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1. 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）

2. 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）

3. 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。

4. 发明授权

US08044206B2 Nitrogen—containing heterocyclic derivatives having 2,6-disubstituted styryl 失效
标题翻译：含2,6-二取代苯乙烯基的含氮杂环衍生物
公开(公告)号：US08044206B2
公开(公告)日：2011-10-25
申请号：US10548197
申请日：2004-03-05
申请人： Kazumi Kikuchi , Makoto Oku , Jiro Fujiyasu , Norio Asai , Toshihiro Watanabe , Yukinori Nagakura , Hiroshi Tomiyama , Motoharu Sonegawa , Kazuo Tokuzaki , Yoshinori Iwai
发明人： Kazumi Kikuchi , Makoto Oku , Jiro Fujiyasu , Norio Asai , Toshihiro Watanabe , Yukinori Nagakura , Hiroshi Tomiyama , Motoharu Sonegawa , Kazuo Tokuzaki , Yoshinori Iwai
IPC分类号： C07D211/08 , A61K31/47
CPC分类号： C07D211/12
摘要： The invention provides a novel nitrogen-containing heterocyclic derivative having 2,6-disubstituted styryl and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the nitrogen-containing heterocyclic derivative and a pharmaceutically acceptable salt thereof, in particular, a pharmaceutical composition effective as a sodium channel inhibitor, having an excellent analgesic action especially on neuropathic pain with minimized side effects.
摘要翻译：本发明提供了具有2,6-二取代苯乙烯基的新型含氮杂环衍生物及其药学上可接受的盐，以及包含含氮杂环衍生物及其药学上可接受的盐的药物组合物，特别是作为钠通道抑制剂，具有优异的镇痛作用，特别是对神经性疼痛具有最小的副作用。

5. 发明申请

US20080070898A1 Piperidine Derivative or Pharmaceutically Acceptable Salt Thereof 审中-公开
标题翻译：哌啶衍生物或其药学上可接受的盐
公开(公告)号：US20080070898A1
公开(公告)日：2008-03-20
申请号：US11661446
申请日：2005-08-31
申请人： Kazumi Kikuchi , Jiro Fujiyasu , Toshihiro Watanabe , Yukinori Nagakura , Hiroshi Tomiyama , Motoharu Sonegawa , Kazuo Tokuzaki , Yoshinori Iwai
发明人： Kazumi Kikuchi , Jiro Fujiyasu , Toshihiro Watanabe , Yukinori Nagakura , Hiroshi Tomiyama , Motoharu Sonegawa , Kazuo Tokuzaki , Yoshinori Iwai
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/553 , A61P25/04 , C07D273/01 , C07D401/06 , C07D413/06
CPC分类号： C07D211/16 , C07D211/18 , C07D211/22 , C07D211/26 , C07D211/34 , C07D211/46 , C07D401/12 , C07D405/12 , C07D413/12 , C07D487/08 , C07D491/10
摘要： The piperidine derivative of the present invention in which the 4-position of the piperidine ring is bonded, via vinylene, to a mono-substituted (—R1) or unsubstituted benzene ring and the 1-position of the piperidine ring has an acyl group [—C(═O)—R4], or a pharmaceutically acceptable salt thereof has an excellent sodium channel inhibition action and an excellent analgesic action and shows a high analgesic effect particularly to neurogenic pain. The present compound is useful as a sodium channel inhibitor of low side effect
摘要翻译：其中哌啶环的4位通过亚乙烯基键合到单取代的（-R 1）或未取代的苯环上的本发明的哌啶衍生物和1-取代的哌啶环具有酰基[-C（-O）-R 4]，或其药学上可接受的盐具有优异的钠通道抑制作用和优异的镇痛作用，并显示出高镇痛作用特别是神经源性疼痛。本发明化合物可用作低副作用的钠通道抑制剂

