846060-58-0Relevant academic research and scientific papers
Identification of a new series of non-peptidic NK3 receptor antagonists
Juhl, Karsten,Hansen, Tore,Kehler, Jan,Khanzhin, Nikolay A.,N?rgaard, Morten B.,Ruhland, Thomas,Larsen, Dorrit B.,Jensen, Klaus G.,Steiniger-Brach, Bj?rn,Nielsen, S?ren M.,Simonsen, Klaus B.
, p. 1498 - 1501 (2011/04/16)
The identification and structure-activity relationships of 2-aminomethyl-1-aryl cyclopropane carboxamides as novel NK3 receptor antagonists are reported. The compound series was optimized to give analogues with low nanomolar binding to the NK3 receptor and brain exposure, leading to activity in vivo in the senktide-induced hypoactivity model in gerbils.
NOVEL ARYLBICYCLO[3.1.0]HEXYLAMINES AND METHODS AND COMPOSITIONS FOR THEIR PREPARATION AND USE
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Page/Page column 95-96, (2008/12/05)
The invention provides novel arylbicyclo[3.1.OJhexylamines, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system
Synthesis of enantiomerically pure milnacipran analogs and inhibition of dopamine, serotonin, and norepinephrine transporters
Roggen, Heidi,Kehler, Jan,Stensbol, Tine Bryan,Hansen, Tore
, p. 2834 - 2837 (2008/02/05)
A series of Milnacipran analogs with variation in the aromatic moiety were prepared in high enantiomeric excess. Structure-activity relationships for two parallel enantiomeric series are described. The (-)-(1R,2S)-naphthyl analog (8h) showed the highest potency in the two series and is a triple reuptake inhibitor of the SERT, NET, and DAT.
CYCLOPROPYL DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS
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Page/Page column 56-57, (2010/02/10)
The present invention relates to cyclopropyl derivatives of formula (I) and salt thereof. These compounds are NK3 receptor antagonists and may therefore be useful for treatment of diseases where the NK3 receptor is implicated, e.g. psychotic disorders.
