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1. 发明授权

US08822699B2 Heterocyclic compound and use thereof 有权
标题翻译：杂环化合物及其用途
公开(公告)号：US08822699B2
公开(公告)日：2014-09-02
申请号：US13223455
申请日：2011-09-01
申请人： Tatsuki Koike , Minoru Nakamura , Yoshihide Tomata , Takafumi Takai , Yasutaka Hoashi , Yuichi Kajita , Tetsuya Tsukamoto , Makoto Kamata
发明人： Tatsuki Koike , Minoru Nakamura , Yoshihide Tomata , Takafumi Takai , Yasutaka Hoashi , Yuichi Kajita , Tetsuya Tsukamoto , Makoto Kamata
IPC分类号： A61K31/42 , C07D263/30 , C07D413/02
CPC分类号： C07D471/04
摘要： The present invention provides a heterocycle derivative having a superior amyloid β production inhibitory activity and/or a superior γ-secretase modulation activity, and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
摘要翻译：本发明提供具有优异淀粉样蛋白的杂环衍生物; 生产抑制活性和/或优异的γ-分泌酶调节活性及其用途。由式（I）表示的化合物或其盐，其中每个符号如本说明书中所定义。

2. 发明申请

US20120059030A1 HETEROCYCLIC COMPOUND AND USE THEREOF 有权
标题翻译：杂环化合物及其用途
公开(公告)号：US20120059030A1
公开(公告)日：2012-03-08
申请号：US13223455
申请日：2011-09-01
申请人： Tatsuki KOIKE , Minoru Nakamura , Yoshihide Tomata , Takafumi Takai , Yasutaka Hoashi , Yuichi Kajita , Tetsuya Tsukamoto , Makoto Kamata
发明人： Tatsuki KOIKE , Minoru Nakamura , Yoshihide Tomata , Takafumi Takai , Yasutaka Hoashi , Yuichi Kajita , Tetsuya Tsukamoto , Makoto Kamata
IPC分类号： A61K31/437 , A61P25/28 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention provides a heterocycle derivative having a superior amyloid β production inhibitory activity and/or a superior γ-secretase modulation activity, and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
摘要翻译：本发明提供具有优异淀粉样蛋白的杂环衍生物; 生产抑制活性和/或优异的γ-分泌酶调节活性及其用途。由式（I）表示的化合物或其盐，其中每个符号如本说明书中所定义。

3. 发明申请

US20130178497A1 FUSED TRIAZOLES FOR THE TREATMENT OR PROPHYLAXIS OF MILD COGNITIVE IMPAIRMENT 有权
标题翻译：用于治疗或预防小儿认知功能障碍的三叉神经痛
公开(公告)号：US20130178497A1
公开(公告)日：2013-07-11
申请号：US13819239
申请日：2011-09-01
申请人： Tatsuki Koike , Minoru Nakamura , Yoshihide Tomata , Takafumi Takai , Yasutaka Hoashi , Yuichi Kajita , Tetsuya Tsukamoto , Makoto Kamata
发明人： Tatsuki Koike , Minoru Nakamura , Yoshihide Tomata , Takafumi Takai , Yasutaka Hoashi , Yuichi Kajita , Tetsuya Tsukamoto , Makoto Kamata
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The present invention provides a heterocycle derivative having a superior amyloid β production inhibitory activity and/or a superior γ-secretase modulation activity, and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
摘要翻译：本发明提供具有优异的淀粉样蛋白β产生抑制活性和/或优异的γ-分泌酶调节活性的杂环衍生物及其用途。由式（I）表示的化合物或其盐，其中每个符号如本说明书中所定义。

