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1. 发明授权

US5834499A 5-HT.sub.3 receptor agonist, novel thiazole derivative and intermediate thereof 失效
标题翻译： 5-HT 3受体激动剂，新型噻唑衍生物及其中间体
公开(公告)号：US5834499A
公开(公告)日：1998-11-10
申请号：US700428
申请日：1996-08-26
申请人： Kiyoshi Iwaoka , Hideki Anan , Naoki Imanishi , Kenichi Kazuta , Hiroyuki Koshio , Takeshi Suzuki , Hirotsune Itahana , Hiroyuki Ito , Keiji Miyata , Mitsuaki Ohta
发明人： Kiyoshi Iwaoka , Hideki Anan , Naoki Imanishi , Kenichi Kazuta , Hiroyuki Koshio , Takeshi Suzuki , Hirotsune Itahana , Hiroyuki Ito , Keiji Miyata , Mitsuaki Ohta
IPC分类号： C07D277/28 , C07D277/60 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/08 , C07D513/04 , C07D519/00 , A61K31/425
CPC分类号： C07D277/60 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/08 , C07D513/04 , Y02P20/55
摘要： A 5-HT.sub.3 receptor against containing a thiazole derivative as the effective ingredient is provided and is represented by the Formula (I): ##STR1## wherein the A ring is substituted or unsubstituted and represents a benzene or a heterocyclic ring with one or two heteroatoms; one of L.sub.1 or L.sub.2 represents a single bond and the other is non-existent or represents an alkylene or alkenylene group; R represents: ##STR2##
摘要翻译： PCT No.PCT / JP95 / 00385 Sec。 371日期：1996年8月26日 102（e）日期1996年8月26日PCT提交1995年3月9日PCT公布。第WO95 / 24399号公报日期1995年9月14日提供了含有噻唑衍生物作为有效成分的5-HT 3受体，并由式（I）表示：其中A环是取代或未取代的，代表苯或具有一个或两个杂原子的杂环; L1或L2之一表示单键，另一个不存在或表示亚烷基或亚烯基; R表示：

2. 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。）

3. 发明授权

US08076348B2 Acylguanidine derivative or salt thereof 失效
标题翻译：酰基胍衍生物或其盐
公开(公告)号：US08076348B2
公开(公告)日：2011-12-13
申请号：US11997956
申请日：2006-08-07
申请人： Hiroyoshi Yamada , Hirotsune Itahana , Ayako Moritomo , Takaho Matsuzawa , Eisuke Nozawa , Shinobu Akuzawa , Koichiro Harada
发明人： Hiroyoshi Yamada , Hirotsune Itahana , Ayako Moritomo , Takaho Matsuzawa , Eisuke Nozawa , Shinobu Akuzawa , Koichiro Harada
IPC分类号： A61K31/435
CPC分类号： C07D209/88 , C07D221/16 , C07D265/38 , C07D333/78 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/06 , C07D413/04 , C07D413/06 , C07D471/04 , C07D491/10 , C07D495/10
摘要： [Problem] To provide a compound which can be used in the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in the treatment of irritable bowel syndrome (IBS) and/or prevention of migraine.[Means for Resolution] It was found that an acylguanidine derivative having a tricyclic structure or a pharmaceutically acceptable salt thereof has a strong antagonism to 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having antagonism to both of the receptors showed superior pharmacological action in comparison with the case of the single use of an antagonist selective for either one of the receptors. Based on the above, the compound of the present invention is useful in preventing and/or treating diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in treating irritable bowel syndrome (IBS) and/or preventing migraine.
摘要翻译： [问题]提供可用于预防和/或治疗5-HT 2B受体和5-HT7受体的疾病的化合物，特别是用于治疗肠易激综合征（IBS）和/或预防偏头痛 [解决方法]发现具有三环结构的酰基胍衍生物或其药学上可接受的盐具有对5-HT 2B受体和5-HT7受体的强拮抗作用。此外，与单次使用对任一受体选择性拮抗剂的情况相比，本发明对两种受体具有拮抗作用的化合物显示出优异的药理作用。基于上述，本发明的化合物可用于预防和/或治疗涉及5-HT 2B受体和5-HT7受体的疾病，特别是用于治疗肠易激综合征（IBS）和/或预防偏头痛。

