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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
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。
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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。
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公开(公告)号：US20100267695A1
公开(公告)日：2010-10-21
申请号：US12741307
申请日：2008-11-26
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 。
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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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公开(公告)号：US06884868B1
公开(公告)日：2005-04-26
申请号：US09926385
申请日：2000-04-25
申请人： Takashi Tojo , Hidenori Ohki , Nobuyuki Shiraishi , Takahiro Matsuya , Hiroshi Matsuda , Kenji Murano , David Barrett , Takashi Ogino , Keiji Matsuda , Masaharu Ichihara , Norio Hashimoto , Atsushi Kanda , Atsushi Ohigashi
发明人： Takashi Tojo , Hidenori Ohki , Nobuyuki Shiraishi , Takahiro Matsuya , Hiroshi Matsuda , Kenji Murano , David Barrett , Takashi Ogino , Keiji Matsuda , Masaharu Ichihara , Norio Hashimoto , Atsushi Kanda , Atsushi Ohigashi
摘要： This invention relates to new polypeptide compound represented by general formula (I), wherein R1, R2, R3, R4, R5 and R6 are as defined in the description or a salt thereof which has antimicrobial activities (especially, antifungal activities), inhibitory activity on β-1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for prophylactic and/or therapeutic treatment of infectious diseases including Pneumocystis carinii infection (e.g. Pneumocystis carinii pneumonia) in a human being or an animal.
摘要翻译： 本发明涉及由通式（I）表示的新的多肽化合物，其中R 1，R 2，R 3，R 3， 4，R 5和R 6如描述中所定义，或其盐具有抗微生物活性（特别是抗真菌活性），对β的抑制活性 -1,3-葡聚糖合酶，其制备方法，涉及包含其的药物组合物，以及用于预防和/或治疗感染性疾病的方法，所述传染病包括人类卡氏肺囊虫感染（例如肺孢子虫卡氏肺炎） 或动物。
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公开(公告)号：US06232290B1
公开(公告)日：2001-05-15
申请号：US09446101
申请日：1999-12-22
申请人： Hidenori Ohki , Kenji Murano , Takashi Tojo , Nobuyuki Shiraishi , Takahiro Matsuya , Hiroshi Matsuda , Hiroaki Mizuno , David Barrett , Keiji Matsuda , Kohji Kawabata
发明人： Hidenori Ohki , Kenji Murano , Takashi Tojo , Nobuyuki Shiraishi , Takahiro Matsuya , Hiroshi Matsuda , Hiroaki Mizuno , David Barrett , Keiji Matsuda , Kohji Kawabata
IPC分类号： A61K3812
摘要： This invention relates to new polypeptide compounds represented by general formula (I), wherein R1, R2, R3 and R4 are as defined in the description or a salt thereof which has antimicrobial activities (especially, antifungal activities), inhibitory activity on &bgr;-1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for prophylactic and/or therapeutic treatment of infectious diseases including Pneumocystis carinii infection (e.g. Pneumocystis carinii pneumonia) in a human being or an animal.
摘要翻译： 本发明涉及由通式（I）表示的新的多肽化合物，其中R1，R2，R3和R4如说明书中所定义或其具有抗微生物活性（特别是抗真菌活性）的盐，对β-1的抑制活性 3-葡聚糖合酶，其制备方法，涉及含有该组合物的药物组合物，以及用于预防和/或治疗感染性疾病的方法，包括卡介菌肺炎卡介菌感染（例如肺孢子虫卡氏肺炎）在人或 动物。
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公开(公告)号：US20110207729A1
公开(公告)日：2011-08-25
申请号：US12672277
申请日：2008-08-07
申请人： Isao Kinoyama , Satoshi Miyamoto , Takehiro Miyazaki , Yohei Koganemaru , Yuichiro Kawamoto , Nobuyuki Shiraishi , Hiroaki Hoshii , Akio Kuroda , Mayako Yamazaki , Minoru Yasuda , Hiroaki Mizuno
发明人： Isao Kinoyama , Satoshi Miyamoto , Takehiro Miyazaki , Yohei Koganemaru , Yuichiro Kawamoto , Nobuyuki Shiraishi , Hiroaki Hoshii , Akio Kuroda , Mayako Yamazaki , Minoru Yasuda , Hiroaki Mizuno
IPC分类号： A61K31/5377 , C07D311/04 , C07D405/12 , C07D413/12 , C07D311/96 , C07D405/04 , C07D407/10 , A61K31/352 , A61K31/4155 , A61K31/496 , A61K31/4433 , A61K31/357 , A61P25/00 , A61P25/18 , A61P25/28
CPC分类号： C07D295/12 , C07C279/22 , C07C317/44 , C07C2601/02 , C07C2602/10 , C07C2602/12 , C07D213/56 , C07D213/61 , C07D213/64 , C07D215/12 , C07D231/12 , C07D239/26 , C07D241/12 , C07D261/08 , C07D277/30 , C07D295/155 , C07D307/52 , C07D307/54 , C07D309/04 , C07D311/04 , C07D311/58 , C07D313/08 , C07D319/18 , C07D333/24 , C07D333/54 , C07D333/56 , C07D335/06 , C07D405/04 , C07D407/04 , C07D409/04 , C07D471/04
摘要： An object of the present invention is to provide a novel and excellent agent for treating or preventing dementia, schizophrenia, and the like, based on the serotonin 5-HT5A receptor modulating action.It was confirmed that a bicyclic acylguanidine derivative which has a characteristic structure that guanidine is bonded to one ring of a bicyclic structure such as chromene and dihydronaphthalene through a carbonyl group and a cyclic group is bonded on the other ring, has a potent 5-HT5A receptor modulating action and an excellent pharmacological action based on this mechanism. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder.
