公开(公告)号：US20070185116A1

公开(公告)日：2007-08-09

申请号：US11597890

申请日：2005-05-30

申请人： Miki Hirai ,  Mari Kusama ,  Toshihiro Hosaka ,  Shuntarou Kohnomi

发明人： Miki Hirai ,  Mari Kusama ,  Toshihiro Hosaka ,  Shuntarou Kohnomi

IPC分类号： A61K31/44 ,  A61K31/505 ,  C07D213/02 ,  C07D239/24

CPC分类号： C07D213/55 ,  C07D213/56 ,  C07D213/57 ,  C07D213/61 ,  C07D213/64 ,  C07D239/26 ,  C07D239/30 ,  C07D239/34 ,  C07D239/42 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D409/04

摘要： The present invention is to provide a bicyclic compound represented by the following formula: wherein Ring Q is pyridine or pyrimidine; Ring A is benzene or a heterocyclic ring; G is Ring B optionally having a substituent(s) R3, or an amino optionally substituted by one or two selected from the group consisting of alkyl(s), aralkyl(s) and cycloalkyl(s); Ring B is benzene, a heterocyclic ring, a cycloalkane or a cycloalkene; R1 is a group selected from the following formulae: R2 and R3 may be the same or different from each other, and each is cyano, nitro, etc.; m is 0, 1 or 2; R4 is hydrogen, a halogen, etc.; and R5 and R6 may be the same or different from each other, and each is hydrogen, an optionally substituted alkyl, etc., or a pharmaceutically acceptable salt thereof, which is a large conductance calcium-activated K channel opener useful for treatment of pollakiuria, urinary incontinence, etc.

摘要翻译： 本发明提供由下式表示的双环化合物：其中环Q是吡啶或嘧啶; 环A是苯或杂环; G是任选具有取代基R 3的环B，或任选被一个或两个选自烷基，芳烷基和环烷基的一个或两个取代基的氨基， ; 环B是苯，杂环，环烷烃或环烯烃; R 1是选自下式的基团：R 2和R 3可以彼此相同或不同，并且各自为 氰基，硝基等; m为0,1或2; R 4是氢，卤素等; R 5和R 6可以彼此相同或不同，各自为氢，任选取代的烷基等，或其药学上可接受的盐， 这是一种用于治疗尿频，尿失禁等的大电导钙激活K通道开放剂

公开(公告)号：US07531655B2

公开(公告)日：2009-05-12

申请号：US10531330

申请日：2003-10-15

申请人： Toshihiro Hosaka ,  Mari Kusama ,  Kiyomi Ohba ,  Rikako Kono ,  Shuntarou Kohnomi

发明人： Toshihiro Hosaka ,  Mari Kusama ,  Kiyomi Ohba ,  Rikako Kono ,  Shuntarou Kohnomi

IPC分类号： C07D409/14

CPC分类号： A61K31/343 ,  A61K31/381 ,  C07D207/337 ,  C07D307/54 ,  C07D333/24 ,  C07D333/28 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14

摘要： There are disclosed a large conductance calcium-activated K channel opener comprising a compound of the formula (I): wherein ring A is a 5-membered heterocyclic ring containing any one of O, N or S, which ring may be substituted by R4, R1 is aryl, heterocyclic or heterocycle-substituted carbonyl; R2 is hydrogen, halogen, carboxy, amino, alkyl, alkoxycarbonyl, alkenyl or cycloalkyl; R3 is aryl, heterocyclic or alkyl; and R4 is hydrogen or alkyl, each of substituents may be substituted, or a pharmaceutically acceptable salt thereof as an active ingredient.

