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1. 发明授权

US08563575B2 Fused heterocyclic compounds 有权
公开(公告)号：US08563575B2
公开(公告)日：2013-10-22
申请号：US13166212
申请日：2011-06-22
申请人： Takahiko Taniguchi , Masato Yoshikawa , Kasei Miura , Tomoaki Hasui , Eiji Honda , Keisuke Imamura , Makoto Kamata , Haruhi Kamisaki
发明人： Takahiko Taniguchi , Masato Yoshikawa , Kasei Miura , Tomoaki Hasui , Eiji Honda , Keisuke Imamura , Makoto Kamata , Haruhi Kamisaki
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： A61K31/4353 , A61K31/4355 , A61K31/437 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4985 , A61K31/5025 , A61K31/519 , A61K31/52 , A61K31/522 , A61K31/551 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/14 , C07D471/04 , C07D471/14 , C07D473/00 , C07D473/28 , C07D487/04 , C07D495/04 , C07D498/04 , C07D498/08 , C07D519/00 , C07F7/10
摘要： The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I): wherein the symbols are defined in the specification.

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

US20110263562A1 BICYCLIC COMPOUND 失效
标题翻译：双相化合物
公开(公告)号：US20110263562A1
公开(公告)日：2011-10-27
申请号：US13094015
申请日：2011-04-26
申请人： Tohru Yamashita , Makoto Kamata , Hideki Hirose , Masataka Murakami , Takuya Fujimoto , Zenichi Ikeda , Tsuneo Yasuma , Ikuo Fujimori , Ryo Mizojiri , Tomoya Yukawa
发明人： Tohru Yamashita , Makoto Kamata , Hideki Hirose , Masataka Murakami , Takuya Fujimoto , Zenichi Ikeda , Tsuneo Yasuma , Ikuo Fujimori , Ryo Mizojiri , Tomoya Yukawa
IPC分类号： A61K31/423 , A61K31/438 , A61K31/439 , C07D417/04 , A61K31/454 , A61K31/416 , A61K31/34 , C07D498/04 , C07D413/14 , C07D413/04 , C07D263/56 , C07D231/56 , C07D307/87 , A61P35/04 , A61P3/04 , A61P3/06 , A61P9/12 , A61P9/00 , A61P3/10 , A61P3/00 , A61K31/497
CPC分类号： C07D413/14 , A61K31/41 , A61K31/415 , A61K31/439 , A61K31/4439 , A61K31/444 , C07D231/54 , C07D263/56 , C07D263/58 , C07D307/81 , C07D401/02 , C07D401/14 , C07D403/02 , C07D405/02 , C07D413/04 , C07D417/04 , C07D487/08 , C07D491/048 , C07D498/04
摘要： The present invention provides to a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy.The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification.
摘要翻译：本发明提供具有ACC抑制作用的化合物，其可用作预防或治疗肥胖症，糖尿病，高血压，高脂血症，心力衰竭，糖尿病并发症，代谢综合征，肌肉减少症，癌症等的药剂，以及具有优越的疗效。本发明涉及由式（I）表示的化合物：其中每个符号如说明书中所定义。