4. 发明申请

US20100168096A1 ACYLGUANIDINE DERIVATIVE OR SALT THEREOF 失效
标题翻译：乙酰胺衍生物或其盐
公开(公告)号：US20100168096A1
公开(公告)日：2010-07-01
申请号：US11997956
申请日：2006-08-07
申请人： Hiroyoshi Yamada , Hirotsune Itahana , Ayako Moritomo , Takaho Matsuzawa , Eisuke Nozawa , Shinobu Akuzawa , Koichiro Harada
发明人： Hiroyoshi Yamada , Hirotsune Itahana , Ayako Moritomo , Takaho Matsuzawa , Eisuke Nozawa , Shinobu Akuzawa , Koichiro Harada
IPC分类号： A61K31/5377 , C07C69/76 , C07D209/56 , C07D401/02 , C07D413/02 , C07D221/16 , C07D211/00 , A61K31/24 , A61K31/403 , A61K31/4439 , A61K31/4355 , A61P1/06 , A61P1/12
CPC分类号： C07D209/88 , C07D221/16 , C07D265/38 , C07D333/78 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/06 , C07D413/04 , C07D413/06 , C07D471/04 , C07D491/10 , C07D495/10
摘要： [Problem] To provide a compound which can be used in the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in the treatment of irritable bowel syndrome (IBS) and/or prevention of migraine.[Means for Resolution] It was found that an acylguanidine derivative having a tricyclic structure or a pharmaceutically acceptable salt thereof has a strong antagonism to 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having antagonism to both of the receptors showed superior pharmacological action in comparison with the case of the single use of an antagonist selective for either one of the receptors. Based on the above, the compound of the present invention is useful in preventing and/or treating diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in treating irritable bowel syndrome (IBS) and/or preventing migraine.
摘要翻译： [问题]提供可用于预防和/或治疗5-HT 2B受体和5-HT7受体的疾病的化合物，特别是用于治疗肠易激综合征（IBS）和/或预防偏头痛 [解决方法]发现具有三环结构的酰基胍衍生物或其药学上可接受的盐具有对5-HT 2B受体和5-HT7受体的强拮抗作用。此外，与单次使用对任一受体选择性拮抗剂的情况相比，本发明对两种受体具有拮抗作用的化合物显示出优异的药理作用。基于上述，本发明的化合物可用于预防和/或治疗涉及5-HT 2B受体和5-HT7受体的疾病，特别是用于治疗肠易激综合征（IBS）和/或预防偏头痛。

5. 发明申请

US20080200551A1 Flourene Derivative 审中-公开
标题翻译： Flourene衍生物
公开(公告)号：US20080200551A1
公开(公告)日：2008-08-21
申请号：US10568684
申请日：2005-02-17
申请人： Hiroyoshi Yamada , Hirotsune Itahana , Ayako Moritomo , Takaho Matsuzawa , Koichiro Harada , Jiro Fujiyasu , Yuji Koga , Makoto Oku , Toshio Okazaki , Shinobu Akuzawa , Toshihiro Watanabe
发明人： Hiroyoshi Yamada , Hirotsune Itahana , Ayako Moritomo , Takaho Matsuzawa , Koichiro Harada , Jiro Fujiyasu , Yuji Koga , Makoto Oku , Toshio Okazaki , Shinobu Akuzawa , Toshihiro Watanabe
IPC分类号： A61K31/166 , C07C233/78 , A61P25/06
CPC分类号： C07D311/96 , A61K31/166 , A61K31/343 , A61K31/351 , A61K31/352 , A61K31/357 , A61K31/385 , A61K31/41 , A61K31/4168 , A61K31/4196 , A61K31/421 , A61K31/426 , A61K31/438 , C07C279/22 , C07D207/20 , C07D209/54 , C07D209/96 , C07D211/70 , C07D221/20 , C07D233/50 , C07D249/14 , C07D257/06 , C07D263/28 , C07D277/18 , C07D303/06 , C07D305/14 , C07D307/94 , C07D309/06 , C07D309/20 , C07D317/12 , C07D319/14 , C07D327/04 , C07D335/04 , C07D339/06
摘要： This invention relates to a novel fluorene derivative having a characteristic structure in which guanidino group or the like functional group is linked to the fluorene structure via carbonyl group, or a salt thereof.The compound of the invention has an advantage in that it has high affinity for serotonin receptor subtypes, particularly for 5-HT2B receptor and 5-HT7 receptor, and shows excellent pharmacological effects in comparison with the conventional compounds which have only one of the antagonistic activities of 5-HT2B receptor and 5-HT7 receptor, this is useful as a prophylactic antimigraine agent having high safety and excellent effect.
摘要翻译：本发明涉及具有胍基等官能团通过羰基与芴结构连接的特征结构的新型芴衍生物或其盐。本发明的化合物具有的优点在于其对5-羟色胺受体亚型具有高亲和力，特别是对于5-HT 2B受体和5-HT 7受体，并且显示出优异的与仅具有5-HT 2B受体和5-HT 7受体的拮抗活性的常规化合物相比，药理作用可用作预防性抗偏头痛药剂安全性高，效果好。

6. 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）

7. 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）

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