摘要翻译： 公开了包含式（I）化合物的大电导钙激活K通道开放剂：其中环A是含有O，N或S中任一个的5元杂环，该环可以被R4取代， R 1是芳基，杂环或杂环取代的羰基; R2是氢，卤素，羧基，氨基，烷基，烷氧基羰基，烯基或环烷基; R3是芳基，杂环或烷基; R 4为氢或烷基，各取代基可被取代，或其药学上可接受的盐作为活性成分。

公开(公告)号：US20060135597A1

公开(公告)日：2006-06-22

申请号：US10531330

申请日：2002-10-15

申请人： Toshihiro Hosaka ,  Mari Kusama ,  Kiyomi Ohba ,  Rikako Kono ,  Shuntarou Kohnomi

发明人： Toshihiro Hosaka ,  Mari Kusama ,  Kiyomi Ohba ,  Rikako Kono ,  Shuntarou Kohnomi

IPC分类号： A61K31/381 ,  A61K31/343

CPC分类号： A61K31/343 ,  A61K31/381 ,  C07D207/337 ,  C07D307/54 ,  C07D333/24 ,  C07D333/28 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14

摘要： There are disclosed a large conductance calcium-activated K channel opener comprising a compound of the formula (I): wherein ring A is a 5-membered heterocyclic ring containing any one of O, N or S, which ring may be substituted by R4, R1 is aryl, heterocyclic or heterocycle-substituted carbonyl; R2 is hydrogen, halogen, carboxy, amino, alkyl, alkoxycarbonyl, alkenyl or cycloalkyl; R3 is aryl, heterocyclic or alkyl; and R4 is hydrogen or alkyl, each of substituents may be substituted, or a pharmaceutically acceptable salt thereof as an active ingredient.

摘要翻译： 公开了一种包含式（I）化合物的大电导钙活化K通道开放剂：其中环A是含有O，N或S中任一个的5元杂环， O 4，R 1是芳基，杂环或杂环取代的羰基; R 2是氢，卤素，羧基，氨基，烷基，烷氧基羰基，烯基或环烷基; R 3是芳基，杂环或烷基; R 4是氢或烷基，各取代基可被取代，或其药学上可接受的盐作为活性成分。

公开(公告)号：US20070060629A1

公开(公告)日：2007-03-15

申请号：US10574529

申请日：2004-10-15

申请人： Yasuhiro Imanishi ,  Nobumasa Awai ,  Miki Hirai ,  Toshihiro Hosaka ,  Rikako Kono

发明人： Yasuhiro Imanishi ,  Nobumasa Awai ,  Miki Hirai ,  Toshihiro Hosaka ,  Rikako Kono

IPC分类号： C07D231/12 ,  C07D261/06 ,  A61K31/42 ,  A61K31/415

CPC分类号： C07D231/12 ,  A61K31/415 ,  A61K31/42 ,  C07D231/38 ,  C07D261/08 ,  C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04

摘要： The present invention provides a large conductance calcium-activated K channel opener comprising a compound of the formula (I): wherein R1 and R3 are each sulfonamide, carbamoyl, acyl, amino, and the like, m and n are each 0 to 2, R2 and R4 are each cyano, nitro, hydroxyl, an alkoxy, a halogen, or an alkyl, Ring A is benzene or a heterocyclic ring, Ring B is benzene, a heterocyclic ring, a cycloalkane etc, and Ring Q is pyrazole or isoxazole, or a pharmaceutically acceptable salt thereof as an active ingredient.

摘要翻译： 本发明提供了包含式（I）化合物的大电导钙激活K通道开放剂：其中R 1和R 3各自为磺酰胺，氨基甲酰基，酰基 ，氨基等，m和n各自为0至2，R 2和R 4各自为氰基，硝基，羟基，烷氧基，卤素或 烷基，环A是苯或杂环，环B是苯，杂环，环烷烃等，环Q是吡唑或异恶唑或其药学上可接受的盐作为活性成分。

公开(公告)号：US07759373B2

公开(公告)日：2010-07-20

申请号：US10474850

申请日：2002-04-15

申请人： Mitsuya Hongu ,  Toshihiro Hosaka ,  Toshihiko Kashiwagi ,  Rikako Kono ,  Hiroyuki Kobayashi

发明人： Mitsuya Hongu ,  Toshihiro Hosaka ,  Toshihiko Kashiwagi ,  Rikako Kono ,  Hiroyuki Kobayashi

