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1. 发明授权

US5776945A 4A-aryldecahydroisoquinoline compound and medicinal use of the same 失效
标题翻译： 4A-芳基十氢异喹啉化合物及其药用
公开(公告)号：US5776945A
公开(公告)日：1998-07-07
申请号：US809226
申请日：1997-05-08
申请人： Hiroshi Nagase , Yoshifumi Imamura , Hiroshi Ohno , Takashi Endo
发明人： Hiroshi Nagase , Yoshifumi Imamura , Hiroshi Ohno , Takashi Endo
IPC分类号： C07D217/16 , C07D405/12 , C07D217/04 , A61K31/46
CPC分类号： C07D405/12 , C07D217/16
摘要： The present invention relates to a 4a-aryldecahydroisoquinoline compound, which is represented by a compound 1, or a pharmacologically acceptable salt thereof. ##STR1## As the results of in vitro and in vivo pharmacological evaluations, it was found that the compounds of the present invention had excellent preventive effects on ischemic death of cerebral neurocytes, suppressive effects on development of cerebral infarction, and strong analgesic and antitussive effects; therefore the compounds of the present invention can be utilized in the medicinal field as a useful cerebral cytoprotective agent, which is aimed at preventing and treating cerebrovascular disorder, ischemic cerebral disorder, cerebral neurocyte disorder, and dementia, an analgesic, and an antitussive.
摘要翻译： PCT No.PCT / JP96 / 02030 Sec。 371日期：1997年5月8日 102（e）日期1997年5月8日PCT PCT 1996年7月19日PCT公布。公开号WO97 / 03968 日期：1997年2月6日本发明涉及由化合物1表示的4a-芳基十氢异喹啉化合物或其药理学上可接受的盐。作为体外和体内药理学评价的结果，发现本发明的化合物对脑神经细胞的缺血性死亡具有优异的预防作用，对脑梗死发展的抑制作用以及强镇痛和镇咳药效果; 因此，本发明的化合物可用作药用领域，作为有用的脑细胞保护剂，其旨在预防和治疗脑血管障碍，缺血性脑病，脑神经细胞病和痴呆，镇痛药和镇咳药。

2. 发明授权

US6147084A Brain cell protective agent 失效
标题翻译：脑细胞保护剂
公开(公告)号：US6147084A
公开(公告)日：2000-11-14
申请号：US262791
申请日：1999-03-04
申请人： Hiroshi Nagase , Yoshifumi Imamura , Takashi Endo , Susumu Matsuda , Yasushi Miyauchi
发明人： Hiroshi Nagase , Yoshifumi Imamura , Takashi Endo , Susumu Matsuda , Yasushi Miyauchi
IPC分类号： A61K31/485 , C07D489/00 , C07D491/08
CPC分类号： A61K31/485 , C07D489/00
摘要： The present invention relates to a novel brain cell protective agent having for its active ingredient a morphinan derivative represented with Compound 1 ##STR1## or pharmacologically acceptable acid addition salt thereof. The compounds used in the present invention were found to have excellent defensive effects against brain nerve cell necrosis in both in vitro and in vivo pharmacological evaluations, and can be used as useful preventive and therapeutic agents of ischemic brain disorders, brain nerve cell disorders and dementia.
摘要翻译：本发明涉及一种新颖的脑细胞保护剂，其具有由化合物1表示的吗啡喃衍生物或其药理学上可接受的酸加成盐。发现本发明中使用的化合物在体外和体内药理学评价中对脑神经细胞坏死具有优异的防御作用，并且可以用作缺血性脑病，脑神经细胞病症和痴呆的有用的预防和治疗剂。

3. 发明授权

US5972953A Brain cell protective agent 失效
公开(公告)号：US5972953A
公开(公告)日：1999-10-26
申请号：US745041
申请日：1996-11-07
申请人： Hiroshi Nagase , Yoshifumi Imamura , Takashi Endo , Susumu Matsuda , Yasushi Miyauchi
发明人： Hiroshi Nagase , Yoshifumi Imamura , Takashi Endo , Susumu Matsuda , Yasushi Miyauchi
IPC分类号： A61K31/485 , C07D489/00
CPC分类号： A61K31/485 , C07D489/00
摘要： The present invention relates to a novel brain cell protective agent having for its active ingredient a morphinan derivative represented with Compound 1 ##STR1## or pharmacologically acceptable acid addition salt thereof. The compounds used in the present invention were found to have excellent defensive effects against brain nerve cell necrosis in both in vitro and in vivo pharmacological evaluations, and can be used as useful preventive and therapeutic agents of ischemic brain disorders, brain nerve cell disorders and dementia.