6. 发明授权

US08802679B2 Glycine compound 有权
标题翻译：甘氨酸化合物
公开(公告)号：US08802679B2
公开(公告)日：2014-08-12
申请号：US13394505
申请日：2010-09-15
申请人： Kousei Yoshihara , Daisuke Suzuki , Susumu Yamaki , Yuji Koga , Norio Seki , Jiro Fujiyasu , Masahiro Neya
发明人： Kousei Yoshihara , Daisuke Suzuki , Susumu Yamaki , Yuji Koga , Norio Seki , Jiro Fujiyasu , Masahiro Neya
IPC分类号： A61K31/497 , C07D403/14
CPC分类号： C07D401/06 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/12 , C07C237/42 , C07C255/60 , C07C271/28 , C07C275/40 , C07C311/05 , C07C311/21 , C07C311/46 , C07C317/32 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D407/14 , C07D413/04 , C07D413/12 , C07D417/04 , C07D471/04 , C07D487/04 , C07D513/04
摘要： Compounds of formula (I) defined herein exhibit VAP-1 inhibitory activity, and as a result, are useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention.
摘要翻译：本文定义的式（I）化合物表现出VAP-1抑制活性，结果可用于预防和/或治疗VAP-1相关疾病，特别是糖尿病性肾病或糖尿病性黄斑水肿，从而完成本发明。

7. 发明申请

US20090197834A1 QUINOLONE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF 失效
标题翻译：喹诺酮衍生物或药物可接受的盐
公开(公告)号：US20090197834A1
公开(公告)日：2009-08-06
申请号：US12293055
申请日：2007-03-14
申请人： Yuji Koga , Takao Okuda , Susumu Watanuki , Takashi Kamikubo , Fukushi Hirayama , Hiroyuki Moritomo , Jiro Fujiyasu , Michihito Kageyama , Toshio Uemura , Jun Takasaki
发明人： Yuji Koga , Takao Okuda , Susumu Watanuki , Takashi Kamikubo , Fukushi Hirayama , Hiroyuki Moritomo , Jiro Fujiyasu , Michihito Kageyama , Toshio Uemura , Jun Takasaki
IPC分类号： A61K31/675 , C07D215/22 , A61K31/47 , C07F9/60
CPC分类号： C07D513/04 , C07D215/22 , C07D215/56 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/14 , C07D487/04 , C07F7/1804 , C07F9/60
摘要： [Problem] To provide a compound having excellent platelet aggregation inhibitory activity.[Means for Resolution] It was found that quinolone derivatives characterized in that these have lower alkyl, cycloalkyl or the like at the 1-position; —N(R0)C(O)-lower alkylene-CO2R0, lower alkylene-CO2R0, lower alkenylene-CO2R0, —O-lower alkylene-CO2R0, —O-(lower alkylene which may be substituted with —CO2R0)-aryl or —O-lower alkenylene-CO2R0 (wherein R0 is H or lower alkyl) at the 3-position; halogen at the 6-position; and amino group substituted with a substituent group having a ring structure at the 7-position, respectively, or pharmaceutically acceptable salts thereof, has excellent P2Y12 inhibitory activity. In addition, it was confirmed that these quinolone derivatives also have excellent platelet aggregation inhibitory activity. Based on the above, these quinolone derivatives or pharmaceutically acceptable salts thereof are useful as platelet aggregation inhibitors.
摘要翻译：提供具有优异血小板聚集抑制活性的化合物。 [解决方法]发现喹诺酮衍生物的特征在于它们在1-位具有低级烷基，环烷基等; -N（R 0）C（O） - 低级亚烷基-CO 2 R 0，低级亚烷基-CO 2 R 0，低级亚烯基-CO 2 R O，-O-低级亚烷基-CO 2 R O，-O-（可被-CO 2 R 0取代的低级亚烷基） - 芳基或 O-低级亚烯基-CO 2 R 0（其中R 0是H或低级烷基）在3-位; 6位卤素; 分别被具有7位具有环结构的取代基取代的氨基或其药学上可接受的盐具有优异的P2Y12抑制活性。此外，证实这些喹诺酮衍生物也具有优异的血小板聚集抑制活性。基于上述，这些喹诺酮衍生物或其药学上可接受的盐可用作血小板聚集抑制剂。

