KOBAYASHI TETSUYA,KOLTUN DMITRY,NOTTE GREGORY,PARKHILL ERIC,ZABLOCKI JEFF
申请号：
NZ60447811
公开号：
NZ604478A
申请日:
2011.06.30
申请国别(地区):
NZ
年份:
2014
代理人:
摘要：
The present disclosure relates to [1,2,4]triazolo[4,3-a]pyridin-3(2H)-one compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1 is aryl, pyridinyl, pyridazinyl, pyrimidinyl, quinolonyl, indazolyl, triazolopyridinyl, imidazopyridinyl, thiadiazolyl, or triazolyl R2, R3, R4, and R5 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same. Compounds of the disclosure are of use in the treatment of conditions related to sodium current including cardiovascular disease selected from one or more of atrial and ventricular arrhythmias, heart failure (including congestive heart failure, diastolic heart failure, systolic heart failure, acute heart failure), Prinzmetal&rsquos (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, ischemia, recurrent ischemia, reperfusion injury, myocardial infarction, acute coronary syndrome, peripheral arterial disease, pulmonary hypertension, and intermittent claudication, diabetes or diabetic peripheral neuropathy, neuropathic pain, epilepsy, seizures, or paralysis.
