Novel Selective Histone Deacetylase 6 (HDAC6) Inhibitors: A Patent Review (2016-2019)

2020 ◽  
Vol 15 (1) ◽  
pp. 32-48 ◽  
Author(s):  
Xingrui He ◽  
Zhen Li ◽  
Xiao-Tao Zhuo ◽  
Zi Hui ◽  
Tian Xie ◽  
...  
Keyword(s):  
Side Effects ◽  
Hdac Inhibitors ◽  
The United States ◽  
World Intellectual Property Organization ◽  
Histone Deacetylase 6 ◽  
Future Design ◽  
Patent Review ◽  
Near Future ◽  
Chemistry Community ◽  
States Patent

Background: Many human diseases are associated with dysregulation of HDACs. HDAC6 exhibits deacetylase activity not only to histone protein but also to non-histone proteins such as α- tubulin, HSP90, cortactin, and peroxiredoxin. These unique functions of HDAC6 have gained significant attention in the medicinal chemistry community in recent years. Thus a great deal of effort has devoted to developing selective HDAC6 inhibitors for therapy with the hope to minimize the side effects caused by pan-HDAC inhibition. Objective: The review intends to analyze the structural feature of the scaffolds, to provide useful information for those who are interested in this field, as well as to spark the future design of the new inhibitors. Methods: The primary tool used for patent searching is SciFinder. All patents are retrieved from the following websites: the World Intellectual Property Organization (WIPO®), the United States Patent Trademark Office (USPTO®), Espacenet®, and Google Patents. The years of patents covered in this review are between 2016 and 2019. Results: Thirty-six patents from seventeen companies/academic institutes were classified into three categories based on the structure of ZBG: hydroxamic acid, 1,3,4-oxadiazole, and 1,2,4-oxadiazole. ZBG connects to the cap group through a linker. The cap group can tolerate different functional groups, including amide, urea, sulfonamide, sulfamide, etc. The cap group appears to modulate the selectivity of HDAC6 over other HDAC subtypes. Conclusion: Selectively targeting HDAC6 over other subtypes represents two fold advantages: it maximizes the pharmacological effects and minimizes the side effects seen in pan-HDAC inhibitors. Many small molecule selective HDAC6 inhibitors have advanced to clinical studies in recent years. We anticipate the approval of selective HDAC6 inhibitors as therapeutic agents in the near future.

scholarly journals Rethinking Patent Law's Presumption of Validity

2016 ◽  
Author(s):  
Mark Lemley
Keyword(s):  
The United States ◽  
Decision Makers ◽  
Patent Office ◽  
High Likelihood ◽  
Long Run ◽  
Patent Review ◽  
Tier System ◽  
Initial Process ◽  
Patent Validity ◽  
States Patent

The United States Patent and Trademark Office is tasked with the job ofreading patent applications and determining which ones qualify for patentprotection. It is a Herculean task, and the Patent Office pursues itsubject to enormous informational and budgetary constraints. Nonetheless,under current law, courts are bound to defer to the Patent Office'sdecisions regarding patent validity. In this Article, we argue for reform.Deference to previous decision-makers is appropriate in instances wherethose previous decisions have a high likelihood of accuracy, and the patentsystem should endeavor to create processes that fit this mold. But grantingsignificant deference to the initial process of patent review isindefensible and counter-productive. Patents should be vulnerable tochallenge until and unless they are significantly evaluated in aninformation-rich environment. At that point, they will have earned andtherefore should be accorded a presumption of validity. Such an approachwould better serve the patent's systems long-run incentive goals, and itwould give patent applicants better incentives to file for genuineinventions but leave their more obvious and incremental accomplishmentsoutside the patent system's purview. Here, we therefore suggest thecreation of a two-tier system of patent validity, with patents that aresubject to intensive scrutiny accorded a strong presumption of validity,while untested patents are left to be evaluated more fully in court.

scholarly journals Inventions and Innovations Related to Better Results in Intestinal Anastomosis: a Patent Review