4. 发明授权

US08957069B2 Benzofuran derivatives 有权
标题翻译：苯并呋喃衍生物
公开(公告)号：US08957069B2
公开(公告)日：2015-02-17
申请号：US13255366
申请日：2010-03-09
申请人： Tetsuya Tsukamoto , Takeshi Wakabayashi , Taiichi Ohra
发明人： Tetsuya Tsukamoto , Takeshi Wakabayashi , Taiichi Ohra
IPC分类号： A61K31/496 , A61K31/541 , A61K31/5377 , A61K31/519 , C07D307/79 , C07D307/80 , C07D307/81 , C07D405/06 , C07D405/14 , C07D487/04 , C07D413/12 , C07D491/113 , C07D417/06 , C07D413/06 , C07D493/10 , C07D405/04 , C07D405/12 , C07D407/04 , C07D407/12 , C07D417/12 , A61K31/551 , C07D413/04
CPC分类号： C07D307/79 , C07D307/80 , C07D307/81 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/04 , C07D407/12 , C07D413/04 , C07D413/12 , C07D417/12 , C07D493/10
摘要： The present invention provides a compound represented by the following formula (I): wherein: Ring A represents an optionally substituted piperazine ring, an optionally substituted morpholine ring, or an optionally substituted bromopiperazine ring; R1 and R2 are the same or different from each other, and represent a hydrogen atom or optionally substituted lower alkyl; R3 and R4 are the same or different from each other, and represent a hydrogen atom or halogenated or non-halogenated lower alkyl; R3 to R7 are the same or different from each other, and represent a hydrogen atom, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted cycloalkyl, optionally substituted aryl, an optionally substituted aromatic heterocyclic ring, optionally substituted amino, or acyl; and represents a single bond or double bond, wherein R2 and R3 do not exist when carbon atoms respectively adjacent to R2: and R3 form a double bond, and there is no case where all of R1 to R7 are hydrogen atoms, and R1 and R2; may form a ring together with an adjacent carbon atom; or a salt thereof.
摘要翻译：本发明提供由下式（I）表示的化合物：其中：环A表示任选取代的哌嗪环，任选取代的吗啉环或任选取代的溴代哌嗪环; R1和R2彼此相同或不同，表示氢原子或任选取代的低级烷基; R3和R4彼此相同或不同，表示氢原子或卤代或非卤代低级烷基; R 3至R 7彼此相同或不同，并且表示氢原子，羟基，任选取代的低级烷基，任选取代的低级烯基，任选取代的低级烷氧基，任选取代的环烷基，任选取代的芳基，任选取代的芳族杂环，任选取代的氨基或酰基; 并且表示单键或双键，其中当分别相邻于R2：和R3的碳原子形成双键时，R2和R3不存在，并且不存在所有R 1至R 7都是氢原子的情况，并且R 1和R 2 ; 可与邻近的碳原子一起形成环; 或其盐。

5. 发明授权

US08865775B2 Anti-inflammatory agent and cancer-preventive agent comprising canolol or prodrug thereof and pharmaceutical, cosmetic and food comprising the same 有权
标题翻译：抗炎药和包含其组合的前药的抗炎剂和药物，化妆品和包含其的食品
公开(公告)号：US08865775B2
公开(公告)日：2014-10-21
申请号：US13354507
申请日：2012-01-20
申请人： Hiroshi Maeda , Tetsuya Tsukamoto , Masae Tatematsu
发明人： Hiroshi Maeda , Tetsuya Tsukamoto , Masae Tatematsu
IPC分类号： A01N31/14 , A61K31/075 , C07C41/00 , C07C43/02 , C07C43/20 , A61K31/09
CPC分类号： A61K31/09
摘要： An anti-inflammatory agent or cancer-preventive agent comprising 4-vinyl-2,6-dimethoxyphenol of the formula (1): or a PD thereof.
摘要翻译：包含式（1）的4-乙烯基-2,6-二甲氧基苯酚或其PD的抗炎剂或防癌剂。

6. 发明申请

US20090023800A1 Cannabinoid receptor modulator 审中-公开
公开(公告)号：US20090023800A1
公开(公告)日：2009-01-22
申请号：US12230483
申请日：2008-08-29
申请人： Shigenori Ohkawa , Tetsuya Tsukamoto , Yoshihiro Kiyota , Mika Goto , Shouzou Yamamoto , Masato Shimojou , Masaki Setou
发明人： Shigenori Ohkawa , Tetsuya Tsukamoto , Yoshihiro Kiyota , Mika Goto , Shouzou Yamamoto , Masato Shimojou , Masaki Setou
IPC分类号： A61K31/352 , C07D307/78 , C07D333/52 , A61P1/00 , A61P31/12 , A61P9/10 , A61P37/00 , A61P25/00 , A61K31/381
CPC分类号： C07D307/83 , A61K31/343 , A61K31/357 , A61K31/381 , A61K31/4025 , A61K31/4178 , A61K31/426 , A61K31/443 , A61K31/453 , A61K31/506 , C07D307/79 , C07D307/86 , C07D333/54 , C07D405/04
摘要： A cannabinoid receptor modulator containing a compound represented by Formula (I0) wherein, X is an oxygen atom, etc., R0 is an optionally substituted acylamino group, ring A0 is a benzene ring which may further have a substituent in addition to R0, and ring B is an optionally substituted 5-membered heterocycle, or a salt thereof or a prodrug thereof.

