1,721,032 research outputs found
1,4-Anthraquinone: A new useful pre-column reagent for the determination of N-acetylcysteine and captopril in pharmaceuticals by high performance liquid chromatography
No full text1,4-Anthraquinone (ANQ) is proposed as a novel pre-column reagent for high performance liquid chromatography (HPLC) determination of N-acetylcysteine (NAC) and captopril (CAP) in pharmaceutical formulations. The derivatization reactions were carried out at room temperature: NAC at pH 8 for 1 min, while CAP at pH 7.5 for 20 min. Both reactions reached completeness at a reagent to thiol molar ratio of about 2.5. The synthesised derivatives were characterized by1H NMR and IR. The chromatographic separations were performed on a C18 Phenomenex Synergi Fusion 4 um (250 mm x mm I.D.) stainless steel column with detection at λ = 300 nm. The mobile phase consisted of methanol/triethylammonium (TEA) phosphate buffer (pH 3; 0.05 mol/L) 75:25 (v/v) at a flow-rate of 0.4 mL/min for NAC and 88:12 (v/v), at a flow-rate of 0.6 mL/min for CAP. The validation parameters (linearity, sensitivity, accuracy, precision, specificity and stability) were highly satisfactory. Linear response was observed (determination coefficient ≥0.9996). Detection limits were about 8 and 18 ng/mL for NAC and CAP, respectively. Intra-day precision (relative standard deviation, R.S.D.) was ≤1.58%, for thiol to internal standard (IS) peak area ratio and ≤0.33%, for thiol and IS retention times (tR), without significant differences between intra- and inter-day data. Thiol recovery studies were satisfactory (99.50%) with R.S.D. ≤0.56%. The results highlight the high sensitivity of the method and the remarkable reactivity and selectivity of the reagent towards the thiol function. The developed method is suitable for the quality control of both thiols in commercial products. The method can be applied in any analytical laboratory not requiring a sophisticated instrumentation
A Patent Review on Thiazole Derivatives (2008-2013)
Full text linkThiazole is a well known five membered heterocyclic compound. Various methods have been worked out for its synthesis. In the
last few decades, a lot of work has been done on thiazole ring to synthetize derivatives directed to a plethora of molecular targets in
order to discover new drug leads. The present review gives an account of the therapeutic patent literature (2008-2013) describing
the applications of thiazole and its derivatives on selected activities. Most of the described compounds are shown to have potential beneficial therapeutic effects, even if all these patents generated few clinical evaluations. However, the thiazole scaffold remains one
of great potential for the chemical pharmaceutical research; it can serve for the design of lead compounds especially in cases where
the target is known and the mechanism of action is well defined.
Small-Molecules Targeting Sirtuin 1: A Patent Review (2012-2015)
No full textSirtuins are a family of enzymes, which govern genome regulation, stress response, metabolic homeostasis and lifespan. Among all the discovered human isoforms (SIRT1-7), SIRT1 emerged as a promising molecular target for the treatment of several diseases. The SIRT1 activators have shown beneficial effects in diabetes, obesity, disorders related to aging, cardiovascular and neurodegenerative diseases. On the other hand, SIRT1 inhibition could be applied in anticancer therapy. This review is focused on patents regarding small molecules targeting SIRT1 registered from 2012 to 2015. The chemical formula, the activation and/or inhibition activity and the application of the most active compounds are considered
Recent Patents on Thiazole Derivatives Endowed with Antitumor Activity
No full textCancer is a disease of remarkable importance in the world today and is projected to become
the primary cause of death within the coming years, therefore the design and development of new antitumor
agents is one of the most pressing research areas in medicinal chemistry. Considering the importance
of thiazole ring as scaffold present in a wide range of therapeutic agents, the medicinal chemists
have been encouraged to synthesize a large number of novel antitumors bearing this heterocycle,
which furnish extensive synthetic possibilities due to the presence of several reaction sites. The present
review describes the patents from 2008 to present concerning new thiazole compounds useful for the
development of new drug molecules. It has been divided according to the molecular target and describes
the pathways involved in the biological activities and the structure of the most potent compounds,
together with the screening results
Small-Molecules Targeting Kinases Involved in Pulmonary Hypertension: a Patent Review (2010-2015)
No full textBackground: Despite the fact that in recent years, a substantial progress has been made in the treatment of pulmonary hypertension, it is still a severe disease characterized by poor prognosis, and the search for new drugs remains a priority. Current remedies address mainly the vasoconstrictor/vasodilator imbalance in the pulmonary circulation, while the causes of the disease are only moderately affected. Recently, the role of receptor and non receptor kinases in pulmonary hypertension has emerged and these targets were extensively considered for the development of new therapeutic strategies. This review discusses the patents on small-molecules targeting kinases involved in
the proliferation/apoptosis imbalance, typically present in pulmonary hypertension.