4. 发明申请

US20100160255A1 SPIRO-CYCLIC COMPOUND 审中-公开
标题翻译：螺旋环化合物
公开(公告)号：US20100160255A1
公开(公告)日：2010-06-24
申请号：US11997021
申请日：2006-07-28
申请人： Makoto Kamata , Kohji Fukatsu , Tohru Yamashita , Naoki Furuyama , Satoshi Endo
发明人： Makoto Kamata , Kohji Fukatsu , Tohru Yamashita , Naoki Furuyama , Satoshi Endo
IPC分类号： A61K31/695 , C07D471/10 , A61K31/4545 , C07D211/06 , A61P3/04 , A61P9/12 , A61P3/06 , A61P9/00 , A61P3/10 , C07D498/10 , A61K31/5386 , C07D487/10 , A61K31/499 , C07F7/02 , C07D413/14 , A61K31/5377
CPC分类号： C07D513/10 , C07D221/20 , C07D401/04 , C07D471/10 , C07D487/10 , C07D491/10 , C07F7/1804
摘要： The present invention provides a compound represented by the formula (I): wherein E is an optionally substituted cyclic group; D is a carbonyl group or a sulfonyl group; A is CH or N; ring P is an optionally further substituted 5- to 7-membered ring; ring Q is an optionally further substituted 5- to 7-membered nonaromatic ring; and ring R is an optionally further substituted and optionally condensed 5- to 7-membered nonaromatic ring, or a salt thereof. The compound of the present invention has an ACC inhibitory activity, is useful for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and has superior properties in the efficacy, duration of activity, specificity, low toxicity and the like.
摘要翻译：本发明提供由式（I）表示的化合物：其中E为任选取代的环状基团; D是羰基或磺酰基; A是CH或N; 环P是任选进一步取代的5-至7-元环; 环Q是任选进一步取代的5-至7-元非芳族环; 并且环R是任选进一步取代的和任选缩合的5-至7-元非芳族环或其盐。本发明化合物具有ACC抑制活性，可用于预防或治疗肥胖症，糖尿病，高血压，高脂血症，心力衰竭，糖尿病并发症，代谢综合征，肌肉减少症等，并且具有优异的功效特性，活动持续时间，特异性，低毒性等。

5. 发明授权

US07601868B2 Amine derivative 失效
标题翻译：胺衍生物
公开(公告)号：US07601868B2
公开(公告)日：2009-10-13
申请号：US10545120
申请日：2004-02-12
申请人： Yuji Ishihara , Makoto Kamata , Shiro Takekawa
发明人： Yuji Ishihara , Makoto Kamata , Shiro Takekawa
IPC分类号： C07C233/65 , C07D207/06 , A61K31/165 , A61K31/40
CPC分类号： C07D211/16 , A61K31/55 , C07C233/73 , C07C235/42 , C07D207/09 , C07D207/12 , C07D211/14 , C07D213/82 , C07D233/24 , C07D295/135
摘要： The present invention provides a compound represented by the formula or salts thereof, wherein, Ar1, Ar, R, R1, R2, Ra1, Ra2, Ra3, Ra4 and Y have meanings described in the specification, having a melanin-concentrating hormone antagonistic, action and useful as an agent for the prophylaxis or treatment of obesity and the like.
摘要翻译：本发明提供由下式表示的化合物或其盐，其中Ar1，Ar，R，R1，R2，Ra1，Ra2，Ra3，Ra4和Y具有说明书中描述的具有黑色素浓缩激素拮抗作用的含义，作用并用作预防或治疗肥胖症等的药剂。

6. 发明授权

US07183415B2 Quinoline compound 失效
标题翻译：喹啉化合物
公开(公告)号：US07183415B2
公开(公告)日：2007-02-27
申请号：US10493427
申请日：2002-10-24
申请人： Yuji Ishihara , Makoto Kamata , Shiro Takekawa , Nobuhiro Suzuki , Koki Kato
发明人： Yuji Ishihara , Makoto Kamata , Shiro Takekawa , Nobuhiro Suzuki , Koki Kato
IPC分类号： C07D215/38 , C07D215/14
CPC分类号： C07D401/06 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/55 , C07D215/38 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04
摘要： A compound, which has a melanin-concentrating hormone antagonistic action and useful as an agent for preventing or treating obesity, and which is represented by the formula: wherein Ar is a cyclic group optionally having substituent(s); X is a bond or a spacer having a main chain of 1 to 6 atoms; R1 and R2 are the same or different and each is a hydrogen atom or a hydrocarbon group optionally having substituent(s), or R1 and R2 may form, together with the adjacent nitrogen atom, a nitrogen-containing heterocycle optionally having substituent(s); Y is a divalent hydrocarbon group optionally having substituent(s) (except CO); R3 is a hydrogen atom or a hydrocarbon group optionally having substituent(s); and ring A and ring B may further have substituents, and when ring B further has a substituent, the substituent may be linked to R1 to form a ring, or a salt thereof, or a prodrug thereof, is provided.
摘要翻译：一种化合物，其具有黑色素浓集激素拮抗作用并且可用作预防或治疗肥胖症的药剂，并且其由下式表示：其中Ar是任选具有取代基的环状基团; X是具有1至6个原子的主链的键或间隔基; R 1和R 2相同或不同，各自为氢原子或任选具有取代基的烃基，或R 1〜 >和R 2可以与相邻的氮原子一起形成任选具有取代基的含氮杂环; Y是任选具有取代基（CO除外）的二价烃基; R 3是氢原子或任选具有取代基的烃基; 并且环A和环B可以进一步具有取代基，并且当环B还具有取代基时，取代基可以与R 1连接形成环，或其盐或其前药，被提供。

