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1. 发明授权

US06841549B1 Condensed imidazole compounds and a therapeutic agent for diabetes mellitus 失效
标题翻译：缩合咪唑化合物和糖尿病治疗剂
公开(公告)号：US06841549B1
公开(公告)日：2005-01-11
申请号：US10018688
申请日：2000-06-30
申请人： Osamu Asano , Hitoshi Harada , Seiji Yoshikawa , Nobuhisa Watanabe , Takashi Inoue , Tatsuo Horizoe , Nobuyuki Yasuda , Kaya Ohashi , Hiroe Minami , Junsaku Nagaoka , Manabu Murakami , Seiichi Kobayashi , Isao Tanaka , Tsutomu Kawata , Naoyuki Shimomura , Hiroshi Akamatsu , Naoki Ozeki , Toshikazu Shimizu , Kenji Hayashi , Toyokazu Haga , Shigeto Negi , Toshihiko Naito
发明人： Osamu Asano , Hitoshi Harada , Seiji Yoshikawa , Nobuhisa Watanabe , Takashi Inoue , Tatsuo Horizoe , Nobuyuki Yasuda , Kaya Ohashi , Hiroe Minami , Junsaku Nagaoka , Manabu Murakami , Seiichi Kobayashi , Isao Tanaka , Tsutomu Kawata , Naoyuki Shimomura , Hiroshi Akamatsu , Naoki Ozeki , Toshikazu Shimizu , Kenji Hayashi , Toyokazu Haga , Shigeto Negi , Toshihiko Naito
IPC分类号： A61P3/10 , A61P43/00 , C07D471/04 , C07D473/00 , C07D473/34 , C07D473/40 , A16K31/33 , C07D239/70 , C07D471/00 , C07D487/00 , A16K31/52
CPC分类号： C07D471/04 , C07D473/00 , C07D473/34 , C07D473/40
摘要： The present invention provides a preventive or therapeutic agent for diabetes mellitus and diabetic complications, which is a new type based on an adenosine A2 receptor antagonist action.That is, it provides a novel condensed imidazole compound which has an adenosine A2 receptor antagonist action, is effective for preventing or treating diabetes mellitus and diabetic complications, and is represented by the formula (I); (wherein R1 represents e.g. an amino group which may be substituted with an alkyl group; R2 represents e.g. hydrogen atom, an alkyl group, a cycloalkyl group or an alkyl group, alkenyl group or alkynyl group which may be substituted with hydrox etc.; R3 represents e.g. an optionally substituted alkyl group, alkenyl group, alkynyl group, aryl group, heteroaryl group, pyridinone group, pyrimidinone group or piperadinone group; Ar represents e.g. an optionally substituted aryl or heteroaryl group; and Q and W are the same as or different from each other and each represents N or CH), a pharmacologically acceptable salt or hydrates thereof.
摘要翻译：本发明提供了一种基于腺苷A2受体拮抗剂作用的新型糖尿病和糖尿病并发症的预防或治疗剂。即提供了具有腺苷A2受体拮抗剂作用的新颖的缩合咪唑化合物，是有效预防或治疗糖尿病和糖尿病并发症，并由式（I）表示;（其中R 1表示例如可被烷基取代的氨基; R 2表示例如氢原子，可以被羟基取代的烷基，环烷基或烷基，烯基或炔基; R 3表示例如任选取代的烷基，烯基，炔基，芳基，杂芳基，吡啶酮基，嘧啶酮基或哌嗪酮基; Ar表示例如任选取代的芳基或杂芳基; Q和W彼此相同或不同，每个代表 N或CH），其药理学上可接受的盐或其水合物。

