公开(公告)号：US08318811B2

公开(公告)日：2012-11-27

申请号：US12223584

申请日：2007-02-05

申请人： Ryotaro Kojima ,  Koichi Nakamaru ,  Tokutarou Yasue

发明人： Ryotaro Kojima ,  Koichi Nakamaru ,  Tokutarou Yasue

IPC分类号： A61K31/137

CPC分类号： A61K31/137 ,  A61K45/06

摘要： A novel therapeutic and prophylactic agent for inflammatory bowel diseases and a method for treating inflammatory bowel diseases is provided. The agent comprises a 2-amino-1,3-propanediol derivative (e.g., 2-amino-2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl-1,3-propanediol hydrochloride) represented by the chemical formula (1) or a pharmaceutically acceptable salt or hydrate thereof: The agent is useful in the treatment or prevention of Crohn's disease, Crohn's disease in large intestine, intestinal Behcet's disease, ulcerative colitis, bleeding rectal ulcer and pouchitis.

摘要翻译： 提供了一种新型的炎症性肠病治疗和预防剂及其治疗炎症性肠病的方法。 该试剂包括由化学式表示的2-氨基-1,3-丙二醇衍生物（例如2-氨基-2- [4-（3-苄氧基苯硫基）-2-氯苯基]乙基-1,3-丙二醇盐酸盐） （1）或其药学上可接受的盐或水合物：该试剂可用于治疗或预防克罗恩病，大肠克罗恩病，肠内切塞特氏病，溃疡性结肠炎，直肠溃疡出血和肠炎。

公开(公告)号：US20090137685A1

公开(公告)日：2009-05-28

申请号：US12223584

申请日：2007-02-05

申请人： Ryotaro Kojima ,  Koichi Nakamaru ,  Tokutarou Yasue

发明人： Ryotaro Kojima ,  Koichi Nakamaru ,  Tokutarou Yasue

IPC分类号： A61K31/138 ,  C07C211/27 ,  A61P1/00

CPC分类号： A61K31/137 ,  A61K45/06

摘要： A novel therapeutic and prophylactic agent for inflammatory bowel diseases and a method for treating inflammatory bowel diseases.The agent comprises a 2-amino-1,3-propanediol derivative (e.g.,2-amino-2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl-1,3-propanediol hydrochloride) represented by the chemical formula (1) or a pharmaceutically acceptable salt or hydrate thereof: The agent is useful in the treatment or prevention of Crohn's disease, Crohn's disease in large intestine, intestinal Behcet's disease, ulcerative colitis, bleeding rectal ulcer and pouchitis.

摘要翻译： 一种新型的炎性肠病治疗和预防剂及其治疗炎症性肠病的方法。 该试剂包括由化学式表示的2-氨基-1,3-丙二醇衍生物（例如2-氨基-2- [4-（3-苄氧基苯硫基）-2-氯苯基]乙基-1,3-丙二醇盐酸盐） （1）或其药学上可接受的盐或水合物：该试剂可用于治疗或预防克罗恩病，大肠克罗恩病，肠内切塞特氏病，溃疡性结肠炎，直肠溃疡出血和肠炎。

公开(公告)号：US20100324057A1

公开(公告)日：2010-12-23

申请号：US12866576

申请日：2009-02-06

申请人： Naoya Yamamuro ,  Koichi Nakamaru ,  Tokutarou Yasue

发明人： Naoya Yamamuro ,  Koichi Nakamaru ,  Tokutarou Yasue

IPC分类号： A61K31/4965 ,  A61K31/137 ,  A61K31/24 ,  A61P1/00

CPC分类号： A61K31/133 ,  A61K31/225 ,  A61K31/27 ,  A61K31/4965 ,  C07D241/08

摘要： A novel therapeutic agent or prophylactic agent for an inflammatory bowel disease is provided. An amino alcohol derivative represented by the general formula (1): which is a sphingosine-1-phosphate receptor agonist or a pharmaceutically acceptable salt or hydrate thereof are a therapeutic agent or prophylactic agent for an inflammatory bowel disease comprises.

