公开(公告)号：US20120225866A1

公开(公告)日：2012-09-06

申请号：US13388442

申请日：2010-08-20

申请人： Kunio Oshima ,  Shuuji Matsumura ,  Hokuto Yamabe ,  Naohiro Isono ,  Noriaki Takemura ,  Shinichi Taira ,  Takashi Oshiyama ,  Yasuhiro Menjo ,  Tsuyoshi Nagase ,  Masataka Ueda ,  Yasuo Koga ,  Sunao Nakayama ,  Kenji Tsujimae ,  Toshiyuki Onogawa ,  Kuninori Tai ,  Motohiro Itotani

发明人： Kunio Oshima ,  Shuuji Matsumura ,  Hokuto Yamabe ,  Naohiro Isono ,  Noriaki Takemura ,  Shinichi Taira ,  Takashi Oshiyama ,  Yasuhiro Menjo ,  Tsuyoshi Nagase ,  Masataka Ueda ,  Yasuo Koga ,  Sunao Nakayama ,  Kenji Tsujimae ,  Toshiyuki Onogawa ,  Kuninori Tai ,  Motohiro Itotani

IPC分类号： A61K31/5513 ,  C07D493/10 ,  A61P9/06 ,  C07D243/14

CPC分类号： C07D491/048 ,  C07D213/38 ,  C07D215/227 ,  C07D243/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04

摘要： The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1) or a salt thereof, wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo; Y1 and Y2 are each independently —N═ or —CH═; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—; XA and XB are each independently a bond, lower alkylene, etc.

摘要翻译： 本发明提供了一种新颖的二氮杂类化合物，其比其他K +通道有效地和选择性地阻断IK电流或Kv1.5通道。 本发明涉及由通式（1）表示的二氮杂化合物或其盐，其中R 1，R 2，R 3和R 4各自独立地为氢，低级烷基，环低级烷基或低级烷氧基低级烷基; R2和R3可以连接形成低级亚烷基; A1是任选被一个或多个选自羟基和氧代的取代基取代的低级亚烷基; Y1和Y2各自独立地为-N =或-CH =; 并且R 5为其中R 6和R 7各自独立地为氢或有机基团的基团; R6和R7可以与相邻基团-XA-N-XB-一起形成环; XA和XB各自独立地为键，低级亚烷基等

公开(公告)号：US08822453B2

公开(公告)日：2014-09-02

申请号：US13388442

申请日：2010-08-20

申请人： Shuuji Matsumura ,  Hokuto Yamabe ,  Naohiro Isono ,  Noriaki Takemura ,  Takashi Oshiyama ,  Tsuyoshi Nagase ,  Masataka Ueda ,  Kuninori Tai

发明人： Shuuji Matsumura ,  Hokuto Yamabe ,  Naohiro Isono ,  Noriaki Takemura ,  Takashi Oshiyama ,  Tsuyoshi Nagase ,  Masataka Ueda ,  Kuninori Tai

IPC分类号： C07D243/12 ,  C07D409/12 ,  C07D495/04 ,  A61K31/551 ,  A61K31/4985 ,  A61P9/06 ,  C07D401/14 ,  C07D471/04 ,  C07D403/12 ,  C07D403/14 ,  C07D401/12

CPC分类号： C07D491/048 ,  C07D213/38 ,  C07D215/227 ,  C07D243/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04

摘要： The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1) or a salt thereof, wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo; Y1 and Y2 are each independently —N═ or —CH═; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—; XA and XB are each independently a bond, lower alkylene, etc.

