sharma
Colorectal cancer (CRC) is the fourth most common cancer worldwide. Targeted therapy drugs (TTDs) are a valid treatment, epithelial growth factor receptor (EGFR) inhibitors being one of the most commonly used for CRC patients. However, this treatment is only useful for patients with wild-type KRAS (wtKRAS) and is effective only on about 40 to 60% of this subset due to the high plasticity of ErbB network. Areas covered: The invention proposes the use of ErbB protein levels and ErbB receptor dimer formation as biomarkers for selecting, predicting and monitoring CRC patients showing sensitivity to the action of EGFR inhibitors to benefit from the combination therapy of EGFR and HER2 inhibitors...
May 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28064544/recent-advances-of-pyrrolopyridines-derivatives-a-patent-and-literature-review
#11
REVIEW
Mohammed I El-Gamal, Hanan S Anbar
Several pyrrolopyridines or azaindoles have been reported in the literature as biologically-active molecules. Most of them are anticancer agents, and few possess other therapeutic effects. Areas covered: The most recent biologically-active pyrrolopyridine derivatives have been reviewed from the patents and research articles published from 2010 to the mid of 2016. Their structural and biological features have been explained. In general, the pyrrolopyridine scaffold mimics the purine ring of the ATP molecule...
May 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28051882/are-sigma-modulators-an-effective-opportunity-for-cancer-treatment-a-patent-overview-1996-2016
#12
REVIEW
Simona Collina, Emanuele Bignardi, Marta Rui, Daniela Rossi, Raffaella Gaggeri, Alice Zamagni, Michela Cortesi, Anna Tesei
Although several molecular targets against cancer have been identified, there is a continuous need for new therapeutic strategies. Sigma Receptors (SRs) overexpression has been recently associated with different cancer conditions. Therefore, novel anticancer agents targeting SRs may increase the specificity of therapies, overcoming some of the common drawbacks of conventional chemotherapy. Areas covered: The present review focuses on patent documents disclosing SR modulators with possible application in cancer therapy and diagnosis...
May 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28033734/selective-histone-deacetylase-small-molecule-inhibitors-recent-progress-and-perspectives
#13
REVIEW
Hai-Tao Qin, Huan-Qiu Li, Feng Liu
Since the first pan-HDAC inhibitor SAHA was approved by U.S. FDA 10 years ago, HDACs including SIRT1-7 have received significant attention due to the fact that aberrant histone deacetylase activtiy has been implicated in a variety of human diseases, such as cancers, virus infection, and neurodegenerative diseases. During the past years, a considerable achievement of development of isoform- or class-selective HDAC inhibitors has been made, yielding many drug candidates for further clinical studies, which represents a state-of-the-art technology in the drug discovery arena...
May 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28024125/recent-progress-on-curcumin-based-therapeutics-a-patent-review-2012-2016-part-i-curcumin
#14
REVIEW
Rita Maria Concetta Di Martino, Barbara Luppi, Alessandra Bisi, Silvia Gobbi, Angela Rampa, Angela Abruzzo, Federica Belluti
curcumin is the main bioactive component contained in Curcuma Longa, largely employed in traditional medicine. Recently, beneficial properties, useful for prevention and treatment of several disorders, have been discovered for this compound. Peculiar structural feature is an α,β-unsaturated carbonyl system essential for establishing contacts with critical cysteine residues of several targets. This distinctive mechanism of action imparts to the molecule the ability to affect a large number of targets, accounting for its pleiotropic behaviour and definition of "privileged structure"...