摘要翻译： 提供了一种用于炎症性肠病的新型治疗剂或预防剂。 由通式（1）表示的氨基醇衍生物：其为鞘氨醇-1-磷酸受体激动剂或其药学上可接受的盐或水合物，是炎症性肠病的治疗剂或预防剂。

公开(公告)号：US08476305B2

公开(公告)日：2013-07-02

申请号：US12866576

申请日：2009-02-06

申请人： Naoya Yamamuro ,  Koichi Nakamaru ,  Tokutarou Yasue

发明人： Naoya Yamamuro ,  Koichi Nakamaru ,  Tokutarou Yasue

IPC分类号： C07C215/00 ,  A61K31/00

CPC分类号： A61K31/133 ,  A61K31/225 ,  A61K31/27 ,  A61K31/4965 ,  C07D241/08

摘要： A novel therapeutic agent or prophylactic agent for an inflammatory bowel disease is provided. An amino alcohol derivative represented by the general formula (1): which is a sphingosine-1-phosphate receptor agonist or a pharmaceutically acceptable salt or hydrate thereof are a therapeutic agent or prophylactic agent for an inflammatory bowel disease comprises.

摘要翻译： 提供了一种用于炎症性肠病的新型治疗剂或预防剂。 由通式（1）表示的氨基醇衍生物：其为鞘氨醇-1-磷酸受体激动剂或其药学上可接受的盐或水合物，是炎症性肠病的治疗剂或预防剂。

公开(公告)号：US4933342A

公开(公告)日：1990-06-12

申请号：US331514

申请日：1989-03-29

申请人： Toshihiro Takahashi ,  Koichiro Hagihara ,  Koichi Nakamaru ,  Yoshikuni Suzuki

发明人： Toshihiro Takahashi ,  Koichiro Hagihara ,  Koichi Nakamaru ,  Yoshikuni Suzuki

IPC分类号： A61K31/495 ,  A61P1/04 ,  C07D401/12 ,  C07D401/14

CPC分类号： C07D401/12 ,  C07D401/14

摘要： Quinoxaline derivatives of formula (I) are provided. ##STR1## wherein A is a hydrogen atom or 2-quinoxalyl group, B is 2-pyridyl or 4-quinolyl group and n is 0 or 1, or a pharmaceutically acceptable acid addition salt thereof. They are useful as antiulcer agents.

公开(公告)号：US4829069A

公开(公告)日：1989-05-09

申请号：US175518

申请日：1988-03-31

申请人： Toshihiro Takahashi ,  Koichi Nakamaru ,  Yoshikuni Suzuki ,  Tatsuo Horaguchi

发明人： Toshihiro Takahashi ,  Koichi Nakamaru ,  Yoshikuni Suzuki ,  Tatsuo Horaguchi

IPC分类号： A61K31/505 ,  A61K31/517 ,  A61P1/04 ,  C07D239/93

CPC分类号： C07D239/93

摘要： 4-Thioquinazoline derivatives of formula (I) are provided. ##STR1## wherein R.sup.1 is a C.sub.1 -C.sub.6 alkylamino group, a phenyl group, a substituted phenyl group or a 5- or 6-membered heterocyclic group containing one or two N, O or S as a hetero atom or atoms, said heterocyclic group optionally being substituted or fused with a benzene ring; n is 1 or 2; or R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, and pharmaceutically acceptable acid addition salts thereof. They are useful as antiulcer agents.

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。

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：US5008266A

公开(公告)日：1991-04-16

申请号：US373024

申请日：1989-07-26

申请人： Toshihiro Takahashi ,  Tatsuo Horaguchi ,  Koichi Nakamaru ,  Yoshikuni Suzuki

发明人： Toshihiro Takahashi ,  Tatsuo Horaguchi ,  Koichi Nakamaru ,  Yoshikuni Suzuki

IPC分类号： A61K31/505 ,  A61K31/517 ,  A61P1/04 ,  A61P43/00 ,  C07D239/95 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

CPC分类号： C07D401/12 ,  C07D239/95 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

摘要： 4(3H)-Quinazolinone derivative of formula (I) are provided. ##STR1## wherein R.sub.1 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, an aryl group, a substituted aryl group, or an aralkyl group; R.sub.2 is a C.sub.1 -C.sub.6 alkylamino group, a phenyl group, a substituted phenyl group, or a 5- or 6-membered heterocyclic group containing one or more N, O or S as a hetero atom or atoms, said heterocyclic group optionally being substituted or fused with a benzene ring; n is 1 or 2; or R.sub.2 represents a geranyl group or a dipyridylmethyl group together with the group --(CH.sub.2).sub.n --; and X is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a halogen atom, and pharmaceutically acceptable acid addition salts thereof. They are useful as antiucler agents.