1,090 results match your criteria Expert Opinion on Therapeutic Patents[Journal]


Treatment of cancer with a combination of LAG-3Ig and anti-PD-1/anti-PD-L1 antibodies: a patent evaluation of US2018271940 A1.

Expert Opin Ther Pat 2019 Apr 16. Epub 2019 Apr 16.

d Laboratorio de Bioquímica, Centro de Química , Instituto de Ciencias, Benemérita Universidad Autónoma de Puebla , Puebla , CP 72750 , México.

Introduction: LAG-3 is checkpoint inhibitor in cancer that coordinates the down regulation of the proliferation of antigen-specific lymphocytes. There is a great need to discover and develop new therapies focused on inhibiting the action of LAG-3 and consequently improving the immune response in the various types of cancer. Authors of patent US2018271940 propose a method to eradicate cancer that utilizes the combination of LAG-3Ig and anti-PD-1 or anti-PD-L1 antibodies. Read More

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http://dx.doi.org/10.1080/13543776.2019.1608947DOI Listing
April 2019
4.297 Impact Factor

Interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitors: an updated patent review (2016-2018).

Expert Opin Ther Pat 2019 Apr 29;29(4):243-259. Epub 2019 Mar 29.

a Merck Sharp & Dohme Corp , a subsidiary of Merck & Co., Inc , Kenilworth , NJ , USA.

Introduction: Interleukin-1 receptor-associated kinase 4 (IRAK4) is the most upstream kinase in Toll/Interleukin-1 receptor (TIR) signaling. Human and rodent genetics support the role of IRAK4 in immune function and the involvement of IRAK4-dependent signaling in certain cancers is hypothesized. The accumulating evidence has motivated the discovery of IRAK4 inhibitors that could be used therapeutically. Read More

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http://dx.doi.org/10.1080/13543776.2019.1597850DOI Listing

Marine natural products as source of new drugs: a patent review (2015-2018).

Expert Opin Ther Pat 2019 Apr 3;29(4):283-309. Epub 2019 Apr 3.

a CSIR Unit for Research and Development of Information Products (CSIR-URDIP) , Pune , India.

Introduction: Natural products from plants, animals, microbes, and minerals have long been a traditional source for the treatment of human diseases. In the past decades, research on natural products for the pharmaceutical industry had declined due to numerous challenges. However, the recent developments in analytical technology, spectroscopy, and high-throughput screening have tremendously revived natural product drug discovery, including contribution from marine-based drugs. Read More

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http://dx.doi.org/10.1080/13543776.2019.1598972DOI Listing
April 2019
2 Reads

A patent update on PDK1 inhibitors (2015-present).

Expert Opin Ther Pat 2019 Apr 29;29(4):271-282. Epub 2019 Mar 29.

a Department of Pharmacy , University of Pisa , Pisa , Italy.

Introduction: 3-Phosphoinositide-dependent kinase 1 (PDK1), the 'master kinase of the AGC protein kinase family', plays a key role in cancer development and progression. Although it has been rather overlooked, in the last decades a growing number of molecules have been developed to effectively modulate the PDK1 enzyme. Areas covered: This review collects different PDK1 inhibitors patented from October 2014 to December 2018. Read More

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http://dx.doi.org/10.1080/13543776.2019.1597852DOI Listing
April 2019
1 Read

A patent update on cannabinoid receptor 1 antagonists (2015-2018).

Expert Opin Ther Pat 2019 Apr 8;29(4):261-269. Epub 2019 Apr 8.

a Center for Drug Discovery , RTI International , RTP , NC , USA.

Introduction: The endocannabinoid system is an important regulator of various physiological processes. Preclinical and clinical studies indicate that attenuation of the endocannabinoid system via antagonism of the type 1 cannabinoid receptor (CB1) is an excellent strategy to treat obesity, metabolic syndrome and associated disorders. However, centrally acting antagonists of CB1 also produce adverse effects like depression and anxiety. Read More

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http://dx.doi.org/10.1080/13543776.2019.1597851DOI Listing
April 2019
2 Reads

Bruton's tyrosine kinase (BTK) inhibitors in treating cancer: a patent review (2010-2018).

Expert Opin Ther Pat 2019 Apr;29(4):217-241

a Department of Medicinal Chemistry, School of Pharmacy, Health Science Center , Xi'an Jiaotong University , Xi'an , Shaanxi P.R. China.

Introduction: Bruton's tyrosine kinase (BTK) plays a critical role in the regulation of survival, proliferation, activation and differentiation of B-lineage cells. It participates by regulating multiple cellular signaling pathways, including B cell receptor and FcR signaling cascades. BTK is abundantly expressed and constitutively active in the pathogenesis of B cell hematological malignancies, as well as several autoimmune diseases. Read More

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http://dx.doi.org/10.1080/13543776.2019.1594777DOI Listing
April 2019
2 Reads

A spotlight on Brexit; what does the future hold for UK drug patent legislation?

Authors:
Robert Watson

Expert Opin Ther Pat 2019 Apr 6;29(4):215-216. Epub 2019 Mar 6.

a Mewburn Ellis LLP , London , United Kingdom.

