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Expert Opinion on Therapeutic Patents

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https://www.readbyqxmd.com/read/28076686/small-molecule-hiv-1-entry-inhibitors-targeting-gp120-and-gp41-a-patent-review-2010-2015
#1
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...
January 19, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28067079/mglu5-negative-allosteric-modulators-a-patent-review-2013-2016
#2
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...
January 19, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28092474/novel-histone-deacetylase-6-hdac6-selective-inhibitors-a-patent-evaluation-wo2014181137
#3
Claudia A Simões-Pires, Philippe Bertrand, Muriel Cuendet
The invention described in this patent (WO2014181137) is related to hydroxamic acid derivatives with inhibitory activity towards histone deacetylases (HDACs), their synthetic process and pharmaceutical formulations, as well as a method for treating patients suffering from a list of selected tumoral, inflammatory, cardiac and chronic disorders. HDACs are known to deacetylate histones and other proteins, which makes HDAC inhibitors able to affect cell survival, cell signaling, transport, and gene expression. Those effects have been associated to the therapeutic success of HDAC inhibitors...
January 16, 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
#4
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...
January 11, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28064544/recent-advances-of-pyrrolopyridines-derivatives-a-patent-and-literature-review
#5
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...
January 9, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28058852/corrigendum
#6
(no author information available yet)
No abstract text is available yet for this article.
January 6, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28056571/compounds-compositions-and-methods-of-agelastatin-alkaloids-patent-evaluation-of-wo2015042239-a1
#7
Takehiko Yoshimitsu, Han W Tun
Agelastatins are a family of tetracyclic alkaloids isolated from marine sponges. The patent examined in this publication covers the chemical synthesis of agelastatins A to F and eight analogues and their therapeutic use against hematologic malignancies. The claim on the chemical synthesis features a novel biomimetic cyclization of a tricyclic precursor, which streamlines scalable access to agelastatins and their analogues. This new synthetic approach can potentially expedite the research on these compounds for therapeutic use against cancers by making them more easily available...
January 5, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28051882/are-sigma-modulators-an-effective-opportunity-for-cancer-treatment-a-patent-overview-1996-2016
#8
Simona Collina, Emanuele Bignardi, Marta Rui, Daniela Rossi, Raffaella Gaggeri, Alice Zamagni, Michela Cortesi, Anna Tesei
Although several molecular targets against cancer have been identified, there is a continuous need for new therapeutic strategies. Sigma Receptors (SRs) overexpression has been recently associated to different cancer conditions. Therefore, novel anticancer agents targeting SRs may increase the specificity of therapies, overcoming some of the common drawbacks of conventional chemotherapy. Areas covered: The present review focuses on patent documents disclosing SR modulators with possible application in cancer therapy and diagnosis...
January 4, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27976971/thiadiazole-inhibitors-a-patent-review
#9
Kamal M Dawood, Thoraya A Farghaly
Four isomeric structures of thiadiazole motifs have outstanding pharmacological inhibitory applications are reported in this review. Thiadiazole nucleus is present in several biologically active natural products and commercial drugs. Most of thiadiazoles reported herein are emphasized to have broad spectrum of medicinal activities. Areas covered: This review represents the recent inhibitory activities of thiadiazole isomeric scaffolds and their broad-spectrum biological applications published as full texts during 2010-2016 as well as the patents published during 2005-2016...
January 4, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28048944/rho-kinase-inhibitors-a-patent-review-2014-2016
#10
Olivier Defert, Sandro Boland
The Rho-kinases (ROCK), ROCK1 and ROCK2, are potent, widespread biochemical modulators which have been extensively studied. Due to the involvement of ROCKs in multiple biological processes, ROCK inhibitors have pleiotropic actions and may be of relevance for a number of therapeutic applications. The drawback is however that their use might be limited by occurrence of side effects. Areas covered: Since the publication of the latest review in 2014, there have been significant advances in the field of ROCK inhibitors...
January 3, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28033734/selective-histone-deacetylase-small-molecule-inhibitors-recent-progress-and-perspectives
#11
Hai-Tao Qin, Huan-Qiu Li, Feng Liu
Since the first pan-HDAC inhibitor SAHA was approved by U.S. FDA 10 years ago, HDACs including SIRT1-7 have received significant attention due to the fact that aberrant histone deacetylase activtiy has been implicated in a variety of human diseases, such as cancers, virus infection, and neurodegenerative diseases. During the past years, a considerable achievement of development of isoform- or class-selective HDAC inhibitors has been made, yielding many drug candidates for further clinical studies, which represents a state-of-the-art technology in the drug discovery arena...
December 29, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27998196/recent-trends-in-neuropathic-pain-patents
#12
Rodolfo do Couto Maia
Neuropathic pain (NP) is one of the most important health problems faced nowadays. NP is a chronic disease that cannot be treated like other pain conditions because it is developed from a nerve injury that evolves into a permanent dysfunction of the central and/or peripheral nervous system. Therefore, it involves the participation of several systems and should be viewed as a multi-factorial disease that needs a whole new pharmacological strategy in order to achieve the desired pain relief. Areas covered: The Espacenet site was used as the main source in order to perform the patent research for NP treatment...