2. 发明授权

US07858809B2 Process for production of pyrazole-fused ring derivatives 失效
标题翻译：吡唑稠环衍生物的制备方法
公开(公告)号：US07858809B2
公开(公告)日：2010-12-28
申请号：US11578134
申请日：2005-04-08
申请人： Shigeto Negi , Toshikazu Shimizu , Hiroshi Kuroda , Naoyuki Shimomura , Manabu Sasho , Yorihisa Hoshino , Manabu Kuboto
发明人： Shigeto Negi , Toshikazu Shimizu , Hiroshi Kuroda , Naoyuki Shimomura , Manabu Sasho , Yorihisa Hoshino , Manabu Kuboto
IPC分类号： C07D231/54
CPC分类号： C07D471/04
摘要： Intermediates useful for the synthesis of pyrazole-fused ring derivatives, such as 7-phenylpyrazolo [1,5-a]pyridine derivatives, and method for producing the same. Method for producing compound represented by the general formula (II), wherein Z1 and Z2 each independently represents a methine group or a nitrogen atom; Rl represents an ethyl group or the like; R5 represents a hydrogen atom or the like; R2 and R3 each independently represents a C1-6 alkyl group or the like, salts thereof, or solvates of both, comprising the step of: reacting a compound represented by the general formula (I), wherein Z1, Z2, R5, R1, R2 and R3 each has the same definition as described above, with an organometallic reagent; and then reacting the resulting product with pentafluoroiodobenzene.
摘要翻译：用于合成吡唑稠合环衍生物如7-苯基吡唑并[1,5-a]吡啶衍生物的中间体及其制备方法。制备由通式（II）表示的化合物的方法，其中Z1和Z2各自独立地表示次甲基或氮原子; R1表示乙基等; R5表示氢原子等; R 2和R 3各自独立地表示C 1-6烷基等，其盐或两者的溶剂合物，包括以下步骤：使通式（I）表示的化合物与其反应，其中Z1，Z2，R5，R1， R2和R3各自具有与上述相同的定义，与有机金属试剂; 然后使所得产物与五氟碘苯反应。

3. 发明申请

US20070191613A1 Process for production of pyrazole-fused ring derivatives 失效
标题翻译：吡唑稠环衍生物的制备方法
公开(公告)号：US20070191613A1
公开(公告)日：2007-08-16
申请号：US11578134
申请日：2005-04-08
申请人： Shigeto Negi , Toshikazu Shimizu , Hiroshi Kuroda , Naoyuki Shimomura , Manabu Sasho , Yorihisa Hoshino , Manabu Kubota
发明人： Shigeto Negi , Toshikazu Shimizu , Hiroshi Kuroda , Naoyuki Shimomura , Manabu Sasho , Yorihisa Hoshino , Manabu Kubota
IPC分类号： C07D231/54
CPC分类号： C07D471/04
摘要： An object of the invention is to find out intermediates usful for the synthesis of pyrazol-fused ring derivatives (such as 7-phenylpyrazolo[1,5-a]pyridine derivatives) and a method for producing the same. A method for producing compound represented by the general formula (II), wherein Z1 and Z2 each independently represents a methine group or a nitrogen atom; R1 represents an ethyl group or the like; R5 represents a hydrogen atom or the like; R2 and R3 each independently represents a C1-6 alkyl group or the like, salts thereof, or solvates of both, comprising the step of: reacting a compound represented by the general formula (I), wherein Z1, Z2, R5, R1, R2 and R3 each has the same definition as described above, with an organometallic reagent; and then reacting the resulting product with pentafluoroiodobenzene.
摘要翻译：本发明的目的是找出有用于合成吡唑稠合环衍生物（如7-苯基吡唑并[1,5-a]吡啶衍生物）的中间体及其制备方法。由通式（II）表示的化合物，其中Z 1和Z 2各自独立地表示次甲基或氮原子的方法; R 1表示乙基等; R 5表示氢原子等; R 2和R 3各自独立地表示C 1-6烷基等，其盐或两者的溶剂合物，包括步骤：使通式（I）表示的化合物，其中Z 1，Z 2，R 5，R 5， 1，R 2和R 3各自具有与上述相同的定义与有机金属试剂; 然后使所得产物与五氟碘苯反应。