May 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28005436/novel-leukotriene-biosynthesis-inhibitors-2012-2016-as-anti-inflammatory-agents
#15
REVIEW
Oliver Werz, Jana Gerstmeier, Ulrike Garscha
Leukotrienes (LTs) are lipid mediators produced from arachidonic acid with a broad variety of bioactivities in allergy and inflammation. The biosynthesis of LTs mainly involves 5-lipoxygenase (5-LO) and its 5-lipoxygenase-activating protein (FLAP), LTA4 hydrolase and LTC4 synthase that all may represent potential targets for LT biosynthesis inhibitors. Areas covered: We introduce the LT biosynthetic pathway and its cellular regulation, the diverse biological actions of LTs and their receptors, and we briefly describe the pharmacological strategies for suppression of LT formation as well as the classes of current LT biosynthesis inhibitors...
May 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27998196/recent-trends-in-neuropathic-pain-patents
#16
REVIEW
Rodolfo do Couto Maia
Neuropathic pain (NP) is one of the most important health problems faced nowadays. NP is a chronic disease that cannot be treated like other pain conditions because it is developed from a nerve injury that evolves into a permanent dysfunction of the central and/or peripheral nervous system. Therefore, it involves the participation of several systems and should be viewed as a multi-factorial disease that needs a whole new pharmacological strategy in order to achieve the desired pain relief. Areas covered: The Espacenet site was used as the main source in order to perform the patent research for NP treatment...
May 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27977313/thioredoxin-reductase-inhibitors-a-patent-review
#17
REVIEW
Baoxin Zhang, Junmin Zhang, Shoujiao Peng, Ruijuan Liu, Xinming Li, Yanan Hou, Xiao Han, Jianguo Fang
Mammalian thioredoxin reductases (TrxRs) are selenocysteine-containing homodimeric flavin enzymes that catalyze the NADPH-dependent reduction of oxidized thioredoxins. Increasing evidence indicates that TrxRs are potential targets for anticancer drug development. This review summarizes patented inhibitors of mammalian TrxRs with an emphasis on those having potential applications in treatment of cancer. Areas covered: A background introduction of TrxR as well as the relevance of TrxR and cancer is provided in the first part of this review...
May 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27977303/tyrosyl-trna-synthetase-inhibitors-a-patent-review
#18
REVIEW
Juan Sun, Peng-Cheng Lv, Hai-Liang Zhu
Bacterial infection has been a consistent and relentless threat to human health because of emerging resistance to existing antibiotics. Therefore, much of the research has been focused on the design of new potent antibacterial agents. Tyrosyl-tRNA synthetase (TyrRS), as a member of aminoacyl-tRNA synthetase family, could recognize the information including the coincident tRNA molecules and the amino acids' structures, which are essential in translating the coded information into protein structures in nucleic acids...
May 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28276283/novel-fused-pyrimidine-and-isoquinoline-derivatives-as-potent-hiv-1-nnrtis-a-patent-evaluation-of-wo2016105532a1-wo2016105534a1-and-wo2016105564a1
#19
REVIEW
Dongwei Kang, Zhipeng Huo, Gaochan Wu, Jiabao Xu, Peng Zhan, Xinyong Liu
In the three patent applications, the impact of changing the pyrimidine core of the rilpivirine (RPV) to a variety of alternative fused cores was explored, culminating in the identification of a series of conformationally restricted compounds with comparable potencies against WT and mutant HIV-1 strains with those of efavirenz (EFV) and RPV, and higher security in the Human Ether-a-go-go-Related Gene (hERG) assay. Areas covered: The present review provides a fused pyrimidine and isoquinoline derivatives as potent HIV-1 NNRTIs, and highlights the conformational restriction strategies in the development of NNRTIs...
April 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28266880/the-challenges-of-joint-performance-to-method-patents
#20
Feng-Chi Chen
Biotech patents are facing increasingly stern challenges. The patent statue holds that a multi-step method patent is not directly infringed unless all steps are carried out and attributed to a single entity. When separate steps are performed jointly by two or more parties, those parties are liable for divided infringement if there exists a direct infringement. Possibilities thus exist for unauthorized but non-infringing joint performance, i.e. enforcing a method patent will be difficult if joint performance stands as a valid defense against direct infringement...
April 2017: Expert Opinion on Therapeutic Patents
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