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http://dx.doi.org/10.1080/13543776.2019.1590335DOI Listing

A therapeutic patent overview of MDM2/X-targeted therapies (2014-2018).

Expert Opin Ther Pat 2019 Mar 1;29(3):151-170. Epub 2019 Mar 1.

a Department of Organic Chemistry, Faculty of Chemistry , Jagiellonian University , Krakow , Poland.

Introduction: MDM2 and MDMX proteins provide the inhibition of p53 tumor suppressor, thus allowing for accelerated mutation-driven cancer microevolution. A pharmacological blockade of MDM2/X-p53 interaction results in p53 reactivation in p53 cells, leading to cancer growth inhibition. Throughout the past 20 years, multiple chemical entities have been proposed to reactivate p53 by antagonizing MDM2/X proteins. Read More

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http://dx.doi.org/10.1080/13543776.2019.1582645DOI Listing
March 2019
3 Reads

A patent update on therapeutic applications of urease inhibitors (2012-2018).

Expert Opin Ther Pat 2019 Mar 6;29(3):181-189. Epub 2019 Mar 6.

a H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences , University of Karachi , Karachi , Pakistan.

Introduction: Urease is a nickel-containing metalloenzyme that is commonly found in different bacteria, plants, algae, and fungi and mediates the growth of many pathogenic bacteria in the acidic environment of the stomach. Despite the large number of molecules known to have excellent urease inhibitory activity, there is an alarming lack of urease inhibitor drugs on the market. Area covered: This review aims to provide a comprehensive overview of the different types of molecules patented as potent urease inhibitors from the year 2012 to 2018. Read More

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http://dx.doi.org/10.1080/13543776.2019.1584612DOI Listing
March 2019
1 Read
4.297 Impact Factor

Aldose reductase inhibitors: 2013-present.

Expert Opin Ther Pat 2019 Mar 27;29(3):199-213. Epub 2019 Feb 27.

a Dipartimento di Farmacia , Università di Pisa , Pisa , Italy.

Introduction: Aldose reductase (ALR2) is both the key enzyme of the polyol pathway, whose activation under hyperglycemic conditions leads to the development of chronic diabetic complications, and the crucial promoter of inflammatory and cytotoxic conditions, even under a normoglycemic status. Accordingly, it represents an excellent drug target and a huge effort is being done to disclose novel compounds able to inhibit it. Areas covered: This literature survey summarizes patents and patent applications published over the last 5 years and filed for natural, semi-synthetic and synthetic ALR2 inhibitors. Read More

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http://dx.doi.org/10.1080/13543776.2019.1582646DOI Listing

Landscape of granted US patents in personalized diagnostics for oncology from 2014 to 2018.

Expert Opin Ther Pat 2019 Mar 6;29(3):191-198. Epub 2019 Feb 6.

a Biotechnology & Pharmaceuticals Group , Global Prior Art, Inc , Boston , MA , USA.

Introduction: Personalized diagnostic testing (PDx) is a key component of the precision medicine toolkit and has shown the most development in cancer applications. Recent changes in the regulatory and legal landscapes regarding PDx development and commercialization have brought uncertainties to both intellectual property strategies and business model development. While the regulatory and legal uncertainties have been well-documented, there has been little reported analysis of the recent patent landscape and movement of IP into the PDx market. Read More

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https://www.tandfonline.com/doi/full/10.1080/13543776.2019.1
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http://dx.doi.org/10.1080/13543776.2019.1575809DOI Listing
March 2019
2 Reads

ATP-competitive DNA gyrase and topoisomerase IV inhibitors as antibacterial agents.

Expert Opin Ther Pat 2019 Mar 6;29(3):171-180. Epub 2019 Feb 6.

a Faculty of Pharmacy , University of Ljubljana , Ljubljana , Slovenia.

Introduction: The bacterial topoisomerases DNA gyrase and topoisomerase IV are validated targets for development of novel antibacterial agents. Fluoroquinolones inhibit the catalytic GyrA and/or ParC(GrlA) subunit and have been commonly used, although these have toxicity liabilities that restrict their use. The ATPase GyrB and ParE(GrlB) subunits have been much less explored and after withdrawal of novobiocin, there are no further marketed inhibitors . Read More

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http://dx.doi.org/10.1080/13543776.2019.1575362DOI Listing
March 2019
2 Reads

Systematic review and technological prospection: ethyl ferulate, a phenylpropanoid with antioxidant and neuroprotective actions.

Expert Opin Ther Pat 2019 02 25;29(2):73-83. Epub 2019 Jan 25.

c Federal University of Piauí , Teresina , Brazil.

Introduction: Ethyl ferulate is a phenylpropanoid with anti-inflammatory, antioxidant and neuroprotective activities of natural and synthetic origin with potential uses in the nutraceutical and pharmaceutical industry. Therefore, the aim of this study was to investigate the current scenario regarding patents and scientific articles available involving the substance in question, regarding aspects such as quantity, areas of knowledge and depositor countries.