4. 发明授权

US5714483A Antitussive 失效
标题翻译：镇咳药
公开(公告)号：US5714483A
公开(公告)日：1998-02-03
申请号：US290837
申请日：1994-10-13
申请人： Hiroshi Nagase , Junzo Kamei , Koji Kawai , Takashi Endo
发明人： Hiroshi Nagase , Junzo Kamei , Koji Kawai , Takashi Endo
IPC分类号： A61K31/485 , A61K31/495 , C07D489/00 , C07D491/18 , C07D491/22 , A61K31/535
CPC分类号： A61K31/495 , A61K31/485 , C07D489/00
摘要： An antitussive having high activity, which is free from side effects such as psychotomimetic, which may also be administered orally is disclosed. The antitussive according to the present invention comprises as an effective ingredient a .delta.-opioid antagonist or a pharamaceutically acceptable salt thereof.
摘要翻译： PCT No.PCT / JP93 / 01855 Sec。 371日期：1994年10月13日 102（e）日期1994年10月13日PCT 1993年12月22日PCT公布。公开号WO94 / 14445 PCT 日期：1994年7月7日公开了一种具有高活性的镇咳药，其也没有副作用，如精神病药，也可以口服给药。根据本发明的止咳剂包含作为有效成分的δ-阿片样拮抗剂或其药物上可接受的盐。

5. 发明授权

US5244904A Indole derivatives 失效
标题翻译： INDOLE DORIVATIVES
公开(公告)号：US5244904A
公开(公告)日：1993-09-14
申请号：US828889
申请日：1992-01-29
申请人： Hiroshi Nagase , Akira Mizusuna , Yoshihiro Onoda , Koji Kawai , Shu Matsumoto , Takashi Endo
发明人： Hiroshi Nagase , Akira Mizusuna , Yoshihiro Onoda , Koji Kawai , Shu Matsumoto , Takashi Endo
IPC分类号： C07D217/06 , C07D217/24 , C07D471/04 , C07D491/056
CPC分类号： C07D471/04 , C07D217/06 , C07D217/24 , Y10S514/885
摘要： This invention is directed to a indole derivative represented by the general formula (1) ##STR1## wherein R.sub.1 stands for alkyl of 1 to 5 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms, cycloalkenylalkyl of 5 to 7 carbon atoms, aralkyl of 7 to 14 carbon atoms, trans-alkenyl of 4 to 5 carbon atoms, allyl, furanyl-2-ylalkyl of 1 to 5 carbon atoms, thienyl-2-ylalkyl of 1 to 5 carbon atoms, vinyloxycarbonyl, trichloroethoxycarbonyl, benzyloxycarbonyl, alkanoyl of 1 to 5 carbon atoms, aralkylcarbonyl of 7 to 14 carbon atoms, 2-furoyl, thiophene-2-carbonyl, cycloalkylcarbonyl of 4 to 7 carbon atoms, alkenylcarbonyl of 3 to 8 carbon atoms, or anisoyl, R.sub.2 for a hydrogen atoms, alkyl of 1 to 3 carbon atoms, benzyl, or alkanoyl of 1 to 5 carbon atoms, R.sub.3 for a hydrogen atoms, a fluorine atom, a chlorine atom, a bromine atom, nitro, or alkyl of 1 to 5 carbon atoms, R.sub.4 for a hydrogen atom, alkyl of 1 to 5 carbon atoms, benzyl, or phenyl, and R.sub.5 for a hydrogen atom, hydroxy, or alkanoyloxy of 1 to 5 carbon atoms, providing that said general formula (1) embraces a (+) form, a (-) form, and a (.+-.) form, or a pharmacologically acceptable salt thereof and to an immunorepressing agent having as an active component thereof the indole derivative or the pharmacologically acceptable salt thereof.
摘要翻译： PCT No.PCT / JP91 / 00759 Sec。 371日期1992年1月29日 102（e）日期1992年1月29日PCT Filed 1991年6月5日PCT公布。 WO91 / 18901 PCT出版物日本1991年12月12日。本发明涉及由通式（1）表示的吲哚衍生物，其中R1代表1至5个碳原子的烷基，4至7个碳原子的环烷基烷基，环烯基烷基 5至7个碳原子的芳烷基，7至14个碳原子的芳烷基，4至5个碳原子的反式链烯基，1至5个碳原子的烯丙基，呋喃基-2-基烷基，1至5个碳原子的噻吩基-2-基烷基，乙氧基羰基，三氯乙氧基羰基，苄氧基羰基，1〜5个碳原子的烷酰基，7〜14个碳原子的芳烷基羰基，2-糠酰基，噻吩-2-羰基，4〜7个碳原子的环烷基羰基，3〜8个碳原子的链烯基羰基，甲氧基苯甲酰基，R2为氢原子，1〜3个碳原子的烷基，苄基或1〜5个碳原子的烷酰基，R3为氢原子，氟原子，氯原子，溴原子，硝基或烷基 1至5个碳原子，R4代表氢原子，1至5个碳原子的烷基，苄基或苯基，R5代表氢原子，羟基 y）或1至5个碳原子的烷酰氧基，条件是所述通式（1）包含（+）形式，（ - ）形式和（+/-）形式或其药理学上可接受的盐，以及作为活性成分的吲哚衍生物或其药理学上可接受的盐的免疫抑制剂。

