Discovery and Early Clinical Development of Isobutyl 1-[8-Methoxy-5-(1-oxo-3H-isobenzofuran-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxylate (LEO 39652), a Novel 'Dual-Soft' PDE4 Inhibitor for Topical Treatment of Atopic Dermatitis

Autor: Thomas Vifian, Tatiana G Stilou, Simon Feldbaek Nielsen, Maja Lambert, Jens Christian Højland Larsen, Tine Skak-Nielsen, Anders Soehoel, Pontus Hegardt, Lene M. Hansen, Nina Østergaard Knudsen, Morten Dahl Sørensen, Mogens Larsen, Cecilia Eskilsson, Steen Laursen, Stefan Eirefelt, Henrik Pettersson, Anna Ollerstam

Publikováno v: Journal of Medicinal Chemistry. 63:14502-14521

We describe the design of a novel PDE4 scaffold and the exploration of the dual-soft concept to reduce systemic side effects via rapid elimination: introducing ester functionalities that can be inactivated in blood as well as by the liver (dual-soft)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1fb38d7abc4b9986a9e38e75c9c4ae01
https://doi.org/10.1021/acs.jmedchem.0c00797

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Autor: Tommy Liljefors, Birthe Jensen, Lene M. Hansen, Karla Frydenvang

Publikováno v: Journal of Chemical Crystallography. 28:545-553

The crystal structures of a pair of diastereomeric salts of (−)-(2R, 3R)-O, O′-di-p-toloyl tartaric acid and (−)- and ( + )-3-N,N-dimethylamino-1,1-diphenyl-1-butanol have been determined. Crystal data: 3: (-)-(R)-C18HC24NO+(-)-(2R,3R)-C20H17O-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b94d108a161620a7c4c4abf5bcd78dc0
https://doi.org/10.1023/a:1023296106521

The acute and short-time effect of supplementation with the combination of n-3 fatty acids and acetylsalicylic acid on platelet function and plasma lipids

Autor: Erik Berg Schmidt, Niels Svaneborg, Steen Dalby Kristensen, Lene M Hansen, Steen Husted, Inge Büllow

Publikováno v: Svaneborg, N, Kristensen, S D, Hansen, L M, Büllow, I, Husted, S E & Schmidt, E B 2002, ' The acute and short-time effect of supplementation with the combination of n-3 fatty acids and acetylsalicylic acid on platelet function and plasma lipids ' Thrombosis Res, vol. 105, pp. 311-316 .
Aalborg University
Svaneborg, N, Kristensen, S D, Hansen, L M, Büllow, I, Husted, S & Schmidt, E B 2002, ' The acute and short-time effect of supplementation with the combination of n-3 fatty acids and acetylsalicylic acid on platelet function and plasma lipids ', Thrombosis Res, vol. 105, pp. 311-316 .

Antiplatelet therapy with acetylsalicylic acid (ASA) is commonly used to reduce the risk of cardio- and cerebrovascular events. Fish consumption has been inversely related to coronary disease, which has been partly attributed to an inhibitory effect

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1dc2cd8566e830d141918b1e943d87e9
https://pure.au.dk/portal/da/publications/the-acute-and-shorttime-effect-of-supplementation-with-the-combination-of-n3-fatty-acids-and-acetylsalicylic-acid-on-platelet-function-and-plasma-lipids(294770a0-b8da-11da-bee9-02004c4f4f50).html

Differences in Agonist Binding Pattern for the GABAA and the AMPA Receptors Illustrated by High-Level AB Initio Calculations

Autor: Lena Tagmose, Per-Ola Norrby, Lene M. Hansen, Tommy Liljefors

Publikováno v: Molecular Modeling and Prediction of Bioactivity ISBN: 9781461368571

γ-Aminobutyric acid (GABA) and (S)-glutamic acid are the endogenous receptor ligands for the GABAA and the AMPA receptor, respectively. The 3-isoxazolol and the 5-isoxazolol rings have been used as bioisosters for the carboxylic acid group in GABA a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::61386704dd24c15fdde03f660073bf34
https://doi.org/10.1007/978-1-4615-4141-7_79

Aryl and cycloalkyl analogues of AMPA: synthetic, pharmacological and stereochemical aspects

Autor: Tommy N. Johansen, Tine B. Stensbøl, Birgitte Nielsen, Bjarke Ebert, Karina Krøjer Søby, Erik Falch, Lene M. Hansen, Povl Krogsgaard-Larsen, Lotte Brehm, Niels Skjærbæk

Publikováno v: University of Copenhagen

We have previously shown that (RS)-2-amino-3-(3-hydroxy-5-phenylisoxazol-4-yl)propionic acid (APPA, 2) is a functional partial agonist at the (RS)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) subtype of excitatory amino acid recep

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e8a8420b61434416bb2f4334d1e3cc4a
https://curis.ku.dk/portal/en/publications/aryl-and-cycloalkyl-analogues-of-ampa-synthetic-pharmacological-and-stereochemical-aspects(0ce2f33f-98a0-4fd9-9bee-03b678098400).html