IPC分类号： A01N43/78 ,  A61K31/425 ,  C07D277/04 ,  C07D277/06

CPC分类号： C07D277/20 ,  A61K31/00 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/421 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/506 ,  C07D233/54 ,  C07D233/68 ,  C07D263/30 ,  C07D263/32 ,  C07D263/34 ,  C07D333/04 ,  C07D333/28 ,  C07D333/52

摘要： A large conductance calcium-activated K channel opener comprising as an active ingredient a nitrogen-containing 5-membered heterocyclic compound represented by the following formula (I): wherein X represents N—R4, O or S, R1 and R2 each independently represent hydrogen, halogen, carboxyl, amino, lower alkyl, lower alkoxycarbonyl, lower alkenyl, cyclo-lower alkyl, carbamoyl, aryl, heterocyclic or heterocyclic-substituted carbonyl group, R3 represents aryl, heterocyclic or lower alkyl group, and R4 represents hydrogen or lower alkyl group, or a pharmaceutically acceptable salt thereof.

摘要翻译： 一种大电导钙活化的K通道开放剂，其包含作为活性成分的由下式（I）表示的含氮5元杂环化合物：其中X表示N-R 4，O或S，R 1和R 2各自独立地表示氢 ，卤素，羧基，氨基，低级烷基，低级烷氧基羰基，低级烯基，环低级烷基，氨基甲酰基，芳基，杂环或杂环取代的羰基，R3表示芳基，杂环或低级烷基，R4表示氢或低级烷基 基团或其药学上可接受的盐。

公开(公告)号：US20100256165A1

公开(公告)日：2010-10-07

申请号：US12795323

申请日：2010-06-07

申请人： Mitsuya Hongu ,  Toshihiro Hosaka ,  Toshihiko Kashiwagi ,  Rikako Kono ,  Hiroyuki Kobayashi

发明人： Mitsuya Hongu ,  Toshihiro Hosaka ,  Toshihiko Kashiwagi ,  Rikako Kono ,  Hiroyuki Kobayashi

IPC分类号： A61K31/497 ,  C07D233/64 ,  A61K31/4178 ,  C07D401/14 ,  A61K31/4439 ,  C07D217/14 ,  A61K31/4725 ,  C07D403/04 ,  A61P13/00 ,  A61P9/10

CPC分类号： C07D277/20 ,  A61K31/00 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/421 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/506 ,  C07D233/54 ,  C07D233/68 ,  C07D263/30 ,  C07D263/32 ,  C07D263/34 ,  C07D333/04 ,  C07D333/28 ,  C07D333/52

摘要： A large conductance calcium-activated K channel opener comprising as an active ingredient a nitrogen-containing 5-membered heterocyclic compound represented by the following formula (I): wherein X represents N—R4, O or S, R1 and R2 each independently represent hydrogen, halogen, carboxyl, amino, lower alkyl, lower alkoxycarbonyl, lower alkenyl, cyclo-lower alkyl, carbamoyl, aryl, heterocyclic or heterocyclic-substituted carbonyl group, R3 represents aryl, heterocyclic or lower alkyl group, and R4 represents hydrogen or lower alkyl group, or a pharmaceutically acceptable salt thereof.

摘要翻译： 一种大电导钙活化的K通道开放剂，其包含作为活性成分的由下式（I）表示的含氮5元杂环化合物：其中X表示N-R 4，O或S，R 1和R 2各自独立地表示氢 ，卤素，羧基，氨基，低级烷基，低级烷氧基羰基，低级烯基，环低级烷基，氨基甲酰基，芳基，杂环或杂环取代的羰基，R3表示芳基，杂环或低级烷基，R4表示氢或低级烷基 基团或其药学上可接受的盐。