4. 发明授权

US5849912A Biphenyl derivatives 失效
标题翻译：联苯衍生物
公开(公告)号：US5849912A
公开(公告)日：1998-12-15
申请号：US855790
申请日：1997-05-12
申请人： Kozo Akasaka , Masahiro Yonaga , Akiharu Kajiwara , Kunizo Higurashi , Kohshi Ueno , Satoshi Nagato , Makoto Komatsu , Noritaka Kitazawa , Masataka Ueno , Yoshiharu Yamanishi , Yoshimasa Machida , Yuki Komatsu , Naoyuki Shimomura , Norio Minami , Toshikazu Shimizu , Atsushi Nagaoka
发明人： Kozo Akasaka , Masahiro Yonaga , Akiharu Kajiwara , Kunizo Higurashi , Kohshi Ueno , Satoshi Nagato , Makoto Komatsu , Noritaka Kitazawa , Masataka Ueno , Yoshiharu Yamanishi , Yoshimasa Machida , Yuki Komatsu , Naoyuki Shimomura , Norio Minami , Toshikazu Shimizu , Atsushi Nagaoka
IPC分类号： C07D295/03 , A61K31/495 , A61P25/18 , C07D213/26 , C07D213/30 , C07D213/38 , C07D213/50 , C07D213/70 , C07D295/02 , C07D295/04 , C07D295/073 , C07D295/088 , C07D295/096 , C07D295/112 , C07D295/135 , C07D295/155 , C07D295/205 , C07D295/26 , C07D307/14 , C07D307/52 , C07D319/06 , C07D339/08 , C07F7/18 , C07D401/06
CPC分类号： C07D213/30 , C07D213/26 , C07D213/38 , C07D213/50 , C07D213/70 , C07D295/02 , C07D295/073 , C07D295/088 , C07D295/096 , C07D295/112 , C07D295/135 , C07D295/155 , C07D295/205 , C07D295/26 , C07D307/14 , C07D307/52 , C07D319/06 , C07D339/08 , C07F7/1856 , C07C2101/02
摘要： A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are defined in the specification, is clinically useful for treating and ameliorating mental disorders such as cerebrovascular disorder, aggressive behavior due to senile dementia, mental excitation, poriomania, delirium, hallucination, hyperkinesia, schizophrenia, emotional disturbance, depression, neurosis, psychophysiologic disorder and anxiety neurosis. The compounds exhibit dopamine 2 receptor antagonism and/or serotonin 2 receptor antagonism.
摘要翻译：由下式（I）表示的联苯衍生物或其药学上可接受的盐：其中R 1，R 2，R 3，R 4和R 5在本说明书中定义，其在临床上可用于治疗和改善精神障碍脑血管障碍，老年性痴呆，精神激动，心脏虚弱，del妄，幻觉，运动过度，精神分裂症，情绪障碍，抑郁，神经症，心理生理障碍和焦虑神经症引起的侵略行为。该化合物表现出多巴胺2受体拮抗作用和/或5-羟色胺2受体拮抗作用。

5. 发明授权

US06281214B1 Biphenyl derivatives 失效
标题翻译：联苯衍生物
公开(公告)号：US06281214B1
公开(公告)日：2001-08-28
申请号：US09166229
申请日：1998-10-05
申请人： Kozo Akasaka , Masahiro Yonaga , Akiharu Kajiwara , Kunizo Higurashi , Kohshi Ueno , Satoshi Nagato , Makoto Komatsu , Noritaka Kitazawa , Masataka Ueno , Yoshiharu Yamanishi , Yoshimasa Machida , Yuki Komatsu , Naoyuki Shimomura , Norio Minami , Toshikazu Shimizu , Atsushi Nagaoka
发明人： Kozo Akasaka , Masahiro Yonaga , Akiharu Kajiwara , Kunizo Higurashi , Kohshi Ueno , Satoshi Nagato , Makoto Komatsu , Noritaka Kitazawa , Masataka Ueno , Yoshiharu Yamanishi , Yoshimasa Machida , Yuki Komatsu , Naoyuki Shimomura , Norio Minami , Toshikazu Shimizu , Atsushi Nagaoka
IPC分类号： A61K31495
CPC分类号： C07D213/30 , C07C2601/02 , C07D213/26 , C07D213/38 , C07D213/50 , C07D213/70 , C07D295/02 , C07D295/073 , C07D295/088 , C07D295/096 , C07D295/112 , C07D295/135 , C07D295/155 , C07D295/205 , C07D295/26 , C07D307/14 , C07D307/52 , C07D319/06 , C07D339/08 , C07F7/1804
摘要： A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: wherein R1, R2, R3, R4, and R5 are defined in the specification, is clinically useful for treating and ameliorating mental disorders such as cerebrovascular disorder, aggressive behavior due to senile dementia, mental excitation, poriomania, delirium, hallucination, hyperkinesia, schizophrenia, emotional disturbance, depression, neurosis, psychophysiologic disorder and anxiety neurosis. The compounds exhibit dopamine 2 receptor antagonism and/or serotonin 2 receptor antagonism.
摘要翻译：由下式（I）表示的联苯衍生物或其药理学上可接受的盐：其中R1，R2，R3，R4和R5在说明书中定义，在临床上可用于治疗和改善精神障碍如脑血管障碍，侵袭性老年性痴呆，精神激素，por妄症，del妄，幻觉，运动过度，精神分裂症，情绪障碍，抑郁症，神经症，心理生理障碍和焦虑神经症的行为。该化合物表现出多巴胺2受体拮抗作用和/或5-羟色胺2受体拮抗作用。

