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    Thienopyrimidine derivatives
    1.
    发明授权
    Thienopyrimidine derivatives 有权
    噻吩并嘧啶衍生物

    公开(公告)号：US08293754B2

    公开(公告)日：2012-10-23

    申请号：US11922233

    申请日：2006-06-13

    申请人： Kotaro Gotanda ,  Atsushi Shinbo ,  Youichi Nakano ,  Hideo Kobayashi ,  Makoto Okada ,  Akira Asagarasu

    发明人： Kotaro Gotanda ,  Atsushi Shinbo ,  Youichi Nakano ,  Hideo Kobayashi ,  Makoto Okada ,  Akira Asagarasu

    IPC分类号： C07D495/04 ,  A61K31/519 ,  A61P25/28

    CPC分类号： C07D495/04

    摘要： This invention provides thienopyrimidine derivatives of the formula, wherein R1 stands for hydrogen atom, an alkyl group or the like; R2 stands for a hydrogen atom, an alkyl or amino group or the like, R3 stands for an alkyl, alkenyl or alkylthio group or the like or a group Y—X—; or R2 and R3 may together form tetramethylene group; X standing for a direct bond or linking group such as CH2, CH(OH), S, O, NH; Y standing for a substituted or unsubstituted aromatic carbocycylic, aromatic heterocylic, cycloalkyl or saturated heterocyclic group or the like; Z stands for S or O, and n is 0 or an integer of 1 to 4, or salts thereof, which exhibit an inhibitory effect on PDE9, and are therefore useful for prevention or treatment of overactive bladder syndrome, pollakiuria, urinary incontinence, dysuria associated with prostatic hyperplasia, urolithiasis, Alzheimer's disease, chronic obstructive pulmonary disease, myocardial infarction, thrombosis, diabetes and the like.

    摘要翻译： 本发明提供下式的噻吩并嘧啶衍生物，其中R1代表氢原子，烷基等; R2表示氢原子，烷基或氨基等，R3表示烷基，烯基或烷硫基等或Y-X-基团; 或者R 2和R 3可以一起形成四亚甲基; X代表直接键或连接基团如CH 2，CH（OH），S，O，NH; Y表示取代或未取代的芳族碳环，芳香杂环，环烷基或饱和杂环基等; Z代表S或O，n为0或1〜4的整数，或其盐，对PDE9具有抑制作用，因此可用于预防或治疗膀胱过度活动症，尿频尿失禁，排尿困难 与前列腺增生，尿石症，阿尔茨海默病，慢性阻塞性肺疾病，心肌梗塞，血栓形成，糖尿病等相关。

    Thienopyrimidine Derivatives
    3.
    发明申请
    Thienopyrimidine Derivatives 有权
    噻吩并嘧啶衍生物

    公开(公告)号：US20090203703A1

    公开(公告)日：2009-08-13

    申请号：US11922233

    申请日：2006-06-13

    申请人： Kotaro Gotanda ,  Atsushi Shinbo ,  Youichi Nakano ,  Hideo Kobayashi ,  Makoto Okada ,  Akira Asagarasu

    发明人： Kotaro Gotanda ,  Atsushi Shinbo ,  Youichi Nakano ,  Hideo Kobayashi ,  Makoto Okada ,  Akira Asagarasu

    IPC分类号： A61K31/4985 ,  C07D495/04 ,  A61K31/519

    CPC分类号： C07D495/04

    摘要： This invention provides thienopyrimidine derivatives of the formula, wherein R1 stands for hydrogen atom, an alkyl group or the like; R2 stands for a hydrogen atom, an alkyl or amino group or the like, R3 stands for an alkyl, alkenyl or alkylthio group or the like or a group Y—X—; or R2 and R3 may together form tetramethylene group; X standing for a direct bond or linking group such as CH2, CH(OH), S, O, NH; Y standing for a substituted or unsubstituted aromatic carbocycylic, aromatic heterocylic, cycloalkyl or saturated heterocyclic group or the like; Z stands for S or O, and n is 0 or an integer of 1 to 4, or salts thereof, which exhibit an inhibitory effect on PDE9, and are therefore useful for prevention or treatment of overactive bladder syndrome, pollakiuria, urinary incontinence, dysuria associated with prostatic hyperplasia, urolithiasis, Alzheimer's disease, chronic obstructive pulmonary disease, myocardial infarction, thrombosis, diabetes and the like.

    摘要翻译： 本发明提供下式的噻吩并嘧啶衍生物，其中R1代表氢原子，烷基等; R2表示氢原子，烷基或氨基等，R3表示烷基，烯基或烷硫基等或Y-X-基团; 或者R 2和R 3可以一起形成四亚甲基; X代表直接键或连接基团如CH 2，CH（OH），S，O，NH; Y表示取代或未取代的芳族碳环，芳香杂环，环烷基或饱和杂环基等; Z代表S或O，n为0或1〜4的整数，或其盐，对PDE9具有抑制作用，因此可用于预防或治疗膀胱过度活动症，尿频尿失禁，排尿困难 与前列腺增生，尿石症，阿尔茨海默病，慢性阻塞性肺疾病，心肌梗死，血栓形成，糖尿病等相关。

    Thienopyrimidine derivatives
    4.
    发明授权
    Thienopyrimidine derivatives 有权
    噻吩并嘧啶衍生物

    公开(公告)号：US08377944B2

    公开(公告)日：2013-02-19

    申请号：US13585060

    申请日：2012-08-14

    申请人： Kotaro Gotanda ,  Atsushi Shinbo ,  Youichi Nakano ,  Hideo Kobayashi ,  Makoto Okada ,  Akira Asagarasu

