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1. 发明申请

US20090069304A1 MMP-13 SELECTIVE INHIBITOR 审中-公开
标题翻译： MMP-13选择性抑制剂
公开(公告)号：US20090069304A1
公开(公告)日：2009-03-12
申请号：US12281216
申请日：2007-03-01
申请人： Mikayo Hayashi , Fumihiko Watanabe
发明人： Mikayo Hayashi , Fumihiko Watanabe
IPC分类号： A61K31/5513 , C07D243/08 , C07D241/04 , A61K31/4965
CPC分类号： C07D209/86 , C07D211/96 , C07D241/04 , C07D243/08 , C07D295/22
摘要： Since it is thought that if the activity of MMP-13 can be inhibited, this will largely contribute to improvement or prevention of progession of pathological states, particularly, osteoarthritis (OA), resulting from or associated with the MMP-13 activity, the development of MMP-13 inhibitors is anticipated. There are provided a compound represented by the general formula (I): wherein R1 is optionally substituted aryl etc.; Z is C1-C5 alkylene which may be substituted and may be interrupted with a substituent selected from Substituent group a etc.; A is the formula: (R6 and R7 are each independently halogen, lower alkyl etc.; m and n are each independently 0, 1, or 2); R2 is a hydrogen atom, optionally substituted lower alkyl etc.; R3 is a hydrogen atom, optionally substituted lower alkyl etc.; R4 is a hydrogen atom; or R3 and R4 may be taken together with an adjacent carbon atom to from a ring; R5 is hydroxy, lower alkyloxy etc.), or an optically active isomer, a pharmaceutically acceptable salt or a solvate thereof, and a pharmaceutical composition containing it as an active ingredient, which has the MMP-13 inhibiting activity.
摘要翻译：由于认为如果可以抑制MMP-13的活性，这将大大有助于改善或预防由MMP-13活性引起或与MMP-13活性相关的病理状态，特别是骨关节炎（OA），发展的MMP-13抑制剂。提供由通式（I）表示的化合物：其中R 1是任选取代的芳基等; Z是可以被取代的C1-C5亚烷基，可以被选自取代基组a等的取代基中断; A是下式：（R 6和R 7各自独立地为卤素，低级烷基等; m和n各自独立地为0,1或2）; R2是氢原子，任选取代的低级烷基等; R3是氢原子，任选取代的低级烷基等; R4是氢原子; 或者R 3和R 4可以与相邻的碳原子一起与环一起取代; R5是羟基，低级烷氧基等）或光学活性异构体，其药学上可接受的盐或溶剂合物，以及含有其作为活性成分的具有MMP-13抑制活性的药物组合物。

2. 发明授权

US08324265B2 Heterocyclic compounds having type I 11β hydroxysteroid dehydrogenase inhibitory activity 有权
标题翻译：具有I 11和bgr的杂环化合物羟类固醇脱氢酶抑制活性
公开(公告)号：US08324265B2
公开(公告)日：2012-12-04
申请号：US12093903
申请日：2006-11-20
申请人： Noriyuki Kurose , Mikayo Hayashi , Tomoyuki Ogawa , Koji Masuda , Eiichi Kojima
发明人： Noriyuki Kurose , Mikayo Hayashi , Tomoyuki Ogawa , Koji Masuda , Eiichi Kojima
IPC分类号： A61K31/551 , A61K31/5377 , A61K31/506 , A61K31/496 , A61K31/454 , A61K31/4439 , A61K31/427 , A61K31/4245 , A61K31/4178 , A61K31/4155 , A61K31/415 , C07D417/06 , C07D417/12 , C07D413/06 , C07D413/12 , C07D409/06 , C07D409/12 , C07D401/14 , C07D401/12 , C07D401/06 , C07D403/06 , C07D403/12 , C07D231/20 , C07D231/18
CPC分类号： C07D231/18 , C07D231/20 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/06 , C07D417/12 , C07D419/06 , C07D471/08 , C07D471/10 , C07D471/12
摘要： Disclosed is a compound useful as a type I 11βhydroxysteroid dehydrogenase inhibitor.A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted alkyl or the like, one of R2 and R4 is a group of formula: —Y—R5, wherein Y is —O— or the like, R5 is substituted alkyl (the substituent is optionally substituted cycloalkyl or the like), optionally substituted branched alkyl or the like, the other of R2 and R4 is hydrogen or optionally substituted alkyl, R3 is a group of formula: —C(═O)—Z—R6, wherein Z is —NR7— or —NR7—W—, R6 is optionally substituted cycloalkyl or the like, R7 is hydrogen or optionally substituted alkyl, W is optionally substituted alkylene, X is ═N— or the like, with the proviso that compounds wherein R2 is 2-(morphorino)ethoxy, R3 is N-(1-adamantyl)carbamoyl and R1 is benzyl are excluded.
摘要翻译：公开了可用作I 11和Bgr的羟基类固醇脱氢酶抑制剂的化合物。由下式表示的化合物：其药学上可接受的盐或溶剂合物，其中R 1为任选取代的烷基等，R 2和R 4中的一个为下式基团：-Y-R 5，其中Y为-O-等，R 5是取代的烷基（取代基是任选取代的环烷基等），任选取代的支链烷基等，R 2和R 4中的另一个是氢或任选取代的烷基，R 3是下列基团：-C（= O ）-Z-R6，其中Z是-NR7-或-NR7-W-，R6是任选取代的环烷基等，R 7是氢或任选取代的烷基，W是任选取代的亚烷基，X是= N-等条件是其中R2是2-（吗啉基）乙氧基，R3是N-（1-金刚烷基）氨基甲酰基和R1是苄基的化合物被排除在外。

