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1. 发明授权

US08299080B2 Substituted imidazo[1,5-A] quinoxalines as a PDE9 inhibitor 有权
标题翻译：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.

2. 发明申请

US20100048556A1 QUINOXALINE DERIVATIVES 有权
标题翻译：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.

3. 发明授权

US08829000B2 Substituted imidazo[1,5-A]quinoxalines as phosphodiesterase 9 inhibitors 有权
标题翻译：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.

4. 发明授权

US08293754B2 Thienopyrimidine derivatives 有权
标题翻译：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。

5. 发明申请

US20100113484A1 TREATING AGENT OF UROPATHY 审中-公开
标题翻译：治疗尿崩症
公开(公告)号：US20100113484A1
公开(公告)日：2010-05-06
申请号：US12448217
申请日：2007-12-12
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 , C07D495/04 , A61P13/00 , A61P13/10
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/519 , C07D495/04
摘要： Disclosed is a treating agent of overactive bladder syndrome, pollakiuria, urinary incontinence, dysuria in benign prostatic hyperplasia or urolithiasis, which comprises a compound having PDE9-inhibiting activity as the active ingredient.
摘要翻译：本发明涉及膀胱过度活动症，尿频尿失禁，良性前列腺增生或尿石症中的排尿困难的治疗剂，其包含具有PDE9抑制活性的化合物作为活性成分。

6. 发明授权

US08377944B2 Thienopyrimidine derivatives 有权
标题翻译：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。

7. 发明申请

US20090203703A1 Thienopyrimidine Derivatives 有权
标题翻译：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。

8. 发明授权

US5221674A Pyridazinone derivatives 失效
标题翻译：哒嗪酮衍生物
公开(公告)号：US5221674A
公开(公告)日：1993-06-22
申请号：US770288
申请日：1991-09-27
申请人： Kikuo Yasuda , Kenyu Shibata , Nobuyoshi Minami , Toshimi Seki , Masafumi Shiraiwa , Tomio Nakao , Katsuhiko Miyasaka , Tsutomu Ishimori , Kotaro Gotanda , Takako Sasaki
发明人： Kikuo Yasuda , Kenyu Shibata , Nobuyoshi Minami , Toshimi Seki , Masafumi Shiraiwa , Tomio Nakao , Katsuhiko Miyasaka , Tsutomu Ishimori , Kotaro Gotanda , Takako Sasaki
IPC分类号： C07D237/04 , C07D401/12 , C07D403/12
CPC分类号： C07D401/12 , C07D237/04 , C07D403/12
摘要： A pyridazinone compound represented by the general formula ##STR1## wherein Ar is ##STR2## in which R.sup.1, R.sup.2 and R.sup.3 may be identical or different, and each represents a hydrogen atom, a lower alkyl group, a trifluoromethyl group, a halogen atom, a cyano group or a nitro group, and R.sup.4 represents a hydrogen atom, a lower alkoxy group, or a lower alkyl group substituted by a lower alkoxy group or a carbamoyl group, and C* is an assymmetric carbon atom,or a salt thereof. This compound is useful for the treatment of diseases of the circulatory system.
摘要翻译：由通式（I）表示的哒嗪酮化合物，其中Ar是其中R 1，R 2和R 3可以相同或不同，并且各自表示氢原子，低级烷基，三氟甲基基团，卤素原子，氰基或硝基，R 4表示氢原子，低级烷氧基或被低级烷氧基或氨基甲酰基取代的低级烷基，C *是不对称碳原子，或其盐。该化合物可用于治疗循环系统疾病。

9. 发明授权

US5082844A Pyridazinone derivatives 失效
标题翻译：吡咯烷酮衍生物
公开(公告)号：US5082844A
公开(公告)日：1992-01-21
申请号：US539741
申请日：1990-06-18
申请人： Kikuo Yasuda , Kenyu Shibata , Nobuyoshi Minami , Toshimi Seki , Masafumi Shiraiwa , Tomio Nakao , Katsuhiko Miyasaka , Tsutomu Ishimori , Kotaro Gotanda , Takako Sasaki
发明人： Kikuo Yasuda , Kenyu Shibata , Nobuyoshi Minami , Toshimi Seki , Masafumi Shiraiwa , Tomio Nakao , Katsuhiko Miyasaka , Tsutomu Ishimori , Kotaro Gotanda , Takako Sasaki
IPC分类号： C07D237/04 , C07D401/12 , C07D403/12
CPC分类号： C07D401/12 , C07D237/04 , C07D403/12
摘要： A pyridazinone compound represented by the general formula ##STR1## wherein Ar is ##STR2## in which R.sup.1, R.sup.2 and R.sup.3 may be identical or different, and each represents a hydrogen atom, a lower alkyl group, a trifluoromethyl group, a halogen atom, a cyano group or a nitro group, and R.sup.4 represents a hydrogen atom, a lower alkoxy group, or a lower alkyl group substituted by a lower alkoxy group or a carbamoyl group, and C* is an asymmetric carbon atom, or a salt thereof. This compound is useful for the treatment of diseases of the circulatory system.

10. 发明授权

US5130314A Carbostyril substituted pyridazinones 失效
标题翻译： CARBOSTYRIL取代的吡咯烷酮
公开(公告)号：US5130314A
公开(公告)日：1992-07-14
申请号：US770287
申请日：1991-09-27
申请人： Kikuo Yasuda , Kenyu Shibata , Nobuyoshi Minami , Toshimi Seki , Masafumi Shiraiwa , Tomio Nakao , Katsuhiko Miyasaka , Tsutomu Ishimori , Kotaro Gotanda , Takako Sasaki
发明人： Kikuo Yasuda , Kenyu Shibata , Nobuyoshi Minami , Toshimi Seki , Masafumi Shiraiwa , Tomio Nakao , Katsuhiko Miyasaka , Tsutomu Ishimori , Kotaro Gotanda , Takako Sasaki
IPC分类号： C07D237/04 , C07D401/12 , C07D403/12
CPC分类号： C07D401/12 , C07D237/04 , C07D403/12
摘要： A pyridazinone compound represented by the general formula ##STR1## wherein Ar is ##STR2## in which R.sup.1, R.sup.2 and R.sup.3 may be identical or different, and each represents a hydrogen atom, a lower alkyl group, a trifluoromethyl group, a halogen atom, a cyano group or a nitro group, and R.sup.4 represents a hydrogen atom, a lower alkoxy group, or a lower alkyl group substituted by a lower alkoxy group or a carbamoyl group, and C* is an assymmetric carbon atom,or a salt thereof. This compound is useful for the treatment of diseases of the circulatory system.

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