Methods: Bibliographic research for the inventions was carried out using Espacenet and Sci-Finder databases, “pulmonary hypertension and kinases” as research query and the range from 2010 to 2015. Only patents published in English were considered. A qualitative analysis of the contents of each patent was made to examine the reported compounds, the studies performed and the resulting conclusions.
Results: The review includes about thirty applications. Moreover, in order to illustrate the pathophisiology of the disease and the mechanisms of the targets, about forty additional papers were reported. Considering that imatinib, a PDGF receptor inhibitor, entered the clinical trials for the treatment of pulmonary hypertension, the first patents were devoted to inhibitors of tyrosine kinase receptors, such as PDGFR and c-Kit. Subsequently, in addition to kinase receptors, the role of other pathways involved in pulmonary hypertension has emerged, and some research groups have focused their attention also on non-receptor kinases. Fifteen patents on this topic reported these new targets and new derivatives. However, in most of the inventions, although the pulmonary
hypertension is among the treatable diseases, the compounds were subjected only to antiproliferative assays and not to specific tests on animal models.
Conclusion: The studies reported in this review confirm the continuous research efforts aimed to identify new targets and new drugs for the treatment of pulmonary hypertension. Several inhibitors of kinase were described. These compounds could inhibit mainly important branching processes and pathological growth of blood vessels, thereby might increase the lifespan of patients
2-Indolinone a versatile scaffold for treatment of cancer: A patent review (2008-2014)
No full text2-Indolinone is a well-known aromatic heterocyclic organic compound. A lot of
work has been done on this bicyclic structure by academic and company researchers to
synthesize compounds directed to a plethora of molecular targets in order to discover new
drug leads. This review presents up-to-date information in the field of cancer therapy research
based on this small building block. Areas covered: The present review gives an account of the
recent patent literature (2008–2014) describing the discovery of 2-indolinone derivatives with
selected therapeutic activities. In this period, a large amount of patents were published on this
topic. We have limited the analysis to 37 patents on 2-indolinone derivatives having potential
clinical application as chemotherapeutic agents. In this review, the therapeutic applications of
2-indolinone derivatives for the treatment of cancer reported in international patents have
been discussed. Expert opinion: 2-Indolinone is the scaffold of the compounds considered from
a medicinal chemistry perspective. Many of them have been developed and marketed for
therapeutic use. In cancer chemotherapy, progress has been made in designing selective 2-
indolinone derivatives. Some of them show preclinical efficacy. However, 2-indolinone has not
exhausted all of its potential in the development of new compounds for clinical applications
and remains a great tool for future research
Imidazo[2,1-b] Thiazole: Introduction, Current and Perspective
Full text linkImidazo[2,1-b]thiazole is a fused heterobicyclic system containing bridgehead
nitrogen atom. Derivatives of this scaffold are especially attractive in the field of
medicinal chemistry because of their broad spectrum of biological activities. The
imidazo[2,1-b]thiazole system constitutes the core unit of the well-known
anthelminthic and immunomodulatory agent Levamisole, marketed
under the trade name Ergamisol© and discovered at Janssen Pharmaceutica in 1966
Going Beyond Counting First Authors in Author Co-citation Analysis
Full text linkThe present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation
counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings
are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that
only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into
account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed
Variations on the Author
Full text link“Variations on the Author” discusses two of Eduardo Coutinho’s recent films (Um Dia na Vida, from 2010, and Últimas Conversas, posthumously released in 2015) and their contribution to the general question of documentary authorship. The director’s filmography is characterized by a consistent yet self-effacing form of authorial self-inscription: Coutinho often features as an interviewer that rather than express opinions propels discourses; an interviewer that is good at listening. This mode of self-inscription characterizes him as an author who is not expressive but who is nonetheless markedly present on the screen. In Um Dia na Vida, however, Coutinho is completely absent form the image, while Últimas Conversas, on the contrary, includes a confessional prologue that moves the director from the margins to the center of his films. This article examines the ways in which these works stand out in the filmography of a director who offers new insights into the notion of cinematic authorship
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