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1.发明公开
公开(公告)号：EP1120412A4
公开(公告)日：2002-09-11
申请号：EP99969719
申请日：1999-09-30
IPC分类号： C07D311/58 , A61K31/35
CPC分类号： C07D311/58
摘要： A process for the preparation of 4-substituted benzopyran derivatives which comprises preparing N-(2-cyanoethyl)-5-fluoro-4-fluoromethyl-4-(4-trifluoromethylphenoxy)-2-pentynamide from 1-fluoro-2-fluoromethyl-3-butyn-2-yl 4-trifluoromethylphenyl ether and cyclizing this pentynamide derivative into 2,2-bis(fluoromethyl)-N-(2-cyanoethyl)-6-trifluoromethyl-2H-1-benzopyran-4-carboxamide; and other processes therefor. The processes make it possible to prepare the benzopyran derivatives in a shortened process time as compared with those of the prior art with high safety through easy purification.
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公开(公告)号：EP1086950A4
公开(公告)日：2002-11-06
申请号：EP99921245
申请日：1999-05-25
发明人： MATSUOKA HIROHARU , KATO NOBUAKI , TAKAHASHI TADAKATSU , MARUYAMA NORIAKI , ISHIZAWA TAKENORI , SUZUKI YUKIO
IPC分类号： A61P29/00 , A61P43/00 , C07D401/04 , C07D401/06 , C07D403/04 , C07D405/04 , C07D405/06 , C07D413/04 , C07D417/04 , C07D417/06 , C07D471/04 , C07D487/04 , A61K31/40 , A61K31/41 , A61K31/42 , A61K31/435 , A61K31/44 , A61K31/495
CPC分类号： C07D401/04 , C07D401/06 , C07D403/04 , C07D405/04 , C07D405/06 , C07D413/04 , C07D417/04 , C07D417/06 , C07D471/04 , C07D487/04
摘要： Indole derivatives and mono- or diazaindole derivatives represented by general formula (1), pharmaceutically acceptable acid-addition salts or base-addition salts thereof or hydrates of the same which have a COX-2 inhibitory activity and are useful as drugs such as anti-inflammatory agents, wherein Het represents an optionally substituted heterocycle; A1 and A2 independently represent each -CH=, etc.; A3 represents -CH2-, etc.; R1 represents 4-fluorophenyl, etc.; R2 represents alkyl; and n is 0, 1 or 2, provided that when A1 and A2 are both -CH=, then A3 is -CH2- or -SO2-.
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