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1. 发明公开

EP1908765A1 THIENOPYRIMIDINE DERIVATIVE 有权
标题翻译：噻吩并嘧啶衍生物
公开(公告)号：EP1908765A1
公开(公告)日：2008-04-09
申请号：EP06766867.3
申请日：2006-06-13
申请人： ASKA Pharmaceutical Co., Ltd.
发明人： GOTANDA, Kotaro , SHINBO, Atsushi , NAKANO, Youichi , KOBAYASHI, Hideo , OKADA, Makoto , ASAGARASU, Akira
IPC分类号： C07D495/04 , A61K31/519 , A61P3/10 , A61P7/02 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/02 , A61P13/04 , A61P13/08 , A61P13/10 , A61P15/10 , A61P25/28
CPC分类号： C07D495/04
摘要： This invention provides thienopyrimidine derivatives of the formula,

wherein R 1 stands for hydrogen atom, an alkyl group or the like; R 2 stands for a hydrogen atom, an alkyl or amino group or the like, R 3 stands for an alkyl, alkenyl or alkylthio group or the like or a group Y-X-; or R 2 and R 3 may together form tetramethylene group; X standing for a direct bond or linking group such as CH 2 , 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代表氢原子，烷基或氨基等，R3代表烷基，烯基或烷硫基等或基团Y-X-; 或者R2和R3可以一起形成四亚甲基; X代表直接键或连接基团，例如CH 2，CH（OH），S，O，NH; Y表示取代或未取代的芳族碳环，芳族杂环，环烷基或饱和杂环基团等; Z代表S或O，n为0或1至4的整数，或它们的盐，它们对PDE9具有抑制作用，因此可用于预防或治疗膀胱活动过度综合征，尿频，尿失禁，排尿困难与前列腺增生，尿石症，阿尔茨海默病，慢性阻塞性肺病，心肌梗塞，血栓形成，糖尿病等有关。

2. 发明公开

EP2050739A1 QUINAZOLINE DERIVATIVE 有权
标题翻译： CHINAZOLINDERIVAT
公开(公告)号：EP2050739A1
公开(公告)日：2009-04-22
申请号：EP07791524.7
申请日：2007-07-24
申请人： ASKA Pharmaceutical Co., Ltd.
发明人： ASAGARASU, Akira , SATO, Shuichiro , OKADA, Makoto
IPC分类号： C07D239/90 , A61K31/517 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/02 , A61P13/04 , A61P13/08 , A61P13/10 , A61P15/10 , A61P25/00 , A61P25/28 , A61P43/00 , C07D401/06 , C07D409/06
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, R 1 stands for phenyl or aromatic heterocyclic group which are optionally substituted with 1 - 3 substituents selected from halogen, C 1-6 alkyl, C 1-6 haloalkyl containing 1 - 6 halogen atoms and C 1-6 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其任选被1-3个选自卤素，C 1-6烷基，含有1-6个卤素原子的C 1-6卤代烷基和C 1-6烷氧基取代; n为1〜3的整数。

3. 发明授权

EP1908765B1 THIENOPYRIMIDINE DERIVATIVE 有权
标题翻译：噻吩并嘧啶衍生物
公开(公告)号：EP1908765B1
公开(公告)日：2014-10-22
申请号：EP06766867.3
申请日：2006-06-13
申请人： ASKA Pharmaceutical Co., Ltd.
发明人： GOTANDA, Kotaro , SHINBO, Atsushi , NAKANO, Youichi , KOBAYASHI, Hideo , OKADA, Makoto , ASAGARASU, Akira
IPC分类号： C07D495/04 , A61K31/519 , A61P3/10 , A61P7/02 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/02 , A61P13/04 , A61P13/08 , A61P13/10 , A61P15/10 , A61P25/28
CPC分类号： C07D495/04

4. 发明公开

EP2103613A1 QUINOXALINE DERIVATIVE 有权
标题翻译： CHINOXALINDERIVAT
公开(公告)号：EP2103613A1
公开(公告)日：2009-09-23
申请号：EP07859852.1
申请日：2007-12-12
申请人： ASKA Pharmaceutical Co., Ltd.
发明人： OKADA, Makoto , SATO, Shuichiro , KAWADE, Kenji , GOTANDA, Kotaro , SHINBO, Atsushi , NAKANO, Youichi , KOBAYASHI, Hideo
IPC分类号： C07D487/04 , A61K31/4985 , A61P3/10 , A61P7/02 , A61P9/10 , A61P9/12 , A61P11/16 , A61P13/02 , A61P13/08 , A61P13/10 , A61P15/10 , A61P25/00 , A61P25/28
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,
R 1 and R 2 each independently stands for hydrogen, halogen, alkyl, alkoxy, acyl, amino and the like,
R 3 stands for alkyl, aryl, saturated carbocyclic group, saturated heterocyclic group, acyl and the like,
R 4 stands for hydrogen, hydroxy, alkyl or amino,
R 5 and R 8 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkoxy, cyano or nitro,
R 6 and R 7 each independently stands for hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, cyano, amino, carbocyclic group, heterocyclic group, COR 9 or SO 2 R 9 ,
R 9 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
A 1 , A 2 and A 3 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，可用作式中式（I）表示的排尿困难等的治疗剂，R 1和R 2各自独立地代表氢，卤素烷基，烷氧基，酰基，氨基等，R 3表示烷基，芳基，饱和碳环基，饱和杂环基，酰基等，R 4表示氢，羟基，烷基或氨基，R 5和R 8 每个独立地代表氢，卤素，烷基，烯基，烷氧基，氰基或硝基，R 6和R 7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，COR 9或SO 2 R 9，R 9表示氢，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，A 1 ，A 2和A 3各自独立地代表N或C.

