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1. 发明授权

US5434148A .beta.-carboline derivative 失效
标题翻译： β-咔啉衍生物
公开(公告)号：US5434148A
公开(公告)日：1995-07-18
申请号：US67931
申请日：1993-05-27
申请人： Koichiro Yamada , Masataka Hikota , Takeshi Yura , Toshiro Shikano , Masaaki Nagasaki
发明人： Koichiro Yamada , Masataka Hikota , Takeshi Yura , Toshiro Shikano , Masaaki Nagasaki
IPC分类号： C07D471/04 , A61K31/44 , A61K31/55 , C07D487/04
CPC分类号： C07D471/04
摘要： Disclosed are .beta.-carboline derivatives represented by the formula: ##STR1## wherein R.sup.1 represents hydrogen atom, a lower alkyl group, a lower alkoxy group or hydroxy group; R.sup.5 represents hydrogen atom, or R.sup.1 and R.sup.5 are bonded to represent a lower alkylenedioxy group; R.sup.2 represents hydrogen atom, a halogen atom, a lower alkoxy group or hydroxy group; R.sup.3 represents hydrogen atom, a carbamoyl lower alkyl group, a lower alkyl group, a carboxy lower alkyl group or a lower alkoxycarbonyl lower alkyl group; R.sup.4 represents hydrogen atom, a lower alkyl group, a carboxy lower alkyl group, a lower alkoxycarbonyl lower alkyl group, a lower alkanoyl group, an arylcarbonyl group, a lower alkanesulfonyl group, a lower alkoxycarbonyl group, an aralkyl group, formyl group or a di(lower alkyl)sulfamoyl group; n represents 0, 1 or 2; and the symbol * represents an asymmetric carbon atom,or a pharmaceutically acceptable salt thereof, and a process for preparing the same.
摘要翻译：公开了由下式表示的β-咔啉衍生物：其中R 1表示氢原子，低级烷基，低级烷氧基或羟基; R 5表示氢原子，或者R 1和R 5相连，表示低级亚烷基二氧基; R2表示氢原子，卤素原子，低级烷氧基或羟基; R3表示氢原子，氨基甲酰基低级烷基，低级烷基，羧基低级烷基或低级烷氧羰基低级烷基; R4表示氢原子，低级烷基，羧基低级烷基，低级烷氧基羰基低级烷基，低级烷酰基，芳基羰基，低级链烷磺酰基，低级烷氧基羰基，芳烷基，甲酰基或二（低级烷基）氨磺酰基; n表示0,1或2; 符号*表示不对称碳原子，或其药学上可接受的盐及其制备方法。

2. 发明授权

US07423175B2 Hydroxy-tetrahydro-naphthalenylurea derivatives 失效
标题翻译：羟基 - 四氢 - 萘基脲衍生物
公开(公告)号：US07423175B2
公开(公告)日：2008-09-09
申请号：US10545556
申请日：2004-02-05
申请人： Takeshi Yura , Muneto Mogi , Hiroshi Fujishima , Klaus Urbahns , Tsutomu Masuda , Yasuhiro Tsukimi , Masaomi Tajimi , Noriyuki Yamamoto , Nagahiro Yoshida , Toshiya Moriwaki
发明人： Takeshi Yura , Muneto Mogi , Hiroshi Fujishima , Klaus Urbahns , Tsutomu Masuda , Yasuhiro Tsukimi , Masaomi Tajimi , Noriyuki Yamamoto , Nagahiro Yoshida , Toshiya Moriwaki
IPC分类号： C07C275/32 , A61K31/17
CPC分类号： C07D295/096 , C07C275/32 , C07C2602/10
摘要： This invention relates to hydroxy-tetrahydro-naphthalenylurea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The hydroxy-tetrahydro-naphthalenylurea derivatives of the present invention have an excellent activity as VR1 antagonist and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.
摘要翻译：本发明涉及可用作药物制剂活性成分的羟基 - 四氢 - 萘基脲衍生物及其盐。本发明的羟基 - 四氢 - 萘基脲衍生物作为VR1拮抗剂具有优异的活性，并且可用于预防和治疗与VR1活性有关的疾病，特别是用于治疗尿失禁，敦促性尿失禁，膀胱过度活动症，慢性疼痛，神经性疼痛，术后疼痛，类风湿关节炎疼痛，神经痛，神经病，痛觉，神经损伤，局部缺血，神经变性，中风，炎性疾病，哮喘和COPD。

