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Expert Opinion on Therapeutic Patents

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https://www.readbyqxmd.com/read/28454500/recent-progress-in-the-development-of-small-molecule-nrf2-modulators-a-patent-review-2012-2016
#1
Haopeng Sun, Jie Zhu, Hongzhi Lin, Kai Gu, Feng Feng
The NF-E2-related factor-2 (Nrf2) is a critical transcription factor that regulates the expression of many phase II and antioxidant genes to maintain the homeostasis. It has many biological functions and plays a central role in the cellular defensive machinery. The abnormal regulation of Nrf2 is closely associated with multiple diseases. Areas covered: This article first discusses the molecular regulatory mechanism of Nrf2-antioxidant response element (ARE) signaling. Then patents and publications about Nrf2 activators and inhibitors from 2012-2016 are reviewed...
May 10, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28447479/autotaxin-inhibitors-a-patent-review-2012-2016
#2
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 devotd in developing synthetic ATX inhibitors as new agents to treat various diseases including cancer and fibrotic diseases...
May 9, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28460551/cancer-stem-cell-csc-inhibitors-a-review-of-recent-patents-2012-2015
#3
Prashant S Kharkar
Cancer stem cells (CSCs) mediate tumor initiation and maintenance. These cells are chemoresistant and possess characteristics such as self-renewal, pluripotency, plasticity and differentiation. They have aberrant or altered signaling pathways depending on tumor microenvironment, tumor type, etc. CSCs are responsible for highly aggressive and invasive form of the disease following chemo- and/or radiotherapy. Eliminating CSCs is likely to improve the survival rate in patients. Several anti-CSC strategies and associated targets have been proposed and validated till date...
May 5, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28425830/tryptase-inhibitors-a-patent-review
#4
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
#5
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
#6
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
#7
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
#8
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
#9
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/28452243/evaluation-of-us-2016-0115161-a1-isoindoline-compounds-and-methods-of-their-use
#10
Rok Frlan, Stanislav Gobec
Immunomodulatory drugs (IMIDs®) are small orally available molecules that modulate the immune system and other biological targets through multiple mechanisms of action and have been successfully used in the treatment of myelodysplastic syndrome and multiple myeloma. However, recent studies of their complex mechanism of action revealed their potential in autoimmune diseases and solid tumors, which intensified scientific interest in these compounds. Areas covered: This patent application claims new IMIDs for the treatment of cancer and disorders associated with angiogenesis and inflammation...
June 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
#11
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...
June 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28121202/progress-of-middle-east-respiratory-syndrome-coronavirus-vaccines-a-patent-review
#12
Jiwon Choi, Mi-Gyeong Kim, Yu-Kyoung Oh, Young Bong Kim
Middle East respiratory syndrome coronavirus (MERS-CoV) has emerged as a new pathogen, causing severe complications and a high case fatality rate. No direct treatments are available as yet, highlighting the importance of prevention through suitable vaccination regimes. The viral spike (S) protein has been characterized as a key target antigen for vaccines. In particular, S protein domains have been utilized to produce high titers of neutralizing antibodies. Areas covered: Since the first report of MERS-CoV infection, a limited number of MERS-CoV-specific patents have been filed...
June 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28117607/leucine-rich-repeat-kinase-2-inhibitors-a-patent-review-2014-2016
#13
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...
June 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28076686/small-molecule-hiv-1-entry-inhibitors-targeting-gp120-and-gp41-a-patent-review-2010-2015
#14
Wen Li, Lu Lu, Weihua Li, Shibo Jiang
It is essential to discover and develop small-molecule HIV-1 entry inhibitors with suitable pharmaceutical properties. Areas covered: We review the development of small-molecule HIV-1 entry inhibitors as evidenced in patents, patent applications, and related research articles published between 2010 and 2015. Expert opinion: HIV-1 Env gp120 and gp41 are important targets for development of HIV-1 entry inhibitors. The Phe43 pocket in gp120 and the highly conserved hydrophobic pocket on gp41 NHR-trimer are important targets for identification of HIV-1 attachment and fusion inhibitors, respectively...
June 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28074661/inosine-5-monophosphate-dehydrogenase-impdh-inhibitors-a-patent-and-scientific-literature-review-2002-2016
#15
Gregory D Cuny, Chalada Suebsuwong, Soumya S Ray
Inosine-5'-monophosphate dehydrogenase (IMPDH) is an enzyme involved in the de novo biosynthesis of guanine nucleotides. To date human IMPDH inhibitors have been approved for prevention of organ transplant rejection and as anti-viral agents. More recently, the use of IMPDH inhibitors for other indications including cancer and pathogenic microorganisms has been pursued. Areas covered: IMPDH inhibitors disclosed primarily in the patent and scientific literature from 2002 to the present are discussed. Several interesting chemotypes that have not been pursued by patent protection are also highlighted...
June 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28067079/mglu5-negative-allosteric-modulators-a-patent-review-2013-2016
#16
Kyle A Emmitte
The pursuit of small molecule mGlu5 NAMs as treatments for a variety of psychiatric and neurodegenerative disorders has developed into a mature field. In addition to extensive preclinical studies, multiple compounds have advanced into clinical trials with the most advanced studies occurring in patients with FXS, PD-LID, and MDD. Areas covered: This review begins with an update of the clinical activity with mGlu5 NAMs, and then moves into a summary of patent applications filed since 2013. The summaries are organized into three separate sections: (1) inventions centered on improvements to existing clinical compounds; (2) new small molecules that maintain the prototypical disubstituted alkyne chemotype found in many mGlu5 NAM compounds; and (3) new small molecules that are not from a disubstituted alkyne chemotype...
June 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27998201/cathepsin-b-and-l-inhibitors-a-patent-review-2010-present
#17
Yu-Yao Li, Jing Fang, Gui-Zhen Ao
Cathepsins play an important role in protein degradation and processing. Aberrant cathepsin B or L is closely associated with many serious diseases such as cancer, osteoporosis and autoimmune disorders. Therefore, development of potent and selective cathepsin B and L inhibitors has aroused much attention in recent years. Although several classes of cathepsin inhibitors are presently available, there are still some problems to solve, such as broad-spectrum inhibition to protease, specially cysteine proteases, which lead to unpredictable side effects in clinical trials...
June 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27828716/glycogen-synthase-kinase-3-gsk-3-inhibitors-a-patent-update-2014-2015
#18
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...
June 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
#19
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
#20
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
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