3. 发明授权

US09051333B2 6,7-dihydroimidazo [2,1-b] [1,3]oxazine bactericides 有权
标题翻译： 6,7-二氢咪唑并[2,1-b] [1,3]恶嗪类杀菌剂
公开(公告)号：US09051333B2
公开(公告)日：2015-06-09
申请号：US14111262
申请日：2012-04-13
申请人： Yoshikazu Kawano , Yoshikazu Haraguchi , Hirofumi Sasaki , Yukitaka Uematsu , Hidetsugu Tsubouchi , Hiromi Yata , Hiroshi Shimizu , Kazuho Kohashi , Motohiro Itotani , Kuninori Tai , Isao Takemura , Mikayo Hayashi , Hiroyuki Hashizume , Miki Matsuba , Izuru Nakamura , Xiuhao Chen , Makoto Matsumoto
发明人： Yoshikazu Kawano , Yoshikazu Haraguchi , Hirofumi Sasaki , Yukitaka Uematsu , Hidetsugu Tsubouchi , Hiromi Yata , Hiroshi Shimizu , Kazuho Kohashi , Motohiro Itotani , Kuninori Tai , Isao Takemura , Mikayo Hayashi , Hiroyuki Hashizume , Miki Matsuba , Izuru Nakamura , Xiuhao Chen , Makoto Matsumoto
IPC分类号： C07D498/04 , A61K31/5383
CPC分类号： C07D498/04
摘要： The present invention provides a novel 6,7-dihydroimidazo[2,1-b][1,3]oxazine compound that has excellent bactericidal action against tubercle bacilli, multidrug-resistant tubercle bacilli, and atypical acid-fast bacilli. Specifically, the present invention provides a compound represented by Formula (1): or a salt thereof, wherein R1 represents tetrahydroisoquinolyl, tetrahydroquinolyl, tetrahydrobenzoazepinyl, benzoxazolyl, benzothiazolyl, indolyl, isoindolinyl, naphthyl, quinolyl, phenyl, biphenylyl, or pyridyl, these groups being optionally substituted, the phenyl, biphenylyl, and pyridyl represented by R1 each being substituted directly or via a linker with at least one group selected from the group consisting of tetrahydropyridyl, diazepanyl, diazabicycloheptanyl, tetrahydrotriazolopyrazinyl, tetrahydroimidazopyrazinyl, azabicyclooctanyl, oxazolyl, piperazinyl, piperidyl, thiazolyl, and the like, each of these groups being optionally substituted; and R2 represents hydrogen or lower alkyl. The present invention further provides a pharmaceutical composition containing the above.
摘要翻译：本发明提供了对结核杆菌，多重耐药性结核杆菌和非典型抗酸杆菌具有优异的杀菌作用的新型6,7-二氢咪唑并[2,1-b] [1,3]恶嗪化合物。具体地说，本发明提供由式（1）表示的化合物或其盐，其中R1表示四氢异喹啉基，四氢喹啉基，四氢苯并氮杂基，苯并恶唑基，苯并噻唑基，吲哚基，异吲哚啉基，萘基，喹啉基，苯基，联苯基或吡啶基。任选被取代的苯基，联苯基和吡啶基，其各自被直接取代或经由具有至少一个选自四氢吡啶基，二氮杂环庚烷基，二氮杂双环庚烷基，四氢三唑并吡嗪基，四氢咪唑并吡嗪基，氮杂双环辛基，恶唑基，哌嗪基，哌啶基，噻唑基等，这些基团各自任选被取代; 并且R 2表示氢或低级烷基。本发明还提供含有上述物质的药物组合物。