5. 发明授权

EP2050739B1 QUINAZOLINE DERIVATIVE 有权
标题翻译： CHINAZOLINDERIVAT
公开(公告)号：EP2050739B1
公开(公告)日：2016-07-06
申请号：EP07791524.7
申请日：2007-07-24
申请人： ASKA Pharmaceutical Co., Ltd.
发明人： ASAGARASU, Akira , SATO, Shuichiro , OKADA, Makoto
IPC分类号： C07D239/90 , A61K31/517 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/02 , A61P13/04 , A61P13/08 , A61P13/10 , A61P15/10 , A61P25/00 , A61P25/28 , A61P43/00 , C07D401/06 , C07D409/06
CPC分类号： C07D239/91 , C07D401/06 , C07D409/06

6. 发明授权

EP2103613B1 QUINOXALINE DERIVATIVE 有权
标题翻译：喹喔啉
公开(公告)号：EP2103613B1
公开(公告)日：2016-02-17
申请号：EP07859852.1
申请日：2007-12-12
申请人： ASKA Pharmaceutical Co., Ltd.
发明人： OKADA, Makoto , SATO, Shuichiro , KAWADE, Kenji , GOTANDA, Kotaro , SHINBO, Atsushi , NAKANO, Youichi , KOBAYASHI, Hideo
IPC分类号： C07D487/04 , A61K31/4985 , A61P3/10 , A61P7/02 , A61P9/10 , A61P9/12 , A61P11/16 , A61P13/02 , A61P13/08 , A61P13/10 , A61P15/10 , A61P25/00 , A61P25/28
CPC分类号： C07D487/04 , C07D487/14

7. 发明授权

EP1627871B1 CYCLIC AMINOPHENYL SULFAMATE DERIVATIVE 有权
标题翻译：环状氨基苯磺酰胺衍生物
公开(公告)号：EP1627871B1
公开(公告)日：2010-04-14
申请号：EP04731745.8
申请日：2004-05-07
申请人： ASKA Pharmaceutical Co., Ltd.
发明人： TAKEGAWA, Shigehiro , IWASHITA, Shigeki , OKADA, Makoto , NAKAGAWA, Takayoshi , KOIZUMI, Naoyuki , FUJII, Tomohito
IPC分类号： C07D211/14 , C07D211/70 , C07D211/62 , C07D295/08 , C07D295/18 , C07D295/22 , A61K31/451 , A61K31/4545 , A61K31/495 , A61P43/00 , A61P35/00 , A61P15/00 , A61P37/06 , A61P25/28 , A61P17/00
CPC分类号： C07D211/32 , C07D211/14
摘要： A cyclic aminophenyl sulfamate derivative represented by the formula (I) (wherein R1 and R2 each represents hydrogen or lower alkyl; R3 and R4 each represents hydrogen, halogeno, cyano, etc.; A represents nitrogen or CH; B represents CH2, SO2, CO, optionally substituted phenyl, etc.; and R5 represents alkyl, phenyl, amino, etc.), or a salt thereof. The derivative has excellent steroid sulfatase inhibitory activity and is useful for the prevention of or treatments for diseases in which steroids such as estrogen and androgen participate.
摘要翻译：式（I）表示的环状氨基苯基氨基磺酸酯衍生物（其中R1和R2各代表氢或低级烷基; R3和R4各自代表氢，卤代，氰基等; A代表氮或CH; B代表CH2，SO2， CO，任选取代的苯基等;并且R 5表示烷基，苯基，氨基等）或其盐。该衍生物具有优良的类固醇硫酸酯酶抑制活性，可用于预防或治疗雌激素和雄激素等类固醇参与的疾病。

8. 发明公开

EP2123301A1 THERAPEUTIC AGENT FOR URINARY TRACT DISEASE 审中-公开
标题翻译：治疗师MITTELFÜRERKRANKUNGEN DER HARNWEGE
公开(公告)号：EP2123301A1
公开(公告)日：2009-11-25
申请号：EP07859850.5
申请日：2007-12-12
申请人： ASKA Pharmaceutical Co., Ltd.
发明人： GOTANDA, Kotaro , SHINBO, Atsushi , NAKANO, Youichi , KOBAYASHI, Hideo , OKADA, Makoto , ASAGARASU, Akira
IPC分类号： A61K45/00 , A61K31/4985 , A61K31/519 , A61P13/00 , A61P13/02 , A61P13/04 , A61P43/00 , C07D487/04 , C07D495/04
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综合征，尿频尿，尿失禁，良性前列腺增生或尿路结石排尿困难的治疗剂，其包含具有PDE9抑制活性的化合物作为活性成分。

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