46475-04-1Relevant academic research and scientific papers
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 (2015/11/09)
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.
New pyrrolidin-, piperidin- and azepin-2-oxocarboxylic acid esters are preferential M1, M3 muscarinic antagonists. Synthesis and bronchospasmolytic activity
Cereda,Ezhaya,Bellora,Schiavi,Sagrada,Doods,Donetti
, p. 411 - 421 (2007/10/02)
A series of new 3-tropanol and 3-quinuclidinol esters of phenyl-substituted pyrrolidin-, piperidin- and azepin-2-oxocarboxylic acid were synthesized and tested for antimuscarinic activity. The compounds showed a preferential in vitro activity at M1 and M3 receptor subtypes and an interesting activity profile in vivo. A potential use as selective bronchospasmolytic agents has been suggested for selected compounds.
