1,720,973 research outputs found
Pharmaceutically active compounds and methods for use
No full textNew fused thiophene compounds are provided and methods of using those conmpounds for a variety of therapeutic indications. Compounds of the invention are particulary useful for treatment of neuropathic pai
Allosteric modulators of the A1 adenosine receptor
No full textTitle compd. I [R1 = H, (un)substituted alkyl, aryl or cycloalkyl; R2, R3 and R4 independently = H, halo, OH, NO2, CN, (un)substituted alkyl, aryl, cycloalkyl or alkoxy; Q = (un)substituted piperidinyl, azepinyl, 5-membered spirocyclic ring, etc.], and their pharmaceutically acceptable salts, are prepd. and disclosed as allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. E.g., II was prepd. and demonstrated an IC50 value of about 100 nM in a functional assay measuring the cAMP level in CHO cells expressing the human A1-adenosine receptor. As allosteric modulators of the A1 adenosine receptor, I should be prove useful for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurol. disease or injury; sleep disorder; epilepsy; and depression
Preparation of substituted purinylpyrazolylacetamides as adenosine A2B receptor antagonists.
No full textThe title compds. I [R1, R2 = (un)substituted alkyl; R3 = H, halo; R4, R5 = H or alkyl; R6 = (un)substituted (hetero)aryl] which are adenosine A2B receptor antagonists and, thus, may be employed for the treatment of conditions and diseases mediated by the adenosine A2B receptor activity, were prepd. Such conditions and diseases include, but are not limited to, chronic and acute inflammatory diseases involving degranulation of mast cells, e.g., asthma, allergic rhinitis and allergic dermatitis; impaired sensitivity to insulin, e.g., type 2 diabetes, non-insulin dependent diabetes, pre-diabetic state, and impaired glucose tolerance; diseases in which angiogenesis is a key component of pathogenesis, e.g., solid tumors and angiogenic retinopathies; apnea of preterm infants; myocardial reperfusion injury; inflammatory bowel disease; autoimmune diseases, such as rheumatoid arthritis, multiple sclerosis, and lupus erythematosus; diseases involving microvascular abnormalities of the retina that are mediated by adenosine A2B receptors, e.g., retinopathy of prematurity, macular degeneration, and diabetic retinopathy; and cardiac diseases including hyperplasia consequent to hypertension, arteriosclerosis, and heart attack. E.g., a multi-step synthesis of II, starting from aniline, was described. Exemplified compds. I were tested in adenosine A2B receptor binding and functional assays (data given). Pharmaceutical compn. comprising the compd. I is disclosed
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
Appropriate Similarity Measures for Author Cocitation Analysis
Full text linkWe provide a number of new insights into the methodological discussion about author cocitation analysis. We first argue that the use of the Pearson correlation for measuring the similarity between authors’ cocitation profiles is not very satisfactory. We then discuss what kind of similarity measures may be used as an alternative to the Pearson correlation. We consider three similarity measures in particular. One is the well-known cosine. The other two similarity measures have not been used before in the bibliometric literature. Finally, we show by means of an example that our findings have a high practical relevance.information science;Pearson correlation;cosine;similarity measure;author cocitation analysis
Dispelling the Myths Behind First-author Citation Counts
Full text linkWe conducted a full-scale evaluative citation analysis study of scholars in the XML research field to explore just how different from each other author rankings resulting from different citation counting methods actually are, and to demonstrate the capability of emerging data and tools on the Web in supporting more realistic citation counting methods. Our results contest some common arguments for the continued
use of first-author citation counts in the evaluation of scholars, such as high correlations between author rankings by first-author citation counts and other citation
counting methods, and high costs of using more realistic citation counting methods that are not well-supported by the ISI databases. It is argued that increasingly available digital full text research papers make it possible for citation analysis studies to go beyond what the ISI databases have directly supported and to employ more
sophisticated methods
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