Areas Covered: To do so, we conducted technological and scientific prospecting on the WIPO, EPO, USPTO and INPI and scientific databases in PubMed, Web of Science and Lilacs databases using the keywords 'ferulic acid ethyl ester' and 'ethyl ferulate' in English and Portuguese. Read More

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http://dx.doi.org/10.1080/13543776.2019.1568410DOI Listing
February 2019
2 Reads

GPR17 receptor modulators and their therapeutic implications: review of recent patents.

Expert Opin Ther Pat 2019 Feb 24;29(2):85-95. Epub 2019 Jan 24.

a School of Pharmacy, Medicinal Chemistry Unit , University of Camerino , Camerino , Italy.

Introduction: The GPR17 receptor, phylogenetically related to both purinergic P2Y and CysLT receptors, is mainly expressed in the CNS and, in general, in organs that can typically undergo ischemic damage. This receptor is involved in various pathologies including stroke, brain and spinal cord trauma, multiple sclerosis and in all diseases characterized by neuronal and myelin dysfunction. Therefore, there is a strong needed to identify molecules capable of binding specifically to GPR17 receptors. Read More

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http://dx.doi.org/10.1080/13543776.2019.1568990DOI Listing
February 2019
3 Reads

A patent review of arginine methyltransferase inhibitors (2010-2018).

Expert Opin Ther Pat 2019 Feb;29(2):97-114

a CAS Key Laboratory of Receptor Research, State Key Laboratory of Drug Research, Drug Discovery and Design Center , Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Shanghai , China.

Introduction: Protein arginine methyltransferases (PRMTs) are fundamental enzymes that specifically modify the arginine residues of versatile substrates in cells. The aberrant expression and abnormal enzymatic activity of PRMTs are associated with many human diseases, especially cancer. PRMTs are emerging as promising drug targets in both academia and industry. Read More

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http://dx.doi.org/10.1080/13543776.2019.1567711DOI Listing
February 2019
12 Reads
4.297 Impact Factor

Research and development of anti-Parkinson's drugs: an analysis from the perspective of technology flows measured by patent citations.

Expert Opin Ther Pat 2019 02 19;29(2):127-135. Epub 2019 Jan 19.

a State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Taipa , China.

Introduction: By 2020, nearly one million people will live with Parkinson's disease (PD) in the U.S. This disorder has a significant impact on patients' quality of life and is a burden on families and society. Read More

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http://dx.doi.org/10.1080/13543776.2019.1567712DOI Listing
February 2019
10 Reads

Selective Tyk2 inhibitors as potential therapeutic agents: a patent review (2015-2018).

Expert Opin Ther Pat 2019 02 22;29(2):137-149. Epub 2019 Jan 22.

a Key Laboratory of Elemene Class Anti-Cancer Chinese Medicine of Zhejiang Province, Hangzhou Normal University , Hangzhou , Zhejiang Province , China.

Introduction: Tyrosine kinase 2 (Tyk2) is a non-receptor tyrosine-protein kinase, an enzyme that in humans is encoded by the TYK2 gene. Tyk2, together with three other family subtypes, namely, Jak1, Jak2, and Jak3, belong to the JAK family. Before 2014, far more publications and patents appeared in public domain attributing to the development of selective Jak2 and Jak3 inhibitors than those for selective Tyk2 and Jak1 inhibitors. Read More

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https://www.tandfonline.com/doi/full/10.1080/13543776.2019.1
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http://dx.doi.org/10.1080/13543776.2019.1567713DOI Listing
February 2019
60 Reads

Scientific and technological prospection on transdermal formulations and complementary therapies for the treatment of primary dysmenorrhea.

Expert Opin Ther Pat 2019 Feb 15;29(2):115-126. Epub 2019 Jan 15.

a Postgraduate Program in Biotechnology - RENORBIO , Focal Point - Federal University of Piauí , Teresina , Brazil.

Introduction: Primary dysmenorrhea (PD) is another term for idiopathic menstrual cramps. Treatments include the use of oral non-steroidal anti-inflammatory drugs (NSAIDs). These drugs have several side effects. Read More

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http://dx.doi.org/10.1080/13543776.2019.1562547DOI Listing
February 2019
4 Reads

The use of terpenes and derivatives as a new perspective for cardiovascular disease treatment: a patent review (2008-2018).

Expert Opin Ther Pat 2019 01 24;29(1):43-53. Epub 2018 Dec 24.

a Department of Physiology , Federal University of Sergipe , Sergipe , Brazil.

Introduction: Terpenes are a class of secondary metabolites that can be found in a variety of animal and plants species. They are considered the most structurally diversified and abundant of all natural compounds. Several studies have shown the application of terpenes, such as carvacrol, linalool, and limonene in many pharmaceutical and medicinal fields, including cardiovascular disorders, the leading cause of death worldwide. Read More

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http://dx.doi.org/10.1080/13543776.2019.1558211DOI Listing
January 2019
2 Reads

Targeted treatment of anaerobic cancer. Patent evaluation of US2016279084 and US2017056350.

Expert Opin Ther Pat 2019 Jan 17;29(1):1-6. Epub 2018 Dec 17.

a Istituto di Biostrutture e Bioimmagini-CNR , Naples , Italy.