4. 发明申请

US20140031342A1 6,7-DIHYDROIMIDAZO [2,1-b] [1,3]OXAZINE BACTERICIDES 有权
标题翻译： 6,7-二氢吲哚并[2,1-b] [1,3]氧化物杀菌剂
公开(公告)号：US20140031342A1
公开(公告)日：2014-01-30
申请号：US14111262
申请日：2012-04-13
申请人： Yoshikazu Kawano , Yoshikazu Haraguchi , Hirofumi Sasaki , Yukitaka Uematsu , Hidetsugu Tsubouchi , Hiromi Yata , Hiroshi Shimizu , Kazuho Kohashi , Motohiro Itotani , Kuninori Tai , Isao Takemura , Mikayo Hayashi , Hiroyuki Hashizume , Miki Matsuba , Izuru Nakamura , Xiuhao Chen , Makoto Matsumoto
发明人： Yoshikazu Kawano , Yoshikazu Haraguchi , Hirofumi Sasaki , Yukitaka Uematsu , Hidetsugu Tsubouchi , Hiromi Yata , Hiroshi Shimizu , Kazuho Kohashi , Motohiro Itotani , Kuninori Tai , Isao Takemura , Mikayo Hayashi , Hiroyuki Hashizume , Miki Matsuba , Izuru Nakamura , Xiuhao Chen , Makoto Matsumoto
IPC分类号： C07D498/04
CPC分类号： C07D498/04
摘要： The present invention provides a novel 6,7-dihydroimidazo[2,1-b][1,3]oxazine compound that has excellent bactericidal action against tubercle bacilli, multidrug-resistant tubercle bacilli, and atypical acid-fast bacilli. Specifically, the present invention provides a compound represented by Formula (1): or a salt thereof, wherein R1 represents tetrahydroisoquinolyl, tetrahydroquinolyl, tetrahydrobenzoazepinyl, benzoxazolyl, benzothiazolyl, indolyl, isoindolinyl, naphthyl, quinolyl, phenyl, biphenylyl, or pyridyl, these groups being optionally substituted, the phenyl, biphenylyl, and pyridyl represented by R1 each being substituted directly or via a linker with at least one group selected from the group consisting of tetrahydropyridyl, diazepanyl, diazabicycloheptanyl, tetrahydrotriazolopyrazinyl, tetrahydroimidazopyrazinyl, azabicyclooctanyl, oxazolyl, piperazinyl, piperidyl, thiazolyl, and the like, each of these groups being optionally substituted; and R2 represents hydrogen or lower alkyl. The present invention further provides a pharmaceutical composition containing the above.
摘要翻译：本发明提供了对结核杆菌，多重耐药性结核杆菌和非典型抗酸杆菌具有优异的杀菌作用的新型6,7-二氢咪唑并[2,1-b] [1,3]恶嗪化合物。具体地说，本发明提供由式（1）表示的化合物或其盐，其中R1表示四氢异喹啉基，四氢喹啉基，四氢苯并氮杂基，苯并恶唑基，苯并噻唑基，吲哚基，异吲哚啉基，萘基，喹啉基，苯基，联苯基或吡啶基。任选被取代的苯基，联苯基和吡啶基，其各自被直接取代或经由具有至少一个选自四氢吡啶基，二氮杂环庚烷基，二氮杂双环庚烷基，四氢三唑并吡嗪基，四氢咪唑并吡嗪基，氮杂双环辛基，恶唑基，哌嗪基，哌啶基，噻唑基等，这些基团各自任选被取代; 并且R 2表示氢或低级烷基。本发明还提供含有上述物质的药物组合物。