3. 发明申请

US20060135505A1 Tetrahydro-naphthalene derivatives as vanilloid receptor antagonists 失效
公开(公告)号：US20060135505A1
公开(公告)日：2006-06-22
申请号：US10537217
申请日：2003-11-28
申请人： Masaomi Tajimi , Toshio Kokubo , Masahiro Shiroo , Yasuhiro Tsukimi , Takeshi Yura , Klaus Urbahns , Noriyuki Yamamoto , Muneto Mogi , Hiroshi Fujishima , Tsutomu Masuda , Nagahiro Yoshida , Toshiya Moriwaki
发明人： Masaomi Tajimi , Toshio Kokubo , Masahiro Shiroo , Yasuhiro Tsukimi , Takeshi Yura , Klaus Urbahns , Noriyuki Yamamoto , Muneto Mogi , Hiroshi Fujishima , Tsutomu Masuda , Nagahiro Yoshida , Toshiya Moriwaki
IPC分类号： A61K31/445 , A61K31/40 , A61K31/397 , A61K31/17
CPC分类号： C07C275/32 , C07C2602/10 , C07D207/27 , C07D211/22 , C07D211/46 , C07D211/62 , C07D295/135
摘要： This invention relates to tetrahydro-naphthalene derivatives of formula (I) in which the variable groups are as defined in the specification and claims, and tautomeric and stereoisomeric forms and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have an excellent activity as VR1 antagonists and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD. The compounds, pharmaceutical compositions containing them, and methods of treatment using them are disclosed and claimed.

4. 发明申请

US20050154230A1 Urea derivatives 审中-公开
标题翻译：尿素衍生物
公开(公告)号：US20050154230A1
公开(公告)日：2005-07-14
申请号：US10499785
申请日：2002-12-13
申请人： Takeshi Yura , Muneto Mogi , Yuka Ikegami , Tsutomu Masuda , Toshio Kokubo , Klaus Urbahns , Nagahiro Yoshida , Makiko Marumo , Masahiro Shiroo , Masaomi Tajimi , Keisuke Takeshita , Toshiya Moriwaki , Yasuhiro Tsukimi
发明人： Takeshi Yura , Muneto Mogi , Yuka Ikegami , Tsutomu Masuda , Toshio Kokubo , Klaus Urbahns , Nagahiro Yoshida , Makiko Marumo , Masahiro Shiroo , Masaomi Tajimi , Keisuke Takeshita , Toshiya Moriwaki , Yasuhiro Tsukimi
IPC分类号： C07D295/12 , A61K31/167 , A61K31/17 , A61K31/216 , A61K31/277 , A61K31/341 , A61K31/36 , A61K31/381 , A61K31/403 , A61K31/416 , A61K31/44 , A61K31/4406 , A61K31/4453 , A61K31/47 , A61K31/472 , A61K31/496 , A61P9/10 , A61P13/10 , A61P25/00 , A61P25/04 , A61P25/28 , A61P29/00 , A61P29/02 , A61P43/00 , C07C275/10 , C07C275/24 , C07C275/28 , C07C275/30 , C07C275/32 , C07C275/34 , C07C275/36 , C07C275/38 , C07C275/40 , C07C275/42 , C07C323/33 , C07C323/43 , C07D209/88 , C07D213/40 , C07D213/75 , C07D215/38 , C07D217/06 , C07D231/56 , C07D295/135 , C07D307/52 , C07D317/06 , C07D317/58 , C07D317/66 , C07D333/20 , C07D333/36
CPC分类号： C07D333/36 , C07C275/24 , C07C275/28 , C07C275/30 , C07C275/32 , C07C275/40 , C07C275/42 , C07C323/43 , C07C2602/10 , C07C2603/18 , C07D209/88 , C07D213/40 , C07D213/75 , C07D217/06 , C07D231/56 , C07D295/135 , C07D307/52 , C07D317/06 , C07D317/58 , C07D333/20
摘要： This invention relates to urea derivatives and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The urea derivatives of the present invention has an excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, incontinence and/or inflammatory disorders.
摘要翻译：本发明涉及尿素衍生物及其盐，其可用作药物制剂的活性成分。本发明的脲衍生物作为VR1拮抗剂具有优异的活性，可用于预防和治疗与VR1活性相关的疾病，特别是用于治疗急性尿失禁，膀胱过度活动症，慢性疼痛，神经性疼痛，术后疼痛，类风湿性关节炎疼痛，神经痛，神经病，酸痛，神经损伤，局部缺血，神经变性，中风，失禁和/或炎症性疾病。

