公开(公告)号：US20090318478A1

公开(公告)日：2009-12-24

申请号：US12310025

申请日：2007-07-24

申请人： Akira Asagarasu ,  Shuichiro Sato ,  Makoto Okada

发明人： Akira Asagarasu ,  Shuichiro Sato ,  Makoto Okada

IPC分类号： A61K31/517 ,  C07D239/88 ,  C07D401/06

CPC分类号： C07D239/91 ,  C07D401/06 ,  C07D409/06

摘要： The invention discloses quinazoline derivatives or salts thereof, which possess PDE9-inhibiting activity and are useful as treating agents of dysuria and the like, the derivatives being represented by the formula (I) in the formula, R1 stands for phenyl or aromatic heterocyclic group which are optionally substituted with 1-3 substituents selected from halogen, C1-6 alkyl, C1-6 haloalkyl containing 1-6 halogen atoms and C1-6 alkoxy; and n is an integer of 1-3.

摘要翻译： 本发明公开了具有PDE9抑制活性的喹唑啉衍生物或其盐，可用作排尿困难等的治疗剂，该衍生物由式中的式（I）表示，R 1表示苯基或芳族杂环基， 任选被1-3个选自卤素，C 1-6烷基，含有1-6个卤原子的C 1-6卤代烷基和C 1-6烷氧基取代的取代基取代; n为1-3的整数。

公开(公告)号：US08299080B2

公开(公告)日：2012-10-30

申请号：US12448212

申请日：2007-12-12

申请人： Makoto Okada ,  Shuichiro Sato ,  Kenji Kawade ,  Kotaro Gotanda ,  Atsushi Shinbo ,  Youichi Nakano ,  Hideo Kobayashi

发明人： Makoto Okada ,  Shuichiro Sato ,  Kenji Kawade ,  Kotaro Gotanda ,  Atsushi Shinbo ,  Youichi Nakano ,  Hideo Kobayashi

IPC分类号： A61K31/495

CPC分类号： C07D487/04 ,  C07D487/14

摘要： The invention discloses quinoxaline derivatives or salts thereof having PDE9-inhibiting activity and being useful as treating agent of dysuria and the like, which are represented by the formula (I) in the formula, R1 and R2 each independently stands for hydrogen, halogen, alkyl, alkoxy, acyl, amino and the like, R3 stands for alkyl, aryl, saturated carbocyclic group, saturated heterocyclic group, acyl and the like, R4 stands for hydrogen, hydroxy, alkyl or amino, R5 and R8 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkoxy, cyano or nitro, R6 and R7 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, cyano, amino, carbocyclic group, heterocyclic group, COR9 or SO2R9, R9 stands for hydrogen, hydroxy, alkyl, amino, pyrrolidin-1-yl, piperidin-1-yl, pyperazin-1-yl or the like, X stands for S or O, and A1, A2 and A3 each independently stands for N or C.

摘要翻译： 本发明公开了具有PDE9抑制活性的喹喔啉衍生物或其盐，可用作式（I）所示的排尿困难等的治疗剂，R 1和R 2各自独立地表示氢，卤素，烷基 烷氧基，酰基，氨基等，R3代表烷基，芳基，饱和碳环基，饱和杂环基，酰基等，R4代表氢，羟基，烷基或氨基，R5和R8各自独立代表氢， 卤素，烷基，烯基，烷氧基，氰基或硝基，R6和R7各自独立地代表氢，卤素，烷基，烯基，炔基，烷氧基，氰基，氨基，碳环基，杂环基，COR9或SO2R9，R9代表氢， 羟基，烷基，氨基，吡咯烷-1-基，哌啶-1-基，哒嗪-1-基等，X表示S或O，并且，A1，A2和A3各自独立地表示N或C.

公开(公告)号：US20100048556A1

公开(公告)日：2010-02-25

申请号：US12448212

申请日：2007-12-12

申请人： Makoto Okada ,  Shuichiro Sato ,  Kenji Kawade ,  Kotaro Gotanda ,  Atsushi Shinbo ,  Youichi Nakano ,  Hideo Kobayashi

发明人： Makoto Okada ,  Shuichiro Sato ,  Kenji Kawade ,  Kotaro Gotanda ,  Atsushi Shinbo ,  Youichi Nakano ,  Hideo Kobayashi

IPC分类号： A61K31/5377 ,  C07D471/04 ,  C07D413/02 ,  A61K31/5025 ,  A61P9/10 ,  A61P13/10 ,  A61P13/12

CPC分类号： C07D487/04 ,  C07D487/14

摘要： The invention discloses quinoxaline derivatives or salts thereof having PDE9-inhibiting activity and being useful as treating agent of dysuria and the like, which are represented by the formula (I) in the formula, R1 and R2 each independently stands for hydrogen, halogen, alkyl, alkoxy, acyl, amino and the like, R3 stands for alkyl, aryl, saturated carbocyclic group, saturated heterocyclic group, acyl and the like, R4 stands for hydrogen, hydroxy, alkyl or amino, R5 and R8 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkoxy, cyano or nitro, R6 and R7 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, cyano, amino, carbocyclic group, heterocyclic group, COR9 or SO2R9, R9 stands for hydrogen, hydroxy, alkyl, amino, pyrrolidin-1-yl, piperidin-1-yl, pyperazin-1-yl or the like, X stands for S or O, and A1, A2 and A3 each independently stands for N or C.

