发明名称 INDOLE DERIVATIVE AND MONO- OR DI-AZIDOINDOLE DERIVATIVE HAVING AMINO BAND
摘要 PROBLEM TO BE SOLVED: To obtain a new compound having cyclooxygenase-2 which inhibits activity associated with the biosynthesis of prostaglandin E2 or the like, capable of exhibiting excellent antiinflammatory activity, improved water-solubility or the like, and useful as an antiinflammatory agent. SOLUTION: A compound of formula I (A1 and A2 are each CH= or N=; R1 is an alkyl or amine; R2 is aryl, a hetero cyclic group or the like; Q is O=, S= or the like; Y and Z are each H, an alkyl or the like), or its salt or hydrate, for example, (1-(4-fluorobenzyl)-5-methanesulfonylindol-2-yl)carbonylphrrolidine. In order to obtain a compound of formula I, for example, a new intermediate of formula III (R3 is an alkyl) is obtained by starting from a compound of formula II (RX is an alkyl; X is a halogen), and the obtained intermediate of formula III is treated, for example, with an amine having a group X and a group Z, or ammonia. The treatment with the amine or ammonia is preferably carried out at 20-40 deg.C by using methanol or the like as reaction solvent.
申请公布号 JP2000136182(A) 申请公布日期 2000.05.16
申请号 JP19980310209 申请日期 1998.10.30
申请人 CHUGAI PHARMACEUT CO LTD 发明人 MATSUOKA KOJI;TAKAHASHI TADAKATSU;MARUYAMA NORIAKI;ISHIZAWA TAKENOBU;KATO YASUHARU
分类号 C07D487/04;A61K31/00;A61K31/40;A61K31/403;A61K31/404;A61K31/435;A61K31/4353;A61K31/4355;A61K31/44;A61K31/495;A61K31/4985;A61K31/535;A61K31/5375;A61K31/5377;A61P29/00;A61P43/00;C07D209/42;C07D403/06;C07D471/04;(IPC1-7):C07D209/42;A61K31/498;A61K31/537 主分类号 C07D487/04
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