6. 发明申请

US20080227815A1 Crystal of Indole Derivative Having Piperidine Ring and Process for Production Thereof 审中-公开
标题翻译：具有哌啶环的吲哚衍生物的晶体及其制备方法
公开(公告)号：US20080227815A1
公开(公告)日：2008-09-18
申请号：US11913931
申请日：2006-05-11
申请人： Takahisa Sakaguchi , Yuichi Suzuki , Koichi Ito , Jun Niijima , Mamoru Miyazawa , Toshikazu Shimizu , Masaharu Gotoda , Naoko Suzuki , Takashi Hasebe
发明人： Takahisa Sakaguchi , Yuichi Suzuki , Koichi Ito , Jun Niijima , Mamoru Miyazawa , Toshikazu Shimizu , Masaharu Gotoda , Naoko Suzuki , Takashi Hasebe
IPC分类号： A61K31/454 , C07D405/14 , A61P25/18 , A61P25/30
CPC分类号： C07D405/14
摘要： A crystal of 1-[1-[2-(7-methoxy-2,2-dimethyl-4-oxochroman-8-yl)-ethyl]piperidin-4-yl]-N-methyl-1H-indole-6-carboxamide fumarate which has peaks at chemical shifts of about 124.0 ppm and about 26.8 ppm in a 13C solid NMR spectrum.
摘要翻译： 1- [1- [2-（7-甲氧基-2,2-二甲基-4-氧代色满-8-基） - 乙基]哌啶-4-基] -N-甲基-1H-吲哚-6- 富马酸甲酰胺，在13 C固体NMR光谱中具有约124.0ppm和约26.8ppm的化学位移的峰。

7. 发明授权

US5565883A Active matrix liquid crystal display unit capable of suppressing flicker and cross talk 失效
标题翻译：有源矩阵液晶显示单元能够抑制闪烁和串扰
公开(公告)号：US5565883A
公开(公告)日：1996-10-15
申请号：US266111
申请日：1994-06-27
申请人： Toshikazu Shimizu
发明人： Toshikazu Shimizu
IPC分类号： G02F1/133 , G02F1/136 , G02F1/1368 , G09G3/20 , G09G3/36
CPC分类号： G09G3/3648 , G09G2320/0209 , G09G2320/0247 , G09G3/2011 , G09G3/2018 , G09G3/3614
摘要： In an active matrix liquid crystal display unit for displaying data on a liquid crystal panel in response to a control signal, a drain driver is supplied with the control signal to supply a first alternating voltage signal of a predetermined phase to odd-numbered drain buses for drain electrodes of thin-film transistors arranged in a matrix of the panel and to supply even-numbered drain buses with a second alternating voltage signal having a reversed phase which is reversed relative to the predetermined phase. A gate driver supplies the gate buses with electric power cyclically in cycles. Preferably, the first and the second alternating voltage signals have a common period which is equal to a time interval during which the electric power is supplied successively to two adjacent ones of the gate buses. This avoids flicker and cross talk in a display of the data. More preferably, the first and the second alternating voltage signals are given either in each cycle or in a preselected plurality of cycles one of a predetermined number of voltages to cope with a greater number of steps of a tone of the display.
摘要翻译：在用于响应于控制信号在液晶面板上显示数据的有源矩阵液晶显示单元中，为漏极驱动器提供控制信号，以将预定相位的第一交流电压信号提供给奇数编号的漏极总线以面板的矩阵形式布置的薄膜晶体管的漏电极，并且为具有反相的第二交流电压信号提供偶数的漏极总线，所述第二交流电压信号相对于预定相位反相。栅极驱动器以周期性循环供电电源。优选地，第一和第二交流电压信号具有等于将电力连续提供给两个相邻栅极总线的时间间隔的公共周期。这避免了数据显示中的闪烁和串扰。更优选地，第一和第二交流电压信号在每个周期中以预定的多个周期中的一个预定数量的电压中给出，以应对显示器的色调的更多数量的步骤。