6. 发明授权

US08637539B2 Remedies for neuropathic pain and model animals of neuropathic pain 有权
标题翻译：神经性疼痛和模型动物的神经性疼痛的补救措施
公开(公告)号：US08637539B2
公开(公告)日：2014-01-28
申请号：US11206489
申请日：2005-08-18
申请人： Hiroshi Nagase , Takashi Endo , Kuniaki Kawamura , Toshiaki Tanaka , Tomohiko Suzuki , Tsutomu Suzuki , Yasushi Kuraishi , Kimiyasu Shiraki
发明人： Hiroshi Nagase , Takashi Endo , Kuniaki Kawamura , Toshiaki Tanaka , Tomohiko Suzuki , Tsutomu Suzuki , Yasushi Kuraishi , Kimiyasu Shiraki
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： A61K31/485 , A61K31/4745 , C07D489/08
摘要： The present invention relates to a therapeutic agent for neuropathic pain containing, as an active ingredient, a compound represented by general formula (I) or a pharmacologically acceptable acid addition salt thereof: (wherein R1, R2, R3, R4, R5, R6, R7, R8, A, and B have the same definitions as those described in the specification), and an animal model produced by administering (+)-4a-(3-hydroxyphenyl)-2-methyl-1,2,3,4,4a,5,12,12a-octohydro-trans-quinolino[2,3-g]isoquinoline. The present invention makes it possible to perform drug treatment for neuropathic pain. The therapeutic effect of a compound against neuropathic pain can also be evaluated.
摘要翻译：本发明涉及神经性疼痛治疗剂，其含有作为活性成分的通式（I）表示的化合物或其药理学上可接受的酸加成盐：（其中R1，R2，R3，R4，R5，R6， R7，R8，A和B具有与说明书中描述的定义相同的定义）和通过给予（+） - 4a-（3-羟基苯基）-2-甲基-1,2,3,4 ，4a，5,12,12a-八氢 - 反 - 喹啉并[2,3-g]异喹啉。本发明使得可以进行神经性疼痛的药物治疗。也可以评价化合物对神经性疼痛的治疗效果。

