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1. 发明授权

US07354949B2 Therapeutic agent for bladder irritative symptoms associated with benign prostatic hyperplasia 失效
公开(公告)号：US07354949B2
公开(公告)日：2008-04-08
申请号：US10472148
申请日：2002-03-29
申请人： Tsuyoshi Yamagata , Kaoru Atsuki , Tetsuji Ohno , Shiro Shirakura , Akira Karasawa
发明人： Tsuyoshi Yamagata , Kaoru Atsuki , Tetsuji Ohno , Shiro Shirakura , Akira Karasawa
IPC分类号： A61K31/38 , A61K31/44 , A61K31/42
CPC分类号： C07D495/04 , A61K31/55
摘要： The present invention provides a therapeutic agent for bladder irritative symptoms associated with benign prostatic hyperplasia comprising, as an active ingredient, a tricyclic compound represented by formula (I): [wherein R1 represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy or halogen; X1-X2-X3 represents CR5═CR6—CR7═CR8, N(O)m═CR6—CR7═CR8, CR5═CR6—N(O)m═CR8, CR5═CR6—CR7═N(O)m, CR5═CR6—O, CR5═CR6—S, O—CR7═CR8, S—CR7═CR8 or O—CR7═N; Y represents 13 CH2S—, —CH2SO—, —CH2SO2—, —CH2O—, —CH═CH—, —(CH2)p—, —SCH2—, —SOCH2—, —SO2CH2— or —OCH2—; and R2 represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl, substituted or unsubstituted lower alkoxy, amino, mono(substituted or unsubstituted lower alkyl)-substituted amino, di(substituted or unsubstituted lower alkyl)-substituted amino, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aralkylamino, substituted or unsubstituted arylamino or a substituted or unsubstituted heteroalicyclic group] or a pharmaceutically acceptable salt thereof.

2. 发明授权

US06211227B1 Tricyclic compounds 失效
标题翻译：三环化合物
公开(公告)号：US06211227B1
公开(公告)日：2001-04-03
申请号：US09417626
申请日：1999-10-14
申请人： Makoto Yoshida , Takashi Seishi , Shigeru Aono , Tsuyoshi Yamagata , Kaoru Atsuki , Toshiaki Kumazawa , Haruki Takai , Koji Suzuki , Akira Karasawa
发明人： Makoto Yoshida , Takashi Seishi , Shigeru Aono , Tsuyoshi Yamagata , Kaoru Atsuki , Toshiaki Kumazawa , Haruki Takai , Koji Suzuki , Akira Karasawa
IPC分类号： A61K3138
CPC分类号： C07D495/04 , C07D313/12 , C07D337/12
摘要： The present invention provides tricyclic compounds which are useful for the treatment of pollakiuria and urinary incontinence and which are represented by general formula (I): (wherein R1 represents hydrogen, substituted or unsubstituted lower alkyl, etc.; X1—X2—X3 represents CR5═CR6—CR7═CR8 (wherein R5, R6, R7 and R8, which may be the same or different, each represents hydrogen, substituted or unsubstituted lower alkyl, hydroxy, substituted or unsubstituted lower alkoxy, etc.), N(O)m═CR5—CR6═CR7 (wherein R5, R6 and R7 have the same significances as defined above, and m represents 0 or 1), S—CR7═CR8 (wherein R7 and R8 have the same significances as defined above), etc.; and when R2 represents hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, a substituted or unsubstituted N-substituted heterocyclic group, (wherein n is 0 or 1; R3 and R4, which may be the same or different, each represents hydrogen, substituted or unsubstituted lower alkyl, trifluoromethyl, etc., or R3 and R4 may be combined together to form cyclic alkyl; and Q represents hydroxy, halogen, etc.), etc., Y represents —CH2SO2—, —SCH2—, —SOCH2—, —SO2CH2—, etc.) and pharmaceutically acceptable salts thereof.
摘要翻译：本发明提供可用于治疗尿频和尿失禁的三环化合物，其由通式（I）表示：其中R 1表示氢，取代或未取代的低级烷基等; X 1 -X 2 -X 3表示CR 5 = CR6-CR7 = CR8（其中R5，R6，R7和R8可以相同或不同，各自表示氢，取代或未取代的低级烷基，羟基，取代或未取代的低级烷氧基等），N（O）m = CR5-CR6 = CR7（其中R5，R6和R7具有与上述相同的含义，m表示0或1），S-CR 7 = CR 8（其中R 7和R 8具有与上述相同的含义）等 ;当R 2表示氢时，取代或未取代的低级烷基，取代或未取代的低级烷氧基，取代或未取代的N-取代的杂环基，（其中n为0或1; R 3和R 4各自可相同或不同）代表氢，取代或未取代的低级烷基，三氟甲基脲基甲基等，或者R 3和R 4可以组合在一起形成环烷基; 和Q表示羟基，卤素等）等，Y表示-CH 2 SO 2 - ， - CH 2 - ， - SOCH 2 - ， - SO 2 CH 2 - 等）及其药学上可接受的盐。