7. 发明授权

US07208495B2 Benzo-fused 5-membered hetrocycle compounds, process for preparation of the same, and use thereof 失效
标题翻译：苯并稠合的5元杂环化合物，其制备方法及其用途
公开(公告)号：US07208495B2
公开(公告)日：2007-04-24
申请号：US10481367
申请日：2002-07-04
申请人： Shigenori Ohkawa , Masaomi Miyamoto , Masahiro Okura , Tetsuya Tsukamoto
发明人： Shigenori Ohkawa , Masaomi Miyamoto , Masahiro Okura , Tetsuya Tsukamoto
IPC分类号： A61K31/497 , A61K31/445 , C07D405/00 , C07D401/00
CPC分类号： A61K31/4525 , A61K31/496 , C07D307/79 , C07D307/80 , C07D307/81 , C07D307/82 , C07D307/83 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/04 , C07D409/04 , C07D409/14
摘要： A compound represented by the formula: (wherein, R1 and R2 are the same or different and each represents a hydrogen atom, hydrocarbon group or heterocyclic group, or R1 and R2 may form, together with the adjacent carbon atom, a 3–8 membered iso- or heterocyclic group, R3 represents a cyclic group, a hydroxy group, a mercapto group that may have oxo, or an amino group, R4 represents a hydrogen atom, a hydrocarbon group, a hydroxy group, a mercapto group which may have oxo, or an amino group, or R2 and R4 may link together to form a double bond, X represents a bond or a linear hydrocarbon group, W represents an oxygen atom or a sulfur atom, ring B represents a 5–8 membered nitrogen-containing heterocyclic group, ring C represents a benzene ring, and— represents a single bond or a double bond), or a salt or a prodrug thereof that has excellent neurodegenerative inhibitory activity and brain penetrability, and is useful as an agent for preventing/treating neurodegenerative diseases.
摘要翻译：由下式表示的化合物（其中，R 1和R 2相同或不同，各自表示氢原子，烃基或杂环基，可以与相邻的碳原子一起形成3-8元的异或杂环基，R 3表示环状基团，羟基，可具有氧代基的巯基或氨基，R 4表示氢原子，烃基，羟基，可具有氧代基的巯基，或氨基或R 2和R 4可以连接在一起形成双键，X表示键或直链烃基，W表示氧原子或硫原子，环B表示5-8元含氮杂环基，环C表示苯环，代表单键或双键）或其盐或前药具有优异的神经变性抑制活性，脑穿透性并且可用作预防/治疗神经变性疾病的药剂。

8. 发明授权

US5492903A Crystalline esters of (+)-(5R, 6S)-6-[(R)-1-hydroxyethyl]-3-(3-pyridyl)-7-oxo-4-thia-1-azabicyclo[3.2.0]h e 失效
标题翻译：（+） - （5R，6S）-6 - [（R）-1-羟乙基] -3-（3-吡啶基）-7-氧代-4-硫杂-1-氮杂双环[3.2.0]庚烷 -2-烯-2-羧酸
公开(公告)号：US5492903A
公开(公告)日：1996-02-20
申请号：US112072
申请日：1993-08-26
申请人： Yoshiharu Maeda , Yukio Ishibashi , Tetsuya Tsukamoto , Masahiro Mizuno
发明人： Yoshiharu Maeda , Yukio Ishibashi , Tetsuya Tsukamoto , Masahiro Mizuno
IPC分类号： C07D499/88 , C07D499/00 , A61K31/425
CPC分类号： C07D499/88
摘要： Crystalline acetoxymethyl and pivaloyloxymethyl esters of (+)-(5R, 6S)-6-[(R)-1-hydroxyethyl]-3-(3-pyridyl)-7-oxo-4-thia-1-azabicyclo-[3.2.0]hept-2-ene-carboxylic acid can be obtained by adding a poor solvent to a solution of acetoxymethyl or pivaloyloxymethyl ester of (+)-(5R, 6S)-6-[(R)-1-hydroxyethyl]-3-(3-pyridyl)-7-oxo-4-thia-1-azabicyclo-[3.2.0]hept-2-ene-carboxylic acid in a good solvent. The crystalline penem compounds obtained show improved stability and are useful antibacterial agents.
摘要翻译：（+） - （5R，6S）-6 - [（R）-1-羟乙基] -3-（3-吡啶基）-7-氧代-4-硫杂-1-氮杂双环[3.2 通过向（+） - （5R，6S）-6 - [（R）-1-羟乙基] - （（R）-1-羟乙基）-6 - [（R）-1-羟基乙基） - 乙酰氧基甲基酯的乙酰氧基甲基或新戊酰氧基甲基酯的溶液中加入不良溶剂， 3-（3-吡啶基）-7-氧代-4-硫杂-1-氮杂双环[3.2.0]庚-2-烯羧酸在良溶剂中反应。获得的结晶青枯烯化合物显示出改进的稳定性，并且是有用的抗菌剂。