公开(公告)号：US20080009506A1

公开(公告)日：2008-01-10

申请号：US11662948

申请日：2005-09-16

申请人： Mari Kusama ,  Tatsuya Watanabe ,  Toshihiro Hosaka ,  Yuko Kubota

发明人： Mari Kusama ,  Tatsuya Watanabe ,  Toshihiro Hosaka ,  Yuko Kubota

IPC分类号： A61K31/4178 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/42 ,  A61K31/44 ,  A61K31/47 ,  A61K31/506 ,  A61P13/00 ,  C07D215/12 ,  C07D403/14 ,  C07D403/04 ,  C07D401/04 ,  C07D277/30 ,  C07D263/08 ,  C07D235/02 ,  C07D233/60 ,  C07D233/56 ,  C07D233/00 ,  C07D513/04 ,  C07D413/04 ,  A61P9/00 ,  A61P11/06 ,  A61K31/497 ,  A61K31/4439 ,  A61K31/425 ,  A61K31/4184 ,  A61K31/4168

CPC分类号： C07D233/64 ,  C07D401/04 ,  C07D403/10 ,  C07D409/04 ,  C07D487/04

摘要： An imidazole compound of the formula: wherein Ring A is benzene or a heterocyclic ring; G is alkylthio, alkylsulfonyl, optionally substituted phenyl, or optionally substituted heterocyclic ring group, etc.; Ring C is imidazole; R1 is carbamoyl, etc.; R2 is cyano, nitro, hydroxyl, an alkoxy, a halogen, carboxy, an alkoxycarbonyl, carbamoyl, amino, an alkyl, etc.; m is 0 to 2; and R4 is hydrogen, an alkyl, etc., or a pharmaceutically acceptable salt thereof, is a large conductance calcium-activated K channel opener useful for treatment of pollakiuria, urinary incontinence, etc.

摘要翻译： 下式的咪唑化合物：其中环A是苯或杂环; G是烷硫基，烷基磺酰基，任选取代的苯基或任选取代的杂环基团等; 环C是咪唑; R 1是氨基甲酰基等; R 2是氰基，硝基，羟基，烷氧基，卤素，羧基，烷氧基羰基，氨基甲酰基，氨基，烷基等; m为0〜2; R 4是氢，烷基等或其药学上可接受的盐，是用于治疗尿频，尿失禁等的大电导钙激活K通道开放剂。

公开(公告)号：US20050075359A1

公开(公告)日：2005-04-07

申请号：US10665528

申请日：2003-09-22

申请人： Rikako Kono ,  Shuntarou Kohnomi ,  Hajime Aihara ,  Toshihiro Hosaka ,  Toshihiko Kashiwagi

发明人： Rikako Kono ,  Shuntarou Kohnomi ,  Hajime Aihara ,  Toshihiro Hosaka ,  Toshihiko Kashiwagi

IPC分类号： A61K31/33 ,  A61K31/415 ,  A61K31/4439 ,  A61K31/18 ,  A61K31/40 ,  A61K31/42 ,  A61K31/425

CPC分类号： A61K31/33 ,  A61K31/415

摘要： There is disclosed a large conductance calcium-activated K channel opener comprising a compound of the formula (I): wherein R1 is aminosulfonyl, alkylsulfonyl, etc., R2 is hydrogen or halogen, R3 and R4 are hydrogen, halogen, alkyl or alkoxy, Ring A is benzene, pyridine, etc., and Ring Q is pyrazol, isoxazol, etc., and Ring Q and Ring A may be combined to each other to form a fused ring of the formula: where X is S or O, R5 is halogen, alkyl, etc., and R3 and R4 are the same as mentioned above, or a pharmaceutically acceptable salt thereof as an active ingredient.

摘要翻译： 公开了一种大电导钙活化的K通道开放剂，其包含式（I）化合物：其中R 1是氨基磺酰基，烷基磺酰基等，R 2是氢或卤素，R 3和R 4，是氢，卤素，烷基或烷氧基，环A是苯，吡啶等，环Q是吡唑，异恶唑等，并且环Q和环A可以相互结合形成稠环 其中X是S或O，R 5是卤素，烷基等，R 3和R 4与上述相同，或其药学上可接受的盐作为活性成分 。