    发明人： Kotaro Gotanda ,  Atsushi Shinbo ,  Youichi Nakano ,  Hideo Kobayashi ,  Makoto Okada ,  Akira Asagarasu

    IPC分类号： C07D495/04 ,  A61K31/519 ,  A61P25/28

    CPC分类号： C07D495/04

    摘要： This invention provides thienopyrimidine derivatives of the formula, wherein R1 stands for hydrogen atom, an alkyl group or the like; R2 stands for a hydrogen atom, an alkyl or amino group or the like, R3 stands for an alkyl, alkenyl or alkylthio group or the like or a group Y—X—; or R2 and R3 may together form tetramethylene group; X standing for a direct bond or linking group such as CH2, CH(OH), S, O, NH; Y standing for a substituted or unsubstituted aromatic carbocyclic, aromatic heterocylic, cycloalkyl or saturated heterocyclic group or the like; Z stands for S or O, and n is 0 or an integer of 1 to 4, or salts thereof, which exhibit an inhibitory effect on PDE9, and are therefore useful for prevention or treatment of overactive bladder syndrome, pollakiuria, urinary incontinence, dysuria associated with prostatic hyperplasia, urolithiasis, Alzheimer's disease, chronic obstructive pulmonary disease, myocardial infarction, thrombosis, diabetes and the like.

    摘要翻译： 本发明提供下式的噻吩并嘧啶衍生物，其中R1代表氢原子，烷基等; R2表示氢原子，烷基或氨基等，R3表示烷基，烯基或烷硫基等或Y-X-基团; 或者R 2和R 3可以一起形成四亚甲基; X代表直接键或连接基团如CH 2，CH（OH），S，O，NH; Y代表取代或未取代的芳族碳环，芳香杂环，环烷基或饱和杂环基等; Z代表S或O，n为0或1〜4的整数，或其盐，对PDE9具有抑制作用，因此可用于预防或治疗膀胱过度活动症，尿频尿失禁，排尿困难 与前列腺增生，尿石症，阿尔茨海默病，慢性阻塞性肺疾病，心肌梗死，血栓形成，糖尿病等相关。

    THIENOPYRIMIDINE DERIVATIVES
    5.
    发明申请
    THIENOPYRIMIDINE DERIVATIVES 有权
    三苯甲基衍生物

    公开(公告)号：US20130023546A1

    公开(公告)日：2013-01-24

    申请号：US13585060

    申请日：2012-08-14

    申请人： Kotaro GOTANDA ,  Atsushi Shinbo ,  Youichi Nakano ,  Hideo Kobayashi ,  Makoto Okada ,  Akira Asagarasu

    发明人： Kotaro GOTANDA ,  Atsushi Shinbo ,  Youichi Nakano ,  Hideo Kobayashi ,  Makoto Okada ,  Akira Asagarasu

    IPC分类号： A61K31/519 ,  A61P13/08 ,  A61P13/00

    CPC分类号： C07D495/04

    摘要： This invention provides thienopyrimidine derivatives of the formula, wherein R1 stands for hydrogen atom, an alkyl group or the like; R2 stands for a hydrogen atom, an alkyl or amino group or the like, R3 stands for an alkyl, alkenyl or alkylthio group or the like or a group Y—X—; or R2 and R3 may together form tetramethylene group; X standing for a direct bond or linking group such as CH2, CH(OH), S, O, NH; Y standing for a substituted or unsubstituted aromatic carbocycylic, aromatic heterocylic, cycloalkyl or saturated heterocyclic group or the like; Z stands for S or O, and n is 0 or an integer of 1 to 4, or salts thereof, which exhibit an inhibitory effect on PDE9, and are therefore useful for prevention or treatment of overactive bladder syndrome, pollakiuria, urinary incontinence, dysuria associated with prostatic hyperplasia, urolithiasis, Alzheimer's disease, chronic obstructive pulmonary disease, myocardial infarction, thrombosis, diabetes and the like.

    摘要翻译： 本发明提供下式的噻吩并嘧啶衍生物，其中R1代表氢原子，烷基等; R2表示氢原子，烷基或氨基等，R3表示烷基，烯基或烷硫基等或Y-X-基团; 或者R 2和R 3可以一起形成四亚甲基; X代表直接键或连接基团如CH 2，CH（OH），S，O，NH; Y表示取代或未取代的芳族碳环，芳香杂环，环烷基或饱和杂环基等; Z代表S或O，n为0或1〜4的整数，或其盐，对PDE9具有抑制作用，因此可用于预防或治疗膀胱过度活动症，尿频尿失禁，排尿困难 与前列腺增生，尿石症，阿尔茨海默病，慢性阻塞性肺疾病，心肌梗塞，血栓形成，糖尿病等相关。

    Substituted imidazo[1,5-A] quinoxalines as a PDE9 inhibitor
    6.
    发明授权
    Substituted imidazo[1,5-A] quinoxalines as a PDE9 inhibitor 有权
    取代的咪唑并[1,5-A]喹喔啉，为PDE9抑制剂

    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.

    QUINOXALINE DERIVATIVES
    7.
    发明申请
    QUINOXALINE DERIVATIVES 有权
    喹啉衍生物

    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.

    Substituted imidazo[1,5-A]quinoxalines as phosphodiesterase 9 inhibitors
    8.
    发明授权
    Substituted imidazo[1,5-A]quinoxalines as phosphodiesterase 9 inhibitors 有权
    取代的咪唑并[1,5-A]喹喔啉，为磷酸二酯酶9抑制剂

    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.