10.3823/2635 ◽  
2021 ◽  
Vol 14 ◽  
Author(s):  
André Takashi Oti ◽  
Rubens Fernando Gonçalves Ribeiro Júnior ◽  
Thyago Cezar Prado Pessôa ◽  
Lainy Carollyne da Costa Cavalcante ◽  
Lucas Nascimento Galvão ◽  
...  
Keyword(s):  
Intestinal Anastomosis ◽  
The United States ◽  
Surgical Instruments ◽  
Patent Office ◽  
Surgical Anastomosis ◽  
Inclusion Criteria ◽  
New Techniques ◽  
Patent Review ◽  
Biological Glues ◽  
States Patent

Objective: To evaluate new techniques and improvements in surgical instruments related to intestinal anastomosis procedures. Methods: A search was conducted on the free database of patents from the National Institute of Industrial Patent Office (INPI) and The United States Patent and Trademark Office (USPTO). Were analyzed all occurrences between 2012 and 2016 related to experimental surgery and intestinal anastomosis. The requests for patents were examined individually and the data collected was the nationality of the applicant, if was physical (PP) or legal (LP) person and if was innovation or invention. At the end, a comparative analysis between the two institutions was performed. Results:  In INPI was found only 5 occurrences. All of them were deposited by legal entity and were inventions. In addition, only one was a national request. In USPTO database, 65 occurrences met the inclusion criteria. Of these, 48 were national applications and only 5 were filed by physical person. Conclusion: More requests were found in US database, predominating national trustee and greater solicitation to inventions than Brazilian database. The main applications for patents are invention of surgical instruments, the development of new biological glues and improvement of mechanical sutures.   Keywords: patents, gastroenterology, surgical anastomosis.

scholarly journals Matrix Microparticles Of Copaiba Oil (Copaifera Langsdorffii) On Renal Physiology: Patent Review

10.3823/2511 ◽  
2017 ◽  
Vol 10 ◽  
Author(s):  
Marcus Vinicius Henriques Brito ◽  
Edson Yuzur Yasojima ◽  
Rubens Fernando Gonçalves Ribeiro Júnior ◽  
Luis Cláudio Pinto ◽  
Mariela Carolina Dos Santos Carballo ◽  
...  
Keyword(s):  
Intellectual Property ◽  
The United States ◽  
World Intellectual Property Organization ◽  
Renal Physiology ◽  
Online Databases ◽  
Patent Review ◽  
Copaiba Oil ◽  
Copaifera Langsdorffii ◽  
Beneficial Action ◽  
Utility Models

PURPOSE: to demonstrate the effect of matrix microparticles of Copaifera langsdorffii (aerial parts of copaiba), aiming to evaluate the discussions and results of the works that demonstrate Its function on the kidneys as well as its effectiveness. METHODS: A bibliographic study was carried out by consulting public online databases of patents, such as the United States Patent and Trademark office, World Intellectual Property Organization and the National Intellectual Property Institute; The following keywords were used: copaiba oil, renal function, kidney, kidney stones, matrix microparticles Copaifera langsdorffii and lithiasis. In this study were included patents of invention, innovations and utility models in the period from January 2007 to May 2016. RESULTS: One patent register was included regarding a method for obtaining microparticles and compounds, having antilithiasic, analgesic, antispasmodic, anti-inflammatory, diuretic and antiseptic activity. CONCLUSION: The patent registry survey demonstrates the possibility of beneficial action of matrix microparticles Copaifera langsdorffii on renal physiology, acting as antilithiasis and even with diuretic properties, thus opening up new possibilities of research of this substance on renal physiology.