摘要翻译： 本发明的目的是提供一种用于治疗或预防基于5-羟色胺5-HT5A受体调节作用的痴呆，精神分裂症等的新颖且优异的药剂。 证实具有特征性结构的双环酰基胍衍生物具有有效的5-HT5A（其具有通过羰基和环状基团键合在一个双环结构的环上，如色烯和二氢萘结合在另一个环上） 受体调节作用和基于该机制的优异的药理作用。 本发明可用作治疗或预防痴呆，精神分裂症，双相情感障碍或注意缺陷多动障碍的优良药剂。
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公开(公告)号：US20110306621A1
公开(公告)日：2011-12-15
申请号：US13148379
申请日：2010-02-08
申请人： Isao Kinoyama , Takehiro Miyazaki , Yohei Koganemaru , Nobuyuki Shiraishi , Yuichiro Kawamoto , Takuya Washio
发明人： Isao Kinoyama , Takehiro Miyazaki , Yohei Koganemaru , Nobuyuki Shiraishi , Yuichiro Kawamoto , Takuya Washio
IPC分类号： A61K31/505 , C07D213/64 , C07D277/30 , C07D213/56 , C07D309/22 , C07D319/18 , C07D333/24 , C07D215/14 , C07D217/04 , C07D217/16 , C07D239/26 , A61K31/166 , A61K31/277 , A61K31/44 , A61K31/426 , A61K31/351 , A61K31/357 , A61K31/381 , A61K31/47 , A61K31/472 , A61P25/28 , A61P25/00 , A61P25/18 , C07C279/22
CPC分类号： C07C279/22 , C07D209/18 , C07D213/56 , C07D213/58 , C07D213/60 , C07D213/61 , C07D213/64 , C07D213/68 , C07D213/84 , C07D215/14 , C07D217/02 , C07D231/12 , C07D231/16 , C07D239/26 , C07D239/28 , C07D263/56 , C07D271/04 , C07D271/06 , C07D271/10 , C07D271/12 , C07D277/20 , C07D277/30 , C07D277/64 , C07D307/16 , C07D307/80 , C07D309/22 , C07D317/42 , C07D317/60 , C07D317/62 , C07D319/18 , C07D333/08 , C07D333/24 , C07D333/28 , C07D333/38
摘要： An object of the present invention is to provide an excellent agent for treating or preventing dementia, schizophrenia based on a serotonin 5-HT5A receptor modulating action.It was confirmed that acylguanidine derivatives, which has the characteristic structure in which the guanidine is bonded to one ring of a naphthalene via a carbonyl group and a cyclic group is bonded to the other ring thereof, exhibit potent 5-HT5A receptor modulating action and excellent pharmacological action based on the action. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder or attention deficit hyperactivity disorder.
