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公开(公告)号:US5512579A
公开(公告)日:1996-04-30
申请号:US275704
申请日:1994-07-18
申请人: Shuhei Miyazawa , Yorohisa Hoshino , Hisashi Shibata , Kazuo Hirota , Takaaki Kameyama , Shinya Abe , Takashi Yamanaka
发明人: Shuhei Miyazawa , Yorohisa Hoshino , Hisashi Shibata , Kazuo Hirota , Takaaki Kameyama , Shinya Abe , Takashi Yamanaka
IPC分类号: A61K31/40 , A61K31/403 , A61K31/435 , A61K31/445 , A61K31/4468 , A61K31/495 , A61K31/535 , A61K31/55 , A61K31/625 , A61P1/00 , A61P1/08 , A61P1/12 , A61P1/14 , A61P25/20 , A61P25/22 , A61P43/00 , C07D207/14 , C07D209/00 , C07D211/58 , C07D221/22 , C07D221/24 , C07D223/32 , C07D451/02 , C07D451/04 , C07D451/14 , C07D471/08 , C07D471/18 , C07D491/08 , C07D498/08 , C07D295/04
CPC分类号: C07D451/02 , C07D207/14 , C07D211/58 , C07D221/24 , C07D451/04 , C07D451/14 , C07D471/08 , C07D491/08 , C07D498/08
摘要: To provide a compound which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio. An aminobenzoic acid derivative represented by the general formula (I) or (II) or a pharmacologically acceptable salt thereof: ##STR1## wherein R.sup.1 represents a group represented by the formula: ##STR2## {wherein A represents a group represented by formula --CH.sub.2 --X--CH.sub.2 -- (wherein X represents O, >N--R.sup.6 or >CHR.sup.7 (wherein R.sup.6 represents lower alkyl and R.sup.7 represents hydrogen or lower alkoxy)), etc.; D and E each represents a group represented by formula --(CH.sub.2).sub.3 --, etc., and R.sup.2 represents lower alkyl. etc.}; R.sup.9 represents alkynyl; R.sup.10 represents amino, etc.; R.sup.11 represents halogen; R.sup.12 and R.sup.13 each represent lower alkyl; a is an integer of 1 to 5; and b is an integer of 0 to 5!.
摘要翻译: 提供以良好平衡的活性比表现出5-羟色胺拮抗作用和乙酰胆碱释放促进活性的化合物。 (I)或(II)表示的氨基苯甲酸衍生物或其药理学上可接受的盐:其中R1表示由下式表示的基团: 其中A表示由式-CH 2 -X-CH 2 - (其中X表示O,> N-R 6或> CHR 7(其中R 6表示低级烷基,且R 7表示氢或低级烷氧基))等表示的基团。 D和E各自表示由式 - (CH 2)3 - 等表示的基团,并且R 2表示低级烷基。 等等。}; R9代表炔基; R10表示氨基等。 R11表示卤素; R 12和R 13各自表示低级烷基; a为1〜5的整数, b为0〜5的整数]。