Introduction: Based on the initial studies of J. Folkman in 1970s, which led to the proposal of the antiangiogenic therapy, many drugs targeting VEGF or its receptors have been developed with some of them approved for cancer treatment. However, these molecules so far have shown only a limited effect on survival benefits in patients. Read More

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https://www.tandfonline.com/doi/full/10.1080/13543776.2019.1
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http://dx.doi.org/10.1080/13543776.2019.1558210DOI Listing
January 2019
13 Reads

Current state on tryptophan 2,3-dioxygenase inhibitors: a patent review.

Expert Opin Ther Pat 2019 01 16;29(1):11-23. Epub 2019 Jan 16.

a Medicinal Chemistry Research Group (CMFA), Louvain Drug Research Institute (LDRI) , Université Catholique de Louvain (UCLouvain) , Brussels , Belgium.

Introduction: Tryptophan-2, 3-dioxygenase (TDO2) is a tryptophan-degrading enzyme constitutively expressed in the liver and to a lesser extend in the brain. Before its link to cancer immunotherapy was discovered in 2011, the search for TDO2 inhibitors was initially driven by depression therapy. In the recent years, TDO2 has drawn an increasing attention as a promising target in both cancer and neuropsychiatric diseases. Read More

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http://dx.doi.org/10.1080/13543776.2019.1556638DOI Listing
January 2019
1 Read

Therapeutic potential of Panax ginseng and its constituents, ginsenosides and gintonin, in neurological and neurodegenerative disorders: a patent review.

Expert Opin Ther Pat 2019 01 11;29(1):55-72. Epub 2018 Dec 11.

c Pharmaceutical Research Center, Pharmaceutical Technology Institute , Mashhad University of Medical Sciences , Mashhad , Iran.

Introduction: Ginseng, Panax ginseng, has been used for various diseases and proven its great efficacy in managing central nervous system diseases.

Areas Covered: This article covers the therapeutic potential of patents on ginseng and its active constituents to develop therapies for neurodegenerative and neurological disorders, since 2010. The literature review was provided using multiple search engines including Google Patent, Espacenet and US Patent in the field of neurodegenerative diseases, Alzheimer's disease, Parkinson's disease, cognitive, and neurological disorders. Read More

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http://dx.doi.org/10.1080/13543776.2019.1556258DOI Listing
January 2019
19 Reads

A decade of nutraceutical patents: where are we now in 2018?

Expert Opin Ther Pat 2018 Dec 29;28(12):875-882. Epub 2018 Nov 29.

a Department of Pharmacy , University of Napoli Federico II , Napoli , Italy.

Introduction: In the last 10 years, nutraceuticals have grown in interest to researchers, industry, and consumers and are now familiar in the collective imagination as a tool for preventing the onset of a disease. Often nutraceuticals are confused with biologically active phytochemicals/botanicals which can have health benefits. This is a misunderstanding however as the term nutraceutical refers to a product that must have a beneficial effect on health proven by clinical testing. Read More

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http://dx.doi.org/10.1080/13543776.2018.1552260DOI Listing
December 2018
14 Reads

Hippo pathway inhibition by blocking the YAP/TAZ-TEAD interface: a patent review.

Expert Opin Ther Pat 2018 Nov 27. Epub 2018 Nov 27.

a Genentech, Inc ., 1 DNA WAY, South San Francisco , CA 94080 , USA.

Introduction: The Hippo pathway represents a new and intriguing opportunity for the treatment of cancer. Activation or overexpression of YAP or TAZ has been shown to lead to cell transformation and tumor development. To date, no small molecule compounds targeting this pathway have progressed to the clinic, illustrating both its potential and its infancy. Read More

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https://www.tandfonline.com/doi/full/10.1080/13543776.2018.1
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http://dx.doi.org/10.1080/13543776.2018.1549226DOI Listing
November 2018
23 Reads

c-Met kinase inhibitors: an update patent review (2014-2017).

Expert Opin Ther Pat 2019 Jan 12;29(1):25-41. Epub 2018 Dec 12.

a Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry , China Pharmaceutical University , Nanjing , P. R. China.

Introduction: The receptor tyrosine kinase c-Met is involved in the formation, metastasis and invasion of various malignant tumors thus it has been an attractive target for anti-tumor drug designing. Many compositions targeting c-Met have been developed in pharmaceutical industry for cancer therapy and some of them are in clinical study now. Among them, Crizotinib was the first small molecular inhibitor approved by FDA in 2011. Read More

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http://dx.doi.org/10.1080/13543776.2019.1552261DOI Listing
January 2019
12 Reads

A patent review of the ubiquitin ligase system: 2015-2018.

Expert Opin Ther Pat 2018 Dec 23;28(12):919-937. Epub 2018 Nov 23.

c Barbara Ann Karmanos Cancer Institute, and Departments of Oncology, Pharmacology and Pathology, School of Medicine , Wayne State University , Detroit , MI , USA.