Medicinal Chemistry Insights into Novel HDAC Inhibitors: An Updated Patent Review (2012-2016)

2017 ◽  
Vol 12 (1) ◽  
pp. 16-34 ◽  
Author(s):  
Peng Zhan ◽  
Xueshun Wang ◽  
Xinyong Liu ◽  
Takayoshi Suzuki
Keyword(s):  
Medicinal Chemistry ◽  
Hdac Inhibitors ◽  
Patent Review

A Review of Recent Patents (2016-2019) on Plant Food Supplements with Potential Application in the Treatment of Neurodegenerative and Metabolic Disorders

2020 ◽  
Vol 11 (2) ◽  
pp. 145-153 ◽  
Author(s):  
Rosalba Leuci ◽  
Leonardo Brunetti ◽  
Antonio Laghezza ◽  
Paolo Tortorella ◽  
Fulvio Loiodice ◽  
...  
Keyword(s):  
Metabolic Disorders ◽  
Food Supplements ◽  
Plant Food ◽  
Fortified Foods ◽  
Patent Review ◽  
Novel Strategy ◽  
Lifestyle Related Diseases ◽  
Near Future ◽  
Prevention And Therapy

In the near future, it is expected that the prevalence of illnesses related to the increasing life expectancies and quality of life, such as neurodegenerative diseases and cardiovascular diseases related to metabolic disorders, will soar to unprecedented levels, leading to high socioeconomic costs. To address this rising threat, natural products are emerging as a novel strategy for the prevention and therapy of these ages- and lifestyle-related diseases, thanks to their high marketability and few side effects. In this patent review, we summarize selected patents for food supplements, functional and fortified foods, filed from 2016 to 2019, categorizing them based on the biological activity of their components.

scholarly journals ArcGIS Urban: an application for plan assessment

2021 ◽  
Vol 1 (1) ◽  
Author(s):  
Ellen Soward ◽  
Jianling Li
Keyword(s):  
United States ◽  
The United States ◽  
Spatial Context ◽  
Future Studies ◽  
Planning Profession ◽  
Gis Tools ◽  
Comprehensive Plans ◽  
Near Future ◽  
The City

AbstractMost cities in the United States rely on zoning to address important planning-related issues within their jurisdictions. Planners often use GIS tools to analyze these issues in a spatial context. ESRI’s ArcGIS Urban software seeks to provide the planning profession with a GIS-based solution for various challenges, including zoning’s impacts on the built environment and housing capacity.This research explores the use of ArcGIS Urban for assessing the existing zoning and comprehensive plans in meeting the projected residential growth in the near future using the City of Arlington, Texas as a case study. The exploration provides examples and lessons for how ArcGIS Urban might be used by planners to accomplish their tasks and highlights the capabilities and limitations of ArcGIS Urban in its current stand. The paper is concluded with some suggestions for future studies.

scholarly journals Response to treatment with intra-articular triamcinolone hexacetonide and triamcinolone acetonide in oligo articular juvenile idiopathic arthritis

2021 ◽  
Vol 19 (1) ◽  
Author(s):  
Rana Harhay ◽  
Wajiha Jeelani ◽  
Barbine Tchamba Agbor Agbor ◽  
Teresa Hennon ◽  
Brian H. Wrotniak ◽  
...  
Keyword(s):  
Juvenile Idiopathic Arthritis ◽  
Side Effects ◽  
Triamcinolone Acetonide ◽  
The United States ◽  
Response To Treatment ◽  
Joint Injection ◽  
Triamcinolone Hexacetonide ◽  
Active Arthritis ◽  
General Response