5. 发明授权

US08088826B2 Tetrahydro-naphthalene derivatives 失效
标题翻译：四氢萘衍生物
公开(公告)号：US08088826B2
公开(公告)日：2012-01-03
申请号：US12103396
申请日：2008-04-15
申请人： Masaomi Tajimi , Toshio Kokubo , Masahiro Shiroo , Yasuhiro Tsukimi , Takeshi Yura , Klaus Urbahns , Noriyuki Yamamoto , Muneto Mogi , Hiroshi Fujishima , Tsutomu Masuda , Nagahiro Yoshida , Toshiya Moriwaki
发明人： Masaomi Tajimi , Toshio Kokubo , Masahiro Shiroo , Yasuhiro Tsukimi , Takeshi Yura , Klaus Urbahns , Noriyuki Yamamoto , Muneto Mogi , Hiroshi Fujishima , Tsutomu Masuda , Nagahiro Yoshida , Toshiya Moriwaki
IPC分类号： A61K31/17
CPC分类号： C07D295/088 , C07C233/29 , C07C233/75 , C07C235/42 , C07C237/40 , C07C275/32 , C07C275/38 , C07C275/40 , C07C275/42 , C07C317/32 , C07C323/44 , C07C2602/10 , C07D207/27 , C07D211/22 , C07D211/46 , C07D211/62 , C07D295/135
摘要： This invention relates to tetrahydro-Naphthalene derivatives and salts thereof which are useful as an active ingredient of pharmaceutical preparations. The tethrahydro—Naphthalene derivatives of the present invention have excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontienence, chronic pain, neuropathic pain, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.
摘要翻译：本发明涉及四氢萘衍生物及其盐，其可用作药物制剂的活性成分。本发明的四氢萘衍生物作为VR1拮抗剂具有优异的活性，可用于预防和治疗与VR1活性相关的疾病，特别是用于治疗尿失禁，膀胱过度活动症，敦促性尿失禁，慢性疼痛，神经性疼痛，手术后疼痛，类风湿性关节炎疼痛，神经痛，神经病，痛觉，神经损伤，局部缺血，神经变性，中风，炎症性疾病，哮喘和COPD。

6. 发明申请

US20080275047A1 TETRAHYDRO-NAPHTHALENE DERIVATIVES 失效
标题翻译：四氢萘衍生物
公开(公告)号：US20080275047A1
公开(公告)日：2008-11-06
申请号：US12103396
申请日：2008-04-15
申请人： Masaomi Tajimi , Toshio Kokubo , Masahiro Shiroo , Yasuhiro Tsukimi , Takeshi Yura , Klaus Urbahns , Noriyuki Yamamoto , Muneto Mogi , Hiroshi Fujishima , Tsutomu Masuda , Nagahiro Yoshida , Toshiya Moriwaki
发明人： Masaomi Tajimi , Toshio Kokubo , Masahiro Shiroo , Yasuhiro Tsukimi , Takeshi Yura , Klaus Urbahns , Noriyuki Yamamoto , Muneto Mogi , Hiroshi Fujishima , Tsutomu Masuda , Nagahiro Yoshida , Toshiya Moriwaki
IPC分类号： A61K31/5375 , A61K31/17 , A61P13/00 , A61K31/167
CPC分类号： C07D295/088 , C07C233/29 , C07C233/75 , C07C235/42 , C07C237/40 , C07C275/32 , C07C275/38 , C07C275/40 , C07C275/42 , C07C317/32 , C07C323/44 , C07C2602/10 , C07D207/27 , C07D211/22 , C07D211/46 , C07D211/62 , C07D295/135
摘要： This invention relates to tetrahydro-naphthalene derivatives and salts thereof which are useful as an active ingredient of pharmaceutical preparations. The tethrahydro-naphthalene derivatives of the present invention have excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontienence, chronic pain, neuropathic pain, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.
摘要翻译：本发明涉及可用作药物制剂活性成分的四氢萘衍生物及其盐。本发明的四氢萘衍生物作为VR1拮抗剂具有优异的活性，可用于预防和治疗与VR1活性有关的疾病，特别是用于治疗尿失禁，膀胱过度活动症，敦促性尿失禁，慢性疼痛，神经性疼痛，手术后疼痛，类风湿性关节炎疼痛，神经痛，神经病，痛觉，神经损伤，局部缺血，神经变性，中风，炎症性疾病，哮喘和COPD。