3. 发明授权

US07276532B2 Remedies for vesical hyperactivity 失效
标题翻译：用于膀胱活动过度的补救措施
公开(公告)号：US07276532B2
公开(公告)日：2007-10-02
申请号：US10472143
申请日：2002-03-29
申请人： Tsuyoshi Yamagata , Kaoru Atsuki , Tetsuji Ohno , Shiro Shirakura , Akira Karasawa
发明人： Tsuyoshi Yamagata , Kaoru Atsuki , Tetsuji Ohno , Shiro Shirakura , Akira Karasawa
IPC分类号： A61K31/38
CPC分类号： C07D495/04 , A61K31/55 , C07D337/12
摘要： The present invention provides a therapeutic agent for overactive bladder comprising, as an active ingredient, a tricyclic compound represented by formula (I): [wherein R1 represents a hydrogen atom, substituted or unsubstituted lower alkyl, and the like; X1—X2—X3 represents CR5═CR6—CR7═CR8, CR5═CR6—S, and the like; Y represents —CH2S—, —SOCH2—, and the like; and R2 represents a hydrogen atom, and the like] or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供一种活性过氧化物的治疗剂，其包含作为活性成分的由式（I）表示的三环化合物：其中R 1表示氢原子，取代或未取代的低级烷基，和类似; X 1 - 2 - - - - - - - - - - - - - - - - - - （3） CR 7 -CR 8，CR 5 -CR 6 -S等; Y表示-CH 2 -S-，-SOCH 2 - 等; 和R 2表示氢原子等]或其药学上可接受的盐。

4. 发明申请

US20060276531A1 Agent for the treatment of bladder irritative symptoms accompanied by benign prostatic hyperplasia 审中-公开
标题翻译：代理治疗膀胱刺激症状伴有良性前列腺增生
公开(公告)号：US20060276531A1
公开(公告)日：2006-12-07
申请号：US11503067
申请日：2006-08-14
申请人： Tsuyoshi Yamagata , Kaoru Atsuki , Tetsuji Ohno , Shiro Shirakura , Akira Karasawa , William de Groat , Naoki Yoshimura , Adrian Sculptoreanu
发明人： Tsuyoshi Yamagata , Kaoru Atsuki , Tetsuji Ohno , Shiro Shirakura , Akira Karasawa , William de Groat , Naoki Yoshimura , Adrian Sculptoreanu
IPC分类号： A61K31/381
CPC分类号： A61K31/55 , A61K31/38 , A61K31/44
摘要： The present invention provides an agent for the treatment of bladder irritative symptoms accompanied by benign prostatic hyperplasia, comprising, as an active ingredient, a compound having a slowly-inactivating A-type K+ channel opening activity or a pharmaceutically acceptable salt thereof, and a method for screening agents for the treatment of bladder irritative symptoms accompanied by benign prostatic hyperplasia, comprising measuring a slowly-inactivating A-type K+ channel opening activity as an index.
摘要翻译：本发明提供了一种用于治疗伴有良性前列腺增生的膀胱刺激症状的药剂，其包含作为活性成分的具有缓慢失活的A型K + / O通道开放活性的化合物或以及用于治疗伴有良性前列腺增生的膀胱刺激症状的筛选剂的方法，包括测量缓慢失活的A型K +通道开放活性作为指标。

5. 发明授权

US07122173B2 Agent for the treatment of bladder irritative symptoms accompanied by benign prostatic hyperplasia 失效
公开(公告)号：US07122173B2
公开(公告)日：2006-10-17
申请号：US10473348
申请日：2002-03-29
申请人： Tsuyoshi Yamagata , Kaoru Atsuki , Tetsuji Ohno , Shiro Shirakura , Akira Karasawa , William C. de Groat , Naoki Yoshimura , Adrian Sculptoreanu
发明人： Tsuyoshi Yamagata , Kaoru Atsuki , Tetsuji Ohno , Shiro Shirakura , Akira Karasawa , William C. de Groat , Naoki Yoshimura , Adrian Sculptoreanu
IPC分类号： A61K10/00 , A61K49/00
CPC分类号： A61K31/55 , A61K31/38 , A61K31/44
摘要： The present invention provides an agent for the treatment of bladder irritative symptoms accompanied by benign prostatic hyperplasia, comprising, as an active ingredient, a compound having a slowly-inactivating A-type K+ channel opening activity or a pharmaceutically acceptable salt thereof, and a method for screening agents for the treatment of bladder irritative symptoms accompanied by benign prostatic hyperplasia, comprising measuring a slowly-inactivating A-type K+ channel opening activity as an index.

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