7. 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。

8. 发明申请

US20110319394A1 FUSED HETEROCYCLIC COMPOUNDS 有权
标题翻译：熔融杂环化合物
公开(公告)号：US20110319394A1
公开(公告)日：2011-12-29
申请号：US13166212
申请日：2011-06-22
申请人： Takahiko TANIGUCHI , Masato YOSHIKAWA , Kasei MIURA , Tomoaki HASUI , Eiji HONDA , Keisuke IMAMURA , Makoto KAMATA , Haruhi KAMISAKI , John F. QUINN , Joseph RAKER , Fatoumata CAMARA , Yi WANG
发明人： Takahiko TANIGUCHI , Masato YOSHIKAWA , Kasei MIURA , Tomoaki HASUI , Eiji HONDA , Keisuke IMAMURA , Makoto KAMATA , Haruhi KAMISAKI , John F. QUINN , Joseph RAKER , Fatoumata CAMARA , Yi WANG
IPC分类号： A61K31/437 , C07D498/04 , A61P25/18 , C07D487/14 , A61K31/522 , A61K31/551 , C07D471/04 , C07D473/00
CPC分类号： A61K31/4353 , A61K31/4355 , A61K31/437 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4985 , A61K31/5025 , A61K31/519 , A61K31/52 , A61K31/522 , A61K31/551 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/14 , C07D471/04 , C07D471/14 , C07D473/00 , C07D473/28 , C07D487/04 , C07D495/04 , C07D498/04 , C07D498/08 , C07D519/00 , C07F7/10
摘要： The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I): wherein the symbols are defined in the specification.
摘要翻译：本发明提供具有PDE抑制作用的化合物，其可用作预防或治疗精神分裂症的药剂。化合物由式（I）表示：其中符号在说明书中定义。

