910028-58-9Relevant 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.
Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors
Zhang, Mingzhu,Jovic, Florence,Vickers, Troy,Dyck, Brian,Tamiya, Junko,Grey, Jonathan,Tran, Joe A.,Fleck, Beth A.,Pick, Rebecca,Foster, Alan C.,Chen, Chen
scheme or table, p. 3682 - 3686 (2009/04/06)
Compounds with various activities and selectivities were discovered through structure-activity relationship studies of bicifadine analogs as monoamine transporter inhibitors. The norepinephrine-selective 2-thienyl compound S-6j was efficacious in a rodent
NOVEL ARYLBICYCLO[3.1.0]HEXYLAMINES AND METHODS AND COMPOSITIONS FOR THEIR PREPARATION AND USE
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Page/Page column 95, (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.
Stereocontrolled synthesis of trisubstituted cyclopropanes: Expedient, atom-economical, asymmetric syntheses of (+)-bicifadine and DOV21947
Xu, Feng,Murry, Jerry A.,Simmons, Bryon,Corley, Edward,Fitch, Kenneth,Karady, Sandor,Tschaen, David
, p. 3885 - 3888 (2007/10/03)
An expedient, atom-economical, asymmetric synthesis of 1-aryl-3- azabicyclo[3.1.0]hexanes, including (+)-Bicifadine and DOV21947, in a single-stage through process without isolation of any intermediates has been developed. The key of this synthesis is the in-depth mechanistic understanding of the complicated epoxy nitrile coupling at each reaction stage. Therefore, the desired trisubstituted cyclopropane can be prepared in high ee and yield by controlling the reaction pathway through manipulating the nitrile anion aggregation state.