摘要翻译： 本发明提供了一种新颖的二氮杂类化合物，其比其他K +通道有效地和选择性地阻断IK电流或Kv1.5通道。 本发明涉及由通式（1）表示的二氮杂化合物或其盐，其中R 1，R 2，R 3和R 4各自独立地为氢，低级烷基，环低级烷基或低级烷氧基低级烷基; R2和R3可以连接形成低级亚烷基; A1是任选被一个或多个选自羟基和氧代的取代基取代的低级亚烷基; Y1和Y2各自独立地为-N =或-CH =; 并且R 5为其中R 6和R 7各自独立地为氢或有机基团的基团; R6和R7可以与相邻基团-XA-N-XB-一起形成环; XA和XB各自独立地为键，低级亚烷基等

公开(公告)号：US08664217B2

公开(公告)日：2014-03-04

申请号：US13591361

申请日：2012-08-22

申请人： Kunio Oshima ,  Takashi Oshiyama ,  Shinichi Taira ,  Yasuhiro Menjo ,  Hokuto Yamabe ,  Shuuji Matsumura ,  Masataka Ueda ,  Yasuo Koga ,  Kuninori Tai ,  Sunao Nakayama ,  Toshiyuki Onogawa ,  Kenji Tsujimae

发明人： Kunio Oshima ,  Takashi Oshiyama ,  Shinichi Taira ,  Yasuhiro Menjo ,  Hokuto Yamabe ,  Shuuji Matsumura ,  Masataka Ueda ,  Yasuo Koga ,  Kuninori Tai ,  Sunao Nakayama ,  Toshiyuki Onogawa ,  Kenji Tsujimae

IPC分类号： C07D243/12 ,  C07D401/12 ,  C07D401/14 ,  C07D491/04 ,  C07D405/14 ,  C07D417/14

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04

摘要： The present invention provides a novel benzodiazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The benzodiazepine compound of the invention is represented by General Formula (1) wherein R1, R2, R3, and R4 are each independently hydrogen or lower alkyl; R2 and R3 may be linked to form lower alkylene; Al is lower alkylene optionally substituted with one or more hydroxy; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; XA and XB are each independently bond, lower alkylene, etc.

摘要翻译： 本发明提供了一种新颖的苯并二氮杂化合物，其比其他K +通道有效地和更有选择地阻断IK电流或Kv1.5通道。 本发明的苯并二氮杂化合物由通式（1）表示，其中R 1，R 2，R 3和R 4各自独立地为氢或低级烷基; R2和R3可以连接形成低级亚烷基; Al是任选被一个或多个羟基取代的低级亚烷基; 并且R 5为其中R 6和R 7各自独立地为氢或有机基团的基团; XA和XB各自独立地键合，低级亚烷基等。

公开(公告)号：US20130040941A1

公开(公告)日：2013-02-14

申请号：US13591361

申请日：2012-08-22

申请人： Kunio Oshima ,  Takashi Oshiyama ,  Shinichi Taira ,  Yasuhiro Menjo ,  Hokuto Yamabe ,  Shuuji Matsumura ,  Masataka Ueda ,  Yasuo Koga ,  Kuninori Tai ,  Sunao Nakayama ,  Toshiyuki Onogawa ,  Kenji Tsujimae

发明人： Kunio Oshima ,  Takashi Oshiyama ,  Shinichi Taira ,  Yasuhiro Menjo ,  Hokuto Yamabe ,  Shuuji Matsumura ,  Masataka Ueda ,  Yasuo Koga ,  Kuninori Tai ,  Sunao Nakayama ,  Toshiyuki Onogawa ,  Kenji Tsujimae

IPC分类号： A61K31/551 ,  C07D243/12 ,  C07D491/048 ,  C07D409/14 ,  C07D495/04 ,  A61P9/06 ,  C07D405/14 ,  C07D413/14 ,  C07D401/12 ,  C07D471/04 ,  C07D513/04 ,  C07D417/14 ,  C07D403/12 ,  C07D401/14

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04

摘要： The present invention provides a novel benzodiazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The benzodiazepine compound of the invention is represented by General Formula (1) wherein R1, R2, R3, and R4 are each independently hydrogen or lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more hydroxy; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; XA and XB are each independently bond, lower alkylene, etc.