摘要翻译： 本发明的目的是提供一种用于治疗或预防基于5-羟色胺5-HT5A受体调节作用的痴呆，精神分裂症的优异剂。 确认了具有通过羰基和环状基团将胍键合到萘的特征结构的酰基胍衍生物与另一个环结合，表现出有效的5-HT5A受体调节作用，优异的 基于行动的药理作用。 本发明可用作治疗或预防痴呆，精神分裂症，双相情感障碍或注意缺陷多动障碍的优良剂。
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公开(公告)号：US20110105460A1
公开(公告)日：2011-05-05
申请号：US13002373
申请日：2009-07-02
申请人： Seiji Yoshimura , Noriyuki Kawano , Tomoaki Kawano , Daisuke Sasuga , Takanori Koike , Hideyuki Watanabe , Hiroki Fukudome , Nobuyuki Shiraishi , Ryosuke Munakata , Hiroaki Hoshii , Kayoko Mihara
发明人： Seiji Yoshimura , Noriyuki Kawano , Tomoaki Kawano , Daisuke Sasuga , Takanori Koike , Hideyuki Watanabe , Hiroki Fukudome , Nobuyuki Shiraishi , Ryosuke Munakata , Hiroaki Hoshii , Kayoko Mihara
IPC分类号： A61K31/4196 , C07D401/12 , A61K31/4439 , C07D249/08 , C07D403/12 , A61K31/506 , C07D413/12 , A61K31/422 , A61K31/4245 , A61K31/5377 , C07D417/12 , A61K31/541 , C07D405/12 , A61K31/427 , C07D413/14 , C07D409/04 , C07D403/10 , C07D471/04 , A61K31/437 , A61P3/10 , A61P25/24 , A61P25/18 , A61P25/28
CPC分类号： C07D249/08 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/10 , C07D417/12
摘要： [Problem] A compound, which can be used for preventing or treating diseases, in which 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided.[Means for Solution] It was found that a triazole derivative, in which one of the 3- and 5-positions of the triazole ring has (di)alkylmethyl or cycloalkyl, each of which is substituted with —O— (aryl or a heterocyclic group, each of which may be substituted, or lower alkylene-cycloalkyl), and the other thereof has aryl, a heterocyclic group or cycloalkyl, each of which may be substituted, or a pharmaceutically acceptable salt thereof exhibits potent 11β-HSD1 inhibitory action. From the above, the triazole derivative of the present invention can be used for preventing or treating diabetes, insulin resistance, dementia, schizophrenia and depression.
摘要翻译： [问题]提供了一种可用于预防或治疗疾病的化合物，其中涉及11种β-羟基类固醇脱氢酶（11＆bgr-HSD1），特别是糖尿病，胰岛素抵抗，痴呆，精神分裂症和抑郁症 。 [解决方案]发现三唑环的3-和5-位之一具有（二）烷基甲基或环烷基的三唑衍生物，其各自被-O-（芳基或杂环） 基团，其各自可以被取代，或低级亚烷基 - 环烷基），另一个具有可以被取代的芳基，杂环基或环烷基，或其药学上可接受的盐显示出有效的11β-HSD1抑制作用 。 由上可知，本发明的三唑衍生物可用于预防或治疗糖尿病，胰岛素抵抗，痴呆，精神分裂症和抑郁症。
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公开(公告)号：US06399567B1
公开(公告)日：2002-06-04
申请号：US09308218
申请日：1999-06-16
申请人： Ryuichi Kanasaki , Shigehiro Takase , Michizane Hashimoto , Hiroshi Hatanaka , Kazutoshi Sakamoto , Seiji Hashimoto , Nobuyuki Shiraishi , Hidenori Ohki , Kohji Kawabata
发明人： Ryuichi Kanasaki , Shigehiro Takase , Michizane Hashimoto , Hiroshi Hatanaka , Kazutoshi Sakamoto , Seiji Hashimoto , Nobuyuki Shiraishi , Hidenori Ohki , Kohji Kawabata
IPC分类号： A61K3812
摘要： This invention relates to new polypeptide compounds represented by the following formula (I): wherein R1 is as defined in the description or a salt thereof which have antimicrobial activities (especially, antifungal activities), inhibitory activity on &bgr;-1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for the prophylactic and/or therapeutic treatment of infectious disease including Pneumocystis carinii infection (e.g., Pneumocystis carinii pneumonia) in a human being or an animal.
摘要翻译： 本发明涉及由下式（I）表示的新多肽化合物：其中R1如说明书中所定义或其具有抗微生物活性（特别是抗真菌活性）的盐，对β-1,3-葡聚糖合酶的抑制活性， 涉及其制备方法，包含其的药物组合物，以及用于预防和/或治疗人或动物中包括卡氏肺囊虫感染（例如卡氏肺囊虫肺炎）的感染性疾病的方法。
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