发明名称 QUATERNARY AMMONIUM SALT COMPOUNDS OF SPIROCYCLOPIPERAZINES, PREPARATION METHODS AND USES THEREOF
摘要 Compounds represented by general formula (I), their stereoisomers, tautomers, derivatives, prodrugs or pharmaceutically acceptable salts, and their preparation methods or uses for the manufacture of a medicament of analgesics. In which R 1 is selected from H, substituted or unsubstituted phenyl, or substituted or unsubstituted heteroaryl; A is bond, or saturated or unsaturated straight-chain or branched-chain hydrocarbon radical; R 2 , R 3 are each independently hydrogen or methyl, which linked with any position of spirocyclo-structure; n and m are each independently integer between 0-2, do not represent 0 at the same time; B and D are each independently C 1 -C 3 straight-chain or branched-chain alkylene; Y is selected from -CHR 4 -, O, S, -S(O)-, -SO 2 -, -NR 4 - and substituted or unsubstituted phenylene, in which R 4 represents H, C 1 -C 6 saturated or unsaturated alkyl, methyl or ethyl substituted by substituted or unsubstituted aryl or heteroaryl; and X- is pharmaceutical acceptable organic or inorganic anion. These compounds can be used as muscarine receptor (M-receptor) and/or nicotine acetylcholine receptor (N-receptor) agonist or antagonist. These compounds have good analgesic effect without side effect such as addiction.
申请公布号 EP2036909(B1) 申请公布日期 2016.05.04
申请号 EP20070721460 申请日期 2007.06.15
申请人 PEKING UNIVERSITY 发明人 LI, RUNTAO;SUN, QI;YE, JIA;YUE, CAIQIN;WANG, XIN;GE, ZEMEI;LI, CHANGLING;CHENG, TIEMING
分类号 C07D487/10;A61K31/495;A61K31/499;A61P25/04;C07D295/06;C07D471/10;C07D498/10;C07D513/10;C07D519/00 主分类号 C07D487/10
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