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公开(公告)号:US06642264B1
公开(公告)日:2003-11-04
申请号:US09958174
申请日:2001-10-05
申请人: Satoshi Hayashibe , Hirotsune Itahana , Masamichi Okada , Atsuyuki Kohara , Kyoichi Maeno , Kiyoshi Yahiro , Itsuro Shimada , Kazuhito Tanabe , Kenji Negoro , Takashi Kamikubo , Shuichi Sakamoto
发明人: Satoshi Hayashibe , Hirotsune Itahana , Masamichi Okada , Atsuyuki Kohara , Kyoichi Maeno , Kiyoshi Yahiro , Itsuro Shimada , Kazuhito Tanabe , Kenji Negoro , Takashi Kamikubo , Shuichi Sakamoto
IPC分类号: A61K31425
CPC分类号: C07D513/04 , A61K31/429
摘要: This invention relates to novel thiazolo[3,2-a]benzoimidazole derivatives represented by the following general formula (I). The compounds provided by the invention act specifically on metabotropic glutamate receptors and are used as medicaments. The invention also provides novel compounds useful as intermediates for the synthesis of the compounds of the invention. (Symbols in the formula represent the following meanings. R1: carbamoyl, carbonyl, oxy, amino, carbonylamino or the like which may be substituted; R2: hydrogen, lower alkyl or the like; and R3, R4 and R5: hydrogen, lower alkyl and the like which may be the same or different from one another.)
摘要翻译: 本发明涉及由以下通式(I)表示的新型噻唑并[3,2-a]苯并咪唑衍生物。 本发明提供的化合物特异性地代表代谢型谷氨酸受体并用作药物。 本发明还提供了可用作合成本发明化合物的中间体的新化合物(式中的符号表示以下含义:R 1:可以被取代的氨基甲酰基,羰基,氧基,氨基,羰基氨基等 R 2:氢,低级烷基等; R 3,R 4和R 5:氢,低级烷基等可以彼此相同或不同。)
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公开(公告)号:US07250429B2
公开(公告)日:2007-07-31
申请号:US10508329
申请日:2003-03-19
申请人: Hirotsune Itahana , Jiro Fujiyasu , Satoshi Hayashibe , Toshihiro Watanabe , Masamichi Okada , Takashi Toya
发明人: Hirotsune Itahana , Jiro Fujiyasu , Satoshi Hayashibe , Toshihiro Watanabe , Masamichi Okada , Takashi Toya
IPC分类号: A61K31/429 , C07D513/04
CPC分类号: A61K31/429 , A61K31/5377 , C07D513/04
摘要: This invention relates to the provision of novel aminomethyl-substituted thiazolobenzimidazole derivatives represented by the following general formula (I) or a salt thereof.The aforementioned derivative or a salt thereof has a metabotropic glutamate receptor action and excellent oral activity and is therefore useful as a medicament. (In the formula, R1: an oxygen-containing saturated hetero ring or the like, Alk1: a lower alkylene, m: 0 or 1, Alk2: a lower alkylene which may be substituted with oxo group, n: 0 or 1, X: a bond, O, S or NR5, R3: H or the like, and R2, R4, R5, R6 and R7: the same or different from one another and each represents H or the like. Provided that R3 does not represent a lower alkyl or a halogeno-lower alkyl when X is a bond and n is 1. Also, R4 represents a group other than Me when m is 1, R1 is OH or OMe and Alk1 is a C1-3 alkylene, and further 1) when X is a bond, n is 1 and R3 is H, or 2) when X is a bond, n is 0 and R3 is cyclohexane.)
