1,721,011 research outputs found
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.
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
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
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
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
An Unexpected Pathway to Enantiomerization of Hemithioketals in Toluene Involving a Dimeric Transition State: A Combined Experimental and Computational Study
No full text5-Alkyl-8-aryl-8-hydroxy-8H-[1,2,4]oxadiazolo[3,4-c][1,4]-thiazin-3-ones (1) and their thioketals (2) represent interesting hits as LTTC blockers as well as inhibitors of MDR1 activity. Compounds 1 contain an unstable chiral centre which can give rise to an enantiomerization process, because of the possible equilibrium with the open-chain forms 4. We have carried out a combined experimental-computational study on the 1/4 equilibrium in toluene by using the 8-(4-bromophenyl)-5-ethyl-8-hydroxy-8H-[1,2,4]oxadiazolo[3,4-c][1,4]-thiazin-3-one (1a), containing two diastereotopic hydrogen atoms. 1H-NMR techniques have allowed to calculate the relevant energy barriers for the enantiomerization process (ca. 20 kcalmol–1). QM computations have individuated a transition state for a concerted asynchronous process occurring on a dimer of 1a with an activation barrier (ca. 23 kcalmol–1) in
rather good agreement with the 1H-NMR experimental value, thus showing how a spontaneous mutarotation process
could occur in non-polar aprotic solvent
p53-dependent and p53-independent anticancer activity of a new indole derivative in human osteosarcoma cells
No full text
Synthesis of 3-(Imidazo[2,1-b]thiazol-6-yl)-2H-chromen-2-one Derivatives and Study of Their Antiviral Activity against Parvovirus B19
Full text linkParvovirus B19 (B19V) is a human pathogenic virus associated with a wide range of clinical conditions. Currently, there are no recognized antiviral drugs for B19V treatment; therefore, efforts in the search for compounds inhibiting B19V replication are now being pursued. Coumarins (chromen-2-ones) are considered a privileged structure for designing novel orally bioavailable and non-peptidic antiviral agents. To further contribute to the development of new drugs against B19V, our research was focused on the synthesis, characterization and evaluation of antiviral activity of some new 3-(imidazo[2,1-b]thiazol-6-yl)-2H-chromen-2-one derivatives. The effects of the synthesized compounds on cell viability and viral replication were investigated by employing two relevant cellular systems, the myeloblastoid cell line UT7/EpoS1 and primary erythroid progenitor cells (EPCs). Some of the tested compounds showed inhibitory activity both on cell viability and on viral replication, depending on the cellular system. These results suggest that the mechanism involved in biological activity is sensitive to small structural changes and that it is possible to direct the activity of the 3-(imidazo[2,1-b]thiazol-6-yl)-2H-chromen-2-one core
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
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