7. 发明授权

US5539119A Indole derivatives 失效
标题翻译：吲哚衍生物
公开(公告)号：US5539119A
公开(公告)日：1996-07-23
申请号：US36521
申请日：1993-03-24
申请人： Hiroshi Nagase , Akira Mizusuna , Yoshihiro Onoda , Koji Kawai , Shu Matsumoto , Takashi Endo
发明人： Hiroshi Nagase , Akira Mizusuna , Yoshihiro Onoda , Koji Kawai , Shu Matsumoto , Takashi Endo
IPC分类号： C07D217/06 , C07D217/24 , C07D471/04 , C07D491/056 , C07D217/14
CPC分类号： C07D471/04 , C07D217/06 , C07D217/24 , Y10S514/885
摘要： This invention is directed to a indole derivative represented by the general formula (1) ##STR1## wherein R.sub.1 stands for alkyl of 1 to 5 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms, cycloalkenylalkyl of 5 to 7 carbon atoms, aralkyl of 7 to 14 carbon atoms, trans-alkenyl of 4 or 5 carbon atoms, allyl, furanyl-2-ylalkyl of 1 to 5 carbon atoms, thienyl-2-ylalkyl of 1 to 5 carbon atoms, vinyloxycarbonyl, trichloroethoxycarbonyl, benzyloxycarbonyl, alkanoyl of 1 to 5 carbon atoms, aralkylcarbonyl of 7 to 14 carbon atoms, 2-furoyl, thiophene-2-carbonyl, cycloalkylcarbonyl of 4 to 7 carbon atoms, alkenylcarbonyl of 3 to 8 carbon atoms, or anisoyl, providing that said general formula (1) embraces a (+) form, a (-) form, and a (.+-.) form, or a pharmacologically acceptable salt thereof and to an immunorepressing agent having as an active component thereof the indole derivative or the pharmacologically acceptable salt thereof.
摘要翻译：本发明涉及由通式（1）表示的吲哚衍生物，其中R1表示1至5个碳原子的烷基，4至7个碳原子的环烷基烷基，5至7个碳原子的环烯基烷基， 7至14个碳原子的芳烷基，4或5个碳原子的反式链烯基，1至5个碳原子的烯丙基，呋喃基-2-基烷基，1至5个碳原子的噻吩基-2-基烷基，乙烯氧基羰基，三氯乙氧羰基，苄氧羰基，具有1至5个碳原子的烷酰基，7至14个碳原子的芳烷基羰基，2-糠酰基，噻吩-2-羰基，4至7个碳原子的环烷基羰基，3至8个碳原子的链烯基羰基或茴香酰基，条件是所述通式（1）包含（+）形式，（ - ）形式和（+/-）形式或其药理学上可接受的盐，并且具有作为其活性成分的吲哚衍生物或药理学上可接受的盐的免疫抑制剂其中。

8. 发明申请

US20060094741A1 Remedies for neuropathic pain and model animals of neuropathic pain 有权
标题翻译：神经性疼痛和模型动物的神经性疼痛的补救措施
公开(公告)号：US20060094741A1
公开(公告)日：2006-05-04
申请号：US11206489
申请日：2005-08-18
申请人： Hiroshi Nagase , Takashi Endo , Kuniaki Kawamura , Toshiaki Tanaka , Tomohiko Suzuki , Tsutomu Suzuki , Yasushi Kuraishi , Kimiyasu Shiraki
发明人： Hiroshi Nagase , Takashi Endo , Kuniaki Kawamura , Toshiaki Tanaka , Tomohiko Suzuki , Tsutomu Suzuki , Yasushi Kuraishi , Kimiyasu Shiraki
IPC分类号： A61K31/4745 , A61K49/00 , C07D471/04
CPC分类号： A61K31/485 , A61K31/4745 , C07D489/08
摘要： The present invention relates to a therapeutic agent for neuropathic pain containing, as an active ingredient, a compound represented by general formula (I) or a pharmacologically acceptable acid addition salt thereof: (wherein R1, R2, R3, R4, R5, R6, R7, R8, A, and B have the same definitions as those described in the specification), and an animal model produced by administering (+)-4a-(3-hydroxyphenyl)-2-methyl-1,2,3,4,4a,5,12,12a-octohydro-trans-quinolino[2,3-g]isoquinoline. The present invention makes it possible to perform drug treatment for neuropathic pain. The therapeutic effect of a compound against neuropathic pain can also be evaluated.
摘要翻译：本发明涉及神经性疼痛治疗剂，其含有作为活性成分的通式（I）表示的化合物或其药理学上可接受的酸加成盐：（其中R 1，R 2， R 2，R 3，R 4，R 5，R 6，R 6， A +和B B具有与说明书中描述的那些相同的定义）和通过给予（+） - 4a-（3- 羟基苯基）-2-甲基-1,2,3,4,4a，5,12,12a-八氢 - 反 - 喹啉并[2,3-g]异喹啉。本发明使得可以进行神经性疼痛的药物治疗。也可以评价化合物对神经性疼痛的治疗作用。

