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Expert Opinion on Therapeutic Patents

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https://www.readbyqxmd.com/read/29053063/a-patent-review-of-monoacylglycerol-lipase-magl-inhibitors-2013-2017
#1
Carlotta Granchi, Isabella Caligiuri, Filippo Minutolo, Flavio Rizzolio, Tiziano Tuccinardi
Monoacylglycerol lipase is a serine hydrolase that plays a major role in the degradation of the endocannabinoid 2-arachidonoylglycerol. Because of this key role, selective inactivation of MAGL represents an interesting approach to obtain desirable effects in several diseases. Furthermore, MAGL is upregulated in cancer cells and primary tumors and its inhibition in aggressive breast, ovarian, and melanoma cancer cells impairs cell migration, invasiveness, and tumorigenicity. Areas covered: This review covers patent literature on MAGL inhibitors and their applications published from 2013 to 2017...
October 20, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28994619/biological-evaluation-of-benzosuberones
#2
Haider Behbehani, Kamal M Dawood, Thoraya A Farghaly
Several natural products containing benzosuberone moiety are clinically reported as anti-tumor agents. Furthermore, several synthetic benzosuberones cited in this review exhibited wide range of theraputic activities such as bacteriostatic, anti-inflammatory, antidepressants and anti-tumor activities. Our recent review provides an overview of the different methods to synthesize the benzosuberones and their extensive biological activities. Areas covered: Thirty-two patents among 130 references are cited in this review that covered the recent inhibitory activities of the benzosuberone scaffolds and their broad area of biological applications up to the first quarter of 2017...
October 10, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28994333/pyruvate-kinase-activators-as-a-therapy-target-a-patent-review-2011-2017
#3
Sevki Adem, Veysel Comakli, Naim Uzun
It is well known that cancer cells have an altered metabolism both to meet the energy needs and to provide initial molecules for the synthesis of macromolecules. To cope with the new metabolic state, different forms of certain enzymes are expressed in extreme amounts. These enzymes are seen as very attractive targets to deal with cancer. Pyruvate kinases isoenzyme M2 (PKM2) is a key enzyme that determines whether glucose is used for energy or synthesis of biosynthetic molecules. The dimeric form of PKM2 main form in several cancer cells serves the formation of synthetic precursors required for the cell growth and proliferation from glycolytic intermediates...
October 10, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28974123/bill-c-30-who-wins-and-who-loses-in-canada-s-pharmaceutical-patent-battles
#4
Aidan Hollis
No abstract text is available yet for this article.
October 3, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28965471/cyclodextrins-improving-the-physicochemical-and-pharmacological-properties-of-antidepressant-drugs-a-patent-review
#5
Tâmara Coimbra Diniz, Tiago Coimbra Costa Pinto, Paula Dos Passos Menezes, Juliane Cabral Silva, Roxana Braga de Andrade Teles, Rosana Christine Cavalcanti Ximenes, Adriana Gibara Guimarães, Mairim Russo Serafini, Adriano Antunes de Souza Araújo, Lucindo José Quintans Júnior, Jackson Roberto Guedes da Silva Almeida
Depression is a serious mood disorder and is one of the most common mental illnesses. Despite the availability of several classes of antidepressants, a substantial percentage of patients are unresponsive to these drugs, which have a slow onset of action in addition to producing undesirable side effects. Some scientific evidence suggests that cyclodextrins (CDs) can improve the physicochemical and pharmacological profile of antidepressant drugs (ADDs). The purpose of this paper is to disclose current data technology prospects involving antidepressant drugs and cyclodextrins...
October 2, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28929814/what-s-new-in-the-diagnosis-of-pancreatic-cancer-a-patent-review-2011-present
#6
Houria Boulaiz, María C Ramos, Carmen Griñán-Lisón, Maria E García-Rubiño, Francisca Vicente, Juan Antonio Marchal
Pancreatic cancer (PC) is the fourth leading cause of cancer-related death in the US with a 5-year survival rate of about 5%. Most patients have advanced metastatic disease mainly due to the lack of an effective early detection, and an extremely poor prognosis. Advancing in the fight against PC requires developing novel observable biomarkers at preclinical stages for early detection. Areas covered: This manuscript is an overview of different PC diagnostic modalities and the latest innovations made to enhance early PC detection through the patents published from 2011 to 2017...
September 20, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28906174/a-patent-review-of-oxytocin-receptor-antagonists-2013-2017
#7
Timothy Katte, Michael Kassiou
No abstract text is available yet for this article.