Introduction: Ubiquitin-proteasome system (UPS) has been validated as a novel anticancer drug target in the past 20 years. The UPS contains two distinct steps: ubiquitination of a substrate protein by ubiquitin activating enzyme (E1), ubiquitin conjugating enzyme (E2), and ubiquitin ligase (E3), and substrate degradation by the 26S proteasome complex. The E3 enzyme is the central player in the ubiquitination step and has a wide range of specific substrates in cancer cells, offering great opportunities for discovery and development of selective drugs. Read More

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https://www.tandfonline.com/doi/full/10.1080/13543776.2018.1
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http://dx.doi.org/10.1080/13543776.2018.1549229DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6398165PMC
December 2018
30 Reads

αβ integrin inhibitors: a patent review.

Expert Opin Ther Pat 2018 Dec 22;28(12):903-917. Epub 2018 Nov 22.

c Research Division of Clinical Pharmacology , Τhe First Affiliated Hospital of Nanjing Medical University , Nanjing , China.

Introduction: The αβ integrin is heterodimeric cell surface receptors expressed on most leukocytes. Mucosal addressing cell adhesion molecule 1(MAdCAM-1) is an exclusive ligand for αβ integrin. Areas covered: This article will highlight the progress that has been made in the discovery and development of αβ integrin inhibitors, and their use in the treatment of inflammatory bowel diseases, multiple sclerosis, asthma, hepatic disorders, human immunodeficiency virus, allergic conjunctivitis and type 1 diabetes. Read More

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http://dx.doi.org/10.1080/13543776.2018.1549227DOI Listing
December 2018
13 Reads
4.300 Impact Factor

Evaluation of WO2014121383 A1: a process for preparation of rufinamide and intermediates.

Expert Opin Ther Pat 2019 Jan 19;29(1):7-10. Epub 2018 Nov 19.

a Department of Chemistry , School of Advanced Sciences, Vellore Institute of Technology , Vellore , India.

Introduction: There is great potential in the synthetic development of rufinamide to treat childhood-onset epilepsy known as Lennox-Gastaut syndrome (LGS). Areas covered: 1,4-disubstituted triazole ring formed by 1,3-dipolar cycloaddition reaction is an important structural motif widely used to construct diverse chemotypes in chemical, biological, and material fields. 1,2,3-triazole ring containing rufinamide, an antiepileptic drug developed by Novartis, is useful in combination with other antiepileptic medicaments for the treatment of childhood-onset epilepsy known as LGS. Read More

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https://www.tandfonline.com/doi/full/10.1080/13543776.2019.1
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http://dx.doi.org/10.1080/13543776.2019.1549230DOI Listing
January 2019
2 Reads
4.297 Impact Factor

T-type calcium channel blockers: a patent review (2012-2018).

Authors:
Ghilsoo Nam

Expert Opin Ther Pat 2018 12 11;28(12):883-901. Epub 2018 Nov 11.

a Center for Neuro-Medicine , Brain Science Institute, Korea Institutes of Science and Technology (KIST) , Seoul , Republic of Korea.

Introduction: T-type calcium channels are attractive targets for potential treatment of epilepsy inflammatory or neuropathic pain, insomnia, Parkinson's disease, and cancer. Three isoforms having different biophysical functions are expressed in peripheral and central nerve. Since the withdrawal of mibefradil, the first compound marketed for selective T-type calcium channel blockade, extensive efforts have been made to identify more selective T-type calcium channel blockers. Read More

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https://www.tandfonline.com/doi/full/10.1080/13543776.2018.1
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http://dx.doi.org/10.1080/13543776.2018.1541982DOI Listing
December 2018
23 Reads

Quorum sensing inhibitors: a patent review (2014-2018).

Expert Opin Ther Pat 2018 10 26:1-17. Epub 2018 Oct 26.

a School of Pharmacy , China Pharmaceutical University , Nanjing , China.

Introduction: Quorum sensing (QS) is a cell density-dependent phenomenon in which specific pathways are activated after autoinducers (AIs) outside the microorganism reach a threshold concentration. QS creates a positive feedback loop that induces a cascade of gene expression and causes biofilm formation, virulence and sporulation. QS signals are diverse, acyl-homoserine lactone (AHL), AI peptide (AIP) and AI-2 are three major categories of QS signals. Read More

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http://dx.doi.org/10.1080/13543776.2018.1541174DOI Listing
October 2018
19 Reads

Bicyclic bis-heteroaryl derivatives as inhibitors of the α-synuclein protein: a patent evaluation of WO2018138088A1.

Authors:
Jacques Joubert

Expert Opin Ther Pat 2018 Oct 25:1-7. Epub 2018 Oct 25.

a Pharmaceutical Chemistry, School of Pharmacy , University of the Western Cape , Bellville , South Africa.

Introduction: Neurodegenerative diseases commonly present misfolding and aggregation of one or more proteins, including α-synuclein, β-amyloid, and tau. Several research efforts have been made to develop therapeutic agents able to reduce the neurotoxic effects of aggregated proteins. Among these, inhibition of α-synuclein by small molecules has been considered as a promising approach. Read More

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https://www.tandfonline.com/doi/full/10.1080/13543776.2018.1
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http://dx.doi.org/10.1080/13543776.2018.1541234DOI Listing
October 2018
6 Reads

Synthetic Toll-like receptor agonists for the development of powerful malaria vaccines: a patent review.

