发明名称 Aminopyridines and their use as anticonvulsants and sodium channel blockers
摘要 A compound of formula I or a pharmaceutically acceptable salt, prodrug or solvate, wherein: R1 is selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, halogen, haloalkyl, cycloalkyl, amino, aminoalkyl, hydroalkyl, alkoxyalkyl, alkoxy, alkylthio, alkylsulfinyl, carboxyalkyl, cyano, alkylamino, aminocarbonyl, alkylaminocarbonyl, arylaminocarbonyl, aralkylaminocarbonyl, alkylcarbonylamino, arylcarbonylamino, alkylcarbonyl, heterocyclocarbonyl, aminosulfonyl, alkylaminosulfonyl and hetercyclosulfonyl, all of which can be optionally substituted; R2 is hydrogen or C1-6 alkyl and R3 is hydrogen, or R2 and R3 form a bond; R4 is hydrogen or C1-6 alkyl; R5, R6. R7 and R8 are independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, halogen, haloalkyl, hydroalkyl, hydroxyl, nitro, amino, aminoalkyl, cyano, amide, carboxyalkyl, alkoxyalkyl, ureido, acylamino, thiol acyloxy, azido, alkoxy, carboxy, carbonylamido and alkylthiol; X is on of O, S, NR9 or CH2 wherein R9 is hydrogen or alkyl; and m is 0-3; and the use of the compound in the preparation of a medicament for treating a disorder responsive to the blockade of sodium channels; or for treating, preventing or ameliorating neuronal loss following global and focal ischemia, neurodegenerative conditions, pain or tinnitus, manic depression, arrhythmias, convulsions or providing local anesthesia; or alleviating or preventing seizure activity.
申请公布号 NZ521870(A) 申请公布日期 2004.08.27
申请号 NZ20010521870 申请日期 2001.03.29
申请人 EURO-CELTIQUE S 发明人 HOGENKAMP, DERK J
分类号 A61K31/44;A61P9/06;A61P9/10;A61P21/02;A61P23/02;A61P25/00;A61P25/04;A61P25/08;A61P25/18;A61P25/24;A61P25/28;A61P43/00;C07D213/74;(IPC1-7):C07D213/74 主分类号 A61K31/44
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