September 14, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28885861/deuterated-drugs-updates-and-obviousness-analysis
#8
Graham S Timmins
The pharmacokinetics and/or toxicity of many known drugs can be modified by selective deuteration, an area of significant commercial interest and scientific and regulatory progress. Areas covered: This review firstly discusses recent developments in deuterated drugs including the FDA approval of deutetrabenazine. Secondly, it discusses 35 U.S.C. §103 'obviousness' as it relates to recent patent prosecution, and also to Inter Partes Review (IPR). IPR is a new post-award review of patentability under §102 or §103, two IPR petitions upon deuterated drugs have been instituted and included §103 arguments...
September 14, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28895472/aldo-keto-reductase-akr-1c3-inhibitors-a-patent-review
#9
Trevor M Penning
AKR1C3 is a drug target in hormonal and hormonal independent malignancies and acts as a major peripheral 17β -hydroxysteroid dehydrogenase to yield the potent androgens testosterone and dihydrotestosterone, and as a prostaglandin (PG) F synthase to produce proliferative ligands for the PG FP receptor. AKR1C3 inhibitors may have distinct advantages over existing therapeutics for the treatment of castration resistant prostate cancer, breast cancer and acute myeloid leukemia. Area Covered: This article reviews the patent literature on AKR1C3 inhibitors using SciFinder which identified inhibitors in the following chemical classes: N-phenylsulfonyl-indoles, N-(benzimidazoylylcarbonyl)- N-(indoylylcarbonyl)- and N-(pyridinepyrrolyl)- piperidines, N-benzimidazoles and N-benzindoles, repurposed nonsteroidal antiinflammatory drugs (indole acetic acids, N-phenylanthranilates and aryl propionic acids), isoquinolines, and nitrogen and sulfur substituted estrenes...
September 12, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28891360/global-patent-landscape-of-programmed-cell-death-1-implications-of-the-rapid-expansion
#10
Xiangjun Kong, Qianru Zhang, Yunfeng Lai, Hao Hu, Xin Chen, Yuanjia Hu
Inhibitors of programmed cell death 1 (PD-1) and its ligands are producing a paradigm shift in cancer treatment. The promising clinical outcomes and a multi-billion dollar market have prompted active research and development and resulted in relentless patent protection. However, the global patent landscape in this field remains unclear. Areas covered: The patent landscape encompassing global patenting activities and developing trends in the field is discussed based on a data set of 1287 patent families. Patenting activities have expanded rapidly in the past three years...
September 11, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28885866/caspase-inhibitors-a-review-of-recently-patented-compounds-2013-2015
#11
Hyemin Lee, Eun Ah Shin, Jae Hee Lee, Deoksoo Ahn, Chang Geun Kim, Ju-Ha Kim, Sung-Hoon Kim
Although many caspase inhibitors have been patented, caspase inhibitors have not entered the market due to their toxicity and poor pharmacokinetic profile. Areas covered: In this article, we review patents (2013-2015) for peptide and non-peptide caspase inhibitors and their compositions. Expert opinion: Noteworthy patents include a peptidic caspase-2 inhibitor for nasal administration and a peptidomimetic caspase-6 inhibitor that can be administered via several routes for the treatment of neurodegenerative diseases...
September 8, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28870136/ectonucleotidase-inhibitors-a-patent-review-2011-2016
#12
Mariya Al-Rashida, Syeda Uroos Qazi, Nayab Batool, Abdul Hameed, Jamshed Iqbal
Ectonucleotidases are a broad family of metallo-ectoenzymes that are responsible for hydrolysing a variety of nucleotides to nucleosides, hence orchestrating the activation of P1 and P2 cell receptors via controlled release of nucleotides and nucleosides. Many disorders such as impaired calcification including aortic calcification, neurological and immunological disorders, platelet aggregation, cell proliferation and metastasis. are characterized by an increase in expression of these ectonucleotidases. Consequently, selective inhibitors of ectonucleotidases are required for therapeutic intervention...
September 5, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28766366/dual-specificity-tyrosine-phosphorylation-regulated-kinase-1a-dyrk1a-inhibitors-a-survey-of-recent-patent-literature
#13
REVIEW
Thu Lan Nguyen, Corinne Fruit, Yann Hérault, Laurent Meijer, Thierry Besson
Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is a eukaryotic serine-threonine protein kinase belonging to the CMGC group. DYRK1A hyperactivity appears to contribute to the development of a number of human malignancies and to cognitive deficits observed in Down syndrome and Alzheimer's disease. As a result, the DYRK1A kinase represents an attractive target for the synthesis and optimization of pharmacological inhibitors of potential therapeutic interest. Like most tyrosine kinase inhibitors developed up to the market, DYRK1A inhibitors are essentially acting by competing with ATP for binding at the catalytic site of the kinase...
November 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28756713/coumarin-derivatives-an-updated-patent-review-2015-2016
#14
REVIEW
Anastasia Detsi, Christos Kontogiorgis, Dimitra Hadjipavlou-Litina
INTRODUCTION: Coumarins belong to the benzopyrone family. They are naturally plant-derived or synthetically obtained substances, presenting a wide variety of biological activities, offering an extented therapeutic profile. Their structural characteristics correlated to physicochemical properties define their pleiotropic biological responses. AREAS COVERED IN THIS REVIEW: Recent patent publications (2015-2016), describing coumarins and their derivatives are analyzed...