8. 发明申请

US20140378459A1 GUANIDINOBENZOIC ACID COMPOUND 有权
标题翻译：胍基苯甲酸化合物
公开(公告)号：US20140378459A1
公开(公告)日：2014-12-25
申请号：US14344377
申请日：2012-09-14
申请人： Jiro Fujiyasu , Kazuhiko Ohne , Susumu Yamaki , Tomoyoshi Imaizumi , Takeshi Hondo , Keisuke Matsuura , Tomohki Satou , Satoshi Sasamura
发明人： Jiro Fujiyasu , Kazuhiko Ohne , Susumu Yamaki , Tomoyoshi Imaizumi , Takeshi Hondo , Keisuke Matsuura , Tomohki Satou , Satoshi Sasamura
IPC分类号： C07C279/18 , C07D215/48 , C07D209/42 , C07D295/13 , C07D333/40 , C07D257/04 , C07D271/07 , C07D233/64 , C07D217/26
CPC分类号： C07C279/18 , C07B2200/07 , C07C2601/02 , C07C2601/14 , C07D207/16 , C07D209/20 , C07D209/42 , C07D211/62 , C07D213/79 , C07D215/20 , C07D215/48 , C07D215/50 , C07D217/26 , C07D233/64 , C07D257/04 , C07D271/06 , C07D271/07 , C07D277/20 , C07D277/56 , C07D295/12 , C07D295/13 , C07D333/38 , C07D333/40
摘要： [Problem]Provided is a compound which is useful as an agent for preventing and/or treating renal diseases. [Means for Solution]The present inventors have conducted extensive studies on compounds having a trypsin inhibitory action, and as a result, they have found that a guanidinobenzoic acid compound has a trypsin inhibitory action, thereby completing the present invention. The guanidinobenzoic acid compound of the present invention can be used as an agent for preventing and/or treating renal disease as an agent which will substitute low-protein diet therapy, and an agent for preventing and/or treating trypsin-related diseases, for example, pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like.
摘要翻译： [问题]提供可用作预防和/或治疗肾脏疾病的药剂的化合物。 [解决方案]本发明人对具有胰蛋白酶抑制作用的化合物进行了广泛的研究，结果发现胍基苯甲酸化合物具有胰蛋白酶抑制作用，从而完成了本发明。本发明的胍基苯甲酸化合物可以用作预防和/或治疗肾脏疾病的药剂，作为代替低蛋白饮食疗法的药剂，以及用于预防和/或治疗胰蛋白酶相关疾病的药剂，例如，胰腺炎，胃食管反流病，肝性脑病，流行性感冒等。

