131770-97-3Relevant articles and documents
Synthesis and biological evaluation of 1,4-diazepane derivatives as T-type calcium channel blockers
Gu, Su Jin,Lee, Jae Kyun,Pae, Ae Nim,Chung, Hye Jin,Rhim, Hyewon,Han, So Yeob,Min, Sun-Joon,Cho, Yong Seo
scheme or table, p. 2705 - 2708 (2010/07/15)
We have synthesized and biologically evaluated 1,4-diazepane derivatives as T-type calcium channel blockers. In this study, we discovered compound 4s, a potential T-type calcium channel blocker with good selectivity over hERG and N-type calcium channels. In addition, it exhibited favorable pharmacokinetic characteristics for further investigation of T-type calcium channel related diseases.
Polymorphic form of a tachykinin receptor antagonist
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, (2008/06/13)
This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic form has advantages over the other known forms of 2-(R)-(1-(R)-(3,5-bis(trifluoro-methyl)-phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.