9. 发明授权

US5849731A Indole derivatives and medical application thereof 失效
标题翻译：吲哚衍生物及其医疗应用
公开(公告)号：US5849731A
公开(公告)日：1998-12-15
申请号：US836742
申请日：1997-05-16
申请人： Hiroshi Nagase , Koji Kawai , Takashi Endo , Shinya Ueno , Masayuki Maeda , Satoshi Sakami
发明人： Hiroshi Nagase , Koji Kawai , Takashi Endo , Shinya Ueno , Masayuki Maeda , Satoshi Sakami
IPC分类号： C07D491/22 , A61K31/475
CPC分类号： C07D491/22
摘要： The present invention relates to indole derivatives represented by the following compound 1 and the pharmacologically acceptable acid addition salt thereof. ##STR1## The compounds of the present invention were found to exhibit strong antitussive and analgesic actions as a result of pharmacological evaluation, and can be used in the pharmaceutical field as effective antitussives and analgesics.
摘要翻译： PCT No.PCT / JP96 / 02791 Sec。 371日期：1997年5月16日 102（e）日期1997年5月16日PCT提交1996年9月26日PCT公布。公开号WO97 / 11948 PCT 日期1997年4月3日本发明涉及由以下化合物1表示的吲哚衍生物及其药理学上可接受的酸加成盐。发现本发明的化合物作为药理学评价的结果表现出强烈的镇咳和镇痛作用，并且可以在制药领域中用作有效的镇咳药和镇痛药。

10. 发明授权

US08823885B2 Projector 有权
标题翻译：投影机
公开(公告)号：US08823885B2
公开(公告)日：2014-09-02
申请号：US13040746
申请日：2011-03-04
申请人： Tomoharu Masuda , Takashi Endo
发明人： Tomoharu Masuda , Takashi Endo
IPC分类号： G02F1/1335 , G03B21/14 , H04N9/31 , G03B33/12
CPC分类号： G03B21/14 , G03B21/006 , G03B21/2053 , G03B21/206 , G03B21/2073 , G03B33/12 , H04N9/3167
摘要： A projector includes: an illuminator that outputs illumination light; a light modulator including a liquid crystal panel and a structural birefringent polarization separation element having a polarization separation surface inclined away from a central axis of the illumination light, the light modulator modulating the illumination light from the illuminator; and a projection system that projects the light modulated by the light modulator, wherein the illumination light outputted from the illuminator has an angular distribution in a first direction, which is perpendicular to the central axis of the illumination light, smaller than the angular distribution in a second direction, which is perpendicular to the first direction and the central axis of the illumination light, and the polarization separation surface of the structural birefringent polarization separation element has a structure that is not periodic along the first direction but is periodic along the second direction.
摘要翻译：投影仪包括：输出照明光的照明器; 一种光调制器，包括液晶面板和结构双折射偏振分离元件，其具有偏离照明光的中心轴倾斜的偏振分离表面，所述光调制器调制来自照明器的照明光; 以及投影系统，投射由光调制器调制的光，其中从照明器输出的照明光在与照明光的中心轴垂直的第一方向上具有小于角度分布的角度分布第二方向，其垂直于照明光的第一方向和中心轴，并且结构双折射偏振分离元件的偏振分离表面具有沿着第一方向不是周期性的结构，但沿着第二方向是周期性的。

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