Expert Opin Ther Pat 2018 11;28(11):837-847

a Department of Chemistry & Centre for Advanced Studies in Chemistry , Panjab University , Chandigarh , India.

Introduction: Currently, there is no efficient vaccine available against clinical malaria. However, continuous efforts have been committed to develop powerful antimalarial vaccine by discovery of novel antigens with in-depth understanding of its nature, immunogenicity, and presentation (delivery adjuvants). Moreover, another important part of vaccine development includes discovery of better immunostimulatory formulation components (immunostimulants). Read More

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https://www.tandfonline.com/doi/full/10.1080/13543776.2018.1
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http://dx.doi.org/10.1080/13543776.2018.1530217DOI Listing
November 2018
17 Reads

Chymase inhibitors for the treatment of cardiac diseases: a patent review (2010-2018).

Expert Opin Ther Pat 2018 11 10;28(11):755-764. Epub 2018 Oct 10.

a Department of Surgery , Wake Forest School of Medicine , Winston Salem , NC , USA.

Introduction: Chymase is primarily found in mast cells (MCs), fibroblasts, and vascular endothelial cells. MC chymase is released into the extracellular interstitium in response to inflammatory signals, tissue injury, and cellular stress. Among many functions, chymase is a major extravascular source for angiotensin II (Ang II) generation. Read More

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http://dx.doi.org/10.1080/13543776.2018.1531848DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6240413PMC
November 2018
18 Reads

Glutaminase inhibitors: a patent review.

Expert Opin Ther Pat 2018 11 11;28(11):823-835. Epub 2018 Oct 11.

a Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College , Huazhong University of Science and Technology , Wuhan , China.

Introduction: The kidney-type glutaminase (GLS) controlling the first step of glutamine metabolism is overexpressed in many cancer cells. Targeting inhibition of GLS shows obvious inhibitory effects on cancer cell proliferation. Therefore, extensive research and development of GLS inhibitors have been carried out in industrial and academic institutions over the past decade to address this unmet medical need. Read More

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https://www.tandfonline.com/doi/full/10.1080/13543776.2018.1
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http://dx.doi.org/10.1080/13543776.2018.1530759DOI Listing
November 2018
19 Reads

FXR modulators for enterohepatic and metabolic diseases.

Expert Opin Ther Pat 2018 11 8;28(11):765-782. Epub 2018 Oct 8.

a State Key Laboratory of Natural Medicines, Key Laboratory of Drug Metabolism and Pharmacokinetics , China Pharmaceutical University , Nanjing , China.

Introduction: Farnesoid X receptor (FXR), a nuclear receptor mainly expressed in enterohepatic tissues, is a master for bile acid, lipid and glucose homeostasis. Additionally, it acts as a cell protector with unclear mechanism but may be implicated in combating against inflammation, fibrosis and cancers. FXR is thus accepted as a promising target particularly for the enterohepatic diseases, and numerous FXR modulators have been patented and developed. Read More

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http://dx.doi.org/10.1080/13543776.2018.1527906DOI Listing
November 2018
42 Reads

Novel platinum agents and mesenchymal stromal cells for thoracic malignancies: state of the art and future perspectives.

Expert Opin Ther Pat 2018 11 26;28(11):813-821. Epub 2018 Sep 26.

a Department of Thoracic Surgery , European Institute of Oncology , Milan , Italy.

Introduction: Non-small cell lung cancer and malignant pleural mesothelioma represent two of the most intriguing and scrutinized thoracic malignancies, presenting interesting perspectives of experimental development and clinical applications.

Areas Covered: In advanced non-small cell lung cancer, molecular targeted therapy is the standard first-line treatment for patients with identified driver mutations; on the other hand, chemotherapy is the standard treatment for patients without EGFR mutations or ALK rearrangement or those with unknown mutation status. Once considered an ineffective therapy in pulmonary neoplasms, immunotherapy has been now established as one of the most promising therapeutic options. Read More

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http://dx.doi.org/10.1080/13543776.2018.1528234DOI Listing
November 2018
5 Reads

Therapeutic potential of oxazole scaffold: a patent review (2006-2017).

Expert Opin Ther Pat 2018 11 26;28(11):783-812. Epub 2018 Sep 26.

a University Institute of Pharmaceutical Sciences, Panjab University , Chandigarh , India.

Introduction: Oxazoles are oxygen and nitrogen containing five membered heterocyclic ring systems that are present in various anticancer, antimicrobial, antihyperglycemic, anti-inflammatory agents etc. of natural origin. These pharmacologically active oxazole derivatives have attracted numerous researchers to explore this scaffold for the design and development of newer potential therapeutic agents. Read More

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https://www.tandfonline.com/doi/full/10.1080/13543776.2018.1
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http://dx.doi.org/10.1080/13543776.2018.1526280DOI Listing
November 2018
14 Reads
4.300 Impact Factor

Carbonic anhydrase inhibitors and their potential in a range of therapeutic areas.

