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1. 发明授权

US06664283B1 Pharmaceuticals for neurogenic pain 失效
标题翻译：药物用于神经源性疼痛
公开(公告)号：US06664283B1
公开(公告)日：2003-12-16
申请号：US10031404
申请日：2002-05-15
申请人： Masamichi Okada , Yukinori Nagakura , Tetsuo Kiso , Takashi Toya , Satoshi Hayashibe
发明人： Masamichi Okada , Yukinori Nagakura , Tetsuo Kiso , Takashi Toya , Satoshi Hayashibe
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。

2. 发明授权

US07250429B2 Aminomethyl-substituted thiazolobenzimidazole compounds 失效
标题翻译：氨基甲基取代的噻唑并噻唑化合物
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 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）

3. 发明申请

US20050148642A1 Aminomethyl-substituted thiazolobenzimidazole derivative 失效
标题翻译：氨基甲基取代的噻唑并噻唑衍生物
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 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）

4. 发明授权

US06642264B1 Thiazolobenzoimidazole derivatives 失效
标题翻译：噻唑并苯并咪唑衍生物
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。）

5. 发明授权

US08211907B2 Fused indane compound 有权
标题翻译：稠油茚满化合物
公开(公告)号：US08211907B2
公开(公告)日：2012-07-03
申请号：US12741307
申请日：2008-11-26
申请人： Satoshi Hayashibe , Shingo Yamasaki , Nobuyuki Shiraishi , Hiroaki Hoshii , Takahiko Tobe
发明人： Satoshi Hayashibe , Shingo Yamasaki , Nobuyuki Shiraishi , Hiroaki Hoshii , Takahiko Tobe
IPC分类号： A61K31/44 , C07D221/06
CPC分类号： C07D209/94 , C07D221/16 , C07D223/32 , C07D265/34 , C07D333/78 , C07D401/06 , C07D401/12 , C07D491/048 , C07D495/04 , C07D498/04 , C07D513/04 , C07D513/06
摘要： To provide a compound which is useful as an NMDA receptor antagonist. The present inventors have studied a compound having an NMDA receptor antagonistic action, and confirmed that the fused indane compound of the present invention has an excellent NMDA receptor antagonistic action, thereby completed the present invention. The fused indane compound of the present invention has an excellent NMDA receptor antagonistic action and can be used as a prophylactic and/or therapeutic agent for Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, intractable depression, attention deficit hyperactivity disorder, migraines, or the like.
摘要翻译：提供可用作NMDA受体拮抗剂的化合物。本发明人研究了具有NMDA受体拮抗作用的化合物，并证实本发明的稠合茚满酮化合物具有优异的NMDA受体拮抗作用，从而完成了本发明。本发明的稠合吲哚化合物具有优异的NMDA受体拮抗作用，可用作阿尔茨海默氏病，脑血管性痴呆，帕金森病，难治性抑郁症，注意力缺陷多动障碍，偏头痛等的预防和/或治疗剂。

6. 发明授权

US08013018B2 Aminoindane derivative or salt thereof 有权
标题翻译：氨基茚满衍生物或其盐
公开(公告)号：US08013018B2
公开(公告)日：2011-09-06
申请号：US12305254
申请日：2007-07-17
申请人： Satoshi Hayashibe , Shingo Yamasaki , Kazushi Watanabe , Nobuyuki Shiraishi , Daisuke Suzuki , Hiroaki Hoshii , Junya Ohmori , Takatoshi Kanayama
发明人： Satoshi Hayashibe , Shingo Yamasaki , Kazushi Watanabe , Nobuyuki Shiraishi , Daisuke Suzuki , Hiroaki Hoshii , Junya Ohmori , Takatoshi Kanayama
IPC分类号： A01N37/12 , A01N37/44 , A01N33/18 , A01N33/24 , A61K31/24 , A61K31/04
CPC分类号： C07C211/42 , C07C215/42 , C07C215/44 , C07C217/52 , C07C235/40 , C07C255/58 , C07C2602/08 , C07D209/40 , C07D221/16 , C07D295/12 , C07D307/82 , C07D333/78
摘要： Provided is a compound that is an NMDA receptor antagonist having a broader safety margin, and is useful as an agent for treating or preventing Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, ischemic apoplexy, or pain.A novel compound or a salt thereof, which is characterized in that it has an amino group and R1 (lower alkyl, cycloalkyl, -lower alkylene-aryl, aryl which may be substituted, and the like) on carbon atoms of indane, cyclopenta[b]thiophene, cyclopenta[b]furan, cyclopenta[b]pyridine, or cyclopenta[c]pyridine ring, or 2,3 -dihydro-1-benzofuran, 2,3-dihydro-1-benzothiophene, indoline ring, or the like, and has R2 and R3 (the same or different, each lower alkyl or aryl) on carbon atoms beside them, and an NMDA receptor antagonist comprising the same as an active component.
摘要翻译：提供了具有更宽安全裕度的NMDA受体拮抗剂的化合物，可用作治疗或预防阿尔茨海默病，脑血管性痴呆，帕金森病，缺血性中风或疼痛的药剂。一种新型化合物或其盐，其特征在于其具有在茚满的环戊二烯基的碳原子上具有氨基和可以被取代的R 1（低级烷基，环烷基， - 低级亚烷基 - 芳基，芳基等） b]噻吩，环戊二烯并[b]呋喃，环戊二烯并[b]吡啶或环戊并[c]吡啶环，或2,3-二氢-1-苯并呋喃，2,3-二氢-1-苯并噻吩，二氢吲哚环，或并且在它们旁边的碳原子上具有R2和R3（相同或不同，各个低级烷基或芳基），以及包含与活性组分相同的NMDA受体拮抗剂。

