Search Results - "Eskildsen, Jørgen"

The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin by Schrøder, Tenna Juul, Christensen, Søren, Lindberg, Samsa, Langgård, Morten, David, Laurent, Maltas, Philip J, Eskildsen, Jørgen, Jacobsen, Jan, Tagmose, Lena, Simonsen, Klaus Bæk, Biilmann Rønn, Lars Christian, de Jong, Inge E M, Malik, Ibrahim J, Karlsson, Jens-Jakob, Bundgaard, Christoffer, Egebjerg, Jan, Stavenhagen, Jeffrey B, Strandbygård, Dorthe, Thirup, Søren, Andersen, Jacob Lauwring, Uppalanchi, Srinivas, Pervaram, Sridhar, Kasturi, Shiva Prasad, Eradi, Pradheep, Sakumudi, Durga Rao, Watson, Stephen P

“…The identification of the novel, selective, orally bioavailable Sortilin inhibitor AF38469 is described. Structure-activity relationships and syntheses are…”
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The synthesis and SAR of 2-arylsulfanylphenyl-1-oxyalkylamino acids as GlyT-1 inhibitors by Smith, Garrick, Mikkelsen, Gitte, Eskildsen, Jørgen, Bundgaard, Christoffer

“…A novel series of GlyT-1 inhibitors is described. The most potent compound, 38, has a GlyT-1 b IC 50 = 59 nM. In vitro and in vivo assessment of CNS…”
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Identification of the first small-molecule ligand of the neuronal receptor sortilin and structure determination of the receptor-ligand complex by Andersen, Jacob Lauwring, Schrøder, Tenna Juul, Christensen, Søren, Strandbygård, Dorthe, Pallesen, Lone Tjener, García-Alai, Maria Marta, Lindberg, Samsa, Langgård, Morten, Eskildsen, Jørgen Calí, David, Laurent, Tagmose, Lena, Simonsen, Klaus Baek, Maltas, Philip James, Rønn, Lars Christian Biilmann, de Jong, Inge E. M., Malik, Ibrahim John, Egebjerg, Jan, Karlsson, Jens-Jacob, Uppalanchi, Srinivas, Sakumudi, Durga Rao, Eradi, Pradheep, Watson, Steven P., Thirup, Søren

“…Sortilin is a type I membrane glycoprotein belonging to the vacuolar protein sorting 10 protein (Vps10p) family of sorting receptors and is most abundantly…”
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Sequential Functionalization of Pyrazole 1-Oxides via Regioselective Metalation:  Synthesis of 3,4,5-Trisubstituted 1-Hydroxypyrazoles by Paulson, Anna Sif, Eskildsen, Jørgen, Vedsø, Per, Begtrup, Mikael

“…A range of 3,5-diarylated and 3,4,5-triarylated 2-(4-methoxybenzyl)pyrazole 1-oxides have been prepared by regioselective deprotonation at C-5 or…”
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Substituted Tetraoxa[8]circulenes - New Members of the Liquid Crystal Family by Eskildsen, Jørgen, Reenberg, Theis, Christensen, Jørn Bolstad

“…A general method for the synthesis of substituted tetraoxa[8]circulenes based on alkylation of 2,3‐bis(bromomethyl)‐1,4‐dimethoxybenzene with acetylides is…”
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Preparation and Structural Properties of 7,8-Dioxa[6]helicenes and 7a,14c-Dihydro-7,8-dioxa[6]helicenes by Eskildsen, Jørgen, Krebs, Frederik C, Faldt, André, Sommer-Larsen, Peter, Bechgaard, Klaus

“…The potentially chiral 7,8-dioxa[6]helicenes 1 − 1c have been prepared by oxidation of their precursors the 7a,14c-dihydro-7,8-dioxa[6]helicenes 3. The crystal…”
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Discovery and optimization of Lu AF58801, a novel, selective and brain penetrant positive allosteric modulator of alpha-7 nicotinic acetylcholine receptors: attenuation of subchronic phencyclidine (PCP)-induced cognitive deficits in rats following oral administration by Eskildsen, Jørgen, Redrobe, John P, Sams, Anette G, Dekermendjian, Kim, Laursen, Morten, Boll, Jette B, Papke, Roger L, Bundgaard, Christoffer, Frederiksen, Kristen, Bastlund, Jesper F

“…In this Letter, we describe a chemical lead optimization campaign starting from a novel, weak α7 nicotinic acetylcholine receptor positive allosteric modulator…”
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7,10-Diazafluoranthene (Acenaphtho[1,2-b]pyrazine) by Eskildsen, Jørgen, Christensen, Jørn

“…7,10-Diazafluoranthene has been reported to be strongly mutagenic in an Ames-test [1], but no details regarding neither the synthesis nor other properties have…”
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Antipsychotic compounds show inhibition of the human nicotinic acetylcholine α-7 receptor at high concentrations by Frederiksen, Kristen, Bundgaard, Christoffer, Dekermendjian, Kim, Redrobe, John P., FullertonStøier, Jonatan, Eskildsen, Jørgen, Bastlund, Jesper F.

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Agonist Response Induced by Nicotinic α-7 Agonist is Inhibited by Antipsychotic Drugs by Frederiksen, Kristen, Jessen, Maja, Støier, Jonatan Fullerton, Dekermendjian, Kim, Redrobe, John Paul, Bundgaard, Christoffer, Eskildsen, Jørgen Calí, Bastlund, Jesper Frank

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Discovery of Lu AF58801, a novel, selective and brain penetrant positive allosteric modulator of alpha-7 nicotinic acetylcholine receptors: Attenuation of subchronic phencyclidine (PCP)-induced cognitive deficits in rats following oral administration by Bastlund, Jesper F., Bundgaard, Christoffer, Dekermendjian, Kim, Papke, Roger L., Redrobe, John P., Frederiksen, Kristen, Eskildsen, Jørgen

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Halogen dance in pyrazole 1-oxides: synthesis of pyrazolo[3,4- c]quinoline 1-oxides by Eskildsen, Jørgen, Østergaard, Niels, Vedsø, Per, Begtrup, Mikael

“…The synthesis of a new series of 3-substituted pyrazolo[3,4- c]quinoline 1-oxides is presented. Regioselective bromine–magnesium exchange of 2-benzylated…”
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Convergent Synthesis of 3-Arylated 1-Hydroxypyrazoles via 3-Metalated Pyrazole-1-oxides by Eskildsen, Jørgen, Kristensen, Jesper, Vedsø, Per, Begtrup, Mikael

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AN IMPROVED SYNTHESIS OF 2,3-bis(BROMOMETHYL)-1,4-DIMETHOXYBENZENE by Eskildsen, Jørgen, Christensen, Trine, Reenberg, Theis, Larsen, Uffe, Christensen, Jørn B.

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Identification of histamine H3 receptor antagonists by Del Tredici, Andria Lee, Eskildsen, Jorgen, Andersen, Carsten B, Ma, Jian‐Nong, Ohrmund, Steven, Petersen, Lauren, Littler, Pey‐Lih, Nugyen, Derek, Fairbairn, Luke, Lameh, Jelveh, Currier, Erika A, Schiffer, Hans H, Burstein, Ethan, Olsson, Roger, Piu, Fabrice

“…Histamine H3 receptors (H3R) regulate the release of histamine and other neurotransmitters in the brain. H3R have been shown to modulate many functions,…”
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