7. 发明授权

US06911443B2 Imidazopyrimidine derivatives and triazolopyrimidine derivatives 失效
标题翻译：咪唑并嘧啶衍生物和三唑并嘧啶衍生物
公开(公告)号：US06911443B2
公开(公告)日：2005-06-28
申请号：US10258628
申请日：2001-04-17
申请人： Takeshi Yura , Arnel B. Concepcion , Gyoonhee Han , Makiko Marumo , Hiroko Yoshino , Norihiro Kawamura , Toshio Kokubo , Hiroshi Komura , Yingfu Li , Timothy B. Lowinger , Muneto Mogi , Noriyuki Yamamoto , Nagahiro Yoshida , Scott Miller , Margaret A. Popp , Aniko M. Redmann , Martha E. Rodriguez , William J. Scott , Ming Wang
发明人： Takeshi Yura , Arnel B. Concepcion , Gyoonhee Han , Makiko Marumo , Hiroko Yoshino , Norihiro Kawamura , Toshio Kokubo , Hiroshi Komura , Yingfu Li , Timothy B. Lowinger , Muneto Mogi , Noriyuki Yamamoto , Nagahiro Yoshida , Scott Miller , Margaret A. Popp , Aniko M. Redmann , Martha E. Rodriguez , William J. Scott , Ming Wang
IPC分类号： A61K31/505 , A61K31/519 , A61K31/5377 , A61K31/541 , A61P1/04 , A61P3/04 , A61P7/02 , A61P7/06 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P21/04 , A61P25/28 , A61P27/02 , A61P27/14 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D487/04 , C07D519/00 , C07D417/10
CPC分类号： C07D487/04
摘要： A compound of the formula (I) in which R1 is —OR11, —SR11, —SOR11, —SO2R11, —NHR11, or —NR12R13 , and R11, R12, and R13 are as defined broadly in the text. R2 is H, C1-C6alkyl, carbamoyl, or an ester group. R3 is thienyl, pyridyl optionally substituted by halogen or C1-C6alkoxy; naphthyl optionally substituted by C1-C6alkoxy; dioxane fused phenyl; dioxacyclopentane fused phenyl; or optionally substituted phenyl. Y is CH or N. A process for preparing such compounds, pharmaceutical compositions containing such compounds, and a method of treating asthma using them are also disclosed and claimed.
摘要翻译：其中R 1为-OR 11，-SR 11，-SOR 11的式（I）化合物， SO 2，-SO 2，R 11，-NHR 11或-NR 12 R 13 ＆lt; / SUP＆gt;和R 11，R 12和R 13如在文中广义地定义的。 R 2是H，C 1 -C 6烷基，氨基甲酰基或酯基。 R 3是噻吩基，任选被卤素或C 1 -C 6烷氧基取代的吡啶基; 任选被C 1 -C 6烷氧基取代的萘基; 二恶烷稠合苯基; 二氧杂环戊烷稠合苯基; 或任选取代的苯基。 Y是CH或N.一种制备这种化合物的方法，含有这些化合物的药物组合物和使用它们治疗哮喘的方法也被公开和要求保护。

8. 发明授权

US6054912A Trip device of circuit breaker 有权
标题翻译：断路器跳闸装置
公开(公告)号：US6054912A
公开(公告)日：2000-04-25
申请号：US371497
申请日：1999-08-10
申请人： Shozo Kaneko , Takeshi Yura
发明人： Shozo Kaneko , Takeshi Yura
IPC分类号： H01H71/24 , H01H71/10 , H01H71/44 , H01H9/00
CPC分类号： H01H71/446 , H01H71/1081
摘要： A trip device of a main circuit breaker is provided which causes only a branch circuit breaker to be set into a tripped state when an abnormal current occurs at a load of the branch circuit breaker while keeping a closed state of the main circuit breaker. The trip device of the circuit breaker has a structure including a trip latch mechanism for opening switching contacts, a stationary core, a movable core which is attracted to the stationary core to release the latch mechanism of a trip lever, an operating pin for interrupting movement of the movable core while the movable core is attracted, an operating spring charged with force when the movable core is attracted, and an inertia roller holding the operating pin, kicked when the operating spring discharges the force, and moved to a position which does not interrupt movement of the movable core. Accordingly, this structure allows a selective tripping system to be implemented simply with small size and low cost.
摘要翻译：提供了一种主断路器的跳闸装置，当保持主断路器的闭合状态时，在分支断路器的负载处发生异常电流时，仅使分支断路器被设定为跳闸状态。断路器的跳闸装置具有包括用于打开开关触点的跳闸闩锁机构的结构，固定铁芯，被吸引到固定铁芯以释放跳闸杆的闩锁机构的可动铁芯，用于中断运动的操作销当可动铁芯被吸引时，可动铁心被吸入时，在可动铁芯被吸引时施加力的操作弹簧和保持操作销的惯性辊在操作弹簧释放力时被踢动，并移动到不可移动的位置可动芯的中断运动。因此，该结构允许选择性跳闸系统简单地以小尺寸和低成本实现。