摘要翻译: 本发明涉及提供由以下通式(I)表示的新型氨基甲基取代的噻唑并苯并咪唑衍生物或其盐。 上述衍生物或其盐具有代谢型谷氨酸受体作用和优异的口服活性,因此可用作药物。 (式中,R 1:含氧饱和杂环等,Alk 1:低级亚烷基,m:0或1,Alk, 2:可以被氧代基取代的低级亚烷基,n:0或1,X:键,O,S或NR 5,R 3 O >:H等,R 2,R 4,R 5,R 6和R 6, 其中R 3彼此相同或不同,并且各自表示H等,条件是R 3不表示低级烷基或卤代低级烷基,当X为 键,n为1.另外,当m为1时,R 4表示除Me以外的基团,R 1是OH或OMe,Alk 1 SUB >是C 1-3亚烷基,进一步1)当X为键时,n为1且R 3为H,或2)当X为键时 ,n为0,R 3为环己烷)
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公开(公告)号:US20050148642A1
公开(公告)日:2005-07-07
申请号:US10508329
申请日:2003-03-19
申请人: Hirotsune Itahana , Jiro Fujiyasu , Satoshi Hayashibe , Toshihiro Watanabe , Masamichi Okada , Takashi Toya
发明人: Hirotsune Itahana , Jiro Fujiyasu , Satoshi Hayashibe , Toshihiro Watanabe , Masamichi Okada , Takashi Toya
IPC分类号: A61K31/429 , A61K31/5377 , A61P9/10 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/28 , A61P43/00 , C07D513/04 , A61K31/43 , C07D498/04
CPC分类号: A61K31/429 , A61K31/5377 , C07D513/04
摘要: This invention relates to the provision of novel aminomethyl-substituted thiazolobenzimidazole derivatives represented by the following general formula (I) or a salt thereof. The aforementioned derivative or a salt thereof has a metabotropic glutamate receptor action and excellent oral activity and is therefore useful as a medicament. (In the formula, R1: an oxygen-containing saturated hetero ring or the like, Alk1: a lower alkylene, m: 0 or 1, Alk2: a lower alkylene which may be substituted with oxo group, n: 0 or 1, X: a bond, O, S or NR5, R3: H or the like, and R2, R4, R5, R6 and R7: the same or different from one another and each represents H or the like. Provided that R3 does not represent a lower alkyl or a halogeno-lower alkyl when X is a bond and n is 1. Also, R4 represents a group other than Me when m is 1, R1 is OH or OMe and Alk1 is a C1-3 alkylene, and further 1) when X is a bond, n is 1 and R3 is H, or 2) when X is a bond, n is 0 and R3 is cyclohexane.)
摘要翻译: 本发明涉及提供由以下通式(I)表示的新型氨基甲基取代的噻唑并苯并咪唑衍生物或其盐。 上述衍生物或其盐具有代谢型谷氨酸受体作用和优异的口服活性,因此可用作药物。 (式中,R 1:含氧饱和杂环等,Alk 1:低级亚烷基,m:0或1,Alk, 2:可以被氧代基取代的低级亚烷基,n:0或1,X:键,O,S或NR 5,R 3 O >:H等,R 2,R 4,R 5,R 6和R 6, 其中R 3彼此相同或不同,并且各自表示H等,条件是R 3不表示低级烷基或卤代低级烷基,当X为 键,n为1.另外,当m为1时,R 4表示除Me以外的基团,R 1是OH或OMe,Alk 1 SUB >是C 1-3亚烷基,进一步1)当X为键时,n为1且R 3为H,或2)当X为键时 ,n为0,R 3为环己烷)
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公开(公告)号:US06664283B1
公开(公告)日:2003-12-16
申请号:US10031404
申请日:2002-05-15
IPC分类号: A61K31415
CPC分类号: A61K31/429 , A61K31/00
摘要: This invention relates to pharmaceuticals for neuropathic pains comprising an mGluR1 receptor antagonist for systemic administration. Drugs efficacious in treating various neuropathic pain can be provided by the invention.
摘要翻译: 本发明涉及用于神经性疼痛的药物,其包含用于全身给药的mGluR1受体拮抗剂。 可以通过本发明提供治疗各种神经性疼痛的药物。
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公开(公告)号:US6096743A
公开(公告)日:2000-08-01
申请号:US809087
申请日:1997-03-05
申请人: Jun-ichi Shishikura , Hiroshi Inami , Shuichi Sakamoto , Shin-ichi Tsukamoto , Masao Sasamata , Masamichi Okada , Mitsuo Fujii
发明人: Jun-ichi Shishikura , Hiroshi Inami , Shuichi Sakamoto , Shin-ichi Tsukamoto , Masao Sasamata , Masamichi Okada , Mitsuo Fujii
IPC分类号: C07D403/04 , A61K31/498 , A61K31/4985 , A61P25/14 , A61P25/28 , C07D241/44 , C07D471/04 , C07D521/00 , C07D403/10
CPC分类号: C07D231/12 , C07D233/56 , C07D241/44 , C07D249/08
摘要: A 1,2,3,4-tetrahydroquinoxalinedione derivative represented by the following formula (I) or salt thereof, an NMDA-glycine receptor and/or AMPA receptor antagonist or kainic acid neurotoxicity inhibitor containing the derivative or salt. In addition, a pharmaceutical composition comprising said compound and a pharmaceutically acceptable carrier: ##STR1## wherein the substituents are as described in the specification.