December 28, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28024125/recent-progress-on-curcumin-based-therapeutics-a-patent-review-2012-2016-part-i-curcumin
#13
Rita Maria Concettaa Di Martino, Barbara Luppi, Alessandraa Bisi, Silviaa Gobbi, Angela Rampa, Angela Abruzzo, Federica Bellutia
curcumin is the main bioactive component contained in Curcuma Longa, largely employed in traditional medicine. Recently, beneficial properties, useful for prevention and treatment of several disorders, have been discovered for this compound. Peculiar structural feature is an α,β-unsaturated carbonyl system essential for establishing contacts with critical cysteine residues of several targets. This distinctive mechanism of action imparts to the molecule the ability to affect a large number of targets, accounting for its pleiotropic behaviour and definition of "privileged structure"...
December 26, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27977313/thioredoxin-reductase-inhibitors-a-patent-review
#14
Baoxin Zhang, Junmin Zhang, Shoujiao Peng, Ruijuan Liu, Xinming Li, Yanan Hou, Xiao Han, Jianguo Fang
Mammalian thioredoxin reductases (TrxRs) are selenocysteine-containing homodimeric flavin enzymes that catalyze the NADPH-dependent reduction of oxidized thioredoxins. Increasing evidence indicates that TrxRs are potential targets for anticancer drug development. This review summarizes patented inhibitors of mammalian TrxRs with an emphasis on those having potential applications in treatment of cancer. Areas covered: A background introduction of TrxR as well as the relevance of TrxR and cancer is provided in the first part of this review...
December 26, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27976968/a-fgfr1-inhibitor-patent-review-progress-since-2010
#15
Tao Yu, Yanyan Yang, Yan Liu, Yinfeng Zhang, Hong Xu, Mengpeng Li, Murugavel Ponnusamy, Kun Wang, Jian-Xun Wang, Pei-Feng Li
FGFR1 is a well known molecular target for anticancer therapy. Many studies have proved that the regulation of FGFR1 activity is a promising therapeutic approach to treat a series of cancers. Therefore, the development of potent inhibitors has consequently become a key focus in the present drug discovery, and it is encouraging that several highly selective FGFR1 inhibitors have been identified from various sources in recent years. Areas covered: This article reviews patents and patent applications related to selective FGFR1 inhibitors published from 2010 to 2016...
December 26, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27967250/bitopic-muscarinic-agonists-and-antagonists-and-uses-thereof-a-patent-evaluation-of-us20160136145a1
#16
Ulrike Holzgrabe, Michael Decker
Bitopic M ligands, that is, ligands that interact both with the ortho- and allosteric binding sites of the M receptor subtypes, hold great potential as novel selective for muscarinic acetylcholine (M) ligands for several therapeutic applications. Areas covered: The patent application describes a set of compounds based on the neurotransmitter acetylcholine applying the Schulman-model for M ligands comprising heterocyclic (often quaternary) amines and a benzene ring (often as benzoic acid esters) to act as bitopic ligands...
December 26, 2016: 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...
December 23, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27967266/therapeutic-applications-of-the-versatile-fatty-acid-mimetic-wy14643
#18
Julius Pollinger, Daniel Merk
WY14643 - also known as pirinixic acid - is a versatile fatty acid mimetic that was originally developed as lipid lowering agent without knowledge of its molecular target. Various later studies discovered somewhat promiscuous activity of the compound on several receptors and enzymes. Pirinixic acid though never having reached clinical use was subjected to many in vivo studies and exerted beneficial effects in a variety of disease models. Areas covered: Inventions claiming the use of WY14643 for numerous indications ranging from the originally intended application in metabolic dysbalances over cancer and inflammation to some rare syndromes have been evaluated...
December 23, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28005436/novel-leukotriene-biosynthesis-inhibitors-2012-2016-as-anti-inflammatory-agents
#19
Oliver Werz, Ulrike Garscha, Jana Gerstmeier
Leukotrienes (LTs) are lipid mediators produced from arachidonic acid with a broad variety of bioactivities in allergy and inflammation. The biosynthesis of LTs mainly involves 5-lipoxygenase (5-LO) and its 5-lipoxygenase-activating protein (FLAP), LTA4 hydrolase and LTC4 synthase that all may represent potential targets for LT biosynthesis inhibitors. Areas covered: We introduce the LT biosynthetic pathway and its cellular regulation, the diverse biological actions of LTs and their receptors, and we briefly describe the pharmacological strategies for suppression of LT formation as well as the classes of current LT biosynthesis inhibitors...
December 22, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27977303/tyrosyl-trna-synthetase-inhibitors-a-patent-review
#20
Juan Sun, Peng-Cheng Lv, Hai-Liang Zhu
Bacterial infection has been a consistent and relentless threat to human health because of emerging resistance to existing antibiotics. Therefore, much of the research has been focused on the design of new potent antibacterial agents. Tyrosyl-tRNA synthetase (TyrRS), as a member of aminoacyl-tRNA synthetase family, could recognize the information including the coincident tRNA molecules and the amino acids' structures, which are essential in translating the coded information into protein structures in nucleic acids...
December 15, 2016: Expert Opinion on Therapeutic Patents
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