Expert Opin Ther Pat 2018 Oct 19;28(10):709-712. Epub 2018 Sep 19.

a NEUROFARBA Department, Sezione di Scienze Farmaceutiche e Nutraceutiche, Sezione di Scienze Farmaceutiche e Nutraceutiche , Università degli Studi di Firenze , Sesto Fiorentino (Firenze) , Italy.

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http://dx.doi.org/10.1080/13543776.2018.1523897DOI Listing
October 2018
1 Read

The sigma-2 (σ-2) receptor: a review of recent patent applications: 2013-2018.

Expert Opin Ther Pat 2018 09 27;28(9):655-663. Epub 2018 Sep 27.

a Moulder Center for Drug Discovery Research , Temple University School of Pharmacy , Philadelphia , PA , USA.

Introduction: The discovery of the sigma-2 receptor and the analogous sigma-1 receptor led to a decade-long quest to determine the true nature of this protein and novel ligands capable of modulating its activity. Despite this challenge, the sigma-2 receptor has been linked to several disease states, and multiple classes of sigma-2 ligands have been published in the 40+ years since its initial discovery.

Areas Covered: This review covers newly published patent applications that describe sigma-2 receptor ligands capable of modulating disease states. Read More

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http://dx.doi.org/10.1080/13543776.2018.1519024DOI Listing
September 2018
16 Reads

Applications of carbonic anhydrases inhibitors in renal and central nervous system diseases.

Expert Opin Ther Pat 2018 10 10;28(10):713-721. Epub 2018 Sep 10.

a NEUROFARBA Department, Sezione di Scienze Farmaceutiche e Nutraceutiche , Università degli Studi di Firenze , Sesto Fiorentino (Firenze) , Italy.

Introduction: There are tissues and organs, among which kidneys and the central nervous system (CNS), rich in various isoforms of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1. Read More

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http://dx.doi.org/10.1080/13543776.2018.1519023DOI Listing
October 2018
3 Reads

Technological development of microemulsions with perspectives for pain treatment: a patent review.

Expert Opin Ther Pat 2018 09 14;28(9):691-702. Epub 2018 Sep 14.

a Medicinal Plants Research nucleus, Center of Health Sciences , Federal University of Piauí , Teresina , Brazil.

Introduction: Microemulsions are thermodynamically stable translucent systems widely used for systemic delivery of drugs. The present study is the first to analyze the biotechnological potential of microemulsion systems for therapeutic purposes, through transdermal route, for pain treatment.

Areas Covered: Patents were searched in the World Intellectual Property Organization (WIPO), European Patent Office (Espacenet), United States Patent and Trademark Office (USPTO) and National Institute of Intellectual Property (INPI). Read More

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https://www.tandfonline.com/doi/full/10.1080/13543776.2018.1
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http://dx.doi.org/10.1080/13543776.2018.1519025DOI Listing
September 2018
30 Reads

Site-specific delivery of polymeric encapsulated microorganisms: a patent evaluation of US20170165201A1.

Expert Opin Ther Pat 2018 Sep 6;28(9):703-708. Epub 2018 Sep 6.

b Wits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, Faculty of Health Sciences, School of Therapeutics Sciences , University of the Witwatersrand , Johannesburg , South Africa.

Introduction: Probiotics inculde live microorganisms therapeutically effective in the treatment of wide range of diseases. Probiotics possibly stimulates the growth of preferred microorganisms, crowds out potentially harmful microorganisms, and reinforces the body's natural defense mechanisms. Microencapsulation of probiotic microorganisms protects them from the destructive environment and prolongs their survival. Read More

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https://www.tandfonline.com/doi/full/10.1080/13543776.2018.1
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http://dx.doi.org/10.1080/13543776.2018.1516752DOI Listing
September 2018
26 Reads
4.297 Impact Factor

5-HT1A receptor ligands and their therapeutic applications: review of new patents.

Expert Opin Ther Pat 2018 09 7;28(9):679-689. Epub 2018 Sep 7.

a Institute of Pharmacology, Polish Academy of Sciences , Kraków , Poland.

Introduction: 5-HTR was one of the first discovered serotonin receptors and is one of the most thoroughly studied. Dysfunctions associated with 5-HTR neurotransmission are linked to several psychiatric disorders, including anxiety, depression, and movement disorders.

Areas Covered: The current review covers patent literature published between January 2012 and May 2018. Read More

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https://www.tandfonline.com/doi/full/10.1080/13543776.2018.1
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http://dx.doi.org/10.1080/13543776.2018.1514011DOI Listing
September 2018
12 Reads

A patent review on PD-1/PD-L1 antagonists: small molecules, peptides, and macrocycles (2015-2018).

Expert Opin Ther Pat 2018 09 10;28(9):665-678. Epub 2018 Sep 10.

a Department of Drug Design , University of Groningen , Groningen , The Netherlands.