9. 发明申请

US20130267494A1 1,4-OXAZEPANE DERIVATIVES 审中-公开
标题翻译： 1,4-OXAZEPANE衍生物
公开(公告)号：US20130267494A1
公开(公告)日：2013-10-10
申请号：US13877810
申请日：2011-10-05
申请人： Yuji Ishichi , Masami Yamada , Taku Kamei , Ikuo Fujimori , Yoshihisa Nakada , Tomoya Yukawa , Nobuki Sakauchi , Yusuke Ohba , Tetsuya Tsukamoto
发明人： Yuji Ishichi , Masami Yamada , Taku Kamei , Ikuo Fujimori , Yoshihisa Nakada , Tomoya Yukawa , Nobuki Sakauchi , Yusuke Ohba , Tetsuya Tsukamoto
IPC分类号： C07D267/10 , C07D413/06 , C07D413/12 , C07D417/12 , C07D413/14 , C07D498/08
CPC分类号： C07D267/10 , C07D413/04 , C07D413/06 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D498/08
摘要： Provided is a compound having a monoamine reuptake inhibitory activity, which is represented by the formula (I) wherein ring A is an optionally substituted 6-membered aromatic ring, ring B is the substituents on ring A are optionally bonded to form, together with ring A, an optionally substituted 9- or 10-membered aromatic fused ring, and other symbols are as defined in the specification, or a salt thereof.
摘要翻译：提供具有单胺再摄取抑制活性的化合物，其由式（I）表示，其中环A是任选取代的6元芳环，环B是环A上的取代基任选地键合以与环一起形成 A，任选取代的9元或10元芳族稠环，以及其它符号如说明书中所定义，或其盐。

10. 发明申请

US20120046277A1 BENZOFURAN DERIVATIVES 有权
标题翻译： BENZOFURAN衍生物
公开(公告)号：US20120046277A1
公开(公告)日：2012-02-23
申请号：US13255366
申请日：2010-03-09
申请人： Tetsuya Tsukamoto , Takeshi Wakabayashi , Taiichi Ohra
发明人： Tetsuya Tsukamoto , Takeshi Wakabayashi , Taiichi Ohra
IPC分类号： A61K31/496 , C07D405/14 , C07D413/10 , A61P25/00 , C07D493/10 , A61K31/551 , A61K31/506 , A61P25/28 , C07D405/10 , A61K31/5377
CPC分类号： C07D307/79 , C07D307/80 , C07D307/81 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/04 , C07D407/12 , C07D413/04 , C07D413/12 , C07D417/12 , C07D493/10
摘要： The present invention provides a compound represented by the following formula (I): wherein: Ring A represents an optionally substituted piperazine ring, an optionally substituted morpholine ring, or an optionally substituted bromopiperazine ring; R1 and R2 are the same or different from each other, and represent a hydrogen atom or optionally substituted lower alkyl; R3 and R4 are the same or different from each other, and represent a hydrogen atom or halogenated or non-halogenated lower alkyl; R3 to R7 are the same or different from each other, and represent a hydrogen atom, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted cycloakyl, optionally substituted aryl, an optionally substituted aromatic heterocyclic ring, optionally substituted amino, or acyl; and represents a single bond or double bond, wherein R2 and R3 do not exist when carbon atoms respectively adjacent to R2: and R3 form a double bond, and there is no case where all of R1 to R7 are hydrogen atoms, and R1 and R2; may form a ring together with an adjacent carbon atom; or a salt thereof.
摘要翻译：本发明提供由下式（I）表示的化合物：其中：环A表示任选取代的哌嗪环，任选取代的吗啉环或任选取代的溴代哌嗪环; R1和R2彼此相同或不同，表示氢原子或任选取代的低级烷基; R3和R4彼此相同或不同，表示氢原子或卤代或非卤代低级烷基; R 3至R 7彼此相同或不同，并且表示氢原子，羟基，任选取代的低级烷基，任选取代的低级烯基，任选取代的低级烷氧基，任选取代的环烷基，任选取代的芳基，任选取代的芳族杂环，任选取代的氨基或酰基; 并且表示单键或双键，其中当分别相邻于R2：和R3的碳原子形成双键时，R2和R3不存在，并且不存在所有R 1至R 7都是氢原子的情况，并且R 1和R 2 ; 可与邻近的碳原子一起形成环; 或其盐。

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