1236302-97-8Relevant articles and documents
Development of a novel tricyclic class of potent and selective FIXa inhibitors
Meng, Dongfang,Andre, Patrick,Bateman, Thomas J.,Berger, Richard,Chen, Yi-Heng,Desai, Kunal,Dewnani, Sunita,Ellsworth, Kenneth,Feng, Daming,Geissler, Wayne M.,Guo, Liangqin,Hruza, Alan,Jian, Tianying,Li, Hong,Metzger, Joe,Parker, Dann L.,Reichert, Paul,Sherer, Edward C.,Smith, Cameron J.,Sonatore, Lisa M.,Tschirret-Guth, Richard,Wu, Jane,Xu, Jiayi,Zhang, Ting,Campeau, Louis-Charles,Orr, Robert,Poirier, Marc,McCabe-Dunn, Jamie,Araki, Kazuto,Nishimura, Teruyuki,Sakurada, Isao,Hirabayashi, Tomokazu,Wood, Harold B.
, p. 5437 - 5443 (2015)
Using structure based drug design, a novel class of potent coagulation factor IXa (FIXa) inhibitors was designed and synthesized. High selectivity over FXa inhibition was achieved. Selected compounds were evaluated in rat IV/PO pharmacokinetic (PK) studies and demonstrated desirable oral PK profiles. Finally, the pharmacodynamics (PD) of this class of molecules were evaluated in thrombin generation assay (TGA) in Corn Trypsin Inhibitor (CTI) citrated human plasma and demonstrated characteristics of a FIXa inhibitor.
FACTOR IXa INHIBITORS
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Page/Page column 35; 58, (2016/09/15)
The present invention provides a compound of Formula I and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels. The compounds are selective Factor IXa inhibitors.
3-amido-3-aryl-piperidines: A novel class of potent, selective, and orally active GlyT1 inhibitors
Pinard, Emmanuel,Alberati, Daniela,Alvarez-Sanchez, Ruben,Brom, Virginie,Burner, Serge,Fischer, Holger,Hauser, Nicole,Kolczewski, Sabine,Lengyel, Judith,Mory, Roland,Saladin, Christian,Schulz-Gasch, Tanja,Stalder, Henri
, p. 428 - 433 (2014/05/06)
3-Amido-3-aryl-piperidines were discovered as a novel structural class of GlyT1 inhibitors. The structure-activity relationship, which was developed, led to the identification of highly potent compounds exhibiting excellent selectivity against the GlyT2 isoform, drug-like properties, and in vivo activity after oral administration.
PIPERIDINE DERIVATIVES
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Page/Page column 26-27, (2010/08/08)
The present invention relates to a compound of formula I wherein R1, R2, and Ar are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical iso