摘要翻译: PCT No.PCT / JP95 / 01922 Sec。 371日期1997年3月5日 102(e)1997年3月5日PCT PCT 1995年9月25日PCT公布。 公开号WO96 / 10023 日本1996年4月4日由下式(I)表示的1,2,3,4-四氢喹喔啉二酮衍生物或其盐,含有该衍生物或盐的NMDA-甘氨酸受体和/或AMPA受体拮抗剂或红藻氨酸神经毒性抑制剂。 此外,包含所述化合物和药学上可接受的载体的药物组合物:其中取代基如说明书中所述。
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公开(公告)号:US5283244A
公开(公告)日:1994-02-01
申请号:US50225
申请日:1993-05-03
申请人: Shuichi Sakamoto , Junya Ohmori , Hirokazu Kubota , Masao Sasamata , Masamichi Okada , Kazuyuki Hidaka
发明人: Shuichi Sakamoto , Junya Ohmori , Hirokazu Kubota , Masao Sasamata , Masamichi Okada , Kazuyuki Hidaka
IPC分类号: C07D241/44 , A61K31/495 , C07D241/52 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04 , C07D521/00 , A61K31/535 , C07D403/02
CPC分类号: C07D231/12 , C07D233/56 , C07D249/08 , C07D403/04
摘要: The present invention is a pyrazine derivative which has glutamate receptor antagonizing activity, represented by formula: ##STR1## wherein Z represents C or N, provided that two Zs are not N atoms at the same time; R.sup.1 represents: ##STR2## wherein ##STR3## represents ##STR4## R.sup.6 represents H or alkyl, and R.sup.7 and R.sup.8 represent each H, alkyl, nitro or phenyl, or alternatively R.sup.7 and R.sup.8 are combined together to represent butadienylene or 1,4-butylene; R.sup.2 and R.sup.3 represent each H, F, cyano, acyl, nitro, alkyl, morpholino or one of said species of R.sup.1 ; R.sup.4 and R.sup.5 represent each H, hydroxyl, alkyl, cycloalkyl, heterocycle, phenyl, or Y-substituted alkyl; Y represents hydroxyl, acyloxy, F-substituted methyl, cycloalkyl, tetrahydrofuryl, carboxyl, alkoxycarbonyl or ##STR5## R.sup.9 and R.sup.10 represent each H or alkyl, or alternatively R.sup.9 and R.sup.10 are combined together to represent a 5- or 6-membered cyclic group which may contain oxygen atom(s).
摘要翻译: PCT No.PCT / JP91 / 01498 Sec。 371日期:1993年5月5日 102(e)日期1993年5月5日PCT 1991年11月1日PCT PCT。 出版物WO92 / 07847 本发明是具有谷氨酸受体拮抗活性的吡嗪衍生物,其由下式表示:(*化学结构*)其中Z表示C或N,条件是两个Z不同时为N原子; R1表示:(*化学结构*)其中(*化学结构*)表示(*化学结构*)R6表示H或烷基,R7和R8表示H,烷基,硝基或苯基,或者R7和R8组合 一起代表丁二烯或1,4-丁烯; R 2和R 3表示每个H,F,氰基,酰基,硝基,烷基,吗啉代或所述R1的一种; R4和R5代表H,羟基,烷基,环烷基,杂环,苯基或Y-取代的烷基; Y表示羟基,酰氧基,F取代的甲基,环烷基,四氢呋喃基,羧基,烷氧基羰基或(*化学结构*)R9和R10表示每个H或烷基,或者R9和R10组合在一起代表5-或6- 可以含有氧原子的多元环状基团。
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7.