7. 发明申请

US20090186916A1 AMINOINDANE DERIVATIVE OR SALT THEREOF 有权
标题翻译：氨基衍生物或其盐
公开(公告)号：US20090186916A1
公开(公告)日：2009-07-23
申请号：US12305254
申请日：2007-07-17
申请人： Satoshi Hayashibe , Shingo Yamasaki , Kazushi Watanabe , Nobuyuki Shiraishi , Daisuke Suzuki , Hiroaki Hoshii , Junya Ohmori , Takatoshi Kanayama
发明人： Satoshi Hayashibe , Shingo Yamasaki , Kazushi Watanabe , Nobuyuki Shiraishi , Daisuke Suzuki , Hiroaki Hoshii , Junya Ohmori , Takatoshi Kanayama
IPC分类号： A61K31/135 , C07C211/38 , C07D333/78 , C07D307/93 , C07D221/04 , A61K31/381 , A61K31/343 , A61K31/44 , A61P25/00
CPC分类号： C07C211/42 , C07C215/42 , C07C215/44 , C07C217/52 , C07C235/40 , C07C255/58 , C07C2602/08 , C07D209/40 , C07D221/16 , C07D295/12 , C07D307/82 , C07D333/78
摘要： Provided is a compound that is an NMDA receptor antagonist having a broader safety margin, and is useful as an agent for treating or preventing Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, ischemic apoplexy, or pain.A novel compound or a salt thereof, which is characterized in that it has an amino group and R1 (lower alkyl, cycloalkyl, -lower alkylene-aryl, aryl which may be substituted, and the like) on carbon atoms of indane, cyclopenta[b]thiophene, cyclopenta[b]furan, cyclopenta[b]pyridine, or cyclopenta[c]pyridine ring, or 2,3-dihydrdo-1-benzofuran, 2,3-dihydrdo-1-benzothiophene, indoline ring, or the like, and has R2 and R3 (the same or different, each lower alkyl or aryl) on carbon atoms beside them, and an NMDA receptor antagonist comprising the same as an active component.
摘要翻译：提供了具有更宽安全裕度的NMDA受体拮抗剂的化合物，可用作治疗或预防阿尔茨海默病，脑血管性痴呆，帕金森病，缺血性中风或疼痛的药剂。一种新型化合物或其盐，其特征在于其具有在茚满的环戊二烯基的碳原子上具有氨基和可以被取代的R 1（低级烷基，环烷基， - 低级亚烷基 - 芳基，芳基等） b]噻吩，环戊二烯并[b]呋喃，环戊二烯并[b]吡啶或环戊二烯并[c]吡啶环，或2,3-二氢-1-苯并呋喃，2,3-二氢-1-苯并噻吩，二氢吲哚环或并且在它们旁边的碳原子上具有R2和R3（相同或不同，各个低级烷基或芳基），以及包含与活性组分相同的NMDA受体拮抗剂。

8. 发明授权

US5521180A Morpholine derivative 失效
标题翻译：吗啉衍生物
公开(公告)号：US5521180A
公开(公告)日：1996-05-28
申请号：US495619
申请日：1995-08-03
申请人： Mitsuo Fujii , Takayuki Suzuki , Satoshi Hayashibe , Shin-ichi Tsukamoto , Shin-ichi Yatsugi , Tokio Yamaguchi
发明人： Mitsuo Fujii , Takayuki Suzuki , Satoshi Hayashibe , Shin-ichi Tsukamoto , Shin-ichi Yatsugi , Tokio Yamaguchi
IPC分类号： C07D265/30 , A61K31/535
CPC分类号： C07D265/30
摘要： A morpholine derivative represented by formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sup.1 and R.sup.3, which may be the same or different, each represent a hydrogen atom or a lower alkyl group; R.sup.2 represents a halogen atom; and the dotted line indicates an optional double bond. These compounds exhibit a selective 5-HT reuptake inhibitory activity and a selective 5-HT.sub.2 receptor antagonistic activity and useful as a therapeutic agent for depression, anxiety, etc. with reduced side effects.
摘要翻译： PCT No.PCT / JP94 / 00186 Sec。 371日期：1995年8月3日 102（e）日期1995年8月3日PCT 1994年2月8日PCT PCT。公开号WO94 / 18182 日本美国专利申请公开说明书（公告）日本公开一般公开说明书（公开号）（Ⅰ）所示的吗啉衍生物或其药学上可接受的盐：其中R 1和R 3可以相同或不同，各自表示氢原子或低级烷基; R2表示卤原子; 虚线表示可选的双键。这些化合物表现出选择性的5-HT再摄取抑制活性和选择性的5-HT2受体拮抗活性，并且可用作抑制，焦虑等的治疗剂，副作用降低。