摘要翻译： 本发明公开了具有PDE9抑制活性的喹喔啉衍生物或其盐，可用作式（I）所示的排尿困难等的治疗剂，R 1和R 2各自独立地表示氢，卤素，烷基 烷氧基，酰基，氨基等，R3代表烷基，芳基，饱和碳环基，饱和杂环基，酰基等，R4代表氢，羟基，烷基或氨基，R5和R8各自独立代表氢， 卤素，烷基，烯基，烷氧基，氰基或硝基，R6和R7各自独立地代表氢，卤素，烷基，烯基，炔基，烷氧基，氰基，氨基，碳环基，杂环基，COR9或SO2R9，R9代表氢， 羟基，烷基，氨基，吡咯烷-1-基，哌啶-1-基，哒嗪-1-基等，X表示S或O，并且，A1，A2和A3各自独立地表示N或C.

公开(公告)号：US6020531A

公开(公告)日：2000-02-01

申请号：US230279

申请日：1999-01-25

申请人： Masafumi Shiraiwa ,  Shuichiro Sato ,  Koji Doguchi

发明人： Masafumi Shiraiwa ,  Shuichiro Sato ,  Koji Doguchi

IPC分类号： C07C323/22 ,  C07D333/54 ,  C07C47/52 ,  C07C45/00 ,  C07D333/52 ,  C07D333/56

CPC分类号： C07C323/22 ,  C07D333/54

摘要： A benzothiophene compound represented by a formula: ##STR1## wherein R.sup.1 represents a lower alkyl group, and R.sup.2 represents a halogen atom; a lower alkyl group; or a cycloalkyl group or cycloalkenyl group which may optionally be substituted with a lower alkyl group, a hydroxy group, an acyloxy group or an oxo group,which is a useful intermediate for synthesizing a 2-sub-stituted-3-(4-substituted benzoyl)-6-hydroxybenzo[b]-thiophene derivative having an antiestrogenic activity can be produced in an industrially advantageous manner by subjecting a compound represented by a formula: ##STR2## to a ring-closing reaction. Further, the novel compound of the formula (II) described above is a useful intermediate in the process of the present invention.

摘要翻译： PCT No.PCT / JP97 / 02440 Sec。 371日期1999年1月25日 102（e）1999年1月25日PCT PCT 1997年7月15日PCT公布。 第WO98 / 03501号公报 日期：1998年1月29日一种由下式表示的苯并噻吩化合物：其中R1表示低级烷基，R2表示卤素原子; 低级烷基; 或可选地被低级烷基，羟基，酰氧基或氧代基取代的环烷基或环烯基，其是合成2-取代的3-（4-取代的） 苯甲酰基）-6-羟基苯并[b] - 噻吩衍生物可以通过使下式表示的化合物进行闭环反应，以工业上有利的方式制备。 此外，上述式（II）的新型化合物是本发明方法中有用的中间体。

公开(公告)号：US08829000B2

公开(公告)日：2014-09-09

申请号：US13617683

申请日：2012-09-14

申请人： Makoto Okada ,  Shuichiro Sato ,  Kenji Kawade ,  Kotaro Gotanda ,  Atsushi Shinbo ,  Youichi Nakano ,  Hideo Kobayashi

发明人： Makoto Okada ,  Shuichiro Sato ,  Kenji Kawade ,  Kotaro Gotanda ,  Atsushi Shinbo ,  Youichi Nakano ,  Hideo Kobayashi

IPC分类号： A61K31/4985 ,  C07D487/04 ,  C07D487/14

CPC分类号： C07D487/04 ,  C07D487/14

摘要： The invention discloses quinoxaline derivatives or salts thereof having PDE9-inhibiting activity and being useful as treating agent of dysuria and the like, which are represented by the formula (I) in the formula, R1 and R2 each independently stands for hydrogen, halogen, alkyl, alkoxy, acyl, amino and the like, R3 stands for alkyl, aryl, saturated carbocyclic group, saturated heterocyclic group, acyl and the like, R4 stands for hydrogen, hydroxy, alkyl or amino, R5 and R8 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkoxy, cyano or nitro, R6 and R7 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, cyano, amino, carbocyclic group, heterocyclic group, COR9 or SO2R9, R9 stands for hydrogen, hydroxy, alkyl, amino, pyrrolidin-1-yl, piperidin-1-yl, pyperazin-1-yl or the like, X stands for S or O, and A1, A2 and A3 each independently stands for N or C.

摘要翻译： 本发明公开了具有PDE9抑制活性的喹喔啉衍生物或其盐，可用作式（I）所示的排尿困难等的治疗剂，R 1和R 2各自独立地表示氢，卤素，烷基 烷氧基，酰基，氨基等，R3代表烷基，芳基，饱和碳环基，饱和杂环基，酰基等，R4代表氢，羟基，烷基或氨基，R5和R8各自独立代表氢， 卤素，烷基，烯基，烷氧基，氰基或硝基，R6和R7各自独立地代表氢，卤素，烷基，烯基，炔基，烷氧基，氰基，氨基，碳环基，杂环基，COR9或SO2R9，R9代表氢， 羟基，烷基，氨基，吡咯烷-1-基，哌啶-1-基，哒嗪-1-基等，X表示S或O，并且，A1，A2和A3各自独立地表示N或C.