公开(公告)号:US6133258A
公开(公告)日:2000-10-17
申请号:US68534
申请日:1998-05-13
申请人: Jun-ichi Shishikura , Hiroshi Inami , Tomoyuki Yasunaga , Masaaki Hirano , Shuichi Sakamoto , Kazushige Ohno , Masamichi Okada , Shin-ichi Tsukamoto
发明人: Jun-ichi Shishikura , Hiroshi Inami , Tomoyuki Yasunaga , Masaaki Hirano , Shuichi Sakamoto , Kazushige Ohno , Masamichi Okada , Shin-ichi Tsukamoto
IPC分类号: A61K31/5415 , A61K31/542 , C07D513/04
CPC分类号: A61K31/5415
摘要: Neuroprotective agents based on inhibition of kainic acid neurotoxicity and compounds useful as neuroprotective agents based on inhibition of kainic acid neurotoxicity. An inhibitors of kainic acid neurotoxicity, comprising as an active ingredient a pyridothiazine derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof, and a pyridothiazine derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein symbols in the formula have the following respective meanings: the ring A: a pyridine ring; ##STR2## R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 may be the same or different and each represent a hydrogen atom or a lower alkyl, cycloalkyl, alkenyl, aryl, carboxyl or lower alkoxycarbonyl group which may have substituent(s), or are not present, with the proviso that R.sup.2 and R.sup.3 may together form a nitrogen-containing heterocyclic group which may have nitrogen atoms as another hetero atom, may be fused with a benzene ring and may have a lower alkyl group as a substituent.
摘要翻译: PCT No.PCT / JP96 / 03339 Sec。 371日期1998年5月13日 102(e)日期1998年5月13日PCT 1996年11月14日PCT PCT。 出版物WO97 / 17970 日期1997年5月22日基于抑制红藻氨酸神经毒性的神经保护剂和基于抑制红藻氨酸神经毒性作用的神经保护剂的化合物。 作为活性成分的红藻氨酸神经毒性抑制剂,含有下述通式(I)所示的吡哆噻嗪衍生物或其药学上可接受的盐,以及下述通式(I)表示的吡哒嗪衍生物或其药学上可接受的盐 其中式中的符号具有以下各自的含义:环A:吡啶环; R 1,R 2,R 3,R 4和R 5可以相同或不同,各自表示氢原子或可以具有取代基或不存在的低级烷基,环烷基,烯基,芳基,羧基或低级烷氧基羰基, 条件是R2和R3可以一起形成可以具有氮原子作为另一个杂原子的含氮杂环基,可以与苯环稠合并且可以具有低级烷基作为取代基。
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公开(公告)号:US6121264A
公开(公告)日:2000-09-19
申请号:US194750
申请日:1998-12-02
IPC分类号: C07D403/04 , A61K31/495 , C07D521/00 , A61K31/498 , C07D403/10 , C07D403/14
CPC分类号: C07D231/12 , C07D233/56 , C07D249/08
摘要: Imidazole-substituted quinoxalinedione derivatives represented by the following general formula (I) or pharmaceutically acceptable salts thereof and pharmaceutical compositions useful as glutamate receptor antagonists and the like, which comprise said compounds or salts thereof and pharmaceutically acceptable carriers. ##STR1## (Each symbol in the formula has the following meaning: A: a group represented by a formula (CH.sub.2).sub.m or a group represented by a formula Ph--(CH.sub.2).sub.p (Ph: a phenyl group),X: an oxygen atom or a group represented by a formula NR.sup.4,R.sup.1 : a hydrogen atom, a hydroxyl group or a triazolyl group, with the proviso that X may be a bond when R.sup.1 is a triazolyl group,R.sup.2 : a hydrogen atom, a nitro group, a halogeno-lower alkyl group, a cyano group, an amino group, a mono- or di-lower alkylamino group or a halogen atom,R.sup.3 and R.sup.4 : may be the same or different from each other and each represents a hydrogen atom or a lower alkyl group,n: 0, 1 or 2,m: an integer of 2 to 6, andp: an integer of 1 to 6.
