847156-32-5Relevant academic research and scientific papers
Synthesis and structure-activity relationships of benzyloxyphenyl derivatives as a novel class of NCX inhibitors: Effects on heart failure
Kuramochi, Takahiro,Kakefuda, Akio,Yamada, Hiroyoshi,Ogiyama, Takashi,Taguchi, Taku,Sakamoto, Shuichi
, p. 725 - 734 (2005)
In the context of heart failure and myocardial ischemia reperfusion, the activity of the sodium-calcium exchanger can lead to calcium overload, which in turn can lead to contractile dysfunction and arrhythmia. Therefore, NCX is an attractive target for treatment of heart failure and myocardial ischemia reperfusion. We have designed and synthesized a series of benzyloxyphenyl derivatives as potential NCX inhibitors, based on compound 4. These derivatives have been evaluated for their inhibitory activity against both the reverse and forward modes of NCX, and two novel potent NCX inhibitors (7i, 10a) were discovered. Compound 7i was evaluated for its efficacy on ouabain-induced tonotropy and arrhythmia in a heart-failure model.
PYRIDYL NON-AROMATIC NITROGENATED HETEROCYCLIC-1-CARBOXYLATE ESTER DERIVATIVE
-
Page/Page column 28, (2008/06/13)
[Problem] To provide a compound usable for treatment of diseases associated with fatty acid amide hydrolase (FAAH), especially for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain. [Means for Solution] We have found that a novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative of the present invention has an excellent effect for increasing an effective bladder capacity, an excellent effect for relieving urinary frequency and an excellent anti-allodynia effect, and is therefore usable for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.