9. 发明申请

US20100267695A1 FUSED INDANE COMPOUND 有权
标题翻译：熔融印花化合物
公开(公告)号：US20100267695A1
公开(公告)日：2010-10-21
申请号：US12741307
申请日：2008-11-26
申请人： Satoshi Hayashibe , Shingo Yamasaki , Nobuyuki Shiraishi , Hiroaki Hoshii , Takahiko Tobe
发明人： Satoshi Hayashibe , Shingo Yamasaki , Nobuyuki Shiraishi , Hiroaki Hoshii , Takahiko Tobe
IPC分类号： A61K31/55 , A61K31/538 , A61K31/435 , A61K31/4365 , C07D223/32 , C07D265/34 , C07D495/04 , C07D491/048 , C07D221/16 , A61P25/22 , A61P25/16 , A61P25/28 , A61P25/24 , A61P25/06 , A61P25/30 , A61P25/18
CPC分类号： C07D209/94 , C07D221/16 , C07D223/32 , C07D265/34 , C07D333/78 , C07D401/06 , C07D401/12 , C07D491/048 , C07D495/04 , C07D498/04 , C07D513/04 , C07D513/06
摘要： [Problems] To provide a compound which is useful as an NMDA receptor antagonist.[Means for Solution] The present inventors have studied a compound having an NMDA receptor antagonistic action, and confirmed that the fused indane compound of the present invention has an excellent NMDA receptor antagonistic action, thereby completed the present invention. The fused indane compound of the present invention has an excellent NMDA receptor antagonistic action and can be used as a prophylactic and/or therapeutic agent for Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, intractable depression, attention deficit hyperactivity disorder, migraines, or the like.
摘要翻译： [问题]提供可用作NMDA受体拮抗剂的化合物。 [解决方案]本发明人研究了具有NMDA受体拮抗作用的化合物，并证实本发明的稠合茚满酮化合物具有优异的NMDA受体拮抗作用，从而完成了本发明。本发明的稠合吲哚化合物具有优异的NMDA受体拮抗作用，可用作阿尔茨海默氏病，脑血管性痴呆，帕金森病，难治性抑郁症，注意力缺陷多动障碍，偏头痛等的预防和/或治疗剂。

10. 发明申请

US20070197594A1 Cyclic amine derivative or salt thereof 审中-公开
标题翻译：环胺衍生物或其盐
公开(公告)号：US20070197594A1
公开(公告)日：2007-08-23
申请号：US11663628
申请日：2005-09-20
申请人： Satoshi Hayashibe , Takatoshi Kanayama , Junya Ohmori , Takahiko Tobe , Kyoichi Maeno , Yoshitsugu Shitaka , Jotarou Suzuki , Shigeki Kawabata , Nobuyuki Shiraishi , Shingo Yamasaki , Daisuke Suzuki , Hiroaki Hoshii
发明人： Satoshi Hayashibe , Takatoshi Kanayama , Junya Ohmori , Takahiko Tobe , Kyoichi Maeno , Yoshitsugu Shitaka , Jotarou Suzuki , Shigeki Kawabata , Nobuyuki Shiraishi , Shingo Yamasaki , Daisuke Suzuki , Hiroaki Hoshii
IPC分类号： A61K31/452 , C07D211/06 , C07D211/22 , C07D407/02 , A61K31/445
CPC分类号： C07C217/74 , C07C215/42 , C07C2601/08 , C07D211/22 , C07D295/088 , C07D307/94 , C07D319/14 , C07D401/06 , C07D405/04 , C07D409/04 , C07D409/10 , C07D413/04 , C07D453/02
摘要： Provided are compounds which are an NMDA antagonist having a broad safety margin and are useful as a treating agent or a preventing agent for Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, ischemic apoplexy, pain, etc. Concretely provided are an amine derivative or its salt characterized in that the amine-containing structure A therein bonds to a 2- or 3-cyclic condensed ring (e.g., indane, tetralone, 4,5,6,7-tetrahydrobenzothiophene, 4,5,6,7-tetrahydrobenzofuran, 7,8-dihydro-6H-indeno[4,5-b]furan, 2,3-dihydro-1H-cyclopenta[1]naphthalene) via X1 (bond or lower alkylene); and an NMDA antagonist containing it as an active ingredient thereof.
摘要翻译：提供作为具有广泛安全余地的NMDA拮抗剂的化合物，可用作阿尔茨海默病，脑血管性痴呆，帕金森病，缺血性中风，疼痛等的治疗剂或预防剂。具体地提供胺衍生物或其盐其特征在于其中含胺结构A与2-或3-环稠合环结合（例如，茚满，四氢萘酮，4,5,6,7-四氢苯并噻吩，4,5,6,7-四氢苯并呋喃， 8-二氢-6H-茚并[4,5-b]呋喃，2,3-二氢-1H-环戊二烯并[1]萘）通过X 1（键或低级亚烷基）; 和含有它作为其活性成分的NMDA拮抗剂。

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