摘要翻译: PCT No.PCT / JP97 / 01905 Sec。 371日期1998年12月2日第 102(e)日期1998年12月2日PCT提交1997年6月5日PCT公布。 公开号WO97 / 46555 日期:1997年12月11日由以下通式(I)表示的咪唑取代的喹喔啉二酮衍生物或其药学上可接受的盐以及用作谷氨酸受体拮抗剂等的药物组合物,其包含所述化合物或其盐和药学上可接受的载体。 (式中的每个符号具有以下含义:A:由式(CH 2)m表示的基团或由式Ph-(CH 2)p(Ph:苯基)表示的基团,X:氧原子或 由式NR4表示的基团,R1:氢原子,羟基或三唑基,条件是当R 1为三唑基时,X可以为键,R 2为氢原子,硝基,卤代 低级烷基,氰基,氨基,一或二低级烷基氨基或卤素原子,R 3和R 4可以相同或不同,表示氢原子或低级烷基 基团,n:0,1或2,m为2〜6的整数,p为1〜6的整数。
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公开(公告)号:US20120069294A1
公开(公告)日:2012-03-22
申请号:US13231057
申请日:2011-09-13
申请人: Hiroshi Ohno , Tatsuya Sakata , Masamichi Okada , Nobuyuki Hara , Naoto Shimizu
发明人: Hiroshi Ohno , Tatsuya Sakata , Masamichi Okada , Nobuyuki Hara , Naoto Shimizu
IPC分类号: G02C5/22
CPC分类号: G02B27/0176 , G02B2027/0178 , G02C5/2263 , G02C2200/18
摘要: A glasses-type shutter holder may include left and right temple parts connected respectively to left and right frame end parts of frame. The left and right temple parts may be foldable respectively with respect to the left and right frame end parts in accordance with movement, for each frame end part and temple part pair, of a contact position at which a movement part provided with one of the temple part and the frame end part of the pair is in contact with a contact part of the other of the temple part and the frame end part of the pair. For each of the pairs, the contact part is in contact with the movement part when the temple part is unfolded to a maximum degree, and a maximum degree of opening of the temple part is varied in accordance with the movement of the movable part.
摘要翻译: 眼镜型快门保持器可以包括分别连接到框架的左框架和右框架端部的左右镜腿部分。 根据对于每个框架端部和镜腿部对的移动,左右镜腿部分可以分别相对于左框架和右框架端部折叠,该接触位置处设置有一个镜腿的移动部件 所述一对的所述框架端部与所述一对的所述镜腿部的另一方的接触部与所述一对的所述框的端部接触。 对于每一对,当镜腿部分展开最大程度时,接触部分与运动部分接触,并且根据可移动部件的移动来改变镜腿部分的最大开度。
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10.
公开(公告)号:US06566796B2
公开(公告)日:2003-05-20
申请号:US09929850
申请日:2001-08-14
申请人: Satoshi Kodama , Reiko Sugihara , Hideki Matsuoka , Yasushi Tanaka , Tatsuhiko Hiratani , Kenji Tahara , Kenichi Mitsuzuka , Kenichiro Takayanagi , Masamichi Okada , Hiroaki Kato , Chohachi Sato
发明人: Satoshi Kodama , Reiko Sugihara , Hideki Matsuoka , Yasushi Tanaka , Tatsuhiko Hiratani , Kenji Tahara , Kenichi Mitsuzuka , Kenichiro Takayanagi , Masamichi Okada , Hiroaki Kato , Chohachi Sato
IPC分类号: H01J2907
CPC分类号: C22C38/04 , C21D8/0236 , C21D8/1233 , C22C38/001 , C22C38/004 , C22C38/02 , C22C38/12 , H01J9/142 , H01J2229/0733
摘要: A method of making a steel sheet for a tension mask, including the steps of: hot rolling a steel consisting essentially of, by weight %, C: less than 0.1%, Si: 0.05% or less, Mn: 0.4 to 2%, P: 0.03% or less, S: 0.03% or less, sol.Al: 0.01% or less, N: 0.010% or more, and the balance of Fe; and annealing the cold rolled steel sheet, followed by a secondary cold rolling at a reduction rate of 35% or higher. The steel sheet produced by this method shows excellent creep resistance during blackening treatment and excellent magnetic shielding property with an anhysteretic permeability of 3400 or more at a DC bias magnetic field of 0.35 Oe, and therefore causes no color-deviation when applied to the tension mask.
摘要翻译: 一种制造张力掩模用钢板的方法,包括以下步骤:将基本上由C:小于0.1%,Si:0.05%以下,Mn:0.4〜2%的重量%组成的钢进行热轧, P:0.03%以下,S:0.03%以下,sol.Al:0.01%以下,N:0.010%以上,余量为Fe; 对冷轧钢板进行退火,然后以35%以上的还原率进行二次冷轧。 通过该方法制造的钢板在0.35Oe的直流偏压磁场下显示优异的抗蠕变性,并且在0.35Oe的直流偏置磁场下具有优异的磁阻屏蔽性,具有3400以上的非磁滞渗透性,因此当施加到张力掩模时不会产生颜色偏差 。
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