5. 发明申请

US20090170832A1 HETEROCYCLIC COMPOUNDS HAVING TYPE I 11beta HYDROXYSTEROID DEHYDROGENASE INHIBITORY ACTIVITY 有权
标题翻译：具有I型11beta羟化酶脱氢酶抑制活性的杂环化合物
公开(公告)号：US20090170832A1
公开(公告)日：2009-07-02
申请号：US12093903
申请日：2006-11-20
申请人： Noriyuki Kurose , Mikayo Hayashi , Tomoyuki Ogawa , Koji Masuda , Eiichi Kojima
发明人： Noriyuki Kurose , Mikayo Hayashi , Tomoyuki Ogawa , Koji Masuda , Eiichi Kojima
IPC分类号： A61K31/55 , C07D231/14 , A61K31/415 , C07D257/04 , A61K31/41 , A61K31/4709 , A61K31/454 , C07D401/06 , C07D403/06 , A61K31/496
CPC分类号： C07D231/18 , C07D231/20 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/06 , C07D417/12 , C07D419/06 , C07D471/08 , C07D471/10 , C07D471/12
摘要： Disclosed is a compound useful as a type I 11βhydroxysteroid dehydrogenase inhibitor.A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted alkyl or the like, one of R2 and R4 is a group of formula: —Y—R5, wherein Y is —O— or the like, R5 is substituted alkyl (the substituent is optionally substituted cycloalkyl or the like), optionally substituted branched alkyl or the like, the other of R2 and R4 is hydrogen or optionally substituted alkyl, R3 is a group of formula: —C(═O)-Z-R6, wherein Z is —NR7— or —NR7—W—, R6 is optionally substituted cycloalkyl or the like, R7 is hydrogen or optionally substituted alkyl, W is optionally substituted alkylene, X is ═N— or the like, with the proviso that compounds wherein R2 is 2-(morphorino)ethoxy, R3 is N-(1-adamantyl)carbamoyl and R1 is benzyl are excluded.
摘要翻译：公开了可用作I型11β-羟基甾类脱氢酶抑制剂的化合物。由下式表示的化合物：其药学上可接受的盐或溶剂合物，其中R 1为任选取代的烷基等，R 2和R 4中的一个为下式基团：-Y-R 5，其中Y为-O-等，R 5为取代烷基（取代基为任选取代的环烷基等），任意取代的支链烷基等，R 2和R 4中的另一个为氢或任意取代的烷基，R 3为下列基团：-C（-O ）-Z-R6，其中Z是-NR7-或-NR7-W-，R6是任选取代的环烷基等，R 7是氢或任选取代的烷基，W是任选取代的亚烷基，X是-N-等条件是其中R2是2-（吗啉基）乙氧基，R3是N-（1-金刚烷基）氨基甲酰基和R1是苄基的化合物被排除在外。

6. 发明申请

US20080167347A1 Ctgf Expression Inhibitor 审中-公开
标题翻译： Ctgf表达抑制剂
公开(公告)号：US20080167347A1
公开(公告)日：2008-07-10
申请号：US11795533
申请日：2006-01-19
申请人： Kaoru Seno , Toshihiro Shinosaki , Satoshi Hata , Isamu Yamada , Hiroki Sato , Mikayo Hayashi
发明人： Kaoru Seno , Toshihiro Shinosaki , Satoshi Hata , Isamu Yamada , Hiroki Sato , Mikayo Hayashi
IPC分类号： A61K31/45 , C07C235/68 , A61K31/167 , C07D211/96
CPC分类号： A61K31/167 , A61K31/45 , C07C235/64 , C07C255/57 , C07C305/24 , C07C309/76 , C07C311/04 , C07C311/08 , C07C311/21 , C07C311/29 , C07C311/46 , C07C317/40 , C07C323/12 , C07C323/62 , C07D207/323 , C07D207/48 , C07D211/96 , C07D213/30 , C07D213/40 , C07D215/48 , C07D233/64 , C07D235/08 , C07D239/34 , C07D239/42 , C07D243/08 , C07D279/02 , C07D295/088 , C07D295/135 , C07D295/155 , C07D295/185 , C07D295/192 , C07D295/26 , C07D307/12 , C07D307/42 , C07D307/52 , C07D307/79 , C07D307/81 , C07D317/60 , C07D333/22 , C07D333/54 , C07D333/58 , C07D335/02 , C07D401/12
摘要： A CTGF expression inhibitor comprising a compound of the formula I: a pharmaceutically acceptable salt or solvate thereof as an active ingredient, (wherein Y is hydroxy or a group of the formula: —NH—SO2—Y′ (wherein Y′ is optionally substituted aryl or optionally substituted alkyl), and R1 to R9 are each independently hydrogen, halogen, optionally substituted alkyl, optionally substituted alkoxy or the like).
摘要翻译：一种CTGF表达抑制剂，其包含式I化合物：其药学上可接受的盐或溶剂化物作为活性成分（其中Y为羟基或式-NH-SO 2 -Y '（其中Y'为任选取代的芳基或任选取代的烷基），R 1至R 9各自独立地为氢，卤素，任选取代的烷基，任选取代的烷氧基或类似）。

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