摘要翻译： 本发明提供了一种新颖的苯并二氮杂化合物，其比其他K +通道有效地和更有选择地阻断IK电流或Kv1.5通道。 本发明的苯并二氮杂化合物由通式（1）表示，其中R 1，R 2，R 3和R 4各自独立地为氢或低级烷基; R2和R3可以连接形成低级亚烷基; A1是任选被一个或多个羟基取代的低级亚烷基; 并且R 5为其中R 6和R 7各自独立地为氢或有机基团的基团; XA和XB各自独立地键合，低级亚烷基等。

公开(公告)号：US08338406B2

公开(公告)日：2012-12-25

申请号：US12918226

申请日：2009-02-20

申请人： Kunio Oshima ,  Takashi Oshiyama ,  Shinichi Taira ,  Yasuhiro Menjo ,  Hokuto Yamabe ,  Shuuji Matsumura ,  Masataka Ueda ,  Yasuo Koga ,  Kuninori Tai ,  Sunao Nakayama ,  Toshiyuki Onogawa ,  Kenji Tsujimae

发明人： Kunio Oshima ,  Takashi Oshiyama ,  Shinichi Taira ,  Yasuhiro Menjo ,  Hokuto Yamabe ,  Shuuji Matsumura ,  Masataka Ueda ,  Yasuo Koga ,  Kuninori Tai ,  Sunao Nakayama ,  Toshiyuki Onogawa ,  Kenji Tsujimae

IPC分类号： C07D243/12 ,  C07D401/12 ,  C07D401/14 ,  C07D491/04 ,  C07D405/14 ,  C07D417/14 ,  A61K31/551 ,  A61P9/06

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04

摘要： The present invention provides a novel benzodiazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The benzodiazepine compound of the invention is represented by General Formula (1) wherein R1, R2, R3, and R4 are each independently hydrogen or lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more hydroxy; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; XA and XB are each independently bond, lower alkylene, etc.

摘要翻译： 本发明提供了一种新颖的苯并二氮杂化合物，其比其他K +通道有效地和更有选择地阻断IK电流或Kv1.5通道。 本发明的苯并二氮杂化合物由通式（1）表示，其中R 1，R 2，R 3和R 4各自独立地为氢或低级烷基; R2和R3可以连接形成低级亚烷基; A1是任选被一个或多个羟基取代的低级亚烷基; 并且R 5为其中R 6和R 7各自独立地为氢或有机基团的基团; XA和XB各自独立地键合，低级亚烷基等。

公开(公告)号：US20100331317A1

公开(公告)日：2010-12-30

申请号：US12918226

申请日：2009-02-20

申请人： Kunio Oshima ,  Takashi Oshiyama ,  Shinichi Taira ,  Yasuhiro Menjo ,  Hokuto Yamabe ,  Shuuji Matsumura ,  Masataka Ueda ,  Yasuo Koga ,  Kuninori Tai ,  Sunao Nakayama ,  Toshiyuki Onogawa ,  Kenji Tsujimae

发明人： Kunio Oshima ,  Takashi Oshiyama ,  Shinichi Taira ,  Yasuhiro Menjo ,  Hokuto Yamabe ,  Shuuji Matsumura ,  Masataka Ueda ,  Yasuo Koga ,  Kuninori Tai ,  Sunao Nakayama ,  Toshiyuki Onogawa ,  Kenji Tsujimae

IPC分类号： A61K31/551 ,  C07D243/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  A61P9/06

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04

摘要： The present invention provides a novel benzodiazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The benzodiazepine compound of the invention is represented by General Formula (1) wherein R1, R2, R3, and R4 are each independently hydrogen or lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more hydroxy; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; XA and XB are each independently bond, lower alkylene, etc.

摘要翻译： 本发明提供了一种新颖的苯并二氮杂化合物，其比其他K +通道有效地和更有选择地阻断IKur电流或Kv1.5通道。 本发明的苯并二氮杂化合物由通式（1）表示，其中R 1，R 2，R 3和R 4各自独立地为氢或低级烷基; R2和R3可以连接形成低级亚烷基; A1是任选被一个或多个羟基取代的低级亚烷基; 并且R 5为其中R 6和R 7各自独立地为氢或有机基团的基团; XA和XB各自独立地键合，低级亚烷基等。