8. 发明授权

US06676468B2 Method of producing a spark plug 有权
标题翻译：火花塞的制造方法
公开(公告)号：US06676468B2
公开(公告)日：2004-01-13
申请号：US09985356
申请日：2001-11-02
申请人： Hiroya Ishiguro , Kozo Takamura , Toshikazu Shimizu
发明人： Hiroya Ishiguro , Kozo Takamura , Toshikazu Shimizu
IPC分类号： H01T2102
CPC分类号： H01T21/02
摘要： In producing a spark plug including a central electrode having a first chip including noble metal and an earth electrode having a second chip including the noble metal, a spark gap being disposed between the first and second chips, a chip including the noble metal. The chip is welded to an end of the central electrode and to an end of the earth electrode. The welded chip is cut to form the first and second chips and the spark gap.
摘要翻译：在制造包括具有包括贵金属的第一芯片的中心电极和具有包括贵金属的第二芯片的接地电极的火花塞时，设置在第一和第二芯片之间的火花隙，包括贵金属的芯片。该芯片焊接到中心电极的一端和接地电极的端部。焊接的芯片被切割以形成第一和第二芯片和火花隙。

9. 发明授权

US06504523B1 Active matrix LCD device 有权
标题翻译：有源矩阵液晶显示装置
公开(公告)号：US06504523B1
公开(公告)日：2003-01-07
申请号：US09723492
申请日：2000-11-28
申请人： Noriaki Sugawara , Kimikazu Matsumoto , Kunimasa Itakura , Tatsuya Shiki , Toshikazu Shimizu , Shoichi Kuroha , Shinichi Nishida
发明人： Noriaki Sugawara , Kimikazu Matsumoto , Kunimasa Itakura , Tatsuya Shiki , Toshikazu Shimizu , Shoichi Kuroha , Shinichi Nishida
IPC分类号： G09G336
CPC分类号： G02F1/134363 , G02F1/133514 , G09G3/3614 , G09G3/3648 , G09G2300/0434 , G09G2320/0247 , G09G2330/021
摘要： An active-matrix LCD device drives the LCD panel by using a dot reversible driving technique. The switching between two sets of input signals or two resolution modes is conducted by applying a DC voltage between the pixel electrode and the common electrode in each pixel before restart of the image display of a switched signal. The DC voltage has the same polarity among the pixels in the pixel array to thereby reduce the flicker after the restart of the image display.
摘要翻译：有源矩阵LCD设备通过使用点可逆驱动技术来驱动LCD面板。在重新开始切换信号的图像显示之前，通过在像素电极和公共电极之间施加直流电压来进行两组输入信号或两种分辨率模式之间的切换。 DC电压在像素阵列中的像素之间具有相同的极性，从而在图像显示重新开始之后减少闪烁。

10. 发明授权

US5583229A Process for the preparation of imidazopyridine derivatives 失效
标题翻译：咪唑并吡啶衍生物的制备方法
公开(公告)号：US5583229A
公开(公告)日：1996-12-10
申请号：US256869
申请日：1994-08-05
申请人： Yoshio Urawa , Ken Furukawa , Toshikazu Shimizu , Yoji Yamagishi , Tomio Tsurugi , Tomio Ichino
发明人： Yoshio Urawa , Ken Furukawa , Toshikazu Shimizu , Yoji Yamagishi , Tomio Tsurugi , Tomio Ichino
IPC分类号： C07C63/72 , C07C65/105 , C07C69/732 , C07C69/76 , C07D213/73 , C07D213/75 , C07D263/10 , C07D263/12 , C07D263/14 , C07D309/12 , C07D413/12 , C07D471/04
CPC分类号： C07D213/73 , C07C63/72 , C07C65/105 , C07C69/732 , C07C69/76 , C07D213/75 , C07D263/10 , C07D263/12 , C07D263/14 , C07D309/12 , C07D413/12 , C07D471/04 , Y02P20/55
摘要： The present invention provides an industrially advantageous process for preparing a 2-alkyl-3-(biphenyl-4-yl)methyl-3H-imidazo[4,5-b]pyridine derivative represented by the following formula (II) which is a precursor of an antagonist against an angiotensin II receptor useful as an antihypertensive drug, a biphenyl derivative which is a precursor of the substituent of the pyridine derivative, a process for the preparation thereof, and an intermediate useful for the preparation of the biphenyl derivative: ##STR1##
摘要翻译： PCT No.PCT / JP93 / 01776 Sec。 371日期：1994年8月5日 102（e）日期1994年8月5日PCT 1993年12月7日PCT公布。公开号WO94 / 13666 日期：1994年6月23日本发明提供了制备由下式（II）表示的2-烷基-3-（联苯-4-基）甲基-3H-咪唑并[4,5-b]吡啶衍生物的工业上有利的方法），其是用作抗高血压药物的血管紧张素II受体的拮抗剂的前体，作为吡啶衍生物的取代基的前体的联苯衍生物，其制备方法和可用于制备联苯衍生物：（II）

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