9. 发明申请

US20060128690A1 Amine derivative 失效
标题翻译：胺衍生物
公开(公告)号：US20060128690A1
公开(公告)日：2006-06-15
申请号：US10545120
申请日：2004-02-12
申请人： Yuji Ishihara , Makoto Kamata , Shiro Takekawa
发明人： Yuji Ishihara , Makoto Kamata , Shiro Takekawa
IPC分类号： A61K31/55 , A61K31/401 , A61K31/445
CPC分类号： C07D211/16 , A61K31/55 , C07C233/73 , C07C235/42 , C07D207/09 , C07D207/12 , C07D211/14 , C07D213/82 , C07D233/24 , C07D295/135
摘要： The present invention provides a compound represented by the formula wherein Ar1 is a cyclic group optionally having substituent(s); R is a hydrogen atom, an optionally halogenated C1-6 alkyl, a phenyl optionally having substituent(s) or a pyridyl optionally having substituent(s); Ra1, Ra2, Ra3 and Ra4 are the same or different and each is a hydrogen atom, an optionally halogenated C1-6 alkyl or the like; Ar is a monocyclic aromatic ring optionally having substituent(s); Y is an optionally halogenated alkylene group; and R1 and R2 are (1) the same or different and each is a hydrogen atom or a C1-6 alkyl, (2) R1 and R2 form a nitrogen-containing heterocycle optionally having substituent(s) together with the adjacent nitrogen atom, or (3) R1 and Y form a nitrogen-containing heterocycle optionally having substituent(s) together with the adjacent nitrogen atom, and R2 is a hydrogen atom or a C1-6 alkyl; provided that when the nitrogen-containing heterocycle formed by R1 and R2 together with the adjacent nitrogen atom is a piperazine, or when R is a C1-4 alkyl, Ar1 is a cyclic group having substituent(s), or a salt thereof, having a melanin-concentrating hormone antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like.
摘要翻译：本发明提供由下式表示的化合物：其中Ar 1是任选具有取代基的环状基团; R是氢原子，任选卤代的C 1-6烷基，任选具有取代基的苯基或任选具有取代基的吡啶基; Ra 1，R 2，R 3，R 3和R 4相同或不同，各自为氢原子，任选卤代的C 1-6烷基等; Ar是任选具有取代基的单环芳环; Y是任选卤代的亚烷基; 且R 1和R 2均为（1）相同或不同，并且各自为氢原子或C 1-6烷基，（ 2）R 1和R 2 2形成任选具有取代基的氮杂环与相邻的氮原子，或（3）R 1， Y和Y形成任选具有取代基的氮杂环与相邻的氮原子一起形成，R 2是氢原子或C 1-6 烷基; 条件是当由R 1和R 2与相邻氮原子一起形成的含氮杂环是哌嗪时，或当R是C 1〜 4个烷基，Ar 1是具有取代基的环状基团或其盐，其具有黑色素浓缩激素拮抗作用并且可用作预防或治疗的药剂肥胖等。

10. 发明申请

US20050209213A1 Quinoline compound 失效
标题翻译：喹啉化合物
公开(公告)号：US20050209213A1
公开(公告)日：2005-09-22
申请号：US10493427
申请日：2002-10-24
申请人： Yuji Ishihara , Makoto Kamata , Shiro Takekawa , Nobuhiro Suzuki , Koki Kato
发明人： Yuji Ishihara , Makoto Kamata , Shiro Takekawa , Nobuhiro Suzuki , Koki Kato
IPC分类号： A61K31/4015 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/55 , A61P3/04 , A61P5/04 , A61P25/22 , A61P25/24 , A61P43/00 , C07D215/38 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D413/02 , C07D41/02
CPC分类号： C07D401/06 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/55 , C07D215/38 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04
摘要： A compound, which has a melanin-concentrating hormone antagonistic action and useful as an agent for preventing or treating obesity, and which is represented by the formula: wherein Ar is a cyclic group optionally having substituent(s); X is a bond or a spacer having a main chain of 1 to 6 atoms; R1 and R2 are the same or different and each is a hydrogen atom or a hydrocarbon group optionally having substituent(s), or R1 and R2 may form, together with the adjacent nitrogen atom, a nitrogen-containing heterocycle optionally having substituent(s); Y is a divalent hydrocarbon group optionally having substituent(s) (except CO); R3 is a hydrogen atom or a hydrocarbon group optionally having substituent(s); and ring A and ring B may further have substituents, and when ring B further has a substituent, the substituent may be linked to R1 to form a ring, or a salt thereof, or a prodrug thereof, is provided.
摘要翻译：一种化合物，其具有黑色素浓集激素拮抗作用并且可用作预防或治疗肥胖症的药剂，并且其由下式表示：其中Ar是任选具有取代基的环状基团; X是具有1至6个原子的主链的键或间隔基; R 1和R 2相同或不同，各自为氢原子或任选具有取代基的烃基，或R 1〜 >和R 2可以与相邻的氮原子一起形成任选具有取代基的含氮杂环; Y是任选具有取代基（CO除外）的二价烃基; R 3是氢原子或任选具有取代基的烃基; 并且环A和环B可以进一步具有取代基，并且当环B还具有取代基时，取代基可以与R 1连接形成环，或其盐或其前药，被提供。

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