Abstract Background Oligo-articular juvenile idiopathic arthritis (Oligo JIA) is the most common subtype of juvenile idiopathic arthritis. Intra-articular corticosteroid (IAC) injection is a mainstay treatment of oligo JIA providing pain relief, improving mobility and preventing further joint destruction in the majority of patients. In 2015, production of triamcinolone hexacetonide (TH) an intra-articular corticosteroid was discontinued in the United States leading to use of triamcinolone acetonide (TA) as an alternative. In this study, we compared response to treatment in children with oligo JIA who underwent therapy with intra-articular TA and TH injection. Methods Our study is a retrospective chart review of children with oligo JIA who were treated with IAC injections with TH between January 2012 and June 2015 and TA between J uly 2015 and December 2018. The two groups were followed at John R. Oishei Children’s Hospital of Buffalo and were evaluated for response to treatment, side effects and predictors of response including duration of disease before treatment, erythrocyte sedimentation rate (ESR), and c-reactive protein (CRP). Response to treatment was defined as at least 6 months follow up without evidence of active arthritis in injected joints. Patients were considered to be non-responders if they continued to show active arthritis during their first follow up after joint injection. The primary objective was to evaluate whether there was a significant difference in rate of response between TH and TA. Results Forty-nine patients, 38 female and 11 male with oligo JIA were included in the study. The average age was 6.7 years. A total of 111 joints were injected includin g 78 knees, 13 ankles, 9 wrists, 4 hips, 4 elbows, 2 TMJ and one subtalar joint. In the TA group, 49% (29/59) did not show response to injection compared to 27% (14/52) in the TH group. After 6 months, response rates were better for individuals injected with TH compared to TA (73% vs. 51%). In general, response to intra-articular TH was superior to TA with P = .016 using chi-square test of independence. This difference in outcome was not influenced by other variables such as duration of illness before treatment (P value 0.784) or elevated ESR and CRP. No difference in side effects between the two groups were noted. Conclusion Our results in conjunction with prior published data suggests that TH intra-articular joint injection in oligo JIA is superior to TA, although future controlled trials are necessary for confirmation. An effective, long lasting treatment can have a great impact on the outcome of these children.

scholarly journals Decline in Marriage Associated with the COVID-19 Pandemic in the United States

2020 ◽  
Vol 6 ◽  
pp. 237802312098032
Author(s):  
Brandon G. Wagner ◽  
Kate H. Choi ◽  
Philip N. Cohen
Keyword(s):  
United States ◽  
The United States ◽  
Cumulative Number ◽  
Short Term ◽  
Know How ◽  
The Social ◽  
Reporting Delays ◽  
Social Upheaval ◽  
Near Future ◽  
Do So

In the social upheaval arising from the coronavirus disease 2019 (COVID-19) pandemic, we do not yet know how union formation, particularly marriage, has been affected. Using administration records—marriage certificates and applications—gathered from settings representing a variety of COVID-19 experiences in the United States, the authors compare counts of recorded marriages in 2020 against those from the same period in 2019. There is a dramatic decrease in year-to-date cumulative marriages in 2020 compared with 2019 in each case. Similar patterns are observed for the Seattle metropolitan area when analyzing the cumulative number of marriage applications, a leading indicator of marriages in the near future. Year-to-date declines in marriage are unlikely to be due solely to closure of government agencies that administer marriage certification or reporting delays. Together, these findings suggest that marriage has declined during the COVID-19 outbreak and may continue to do so, at least in the short term.

Patents for Critical Pharmaceuticals: The AZT Case

1991 ◽  
Vol 17 (1-2) ◽  
pp. 145-180
Author(s):  
Evan Ackiron
Keyword(s):  
The United States ◽  
Incentive System ◽  
The Public ◽  
Incentive Programs ◽  
The Past ◽  
Research And Innovation ◽  
Monopoly Pricing ◽  
Conflicting Interests ◽  
Necessary Evil ◽  
Near Future

Patents and other statutory types of market protections are used in the United States to promote scientific research and innovation. This incentive is especially important in research intensive fields such as the pharmaceutical industry. Unfortunately, these same protections often result in higher monopoly pricing once a successful product is brought to market. Usually this consequence is viewed as the necessary evil of an incentive system that encourages costly research and development by promising large rewards to the successful inventor. However, in the case of the AIDS drug Zidovudine (AZT), the high prices charged by the pharmaceutical company owning the drug have led to public outcry and a re-examination of government incentive systems.This Note traces the evolution of these incentive programs — the patent system, and, to a lesser extent, the orphan drug program — and details the conflicting interests involved in their development. It then demonstrates how the AZT problem brings the interest of providing inventors with incentives for risky innovative efforts into a sharp collision with the ultimate goal of such systems: ensuring that the public has access to the resulting products at a reasonable price. Finally, the Note describes how Congress and the courts have attempted to resolve these problems in the past, and how they might best try to solve the AZT problem in the near future.

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