9. 发明申请

US20090054352A1 BENZENE DERIVATIVE OR SALT THEREOF 失效
标题翻译：苯甲醛衍生物或其盐
公开(公告)号：US20090054352A1
公开(公告)日：2009-02-26
申请号：US12091099
申请日：2006-11-07
申请人： Fukushi Hirayama , Jiro Fujiyasu , Daisuke Kaga , Kenji Negoro , Daisuke Sasuga , Norio Seki , Ken-ichi Suzuki
发明人： Fukushi Hirayama , Jiro Fujiyasu , Daisuke Kaga , Kenji Negoro , Daisuke Sasuga , Norio Seki , Ken-ichi Suzuki
IPC分类号： A61K31/706 , C07D401/12 , A61K31/444 , A61K31/513 , C07D413/14 , A61K31/5377 , A61K31/553 , C07H17/02
CPC分类号： C07D213/75 , C07D211/76 , C07D213/64 , C07D239/36 , C07D241/18 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14
摘要： Problem: To provide compounds which have an anticoagulation effect based on their ability to inhibit the activated blood coagulation factor X and are useful as coagulation inhibitors or agents for prevention or treatment for diseases caused by thrombi or emboli.Means for Solution: Benzene derivatives or their salts having a characteristic chemical structure with a phenol ring and a benzene ring bonding to each other via an amide bond, in which the phenol ring further bonds to a benzene ring or a heteroaryl ring via an amide bond. They have an excellent effect of inhibiting the activated blood coagulation factor X, and especially have an excellent oral activity.
摘要翻译：问题：提供基于其抑制活化凝血因子X的能力具有抗凝作用的化合物，并且可用作凝血抑制剂或用于预防或治疗由血栓或栓塞引起的疾病的药剂。解决方法：苯衍生物或其具有特征化学结构的苯酚环和苯环通过酰胺键彼此键合，其中酚环还通过酰胺键与苯环或杂芳基环键合。它们具有抑制活化凝血因子X的优异效果，特别是具有优异的口服活性。

10. 发明授权

US09199927B2 Guanidinobenzoic acid compound 有权
标题翻译：胍基苯甲酸化合物
公开(公告)号：US09199927B2
公开(公告)日：2015-12-01
申请号：US14344377
申请日：2012-09-14
申请人： Jiro Fujiyasu , Kazuhiko Ohne , Susumu Yamaki , Tomoyoshi Imaizumi , Takeshi Hondo , Keisuke Matsuura , Tomohki Satou , Satoshi Sasamura
发明人： Jiro Fujiyasu , Kazuhiko Ohne , Susumu Yamaki , Tomoyoshi Imaizumi , Takeshi Hondo , Keisuke Matsuura , Tomohki Satou , Satoshi Sasamura
IPC分类号： A61K31/47 , C07C229/02 , C07D215/38 , C07C279/18 , C07D213/79 , C07D215/20 , C07D215/48 , C07D215/50 , C07D333/38 , C07D333/40 , C07D233/64 , C07D257/04 , C07D271/06 , C07D207/16 , C07D277/20 , C07D277/56 , C07D209/20 , C07D209/42 , C07D295/12 , C07D211/62 , C07D217/26 , C07D271/07 , C07D295/13
CPC分类号： C07C279/18 , C07B2200/07 , C07C2601/02 , C07C2601/14 , C07D207/16 , C07D209/20 , C07D209/42 , C07D211/62 , C07D213/79 , C07D215/20 , C07D215/48 , C07D215/50 , C07D217/26 , C07D233/64 , C07D257/04 , C07D271/06 , C07D271/07 , C07D277/20 , C07D277/56 , C07D295/12 , C07D295/13 , C07D333/38 , C07D333/40
摘要： [Problem]Provided is a compound which is useful as an agent for preventing and/or treating renal diseases.[Means for Solution]The present inventors have conducted extensive studies on compounds having a trypsin inhibitory action, and as a result, they have found that a guanidinobenzoic acid compound has a trypsin inhibitory action, thereby completing the present invention. The guanidinobenzoic acid compound of the present invention can be used as an agent for preventing and/or treating renal disease as an agent which will substitute low-protein diet therapy, and an agent for preventing and/or treating trypsin-related diseases, for example, pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like.
摘要翻译： [问题]提供可用作预防和/或治疗肾脏疾病的药剂的化合物。 [解决方案]本发明人对具有胰蛋白酶抑制作用的化合物进行了广泛的研究，结果发现胍基苯甲酸化合物具有胰蛋白酶抑制作用，从而完成了本发明。本发明的胍基苯甲酸化合物可以用作预防和/或治疗肾脏疾病的药剂，作为代替低蛋白饮食疗法的药剂，以及用于预防和/或治疗胰蛋白酶相关疾病的药剂，例如，胰腺炎，胃食管反流病，肝性脑病，流行性感冒等。

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