November 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28753410/pyrimido-4-5-b-indole-derivatives-and-use-thereof-in-the-expansion-of-hematopoietic-stem-cells-us2015011543-a1-a-patent-evaluation
#15
Stuti Agarwal, Hitesh Agarwal, Nilesh Zaware
There is an unmet need of strategies for ex-vivo expansion of hematopoetic stem cells (HSCs) without loss of their primitive nature or stemness. We evaluate here a patent that attempts to address this need via key small molecules 1 and 40 that possess a pyrimido[4,5-b]indole core. Areas covered: (i) Discussion on literature reports of diverse strategies for ex-vivo expansion of stem cells. (ii) Synthetic scheme to 1, and general synthetic schemes for compounds 1-55 reported in the patent application. (iii) Analysis of the in vitro biological data for 1 and 40...
November 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28749251/identification-of-spirocyclic-or-phosphate-substituted-quinolizine-derivatives-as-novel-hiv-1-integrase-inhibitors-a-patent-evaluation-of-wo2016094197a1-wo2016094198a1-and-wo2016154527a1
#16
REVIEW
Xiqiang Cheng, Ping Gao, Lin Sun, Ye Tian, Peng Zhan, Xinyong Liu
Highly active antiretroviral therapy (HAART) has been widely adopted to control the HIV-1 infection successfully. HIV-1 integrase (IN) inhibitors are primary drugs in HAART regimens targeting integration step in the HIV-1 life cycle. However, due to the emergence of viral resistance and cross-resistance amongst drugs, there is a pressing need for new and potent IN inhibitors. This review covers the three patents describing spirocyclic and phosphate substituted quinolizine derivatives as novel HIV-1 IN inhibitors for the discovery of new anti-HIV-1 drug candidates...
November 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28742403/lpxc-inhibitors-a-patent-review-2010-2016
#17
REVIEW
Dmitrii V Kalinin, Ralph Holl
The Zn(2+)-dependent deacetylase LpxC is an essential enzyme of lipid A biosynthesis in Gram-negative bacteria and a promising target for the development of antibiotics selectively combating Gram-negative pathogens. Researchers from industry and academia have synthesized structurally diverse LpxC inhibitors, exhibiting different LpxC inhibitory and antibacterial activities. Areas covered: A brief introduction into the structure and function of LpxC, showing its suitability as antibacterial target, along with the structures of several reported LpxC inhibitors, is given...
November 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28665163/what-s-new-in-treatment-of-pancreatic-cancer-a-patent-review-2010-2017
#18
REVIEW
Maria C Ramos, Houria Boulaiz, Carmen Griñan-Lison, Juan Antonio Marchal, Francisca Vicente
Pancreatic cancer (PC) is one of the most lethal cancers, with a median overall survival of less than 1 year and a 5-year survival of ~5%. The poor survival rate is likely due to lack of early diagnosis, fast disease course, high metastasis rate and disappointing treatment outcome. Therefore, at this stage, any new method that provides a treatment against PC without the undesirable side effects of chemotherapy and radiation is urgently needed. Areas covered: This review summarizes the latest advances in the treatment of PC through the patents published from 2010 to 2017...
November 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28621561/a-patent-review-of-two-fruitful-decades-1997-2016-of-isocoumarin-research
#19
REVIEW
Hidayat Hussain, Ivan R Green
Isocoumarins comprise a six-membered oxygen heterocycle (α-pyranone) along with one aromatic ring and are known to possess interesting biological properties. During the last two decade (1997-2016), isocoumarin chemistry has attracted attention due to its biological and pharmaceutical effects viz., anticancer, anti-diabetic, antibacterial, antimalarial, and fungicidal effects. Areas covered: This review covers the patents on the therapeutic activities of natural and synthetic isocoumarins over the last two decades (1997-2016)...
November 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28699813/prolylcarboxypeptidase-prcp-inhibitors-and-the-therapeutic-uses-thereof-a-patent-review
#20
REVIEW
Thomas H Graham
Prolylcarboxypeptidase (PrCP) is a serine protease that produces or degrades signaling proteins in several important pathways including the renin-angiotensin system (RAS), kallikrein-kinin system (KKS) and pro-opiomelanocortin (POMC) system. PrCP has the potential to be a therapeutic target for cardiovascular, inflammatory and metabolic diseases. Numerous classes of PrCP inhibitors have been developed by rational drug design and from high-throughput screening hits. These inhibitors have been tested in mouse models to assess their potential as new therapeutics...
October 2017: Expert Opinion on Therapeutic Patents
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