公开(公告)号：US5252580A

公开(公告)日：1993-10-12

申请号：US947169

申请日：1992-09-18

申请人： Toshihiro Takahashi ,  Hitoshi Inoue ,  Masato Horigome ,  Kenichi Momose ,  Masanori Sugita ,  Kouichi Katsuyama ,  Chikako Suzuki ,  Shinji Nagai ,  Masao Nagase ,  Koichi Nakamaru

发明人： Toshihiro Takahashi ,  Hitoshi Inoue ,  Masato Horigome ,  Kenichi Momose ,  Masanori Sugita ,  Kouichi Katsuyama ,  Chikako Suzuki ,  Shinji Nagai ,  Masao Nagase ,  Koichi Nakamaru

IPC分类号： A61K31/395 ,  A61K31/435 ,  A61K31/437 ,  A61P1/04 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D519/00 ,  A61K31/445 ,  C07D401/06

CPC分类号： C07D471/04

摘要： Disclosed are indole derivatives of formula (I) ##STR1## wherein Y represents H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or halogen;Z represents --CH.sub.2 N(R.sub.5)--;R represents H or --CH.sub.2 CH.sub.2 X where X represents pyridyl, aralkyloxy or substituted amino of NR.sub.6 R.sub.7 where R.sub.6 represents H, C.sub.1 -C.sub.6 alkyl, aralkyl, C.sub.1 -C.sub.6 alkoxycarbonyl, aralkyloxycarbonyl or halogenated C.sub.1 -C.sub.6 alkoxycarbonyl and R.sub.7 represents H, C.sub.1 -C.sub.6 alkyl or aralkyl, or together with R.sub.2 may form a ring of --(CH.sub.2).sub.n -- (n is 1-4) or ##STR2## R.sub.1 represents H, C.sub.1 -C.sub.6 alkyl, aralkyl or arylsulfonyl; R.sub.2 represents C.sub.1 -C.sub.6 alkyl, hydroxy, C.sub.1 -C.sub.6 alkoxy or aralkyloxy;R.sub.3 represents H, C.sub.1 -C.sub.6 alkyl, aralkyl or halogenated C.sub.1 -C.sub.6 alkyl;R.sub.4 and R.sub.5 may be the same or different and each represents H, C.sub.1 -C.sub.6 alkyl or aralkyl or both may together form a ring of --(CH.sub.2).sub.m -- (m is 3 or 4);or pharmaceutically acceptable acid addition salts thereof. They are useful as an antiulcer agent.

公开(公告)号：US5380723A

公开(公告)日：1995-01-10

申请号：US228505

申请日：1994-04-15

申请人： Toshihiro Takahashi ,  Hitoshi Inoue ,  Masato Horigome ,  Kenichi Momose ,  Masanori Sugita ,  Kouichi Katsuyama ,  Chikako Suzuki ,  Shinji Nagai ,  Masao Nagase ,  Koichi Nakamaru

发明人： Toshihiro Takahashi ,  Hitoshi Inoue ,  Masato Horigome ,  Kenichi Momose ,  Masanori Sugita ,  Kouichi Katsuyama ,  Chikako Suzuki ,  Shinji Nagai ,  Masao Nagase ,  Koichi Nakamaru

IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/454 ,  A61K31/47 ,  A61K31/4725 ,  A61K31/5377 ,  A61P1/04 ,  C07D209/14 ,  C07D209/16 ,  C07D401/04 ,  C07D401/14 ,  C07D413/04 ,  C07D403/14 ,  C07D413/14

CPC分类号： C07D401/14 ,  C07D209/16

摘要： Disclosed are indole derivatives of formula (I) ##STR1## wherein X and Y each independently represent H or --CH.sub.2 CH.sub.2 R; R represents pyridyl or substituted amino of NR.sub.1 R.sub.2 ;R.sub.1 represents H or C.sub.1 -C.sub.6 alkyl;R.sub.2 represents 2-(3-indolyl)ethyl or aralkyl; orR.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached may form an N-containing 5 to 6 membered hetero ring, an N, O-containing hetero ring, which hetero ring may be fused with benzene;n is an integer of 4 to 8;with the proviso that X and Y both do not represent H or piperizinoethyl when n is 4, or pharmaceuticaly acceptable acid addition salts thereof. They are useful as an antiulcer agent.

摘要翻译： 公开了式（I）的吲哚衍生物其中X和Y各自独立地表示H或-CH 2 CH 2 R; R代表NR1R2的吡啶基或取代氨基; R1代表H或C1-C6烷基; R2代表2-（3-吲哚基）乙基或芳烷基; 或R 1和R 2与它们所连接的氮原子一起可以形成含N的5至6元杂环，含N，O的杂环，该杂环可以与苯稠合; n为4〜8的整数， 条件是当n为4时X和Y都不表示H或哌嗪子基，或其药学上可接受的酸加成盐。 它们作为抗溃疡剂是有用的。

公开(公告)号：US5326879A

公开(公告)日：1994-07-05

申请号：US949028

申请日：1992-09-22

申请人： Toshihiro Takahashi ,  Hitoshi Inoue ,  Masato Horigome ,  Kenichi Momose ,  Masanori Sugita ,  Kouichi Katsuyama ,  Chikako Suzuki ,  Shinji Nagai ,  Masao Nagase ,  Koichi Nakamaru

发明人： Toshihiro Takahashi ,  Hitoshi Inoue ,  Masato Horigome ,  Kenichi Momose ,  Masanori Sugita ,  Kouichi Katsuyama ,  Chikako Suzuki ,  Shinji Nagai ,  Masao Nagase ,  Koichi Nakamaru

IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/454 ,  A61K31/47 ,  A61K31/4725 ,  A61K31/5377 ,  A61P1/04 ,  C07D209/14 ,  C07D209/16 ,  C07D401/04 ,  C07D401/14 ,  C07D413/04 ,  C07D403/06

CPC分类号： C07D401/14 ,  C07D209/16

摘要： Disclosed are indole derivatives of formula (I) ##STR1## wherein X and Y each independently represent H or --CH.sub.2 CH.sub.2 R;R represents pyridyl or substituted amino of NR.sub.1 R.sub.2 ;R.sub.1 represents H or C.sub.1 -C.sub.6 alkyl;R.sub.2 represents 2-(3-indolyl)ethyl or aralkyl; orR.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached may form an N-containing 5 to 6 membered hetero ring, an N, O-containing hetero ring, which hetero ring may be fused with benzene;n is an integer of 4 to 8;with the proviso that X and Y both do not represent H or piperizinoethyl when n is 4, or pharmaceuticaly acceptable acid addition salts thereof. They are useful as an antiulcer agent.

摘要翻译： 公开了式（I）的吲哚衍生物代表H或-CH 2 CH 2 R; R代表NR1R2的吡啶基或取代氨基; R1代表H或C1-C6烷基; R2代表2-（3-吲哚基）乙基或芳烷基; 或R 1和R 2与它们所连接的氮原子一起可以形成含N的5至6元杂环，含N，O的杂环，该杂环可以与苯稠合; n为4〜8的整数， 条件是当n为4时X和Y都不表示H或哌嗪子基，或其药学上可接受的酸加成盐。 它们作为抗溃疡剂是有用的。