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Expert Opinion on Therapeutic Patents

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https://www.readbyqxmd.com/read/29210300/fak-inhibitors-in-cancer-a-patent-review
#1
Peng-Cheng Lv, Ai-Qin Jiang, Wei-Ming Zhang, Hai-Liang Zhu
Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase that localizes at sites of cell adhesion to the extracellular matrix (ECM) and mediates signalling events downstream of integrin engagement of the ECM. FAK is known to regulate cell survival, proliferation and migration. Areas covered: FAK expression has also been shown to be up-regulated in many cancer types. Previous study also indicates that FAK-mediated signaling and functions are intrinsically involved in the progression of tumor aggressiveness, suggesting that FAK is a promising target for anticancer therapies...
December 6, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/29171765/serine-protease-inhibitors-to-treat-inflammation-a-patent-review-2011-2016
#2
Chahrazade El Amiri, Feryel Soualmia
Introduction Inflammation is a physiological part of the complex biological response of tissues to counteract various harmful signals. This process involves diverse actors such as immune cells, blood vessels, and nerves as sources of mediators for inflammation control. Among them serine proteases are key elements in both physiological and pathological inflammation. Areas covered Serine protease inhibitors to treat inflammatory diseases are being actively investigated by various industrial and academic institutions...
November 24, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/29168921/bauhinia-forficata-in-the-treatment-of-diabetes-mellitus-a-patent-review
#3
Bárbara Verônica Cardoso de Souza, Regilda Saraiva Dos Reis Moreira Araújo, Oskar Almeida Silva, Lucas Costa Faustino, Maria Fabrícia Beserra Gonçalves, Mirian Lima Dos Santos, Grasielly Rocha Souza, Lindalva Moura Rocha, Mônica Larissa Sousa Cardoso, Lívio César Cunha Nunes
Diabetes Mellitus has been considered an epidemic by the World Health Organization, with a high risk of morbidity and mortality. The treatment of this pathology consists in glycemic control, which can be done by oral hypoglycemic agents, insulin therapy, dietary guidance, regular physical activity, and psychosocial support. In addition, other adjuvant treatments are employed, such as phytotherapic, and one of the most used plants is Bauhinia forficata. Areas covered: in the current review, patents using Bauhinia forficata for the Diabetes Mellitus treatment have been analyzed...
November 23, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/29166791/evaluation-of-wo2017098421-gsk-s-benzothiazine-compounds-as-cd73-inhibitor-filings
#4
Ya-Ping Gong, Ren-Zhong Wan, Zhao-Peng Liu
There are considerable interests in the development of novel small-molecule CD73 inhibitors for the treatment of cancers, autoimmune diseases, precancerous syndromes, and other diseases associated with CD73 activity. Areas covered: The application claims novel substituted benzothiadiazine derivatives as CD73 inhibitors for the treatment of cancer, precancerous syndromes, AIDS, autoimmune diseases, infections, atherosclerosis, and ischemia-reperfusion injury. Many of the exemplified compounds have pIC50 values between 5 to 8...
November 22, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/29140125/diabetes-area-patent-participation-analysis-part-ii-years-2011-2016
#5
Markus Boehm, Matthew Crawford, Jamie E Moscovitz, Philip A Carpino
Diabetes is a metabolic disease characterized by elevated levels of plasma glucose. When untreated, diabetes increases the risk of developing co-morbidities such as cardiovascular disease. Several drugs, often used as part of combination therapies, have been approved to treat the disease, but these drugs will eventually fail to effectively control blood glucose levels, at which point insulin replacement therapy is required. A medical need exists for new anti-diabetic drugs that exhibit good efficacy with improved safety/toleration profiles and can be added on top of existing therapies, or that can provide additional benefits beyond glucose lowering such as pancreatic beta (β)-cell protection...
November 15, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/29130358/gelatinase-inhibitors-a-patent-review-2011-2017
#6
Xun Li
Gelatinase represents a promising biotarget in new drug development as it is closely related to various pathological events, including but not limited to neoplasm, aging, respiratory and neurological disorders. Gelatinase inhibitors are thereby designated as chemotherapeutics or as mechanistic probe to figure out the unrecognized functions of MMP members. Areas covered: The focus of this article is to highlight recently issued patents concerning the naturally available or synthetic gelatinase inhibitors (2011-2017), where the chemical structures, SAR investigation, biological application...
November 12, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/29053063/a-patent-review-of-monoacylglycerol-lipase-magl-inhibitors-2013-2017
#7
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
#8
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
#9
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
#10
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
#11
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/28895472/aldo-keto-reductase-akr-1c3-inhibitors-a-patent-review
#12
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 19, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28906174/a-patent-review-of-oxytocin-receptor-antagonists-2013-2017
#13
Timothy A Katte, Michael Kassiou
No abstract text is available yet for this article.
September 18, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28885861/deuterated-drugs-updates-and-obviousness-analysis
#14
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/29119843/statement-of-retraction
#15
(no author information available yet)
No abstract text is available yet for this article.
December 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
#16
REVIEW
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...
December 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
#17
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
#18
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
#19
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
#20
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
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