9. 发明授权

US4611188A Circuit breaker 失效
标题翻译：断路器
公开(公告)号：US4611188A
公开(公告)日：1986-09-09
申请号：US707687
申请日：1985-03-04
申请人： Wasaburo Murai , Takeshi Yura
发明人： Wasaburo Murai , Takeshi Yura
IPC分类号： H01H73/38 , H01H71/10 , H01H71/24 , H01H71/38 , H01H83/00
CPC分类号： H01H71/2409 , H01H71/1009 , H01H71/1072 , H01H71/2418 , H01H71/38
摘要： It is the main object of this invention to provide a circuit breaker in which the movable contacts have sufficient opening force and opening distance, and in which the breaking time is short. In order to attain the object, the circuit breaker of this invention is provided with a dead center link mechanism comprising a movable contact link which is rotatably supported by the arms of a cross bar which is operated so as to be capable of opening-closing the circuit and tripping by means of a trip-free mechanism, and a toggle spring which is bridged between the cross bar and the movable contact link. When a large current such as a short-circuit current flows, a movable steel plate attracted by an electromagnet for instantaneously tripping hits a rod for supporting the movable contacts which is connected to the movable contact link, whereby the dead center link mechanism makes the movable contacts open at high speed from the fixed contacts. As a result of such an operation, the current-limiting effect in this circuit breaker is excellent and breaking performance is improved.
摘要翻译：本发明的主要目的是提供一种断路器，其中可动触头具有足够的开启力和开启距离，并且断路时间短。为了实现该目的，本发明的断路器设置有死点连杆机构，该死点连杆机构包括可动接触连杆，该可动接触连杆由可横向摇动的臂可旋转地支撑，该横杆被操作以能够打开通过无跳闸机构的电路和跳闸，以及桥接在横杆和可动触头连杆之间的肘节弹簧。当诸如短路电流的大电流流动时，用于瞬时跳闸的电磁体吸引的可动钢板撞击用于支撑可动触头的杆，所述活动触点连接到可动触点，从而死点连杆机构使可动触头触点从固定触点高速打开。作为这种操作的结果，该断路器中的限流效果优异，并且提高了断路性能。

10. 发明授权

US08173841B2 Tetrahydro-naphthalene derivatives 失效
标题翻译：四氢萘衍生物
公开(公告)号：US08173841B2
公开(公告)日：2012-05-08
申请号：US13052482
申请日：2011-03-21
申请人： Masaomi Tajimi , Toshio Kokubo , Masahiro Shiroo , Yasuhiro Tsukimi , Takeshi Yura , Klaus Urbahns , Noriyuki Yamamoto , Muneto Mogi , Hiroshi Fujishima , Tsutomu Masuda , Nagahiro Yoshida , Toshiya Moriwaki
发明人： Masaomi Tajimi , Toshio Kokubo , Masahiro Shiroo , Yasuhiro Tsukimi , Takeshi Yura , Klaus Urbahns , Noriyuki Yamamoto , Muneto Mogi , Hiroshi Fujishima , Tsutomu Masuda , Nagahiro Yoshida , Toshiya Moriwaki
IPC分类号： C07C273/00 , A61K31/17
CPC分类号： C07D295/088 , C07C233/29 , C07C233/75 , C07C235/42 , C07C237/40 , C07C275/32 , C07C275/38 , C07C275/40 , C07C275/42 , C07C317/32 , C07C323/44 , C07C2602/10 , C07D207/27 , C07D211/22 , C07D211/46 , C07D211/62 , C07D295/135
摘要： This invention relates to tetrahydro-naphthalene derivatives and salts thereof which are useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontinence, chronic pain, neuropathic pain, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.
摘要翻译：本发明涉及可用作药物制剂活性成分的四氢萘衍生物及其盐。本发明的四氢萘衍生物作为VR1拮抗剂具有优异的活性，可用于预防和治疗与VR1活性相关的疾病，特别是用于治疗尿失禁，膀胱过度活动症，急迫性尿失禁，慢性疼痛，神经性疼痛，手术后疼痛，类风湿性关节炎疼痛，神经痛，神经病，痛觉，神经损伤，局部缺血，神经变性，中风，炎症性疾病，哮喘和COPD。

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