Introduction: The protein-protein interaction PD1/PD-L1 is an important immune checkpoint and several recently approved monoclonal antibodies show promising anti cancer activities in the clinical practice. However, only a small percentage of cancer patients benefit from PD1/PD-L1 directed mAbs. Moreover, some patients experience immune related side effects upon treatment with these mAbs. Read More

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http://dx.doi.org/10.1080/13543776.2018.1512706DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6323140PMC
September 2018
32 Reads

Arginine-lowering enzymes against cancer: a technocommercial analysis through patent landscape.

Expert Opin Ther Pat 2018 08;28(8):603-614

b Enzyme Biotechnology Laboratory, Department of Microbiology , Maharshi Dayanand University , Rohtak , Haryana , India.

Introduction: Rise in incidence of various cancers and growing adoption of biological therapy to avoid side effects of conventional cancer therapies is driving the growth of the cancer biotherapy market globally. One such therapy available for the treatment of certain tumors employs arginine-lowering enzymes (ALEs). Several patents have been filed in this technology domain, and many Phase I/II clinical trials of the ALEs especially arginine deiminase (ADI) are underway. Read More

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http://dx.doi.org/10.1080/13543776.2018.1508452DOI Listing
August 2018
11 Reads

Innovative strategies in the diagnosis and treatment of tuberculosis: a patent review (2014-2017).

Expert Opin Ther Pat 2018 08 13;28(8):615-623. Epub 2018 Aug 13.

a School of Pharmacy & Technology Management , SVKM's NMIMS , Shirpur , India.

Introduction: Tuberculosis (TB) is a disease caused due to an infection of Mycobacterium tuberculosis (M TB) bacilli affecting millions of people worldwide. It is the ninth leading cause of death and ranks above the HIV/AIDS. The unique intracellular life cycle, more dangerous drug-resistant forms of bacilli, and insufficient investments in the TB research and development hindered the occurrence of optimum diagnostic, preventive, and treatment strategy against this disease. Read More

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http://dx.doi.org/10.1080/13543776.2018.1508454DOI Listing
August 2018
7 Reads

Future perspectives for cryptococcosis treatment.

Expert Opin Ther Pat 2018 08 7;28(8):625-634. Epub 2018 Aug 7.

a Instituto Nacional de Ciência e Tecnologia de Inovação em Doenças Negligenciadas (INCT-IDN), Centro de Desenvolvimento Tecnológico em Saúde (CDTS) , Fundação Oswaldo Cruz (Fiocruz) , Rio de Janeiro/RJ , Brazil.

Introduction: Cryptococcosis is one of the most devastating human fungal infections. Despite its impact, none of the standard antifungals were developed after 1990. New, improved, less toxic, affordable and widely available treatment is, therefore, imperative. Read More

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http://dx.doi.org/10.1080/13543776.2018.1503252DOI Listing
August 2018
2 Reads

Carbonic anhydrase inhibitors as antitumor/antimetastatic agents: a patent review (2008-2018).

Expert Opin Ther Pat 2018 10 9;28(10):729-740. Epub 2018 Aug 9.

a Department of NEUROFARBA, Section of Pharmaceutical and Nutraceutical Sciences , University of Florence , Sesto Fiorentino (Firenze) , Italy.

Introduction: Human carbonic anhydrases (CA, EC 4.2.1. Read More

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http://dx.doi.org/10.1080/13543776.2018.1508453DOI Listing
October 2018
15 Reads

Evaluation of WO2017018805: 1,3,4-oxadiazole sulfamide derivatives as selective HDAC6 inhibitors.

Expert Opin Ther Pat 2018 Aug 7;28(8):647-651. Epub 2018 Aug 7.

a Institute of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences , Shandong University , Jinan , PR China.

Introduction: There are great potential in the development of selective HDAC6 inhibitors for the treatment of infectious diseases, neoplasms, endocrine diseases, and other diseases associated with HDAC6 activity. Areas covered: The application claims 1,3,4-oxadiazole sulfamide derivatives as selective HDAC6 inhibitors for the treatment of infectious diseases, neoplasms, endocrine, nutritional, and metabolic diseases; mental and behavioral disorders; neurological diseases; diseases of the eye and adnexa; cardiovascular diseases; respiratory diseases; digestive diseases; diseases of the skin and subcutaneous tissue; disease of the musculoskeletal system and connective tissue; or congenital malformations, deformations and chromosomal abnormalities. Many of the exemplified compounds showed nanomole potency against HDAC6 and were more than 5000-fold selectivity for HDAC6 over HDAC1. Read More

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http://dx.doi.org/10.1080/13543776.2018.1508451DOI Listing
August 2018
28 Reads

Circulating miRNAs as biomarkers for early diagnosis of coronary artery disease.

Expert Opin Ther Pat 2018 08 31;28(8):591-601. Epub 2018 Jul 31.

a Institute for Translational Medicine, Qingdao University , Qingdao , China.

Introduction: Coronary artery disease (CAD) contributes to a huge number of human death worldwide. The early diagnosis can arrest the development of CAD and effectively lower the mortality rate. Recently, circulating miRNAs emerged as CAD biomarkers. Read More

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http://dx.doi.org/10.1080/13543776.2018.1503650DOI Listing
August 2018
38 Reads
4.300 Impact Factor